JPH044293B2 - - Google Patents

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Publication number
JPH044293B2
JPH044293B2 JP56061541A JP6154181A JPH044293B2 JP H044293 B2 JPH044293 B2 JP H044293B2 JP 56061541 A JP56061541 A JP 56061541A JP 6154181 A JP6154181 A JP 6154181A JP H044293 B2 JPH044293 B2 JP H044293B2
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JPS56167617A (en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Feeding, Discharge, Calcimining, Fusing, And Gas-Generation Devices (AREA)
  • External Artificial Organs (AREA)
  • Separation Using Semi-Permeable Membranes (AREA)
  • Control Of Throttle Valves Provided In The Intake System Or In The Exhaust System (AREA)
  • Infusion, Injection, And Reservoir Apparatuses (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Description

【発明の詳細な説明】 本発明は、医薬を人体のような流体環境に排出
する浸透性医薬製剤に関する。
医薬を胃腸管に排出するための、錠剤の形で製
造される浸透性医薬製剤は、フエリツクステーウ
エス（Felix Theeuwes）とタケルヒグチ
（Takeru Higuchi）の両者に付与されたアメリ
カ国特許第3845770号及び同第3916899号明細書で
公知である。これらの特許明細書に示されている
典型的な医薬製剤は医薬を含有している区画室を
包囲している半透性壁から成つている。この半透
性壁は、外部流体に対しては透過性であるが、医
薬の通過に対しては実質的に不透過性である。こ
の半透性壁には、これを貫通して系から医薬を排
出するための通路がある。系は、流体が半透性壁
を通つて区画室に壁の透過性と壁を横切る浸透圧
の圧力勾配によつて決まる速度で連続浸透して可
溶性の医薬を含有する溶液を形成し、この溶液を
系から時間の経過に沿つて分配することによつて
医薬を放出する。
フエリツクステーウエスに付与されたアメリカ
国特許第4036228号明細書において、特許権者は、
排出困難な医薬、特に水性タイプの流体に実際上
不溶性である医薬を排出する浸透性医薬製剤を開
示している。この製剤は、これに酸性成分と塩基
性成分から成る起泡性カツプルを満たすことによ
つて使用される。作用下においてその製剤が流体
環境中にあると、その起泡性カツプルは、流体を
製剤に浸透させ、それによつてカツプルを湿潤
し、反応させ、そして起泡性溶液を製剤内に生成
させる。起泡性溶液は製剤内に中性状態を作り出
し、そしてその医薬を製剤から分配する。このア
メリカ国特許は、それ自体酸性環境中で限定され
た溶解性を示す医薬の排出、塩基性成分だけの使
用及び使用環境における起泡の生成には指向して
いない。
本発明は、多くの抗炎症剤が浸透性医薬製剤か
ら制御された速度で排出するのは困難であるとい
うことの発見にある。抗炎症剤は、胃液のような
水性の酸性環境において溶解性が乏しく、従つて
これら医薬は、浸透性医薬製剤からの排出時に胃
液と接触して沈殿する。この現象は、医薬製剤の
半透性壁の通路出口においてその外表面に起こ
り、そこに医薬を沈殿、蓄積させる。沈殿した医
薬は、浸透性製剤の通路を通る溶液の流れを妨害
する。本発明は、医薬を二酸化炭素生成化合物と
混合することによつてその医薬を排出するもので
ある。ここで、前記化合物は、製剤からの放出時
及び胃領域中の酸との接触時に酸と反応し、二酸
化炭素ガスを生成させるものである。この物理作
用とガスは、付随的に医薬製剤の通路を開放に保
ちながら、医薬を細かく分散した形で医薬製剤か
ら分配する。
本発明を図面を参照して説明すると、第１図は
医薬を排出するのに用いられる浸透性医薬製剤１
０を説明するものである。浸透性医薬製剤１０
は、切欠部に見られる通り、区画室１２を包囲、
形成している半透性重合体から形成される壁１１
から成る。壁１１には、それを貫通して通路１３
があり、該通路１３を介して区画室１２を医薬製
剤１０の外面と接続させ、医薬製剤１０から点で
表される医薬１４とダツシユで表され、二酸化炭
素生成基を有する塩基性化合物１５とを排出する
ようになつている。
第２図は医薬を排出するのに用いられる浸透性
医薬製剤１０を説明するものであるる。この浸透
性医薬製剤は、切欠部に見られる通り、区画室１
２の内側に面している微孔質単層１６を積層して
有する半透性重合体から形成される壁１１から成
つている。図示しないが、もう１つの実施態様に
おいて、微孔質単層１６は半透性壁１１の外表面
にあることもできる。第２図において、装置１０
は壁１１と微孔質単層１６によつて形成される半
透性微孔質積層体を貫通して通路１３を有し、該
通路１３を介して区画室１２を製剤１０の表面と
接続させ、医薬１４及び二酸化炭素生成化合物１
５を製剤１０から排出するようになつている。
浸透性医薬製剤１０の半透性壁は、医薬、二酸
化炭素生成化合物又は病人に悪影響を及ぼさない
半透性物質から形成される。この半透性壁は水及
び生物の流体のような外部流体の通過に対しては
透過性であるが、医薬、溶質などの通過に対して
は本質的に不透過性である重合体物質から形成さ
れる。本発明の製剤を製造するのに有用な選択透
過性の重合体として、セルロースアクリレート、
セルロースジアクリレート、セルローストリアク
リレート、セルロースアセテート、セルロースジ
アセテート、セルローストリアセテート、ポリア
ミド、ポリウレタンなどより成る群から選ばれる
重合体が挙げられる。浸透性医薬製剤の製造に適
当な半透性重合体は、アメリカ国特許第3845770
号、同第3916899号、同第4008719号、同第
4036228号及び同第4111210号明細書に開示されて
いる。第２図に示される実施態様において、半透
性壁１１は、微孔質単層１６と層状配置の関係に
ある半透性単層１１から成る積層体であることが
できる。半透性単層１１は上記の重合体から形成
される。微孔質単層１６は、多数の微孔と製剤に
流体を通す連続微孔路を有する。微孔質単層は、
製剤が使用環境中で作用下にあるとき単層から溶
出又は浸出する細孔形成剤が入つている前記重合
体から成つていることができる。細孔形成剤は無
毒性で、且つ壁を形成している物質と反応しない
ものである。これら細孔形成剤がその単層から除
去されると、その中に微孔路ができ、流体を満た
し、従つて、これら微孔路は、流体を医薬製剤に
入れる手段となる。典型的な細孔形成剤として、
塩化ナトリウム、塩化カリウム、ソルビトール、
マンニトール、ポリエチレングリコール、ヒドロ
キシプロピルメチルセルロース、ヒドロキシプロ
ピルブチルセルロースなどの物質が挙げられる。
半透性単層及び微孔質単層から成る積層壁を有す
る浸透性医薬製剤は、アメリカ国特許第4160452
号明細書に開示されている。
本発明において広範に用いられている医薬とい
う表現には、浸透性医薬製剤から排出して有利且
つ有用な結果を生むことができる任意の化合物、
物質の組成物又はそれらの混合物が包含される。
医薬という用語についてさらに明確に述べると、
これには動物、鳥類、魚類及びは虫類に局所的又
は全身的効果を生む任意の物質が包含される。動
物という用語は山羊、牛、馬、犬、ねこなどのよ
うな霊長類、人間、家畜、愛がん動物及び農放牧
動物を包含する。動物という用語はまたマウス、
ラツト及びモルモツトのような実験動物も包含す
る。本発明の方法によつて排出することができる
医薬には中枢神経系作用剤、催眠剤、鎮静剤、精
神神経賦活剤、トランキライザー、抗抑制剤、鎮
痙剤、筋弛緩剤、抗パーキンソン剤、麻酔剤、抗
炎症剤、局所麻酔剤、抗マラリア剤、ホルモン
剤、交感神経興奮剤、利尿剤、駆虫剤、ネオプラ
スチツクス、低血糖症剤、興奮剤、栄養剤のよう
な無機及び有機医薬がある。さらに好ましい実施
態様において、医薬という用語は中性及び酸性環
境に実際上不溶である、すなわち限定された溶解
性を持つ医薬を包含する。すなわち、これらの医
薬はこのような環境中で沈殿するのである。中性
という表現は水及び同様の生物環境を含み、また
酸という表現は胃及びその中に生成する塩酸、腟
及びその中に生成する乳酸などを含む。本明細書
において用いられている酸性体液という熟語は胃
液、腟液などの酸環境を指している。
本発明の方法により、上記環境に排出するのに
適当な医薬の１つの特定の群は、酸性抗炎症剤で
ある。抗炎症剤としては、アリールカルボン酸剤
及びエノル酸剤が挙げられる。アリールカルボン
酸剤の例には、アルクロフエナツク、すなわち、
４−アリルオキシ−３−クロロ−フエニル酢酸；
アスピリン、すなわち、アセチルサリチル酸；フ
エノプロフエン、すなわち、dl−２−（３−フエ
ノキシフエニル）プロピオン酸；フルフエナミン
酸、すなわち、２−（３−トリフルオロメチルア
ニリノ）安息香酸；イブプロフエン、すなわち、
２−（４−イソブチルフエニル）プロピオン酸；
インドメタシン、すなわち、５−メトキシ−２−
メチル−１−（4′−クロロベンゾイル）−３−イン
ドール−酢酸；ケトプロフエン、すなわち、２−
（３−ベンゾイルフエニル）プロピオン酸；メチ
アジニン酸、すなわち、10−メチル−２−フエノ
チアジニル酢酸；ナプロキセン、すなわち、ｄ−
２−（6′−メトキシ−2′−ナフチル）プロピオン
酸；ニフルミン酸、すなわち、３−トリフルオロ
メチル−２−フエニル−アミノニコチン酸；トル
メチン、すなわち、１−メチル−５−ｐ−トルオ
イルピロール−２−酢酸；及びサリンダツク、す
なわち、シス−５−フルオロ−２−メチル−１−
〔ｐ−（メチルスルフイニル）−ベンジリデン〕イ
ンデン−３−酢酸がある。エノル酸剤の例には、
アザプロパゾン、即ち、３−ジメチルアミノ−７
−メチル−１，２−（ｎ−プルピルマロニル）−１
−２，ジヒドロ−１，２，４−ベンゾトリアジ
ン；フエニルブタゾン、即ち、３，５−ジオキソ
−４−ｎ−ブチル−１，２−ジフエニルピラゾリ
ジン；プレナゾン、すなわち、４−プレニル−
１，２−ジフエニル−３，５−ピラゾリジンジオ
ン；サドキシカム、すなわち、４−ヒドロキシ−
２−メチル−Ｎ−（２−チアゾリル）−2H−１，
２−ベンゾチアジン−３−カルボキサミド−１，
１−ジオキシドなどの化合物がある。他の抗炎症
剤には、ジクロフエナツク、すなわち、２−〔２，
６−ジクロロフエニル）アミノ〕ベンゼン酢酸；
及びペルオキシカム、すなわち、2H−１，２−
ベンゾチアジン−３−カルボキサミドがある。
本発明の方法によつて排出することができる、
水に実際上不溶の、又は水に極めてわずかしか溶
解しない他の医薬の例には、ジフエニドール、メ
クリジン塩酸塩、プロクロルペルアジンマレエー
ト、アニシンドン、ジフエナジオーン、エリトリ
チルテトラナイトレート、ジゾキシン、レスパー
ピン、アセタゾールアミド、メタゾールアミド、
ベンドロフルメチアジド、クロルプロパミド、ト
ラザミド、アロプリノール、アルミニウムアスピ
リン、サリチル酸、サリチル酸ナトリウム、サリ
チルアミド、アセトアミノフエン、アセトフエネ
チジン、コルヒチン、メフエナミン酸、オクスフ
エンブタゾン、ゾメピラツク、メソトレキセー
ト、アセチルスルフイソキサゾール、ヒドロコー
チゾン、デスオキシコルチコステロンアセテー
ト、コルチソンアセテート、トリアミノロン、17
−エストラジオール、17−ヒドロキシプロゲステ
ロン、19−ノルプロゲステロン、プレドニソロ
ン、プロゲステロン、ノルエチンドロンアセテー
ト、ノルエチノドレルなどの化合物がある。
医薬製剤中に存在する医薬の量は、ホストに投
与すべき医薬の活性と量に応じて変わる。一般
に、この製剤は、0.5mg〜３ｇ、又はそれ以上の
医薬を含み、例えば、個々の製剤は25mg、50mg、
125mg、250mg、1.5ｇなどの量で医薬を含有して
いる。医薬は、分散体、顆粒、粉末、圧縮塊、フ
イルムなどの形態のような各種形態で製剤中に存
在することができる。また、医薬は結合剤、希釈
剤、分散剤、安定剤、染料などの添加剤と混合す
ることができる。有利な医薬、それらの溶解性、
それらの投与量は、マツクパブリツシング社
（Mack Publishing Co.）（イーストン
〔Easton〕、ペンシルバニア〔Penna〕）刊行のレ
ミングトン（Remington）著「フアーマシユー
テイカル サイエンセス（Pharmaceutical
Sciences）」第15版 （1975年）；サウンダー社（Saunder Company） （フイラデルフイア〔Philadelphia〕、ペンシル
バニア）刊行のフアルコナー（Falconer）他著
「ザ ドラツグ、ザ ナース、ザ ペーシヤント、
インクルーデイング カレント ドラツグ ハン
ドブツク（The Drug，the Nurse，the
Patient，Including Current Drug Handbook）」
（1974〜1976年）；メデイカル エコノミツクス社
（Medical Economics Co.）（オラデル
〔Oradell〕、ニユージヤージー〔N.J.〕）刊行の
「フイジシアン デスク レフアレンス
（Physician Desk Reference）」第33版（1979
年）、「アン オブ アラージー（Ann.of
Allergy）」第41巻、第75〜77ページ（1979年）；
「アルゼニム フオルシユ（Arzenim.Forsch.）」
第25巻、第1629〜1635ページ（1975年）；及びJ.
Inter.Med.Res.第７巻、第335〜338ページ（1979
年）においてこの技術分野に知られている。
本発明の目的に適当なガス生成化合物は、製薬
上許容でき、そしてａ）半透性壁を横切つて濃度
勾配を示し、且つ医薬製剤中に流体を浸透させ、
ｂ）緩衝剤として作用し、且つ医薬製剤に入つて
くる流体に溶解して医薬を含有する溶液を形成
し、ｃ）医薬製剤の外側において通路を囲む隣接
区域のPHを医薬の沈殿速度を下げるのに十分高い
値まで上昇させ、そしてｄ）医薬製剤の外側で、
通路の環境界面においてその環境の酸と反応し
て、医薬を細かく分散した形で医薬製剤から放出
させる二酸化炭素の起泡を生成させる固体の塩基
性化合物が好ましい。この塩基性化合物には、ア
ルカリ金属炭酸塩及び重炭酸塩、アルカリ土類金
属炭酸塩及び重炭酸塩、並びにそれらの混合物の
ような無毒性の金属炭酸塩及び重炭酸塩がある。
好ましい化合物は、水に可溶で、且つ環境の酸と
接触して速やかに起泡を生成するものである。水
中での溶解度が異なる化合物の混合物を水に非常
によく溶解しうる少なくとも１種の化合物ととも
に使用することもできる。典型的化合物として炭
酸リチウム、炭酸ナトリウム、炭酸カリウム、重
炭酸リチウム、重炭酸ナトリウム、重炭酸カリウ
ム、炭酸マグネシウム、炭酸カルシウム、重炭酸
マグネシウムなどの塩がある。炭酸アンモニウ
ム、重炭酸アンモニウム、セスキ炭酸アンモニウ
ム、セスキ炭酸ナトリウムなどの塩も有用なガス
生成化合物である。これらの化合物は、水に溶解
するとき７より大きいPH、通常８と12の間のPHを
示す。任意であるが、共通イオン効果のない医薬
とガス生成化合物を選ぶのがしばしば望ましく、
かくして医薬製剤に入つてくる流体中のそれらそ
れぞれの溶解度は最大になる。区画室に収容され
る塩基性化合物又はその混合物の量は一般に約
0.5mg〜３ｇ、又はそれ以上、好ましくは25〜750
mgである。塩基性化合物及びそれらの水中におけ
る溶解度についてはケミカル ラバー社
（Chemical Rubber Co.）（クリーブランド
〔Cleveland〕、オハイオ〔Ohio〕）刊行の「ザ
ハンドブツク オブ ケミストリー アンド フ
イジツクス（The Handbook of Chemistry
and Physics）」第48版（1968年）に開示されて
いる。
医薬及び塩基性化合物は、また、結合剤及び潤
滑剤として用いることができる。医薬及び塩基性
化合物は、水溶性結合剤に混合されるか、又は水
と接触すると医薬及び塩基性化合物を放出する水
不溶性結合剤に混合される。典型的な水溶性結合
剤には、ポリ（エチレングリコール）、ゼラチン、
寒天、カルボキシセルロース、エチルメチル−セ
ルロース、ポリ（ビニルアルコール）、ポリ（ビ
ニルピロリドン）、水溶性殿粉誘導体などがある。
典型的な潤滑剤には、ステアリン酸、ステアリン
酸マグネシウム、ステアリン酸亜鉛などがある。
使用される結合剤及び潤滑剤の量は一般に約0.1
〜150mg、又はそれ以上である。
本発明の浸透性医薬製剤は、標準的な方法で製
造される。例えば、１つの実施態様において、医
薬を塩基性化合物及び他の成分と、ボールミルで
粉砕し、カレンダリングし、撹拌し、そして所定
の形状にプレス成形することによつて混合する。
医薬製剤の壁を形成する物質は、浸漬、モールデ
イング又は噴霧によつて、プレス成形された混合
物に適用することができる。壁を適用する１つの
方法は空気懸濁法である。空気懸濁法は、単層か
ら、又は複雑層から形成される壁を作るのに用い
ることができる。空気懸濁法は、アメリカ国特許
第2799241号；J.Am.Pharm.Assoc.第48巻、第
451〜459ページ（1959年）；及び同第49巻、第82
〜84ページ（1960年）に記載されている。壁を貫
通する浸透通路又は孔は機械的にドリリングする
か、レーザーでドリリングするか、パンチングす
るか、又はダイで切ることによつて作られる。レ
ーザーを用いて通路を形成する方法はアメリカ国
特許第3916899号及び同第4088864号明細書に記載
されている。他の標準的な製造方法は「モダーン
プラスチツク エンサイクロペデイア
（Modern Plastic Encyclopedia）」第46巻、第62
〜70ページ（1969年）；マツク パブリツシング
社（イーストン、ペンシルバニア）刊行の、「レ
ミングトンズ フアーマシユーテイカル サイエ
ンセス」第14版、第1649〜1698ページ（1970
年）；及びリー アンド フエビガー社（Lea
＆ Febiger Co.）（フイラデルフイア
〔Philadelphia〕、ペンシルバニア〔Penn.〕）刊行
のラチマン（Lachman）他著「ザ セラピー
アンド プラクテイス オブ インダストリアル
フアーマシー（The Therapy and Practice
of Industrial Pharmacy）第197〜225ページ
（1970年）に記載されている。
次の実施例は本発明を単に説明するだけのもの
であり、いずれの点でも本発明の範囲を限定する
ものと考えるべきでない。
実施例 １ 非ステロイド系抗炎症剤のインドメタシンナト
リウムの排出のための経口浸透性医薬製剤を次の
ようにして製造した。医薬製剤の区画室にいれる
ための医薬組成物を、105.2mgのインドメタシン
ナトリウム三水和物、142mgの重炭酸カリウム、
5.0mgのポリビニルピロリドン及び7.1mgのステア
リン酸を完全に配合し、次いでその均質な配合物
を予備区画室形成用医薬調合物に圧縮成形するこ
とによつて調製した。次に、圧縮成形した医薬調
合物を空気懸濁機に入れ、微孔質単層形成組成物
を被覆した。微孔質単層組成物は、45重量％の、
アセチル含量が39.8％のセルロースアセテート、
27.5重量％のヒドロキシプロピルメチルセルロー
ス及び27.5重量％のポリエチレングリコール4000
から成つていた。微孔質単層は、塩化メチレン−
95％エタノール溶剤（80：20、重量：重量）から
形成した。微孔質単層は厚さ５ミルであつた。
次に、半透性外層を空気懸濁機中で微孔質単層
の上に積層した。半透性層形成組成物は50重量％
の、アセチル含量が39.8％のセルロースアセテー
ト及び50重量％の、アセチル含量が32％のセルロ
ースアセテートから成つていた。半透性単層は塩
化メチレンと95％エタノールから成る混合溶剤
（80：20、重量：重量）から適用した。この系を
乾燥し、そして10ミルの通路を積層壁を貫通して
レーザーでドリリングした。この系は、インドメ
タシンを８mg／時間の速度で放出する。この医薬
製剤は作用下において通路出口端で酸性胃液と接
触すると、医薬をケバ状態で分散させる二酸化炭
素の気泡を生成させて起泡する溶液を放出する。
実施例 ２ インドメタシンを制御して連続排出する経口浸
透性医薬製剤を前記の一般的操作を行うことによ
つて作つた。本製剤において、区画室は56.4％の
炭酸カリウム、37.6％のインドメタシンナトリウ
ム三水和物、３％のプロビドン （Providone
）及び３％のステアリン酸から成る医薬調合物
を収容していた。圧縮成形後の調合物は、直径
7.93mm、面積1.6cm2及び密度1.65ｇ／mlを有してい
た。製剤は45重量％の、アセチル含量が39.8％の
セルロースアセテート、45重量％のソルビトール
及び10重量％のポリエチレングリコール400から
本質的に成る微孔質内層を含む積層された壁を有
していた。内層は塩化メチレン−メタノール−水
（62：35：３重量比）から成る溶剤から適用した。
この微孔質単層の上に半透性層を積層した。半透
性層は50重量％の、アセチル含量が39.8％のセル
ロースアセテート及び50重量％の、アセチル含量
が32％のセルロースアセテートから成つている。
半透性層は塩化メチレンとメタノール（80：20重
量比）から成る溶剤から適用した。微孔質形成層
は、厚さ５ミルで、半透性層は厚さ2.4ミルであ
つた。この製剤は、９ミルの通路を有し、インド
メタシンを８mg／時間の速度で排出した。この製
剤は、通路の環境界面において、及び通路付近の
製剤の壁の上において急速な沈殿を実質的に起こ
さずに医薬を排出する。
実施例 ３ 微孔質形成単層が厚さ１ミル、半透性単層が厚
さ2.7ミルで、医薬の放出速度が８mg／時間であ
る点を除いて実施例２に記載の条件を用いて実施
例２の操作を繰り返した。
実施例 ４ (a)微孔質単層が厚さ５ミル、半透性単層が厚さ
3.4ミル及び医薬製剤の医薬放出速度が６mg／時
間である、及び(b)微孔質単層が厚さ５ミル、半透
性単層が厚さ1.7ミル及び系の医薬放出速度が12
mg／時間である実施例１及び２の浸透性医薬製剤
を本実施例で製造した。
実施例 ５ 胃腸管中でアリールカルボン酸系抗炎症剤を放
出する一連の経口浸透性医薬製剤を本発明に従つ
て調製する。この製剤は、40〜250mgのインドメ
タシンナトリウム、好ましくは85〜125mgのイン
ドメタシンナトリウム三水和物（これは70〜100
mgのインドメタシンに相当する）、50〜300mg、好
ましくは130〜190mgの重炭酸カリウム、２〜20
mg、好ましくは５〜10mgの結合剤及び２〜20mg、
好ましくは５〜10mgの潤滑剤を収容する。この製
剤は、0.10〜0.16mmの厚さを持つ18〜25mgの重さ
の内側微孔質形成単層と0.035〜0.100mmの厚さを
持つ６〜20mgの重さの外側半透性単層を有する。
この製剤は0.18〜0.38mmの通路を有し、医薬を５
〜15mg／時間の速度で放出する。
本発明により生まれる予期されない利点は第３
図及び第４図に認められる。第３図はガス生成塩
基性化合物なしで製造した浸透性医薬製剤からの
インドメタシンの放出を示している。この製剤
は、塩酸を含有する人工胃液の存在下で医薬を放
出するが、しかしながら医薬は製剤の壁及び通路
の出口部に沈殿し、従つて医薬は環境の流体中に
は認められない。医薬は第３図に示されるように
時間基準で分析されている。第４図は、塩基性の
ガス生成化合物により製造した浸透性医薬製剤か
らのインドメタシンの放出を示している。この製
剤は作用下において本発明による両人工胃腸管液
に医薬を放出する。
【図面の簡単な説明】
第１図は、縮尺して製図したものでないが、医
薬を排出するのに用いられ、半透性壁によりつく
られた浸透性医薬製剤の切欠図であり、第２図
は、縮尺して製図したものでないが、医薬を排出
するのに用いられる、微孔質半透性壁により作ら
れた浸透性医薬製剤の切欠図であり、第３図は、
浸透性医薬製剤からガス生成化合物なしで放出さ
れる貧溶解性医薬の放出パターンを示すグラフで
あり、そして第４図は、浸透性医薬製剤からガス
生成化合物とともに放出される貧溶解性医薬の放
出パターンを示すグラフである。 １０…浸透性医薬製剤、１１…半透性壁、１２
…区画室、１３…通路、１４…医薬、１５…塩基
性化合物、１６…微孔質単層。

Claims (1)

    【特許請求の範囲】
  1. １ 流体の通過に対しては透過性であるが、医薬
    の通過に対しては実質的に不透過性である半透性
    の重合体壁、この壁によつて包囲、形成された区
    画室および前記壁中に形成された前記医薬を排出
    するための通路から成り、前記区画室は、酸流体
    環境で沈殿する医薬と、二酸化炭素生成基を有す
    る非毒性塩基性化合物を含み、該塩基性化合物は
    区画室中に吸収される流体に可溶性であり、か
    つ、この流体に対して前記の壁を横切つて浸透圧
    の圧力勾配を示す、医薬を酸流体環境に排出する
    ための浸透性医薬製剤において、該医薬製剤の外
    側で該塩基性化合物を該酸流体環境と反応させる
    ことにより、通路の出口でガスを発生させ、泡立
    ちを生じさせ該通路の出口で医薬の沈殿を少なく
    することを特徴とする、通路の出口と酸流体環境
    の界面における医薬の沈殿を少なくするように改
    良された浸透性医薬製剤。
JP6154181A 1980-04-25 1981-04-24 Permeation device Granted JPS56167617A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US06/143,644 US4265874A (en) 1980-04-25 1980-04-25 Method of delivering drug with aid of effervescent activity generated in environment of use

Publications (2)

Publication Number Publication Date
JPS56167617A JPS56167617A (en) 1981-12-23
JPH044293B2 true JPH044293B2 (ja) 1992-01-27

Family

ID=22504961

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Application Number Title Priority Date Filing Date
JP6154181A Granted JPS56167617A (en) 1980-04-25 1981-04-24 Permeation device

Country Status (11)

Country Link
US (1) US4265874A (ja)
EP (1) EP0040899B1 (ja)
JP (1) JPS56167617A (ja)
AT (1) ATE9267T1 (ja)
DE (1) DE3165901D1 (ja)
DK (1) DK152482C (ja)
ES (2) ES267593Y (ja)
GR (1) GR73519B (ja)
IE (1) IE51216B1 (ja)
NZ (1) NZ196561A (ja)
PT (1) PT72796B (ja)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20150137871A (ko) * 2014-05-30 2015-12-09 디씨에스이엔지 주식회사 회전속도비를 이용하여 회전체내 절삭툴을 제어할 수 있는 오비탈식 파이프 절삭장치

Families Citing this family (746)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2470599A1 (fr) * 1979-12-07 1981-06-12 Panoz Donald Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenus
US4344929A (en) * 1980-04-25 1982-08-17 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
JPS5770816A (en) * 1980-10-17 1982-05-01 Ono Pharmaceut Co Ltd Multilayered film preparation of prostagladin of prolonged action
FR2525474A1 (fr) * 1982-04-26 1983-10-28 Roussel Uclaf Nouvelle forme pharmaceutique orale de clometacine
US4478596A (en) * 1982-11-26 1984-10-23 Michelson Paul E Delivery system for physiologically active agents
US4613330A (en) * 1982-11-26 1986-09-23 Michelson Paul E Delivery system for desired agents
NZ206600A (en) * 1983-05-11 1987-01-23 Alza Corp Osmotic drug delivery device
JPH075457B2 (ja) * 1983-08-16 1995-01-25 ザ ウエルカム フアウンデ−シヨン リミテツド 調節された方法による有効成分の放出を可能にする医薬組成物
US4670578A (en) * 1983-08-29 1987-06-02 Merck & Co., Inc. Process for crystalline salts of L or (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine esters
EP0137364A3 (en) * 1983-09-23 1986-10-22 Merck & Co. Inc. Suppository form of an osmotic therapeutic system
US4627850A (en) * 1983-11-02 1986-12-09 Alza Corporation Osmotic capsule
GB2150434B (en) * 1983-12-01 1987-11-04 Alza Corp Constant rate release systems
GB2150830B (en) * 1983-12-05 1987-08-19 Alza Corp Drug dispenser
US4725427A (en) * 1984-03-13 1988-02-16 Albion International, Inc. Effervescent vitamin-mineral granule preparation
US4595583A (en) * 1984-03-19 1986-06-17 Alza Corporation Delivery system controlled administration of beneficial agent to ruminants
US4717566A (en) * 1984-03-19 1988-01-05 Alza Corporation Dosage system and method of using same
EP0166354B1 (en) 1984-06-26 1992-08-05 Merck & Co. Inc. Benzofused lactam compounds and pharmaceutical compositions containing them
US4693895A (en) * 1984-10-26 1987-09-15 Alza Corporation Colon delivery system
US4624847A (en) * 1985-04-22 1986-11-25 Alza Corporation Drug delivery device for programmed delivery of beneficial drug
US4627971A (en) * 1985-04-22 1986-12-09 Alza Corporation Osmotic device with self-sealing passageway
US4675174A (en) * 1985-08-16 1987-06-23 Alza Corporation Veterinary dispenser delivering beneficial agent by gas power generated in situ
US4723957A (en) * 1986-02-07 1988-02-09 Alza Corp. System for delivering drug with enhanced bioacceptability
US4971790A (en) * 1986-02-07 1990-11-20 Alza Corporation Dosage form for lessening irritation of mocusa
US4662880A (en) * 1986-03-14 1987-05-05 Alza Corporation Pseudoephedrine, brompheniramine therapy
US4753802A (en) * 1986-03-19 1988-06-28 Alza Corporation Verapamil dosage form
US4847093A (en) * 1986-06-19 1989-07-11 Alza Corporation Dosage form with means for governing rate of gas formation
US5099063A (en) * 1986-11-05 1992-03-24 Merck & Co., Inc. Certain phosphinic acid derivatives having antibacterial activity
US5143908A (en) * 1986-11-05 1992-09-01 Merck & Co., Inc. Antibacterial agents and potentiators of carbapenem antibiotics
US4715994A (en) * 1986-11-05 1987-12-29 Merck & Co., Inc. Novel antibacterial agents and potentiators of carbapenem antibiotics
US4874388A (en) * 1987-06-25 1989-10-17 Alza Corporation Multi-layer delivery system
US5499979A (en) * 1987-06-25 1996-03-19 Alza Corporation Delivery system comprising kinetic forces
US5110597A (en) * 1987-06-25 1992-05-05 Alza Corporation Multi-unit delivery system
US5023088A (en) * 1987-06-25 1991-06-11 Alza Corporation Multi-unit delivery system
US5938654A (en) * 1987-06-25 1999-08-17 Alza Corporation Osmotic device for delayed delivery of agent
US4957494A (en) * 1987-06-25 1990-09-18 Alza Corporation Multi-layer delivery system
JPS6413097A (en) * 1987-07-06 1989-01-17 Mitsubishi Chem Ind Phosphonic acid derivative
US5041644A (en) * 1987-07-06 1991-08-20 Merck & Co., Inc. Peptide derivatives of β-chloro-L(Z)-dehydro-glutamic acid
EP0318066B1 (en) 1987-09-22 1992-07-29 Merck & Co. Inc. Aryl-substituted thiophene 3-ols, derivatives and analogs, as lipoxygenase inhibitors
US5030732A (en) * 1988-03-03 1991-07-09 Merck & Co., Inc. Aminoethylphosphinic acid derivatives
US5211957A (en) * 1988-03-25 1993-05-18 Ciba-Geigy Corporation Solid rapidly disintegrating dosage form
CH675537A5 (ja) * 1988-03-25 1990-10-15 Ciba Geigy Ag
US5145990A (en) * 1988-10-28 1992-09-08 Merck & Co., Inc. Phosphorous containing dhp enzyme inhibitors
US4962097A (en) * 1988-10-28 1990-10-09 Merck & Co., Inc. Method of treating bacterial infection with phosphorus containing DHP enzyme inhibitors
US5147867A (en) * 1988-10-28 1992-09-15 Merck & Co., Inc. Phosphorus containing enzyme inhibitors
US4942039A (en) * 1989-05-09 1990-07-17 Miles Inc. Effervescent analgesic antacid composition having reduced sodium content
US5223264A (en) * 1989-10-02 1993-06-29 Cima Labs, Inc. Pediatric effervescent dosage form
US5089530A (en) 1990-08-03 1992-02-18 Merck & Co., Inc. Novel fermentation product with antiparasitic activity
US5443459A (en) * 1991-01-30 1995-08-22 Alza Corporation Osmotic device for delayed delivery of agent
SG84487A1 (en) 1991-04-17 2001-11-20 Merck & Co Inc Ophthalmic compositions comprising combinations of a carbonic anhydrase inhibitor and a b-adrenergic antagonist
US5198229A (en) * 1991-06-05 1993-03-30 Alza Corporation Self-retaining gastrointestinal delivery device
US5223265A (en) * 1992-01-10 1993-06-29 Alza Corporation Osmotic device with delayed activation of drug delivery
US5639782A (en) * 1992-03-04 1997-06-17 Center For Innovative Technology Neolignan derivatives as platelet activating factor receptor antagonists and 5-lipoxygenase inhibitors
US5434151A (en) * 1992-08-24 1995-07-18 Cytomed, Inc. Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase
US5463083A (en) * 1992-07-13 1995-10-31 Cytomed, Inc. Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
ATE196903T1 (de) 1992-07-13 2000-10-15 Cytomed Inc 2,5-diaryl tetrahydro-thiopene, -furane und analoge zur behandlung von entzündungs-und immunkrankheiten
US5498255A (en) * 1993-08-17 1996-03-12 Alza Corporation Osmotic device for protracted pulsatile delivery of agent
US5403952A (en) * 1993-10-08 1995-04-04 Merck & Co., Inc. Substituted cyclic derivatives as novel antidegenerative agents
US5750565A (en) * 1995-05-25 1998-05-12 Cytomed, Inc. Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
US5703093A (en) * 1995-05-31 1997-12-30 Cytomed, Inc. Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
US5792776A (en) * 1994-06-27 1998-08-11 Cytomed, Inc., Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
US6348571B1 (en) 1994-09-12 2002-02-19 Northwestern University Corticotropin release inhibiting factor and methods of using same
US5767113A (en) * 1995-05-10 1998-06-16 The Salk Institute For Biological Studies Compounds useful for concurrently activating glucocorticoid-induced response and reducing multidrug resistance
US6558708B1 (en) 1995-05-17 2003-05-06 Cedars-Sinai Medical Center Methods for manipulating upper gastrointestinal transit, blood flow, and satiety, and for treating visceral hyperalgesia
US7048906B2 (en) * 1995-05-17 2006-05-23 Cedars-Sinai Medical Center Methods of diagnosing and treating small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions
EP0827402A2 (en) * 1995-05-17 1998-03-11 Cedars-Sinai Medical Center Compositions containing fatty acids for improving digestion and absorption in the small intestine
US6861053B1 (en) * 1999-08-11 2005-03-01 Cedars-Sinai Medical Center Methods of diagnosing or treating irritable bowel syndrome and other disorders caused by small intestinal bacterial overgrowth
US5817335A (en) * 1995-05-26 1998-10-06 Alza Corporation Osmotic device with high drug loading and delayed activation of drug delivery
US5756540A (en) * 1995-06-02 1998-05-26 Mcw Research Foundation, Inc. Methods for in vivo reduction of nitric oxide levels and compositions useful therefor
US5741815A (en) * 1995-06-02 1998-04-21 Lai; Ching-San Methods for in vivo reduction of nitric oxide levels and compositions useful therefor
US5800422A (en) * 1995-06-02 1998-09-01 Alza Corporation Osmotic device with delayed activation of drug delivery and complete drug release
US6372713B1 (en) * 1995-09-08 2002-04-16 The Board Of Trustees Of Northwestern University Anti-depressant effects of corticotropin release inhibiting factor
US5747532A (en) * 1995-11-21 1998-05-05 Medinox, Inc. Combinational therapeutic methods employing nitric oxide scavengers and compositions useful therefor
US6723531B2 (en) 1996-04-05 2004-04-20 The Salk Institute For Biological Studies Method for modulating expression of exogenous genes in mammalian systems, and products related thereto
US5902605A (en) * 1996-04-18 1999-05-11 Alza Corporation Drug delivery device with minimal residual drug retention
US5785688A (en) * 1996-05-07 1998-07-28 Ceramatec, Inc. Fluid delivery apparatus and method
US5939460A (en) * 1996-07-08 1999-08-17 Idun Pharmaceuticals, Inc. Method of inhibiting NADPH oxidase
US5677318A (en) * 1996-07-11 1997-10-14 Merck Frosst Canada, Inc. Diphenyl-1,2-3-thiadiazoles as anti-inflammatory agents
US5922761A (en) * 1996-09-06 1999-07-13 Medinox, Inc. Methods for in vivo reduction of iron levels and compositions useful therefor
CN1230178A (zh) 1996-09-10 1999-09-29 麦地诺克斯公司 含聚二硫代氨基甲酸酯的大分子和其用于治疗和诊断应用的用途
US5858402A (en) * 1997-02-11 1999-01-12 Medinox, Inc. Methods for in vivo reduction of cyanide levels and compositions useful therefor
US5916910A (en) 1997-06-04 1999-06-29 Medinox, Inc. Conjugates of dithiocarbamates with pharmacologically active agents and uses therefore
US6294350B1 (en) 1997-06-05 2001-09-25 Dalhousie University Methods for treating fibroproliferative diseases
US5985592A (en) * 1997-06-05 1999-11-16 Dalhousie University Uses for pentoxifylline or functional derivatives/metabolites thereof
US5840721A (en) 1997-07-09 1998-11-24 Ontogen Corporation Imidazole derivatives as MDR modulators
US7105496B2 (en) 1998-07-23 2006-09-12 Northwestern University Methods and compositions for inhibiting angiogenesis
US6797691B1 (en) 1997-07-23 2004-09-28 Northwestern University Methods and compositions for inhibiting angiogenesis
US20030220234A1 (en) * 1998-11-02 2003-11-27 Selvaraj Naicker Deuterated cyclosporine analogs and their use as immunodulating agents
AU9797998A (en) 1997-10-10 1999-05-03 Trustees Of The University Of Pennsylvania, The Compositions and methods for inhibiting arginase activity
EP1037621A4 (en) 1997-10-15 2004-01-21 Univ Jefferson NITROGEN OXYD DONOR COMPOSITIONS, METHODS, APPARATUS, AND KITS FOR PREVENTING OR REDUCING VASCARSIONS OR VASCULAR SPAS IN A MAMMAL
US6750201B1 (en) * 1997-10-17 2004-06-15 The Trustees Of The University Of Pennsylvania Compositions and methods for promoting internalization and degradation of urokinase-type plasminogen activator
US6984773B1 (en) * 1998-01-09 2006-01-10 The Salk Institute For Biological Studies Transgenic mice expressing a human SXR receptor polypeptide
US6756491B2 (en) 1998-01-09 2004-06-29 The Salk Institute For Biological Studies Steroid-activated nuclear receptors and uses therefor
WO1999047549A1 (en) * 1998-03-16 1999-09-23 Ontogen Corporation PIPERAZINES AS INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE (FBPase)
US6287605B1 (en) * 1998-04-17 2001-09-11 The Trustees Of The University Of Pennsylvania Compositions and methods useful in treatment and prevention of HIV-1 infection
WO1999058640A2 (en) 1998-05-11 1999-11-18 Philadelphia Health And Education Corporation Mct-1, a human oncogene
US6333318B1 (en) 1998-05-14 2001-12-25 The Salk Institute For Biological Studies Formulations useful for modulating expression of exogenous genes in mammalian systems, and products related thereto
US20030220258A1 (en) * 2001-12-21 2003-11-27 Robbert Benner Treatment of ischemic events
US20050203187A1 (en) * 1998-06-01 2005-09-15 Verbiscar Anthony J. Formulations useful for the treatment of varicella zoster virus infections and methods for the use thereof
US6596770B2 (en) 2000-05-05 2003-07-22 Medinox, Inc. Therapeutic methods employing disulfide derivatives of dithiocarbamates and compositions useful therefor
US6093743A (en) 1998-06-23 2000-07-25 Medinox Inc. Therapeutic methods employing disulfide derivatives of dithiocarbamates and compositions useful therefor
US6265420B1 (en) 1998-06-23 2001-07-24 Medinox, Inc. Use of nitric oxide scavengers to treat side effects caused by therapeutic administration of sources of nitric oxide
US20030064917A1 (en) * 1998-07-23 2003-04-03 Crawford Susan E. Methods and compositions for inhibiting angiogenesis
WO2000009118A1 (en) 1998-08-13 2000-02-24 The Wistar Institute Methods for reducing atherosclerotic plaques
US6565854B2 (en) 1998-08-13 2003-05-20 Philadelphia Health And Education Corporation Antimicrobial histone H1 compositions, kits, and methods of use thereof
US6646113B1 (en) * 1998-09-17 2003-11-11 The Trustees Of The University Of Pennsylvania Nucleic acid molecule encoding human survival of motor neuron-interacting protein 1 (SIP1) deletion mutants
US20020138856A1 (en) * 1998-10-23 2002-09-26 Northwestern University Compositions and methods useful for treatment of depressive disorder based on an animal model
DE60036915T2 (de) 1999-01-13 2008-08-07 Alchemia Oncology Pty Ltd., Hawthorn Verwendung von hyaluronan zur herstellung eines medikaments zur erhöhung der wirksamkeit von zytotoxischen arzneimitteln
WO2000041731A1 (en) 1999-01-19 2000-07-20 The Children's Hospital Of Philadelphia Reverse gene therapy
US6395029B1 (en) 1999-01-19 2002-05-28 The Children's Hospital Of Philadelphia Sustained delivery of polyionic bioactive agents
US7282489B2 (en) * 2000-01-19 2007-10-16 The Children's Hospital Of Philadelphia Compositions and methods for performing reverse gene therapy
US7141417B1 (en) * 1999-02-25 2006-11-28 Thomas Jefferson University Compositions, kits, and methods relating to the human FEZ1 gene, a novel tumor suppressor gene
CA2364653A1 (en) 1999-02-25 2000-08-31 Merck Frosst Canada & Co. Pde iv inhibiting compounds, compositions and methods of treatment
US6221855B1 (en) 1999-03-11 2001-04-24 Wake Forest University Regulation of nucleic acid expression by heparan sulfate and biological equivalents thereof
US6428968B1 (en) 1999-03-15 2002-08-06 The Trustees Of The University Of Pennsylvania Combined therapy with a chemotherapeutic agent and an oncolytic virus for killing tumor cells in a subject
US6025502A (en) * 1999-03-19 2000-02-15 The Trustees Of The University Of Pennsylvania Enantopselective synthesis of methyl phenidate
US6251927B1 (en) 1999-04-20 2001-06-26 Medinox, Inc. Methods for treatment of sickle cell anemia
AU4803800A (en) 1999-04-27 2000-11-10 Trustees Of The University Of Pennsylvania, The Compositions, methods, and kits relating to LTiGTresistinLT/iGT
US6420545B1 (en) 1999-05-24 2002-07-16 The Trustees Of The University Of Pennsylvania CD4-independent HIV envelope proteins as vaccines and therapeutics
US7160694B2 (en) 1999-06-14 2007-01-09 Millennium Pharmaceuticals, Inc. Nucleic acids encoding TANGO405 and functional fragments and uses thereof
US7033780B1 (en) * 1999-06-14 2006-04-25 Millennium Pharmaceuticals, Inc. Nucleic acids corresponding to TANGO 294 a gene encoding a lipase—like protein
US6964854B1 (en) 1999-07-13 2005-11-15 Science & Technology Corporation Compositions and methods useful for the diagnosis and treatment of heparin induced thrombocytopenia/thrombosis
CA2382727A1 (en) 1999-10-08 2001-04-19 Ontogen Corporation Methods of enhancing chemotherapy with the use of an imidazole
US20020147197A1 (en) * 1999-10-08 2002-10-10 Newman Michael J. Methods and compositions for enhancing pharmaceutical treatments
CA2387018C (en) 1999-10-12 2008-02-12 Chemocentryx, Inc. Chemokine receptor
US6274627B1 (en) 1999-10-12 2001-08-14 Medinox, Inc. Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor
US7057015B1 (en) 1999-10-20 2006-06-06 The Salk Institute For Biological Studies Hormone receptor functional dimers and methods of their use
JP3417370B2 (ja) 1999-12-09 2003-06-16 株式会社村田製作所 非可逆回路素子及び通信機装置
US6559128B1 (en) 2000-01-21 2003-05-06 Northwestern University Inhibitors of G protein-mediated signaling, methods of making them, and uses thereof
US20030212021A1 (en) * 2001-01-25 2003-11-13 Frost Gregory I. Myeloid colony stimulating factor and uses thereof
US6464688B1 (en) 2000-02-15 2002-10-15 Microsolutions, Inc. Osmotic pump delivery system with flexible drug compartment
JP2001320205A (ja) 2000-03-02 2001-11-16 Murata Mfg Co Ltd 非可逆回路素子および通信装置
US7358330B2 (en) * 2001-03-29 2008-04-15 Biotempt B.V. Immunoregulatory compositions
US6509315B1 (en) 2000-04-07 2003-01-21 The Trustees Of The University Of Pennsylvania Didemnin analogs and fragments and methods of making and using them
IL152111A0 (en) * 2000-04-07 2003-07-31 Univ Pennsylvania Tamandarin and didemnin analogs and methods of making and using them
WO2001087870A1 (en) 2000-05-15 2001-11-22 Darwin Discovery Limited Hydroxamic acid derivatives
US6613801B2 (en) 2000-05-30 2003-09-02 Transtech Pharma, Inc. Method for the synthesis of compounds of formula I and their uses thereof
US6908741B1 (en) * 2000-05-30 2005-06-21 Transtech Pharma, Inc. Methods to identify compounds that modulate RAGE
AU2001275043A1 (en) 2000-05-31 2001-12-11 Drugtech Corporation Mineral supplement
WO2001097752A2 (en) * 2000-06-20 2001-12-27 The Trustees Of The University Of Pennsylvania Compositions comprising urokinase for modulating muscle contractility and angiogenisis
US6429223B1 (en) 2000-06-23 2002-08-06 Medinox, Inc. Modified forms of pharmacologically active agents and uses therefor
US9066919B2 (en) * 2000-07-14 2015-06-30 Alchemia Oncology Pty Limited Hyaluronan as a chemo-sensitizer in the treatment of cancer
AUPQ879500A0 (en) * 2000-07-14 2000-08-10 Meditech Research Limited Hyaluronan as cytotoxic agent, drug presensitizer and chemo-sensitizer in the treatment of disease
US7223563B2 (en) 2000-07-19 2007-05-29 Advanced Research And Technology Institute Fibroblast growth factor (FGF23) nucleic acids
WO2002019965A2 (en) * 2000-09-07 2002-03-14 Science & Technology Corporation @ Unm Heat shock response and virus replication
US7538097B2 (en) * 2000-09-26 2009-05-26 Halozyme, Inc. Inhibition of antigen presentation with poorly catabolized polymers
US20040102367A1 (en) * 2001-02-23 2004-05-27 Gage Fred H Gene expression system based on chimeric receptors
WO2002070473A2 (en) * 2001-03-05 2002-09-12 Transtech Pharma, Inc. Carboxamide derivatives as therapeutic agents
JP2004523565A (ja) * 2001-03-05 2004-08-05 トランス　テック　ファーマ，インコーポレイテッド 治療因子としてのベンゾイミダゾール誘導体
WO2002070667A2 (en) * 2001-03-05 2002-09-12 Transtech Pharma, Inc. High level insect expression of rage proteins
US7294472B2 (en) * 2001-03-14 2007-11-13 Caden Biosciences Method for identifying modulators of G protein coupled receptor signaling
US7208279B2 (en) * 2001-03-14 2007-04-24 Caden Biosciences, Inc. Method for identifying inhibitors of G protein coupled receptor signaling
ITMI20010733A1 (it) 2001-04-05 2002-10-05 Recordati Chem Pharm Uso di inibitori dell'isoenzina cox-2 per il trattamento dell'incontinenza urinaria
US6727287B2 (en) 2001-04-16 2004-04-27 Pts International, Inc. Toluene sulfonamide-containing anti-tumor composition and method of use thereof
US6632217B2 (en) * 2001-04-19 2003-10-14 Microsolutions, Inc. Implantable osmotic pump
CN1157388C (zh) * 2001-05-29 2004-07-14 北京大学 哌嗪基二硫代甲酸酯类化合物,它们的制备方法和在抗肿瘤药物中的应用
RU2259825C9 (ru) 2001-06-18 2006-04-10 БиоДием Лимитед Вещества, проявляющие антимикробную, антигрибковую, антипротозойную активности
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
AU2002322515A1 (en) * 2001-07-17 2003-03-03 Keith Choate Compositions, methods, and kits related to treating and diagnosing hypertension
US6884619B2 (en) 2001-07-17 2005-04-26 Yale University Inhibition of BEHAB cleavage and primary central nervous system (CNS) tumors
GB0119396D0 (en) * 2001-08-09 2001-10-03 Celltech R&D Ltd Hydroxamic acid derivatives
US9056048B2 (en) * 2001-08-16 2015-06-16 The Trustees Of The University Of Pennsylvania Synthesis and use of cationic steroids for anti-inflammatory drug therapy
DE60236520D1 (de) * 2001-08-16 2010-07-08 Univ Pennsylvania Synthese und verwendung von reagenzien für die verbesserte dna-lipofektion und/oder prodrug- und arzneimitteltherapien mit langsamer freisetzung
US20050042303A1 (en) * 2001-08-27 2005-02-24 Brown Tracey Jean Therapeutic protocols
US20030069071A1 (en) * 2001-09-28 2003-04-10 Tim Britt Entertainment monitoring system and method
WO2003033526A2 (en) 2001-10-19 2003-04-24 Isotechnika Inc. Synthesis of cyclosporin analogs
US6555563B1 (en) 2001-11-16 2003-04-29 Medinox, Inc. Heteroaryl substituted amidinyl and imidazolyl compounds and methods employing same for the treatment of inflammation
US7871619B2 (en) * 2001-11-30 2011-01-18 Chemocentryx, Inc. Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors
US7442512B2 (en) * 2001-11-30 2008-10-28 Chemocentryx, Inc. Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors
US7413866B2 (en) * 2001-11-30 2008-08-19 Chemocentryx, Inc. Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors
US7253007B2 (en) * 2001-11-30 2007-08-07 Chemocentryx, Inc. Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors
PE20030701A1 (es) * 2001-12-20 2003-08-21 Schering Corp Compuestos para el tratamiento de trastornos inflamatorios
WO2003055482A1 (en) 2001-12-21 2003-07-10 Novo Nordisk A/S Amide derivatives as gk activators
AR038136A1 (es) 2002-01-24 2004-12-29 Merck Frosst Canada Inc Cicloalcanindoles con sustitucion con fluor composiciones que contienen estos compuestos y metodos de tratamiento
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US20030175346A1 (en) * 2002-02-01 2003-09-18 Anne Billotte Osmotic delivery system
US20030161882A1 (en) * 2002-02-01 2003-08-28 Waterman Kenneth C. Osmotic delivery system
US7378111B2 (en) * 2002-02-20 2008-05-27 The Trustees Of The University Of Pennsylvania Regulation of GSK-3α activity for the treatment or prevention of Alzheimer's disease
EP1482931B1 (en) * 2002-03-05 2011-10-19 TransTech Pharma, Inc. Mono- and bicyclic azole derivatives that inhibit the interaction of ligands with rage
AU2003221706B2 (en) 2002-04-11 2008-02-28 Merck Sharp & Dohme Corp. 1H-Benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators
US7622117B2 (en) * 2002-04-17 2009-11-24 Dynamis Therapeutics, Inc. 3-deoxyglucosone and skin
US7378438B2 (en) * 2002-04-19 2008-05-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Beta-agonist compounds comprising nitric oxide donor groups and reactive oxygen species scavenger groups and their use in the treatment of respiratory disorders
CA2484797A1 (en) * 2002-05-06 2003-11-13 Washington University Methods of treatment of glaucoma and other conditions mediated by nos-2 expression via inhibition of the egfr pathway
US20080051428A1 (en) * 2002-05-15 2008-02-28 Davis Paul J Pyrroloquinoline quinone drugs and methods of use thereof
AUPS234402A0 (en) * 2002-05-15 2002-06-13 Auckland Uniservices Limited Anti-tumour polycyclic carboxamides
EP2399903A1 (en) 2002-05-24 2011-12-28 Millennium Pharmaceuticals, Inc. Ccr9 inhibitors and methods of use thereof
US7589199B2 (en) 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
US7842693B2 (en) * 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
US20050256130A1 (en) * 2002-06-12 2005-11-17 Chemocentryx, Inc. Substituted piperazines
MXPA04012393A (es) 2002-06-12 2005-06-17 Chemocentryx Derivados de piperazina 1-aril-4-substituidos para utilizar como antagonistas ccr1 para tratamiento de inflamacion y desordenes inmunes.
US6727241B2 (en) 2002-06-12 2004-04-27 Chemocentryx Anti-inflammatory compositions and methods of use
US6620813B1 (en) 2002-06-21 2003-09-16 Medinox, Inc. Hydroxamate derivatives of non-steroidal anti-inflammatory drugs
US20040077691A1 (en) * 2002-06-21 2004-04-22 Medinox, Inc. Hydroxamate derivatives of non-steroidal anti-inflammatory drugs
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
EP1558585B1 (en) 2002-10-04 2013-09-25 Prana Biotechnology Limited Neurologically-active compounds
WO2004037206A2 (en) * 2002-10-23 2004-05-06 University Of Hawaii Methods for diagnosing and treating pre-term labor
AU2003278565A1 (en) * 2002-10-25 2004-05-13 Yissum Research Development Company Of The Hebrew University Of Jerusalem Steroid compounds comprising superoxide dismutase mimic groups and nitric oxide donor groups, and their use in the preparation of medicaments
AU2003284984B2 (en) 2002-10-30 2008-10-23 Merck Sharp & Dohme Corp. Gamma-aminoamide modulators of chemokine receptor activity
ATE468114T1 (de) 2002-11-08 2010-06-15 High Point Pharmaceuticals Llc Sichere chemische entkuppler zur behandlung von fettsucht
US20050143449A1 (en) * 2002-11-15 2005-06-30 The Salk Institute For Biological Studies Non-steroidal farnesoid X receptor modulators and methods for the use thereof
US7741519B2 (en) 2007-04-23 2010-06-22 Chemocentryx, Inc. Bis-aryl sulfonamides
AU2003298661B2 (en) 2002-11-18 2007-05-10 Chemocentryx, Inc. Aryl sulfonamides
US20070021466A1 (en) * 2002-11-18 2007-01-25 Solomon Ungashe CCR2 inhibitors and methods of use thereof
US7420055B2 (en) 2002-11-18 2008-09-02 Chemocentryx, Inc. Aryl sulfonamides
US7227035B2 (en) * 2002-11-18 2007-06-05 Chemocentryx Bis-aryl sulfonamides
RU2342388C2 (ru) * 2002-11-22 2008-12-27 Джапан Тобакко Инк. Конденсированные бициклические азотсодержащие гетероциклы, обладающие dgat ингибирующим действием
US20060166894A1 (en) * 2002-11-29 2006-07-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ace-inhibitors having antioxidant and no-donor activity
MXPA05006507A (es) * 2002-12-20 2006-02-17 Chemocentryx Inhibidores de ccxckr2 expresado en tumor humano.
ATE404543T1 (de) 2002-12-20 2008-08-15 Sosei R & D Ltd Benzoxazocine und ihre verwendung als monoamin- wiederaufnahme inhibitoren
US8337861B2 (en) * 2003-01-09 2012-12-25 The Trustees Of The University Of Pennsylvania Compositions, methods and kits for enhancing the immunogenicity of a bacterial vaccine vector
AU2003900927A0 (en) * 2003-02-28 2003-03-13 Biodiem Ltd Growth promotion method
JP2006523214A (ja) * 2003-03-21 2006-10-12 ジユーリー，マデレーン・エム タマンダリン類似物およびこれらのフラグメントそして製造方法および使用方法
ATE482747T1 (de) 2003-04-11 2010-10-15 High Point Pharmaceuticals Llc Neue amide derivate und deren pharmazeutische verwendungen
JO2355B1 (en) 2003-04-15 2006-12-12 ميرك شارب اند دوم كوربوريشن Hereditary calcitonin polypeptide receptor antagonists
WO2004100929A1 (en) 2003-05-12 2004-11-25 Synergia Pharma, Inc. Threo-dops controlled release formulation
US8158149B2 (en) * 2004-05-12 2012-04-17 Chelsea Therapeutics, Inc. Threo-DOPS controlled release formulation
AR041089A1 (es) 2003-05-15 2005-05-04 Merck & Co Inc Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas
CN1805743A (zh) * 2003-05-20 2006-07-19 特兰斯泰克制药公司 用作逆转淀粉样变性及其他与之相关疾病的rage拮抗剂
CN102358738A (zh) 2003-07-30 2012-02-22 里格尔药品股份有限公司 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途
JP2007501801A (ja) * 2003-08-07 2007-02-01 日本たばこ産業株式会社 ピロロ［１，２−ｂ］ピリダジン誘導体
JP2007501813A (ja) 2003-08-08 2007-02-01 ノボ　ノルディスク　アクティーゼルスカブ 新生血管形成と関連した症状を治療および診断するためのインターロイキン−２０
WO2005025513A2 (en) * 2003-09-12 2005-03-24 The Regents Of The Univeristy Of California Guanidinium derivatives for improved cellular transport
WO2005033297A1 (en) * 2003-09-19 2005-04-14 The Rockefeller University Compositions, methods and kits relating to reprogramming adult differentiated cells and production of embryonic stem cell-like cells
MXPA06003474A (es) 2003-09-30 2006-06-05 Novo Nordisk As Agonistas de receptores de melanocortina.
ES2428358T3 (es) 2003-10-17 2013-11-07 Novo Nordisk A/S Terapia de combinación
US20100247540A1 (en) * 2003-10-30 2010-09-30 Chemocentryx, Inc. Methods and Compositions For Modulating Angiogenesis
JP2007514665A (ja) * 2003-12-12 2007-06-07 ミオゲン インコーポレイティッド エノキシモン製剤ならびに心肥大および心不全の治療へのそれらの使用方法
WO2005058842A1 (en) * 2003-12-15 2005-06-30 Laboratoire Theramex 1-n-phenyl-amino-1h-imidazole derivatives and pharmaceutical compositions containing them
PT1723128E (pt) 2004-01-06 2013-02-27 Novo Nordisk As Heteroaril-ureias e o seu uso como activadores da glicoquinase
CN1950082B (zh) * 2004-03-03 2013-02-06 凯莫森特里克斯股份有限公司 双环和桥连的含氮杂环化物
US7435831B2 (en) * 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
US20060003020A1 (en) * 2004-03-11 2006-01-05 The Regents Of The University Of Michigan Anti-metastatic ability of mibefradil and gadolinium
CA2559211A1 (en) 2004-03-19 2005-09-29 Yale University Detection, isolation and uses of renalase (monoamine oxidase c)
CA2560538A1 (en) * 2004-03-22 2005-10-06 Myogen, Inc. (r)-enoximone sulfoxide and its use in the treatment of pde-iii mediated diseases
WO2005092332A1 (en) * 2004-03-22 2005-10-06 Myogen, Inc. (s) - enoximone sulfoxide and its use in the treatment of pde-iii mediated diseases
US7169807B2 (en) * 2004-04-09 2007-01-30 Allergan, Inc. 10-Hydroxy-11-dihydroprostaglandin analogs as selective EP4 agonists
NZ551775A (en) 2004-06-01 2010-12-24 Univ Virginia Dual small molecule inhibitors of cancer and angiogenesis
RU2007101074A (ru) 2004-06-14 2008-07-20 Зозер Б. САЛАМА (DE) Фармацевтическая противораковая композиция пролина или его производных и противоопухолевого антитела
US7740861B2 (en) * 2004-06-16 2010-06-22 University Of Massachusetts Drug delivery product and methods
CA2572179A1 (en) * 2004-06-23 2006-01-19 Myogen, Inc. Enoximone formulations and their use in the treatment of pde-iii mediated diseases
CA2571409C (en) * 2004-06-24 2012-01-24 Wisconsin Alumni Research Foundation Neoglycorandomization and digitoxin analogs
US8507411B2 (en) * 2004-06-24 2013-08-13 Wisconsin Alumni Research Foundation Neoglycorandomization and digitoxin analogs
CA2571782C (en) * 2004-07-02 2012-07-03 Allergan, Inc. Prostaglandin analogs
AP2007003893A0 (en) * 2004-08-03 2007-02-28 Transtech Pharma Inc Rage fusion proteins and methods of use
US7183310B2 (en) * 2004-08-10 2007-02-27 Allergan, Inc. Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents
US7101904B2 (en) * 2004-08-10 2006-09-05 Allergan, Inc. Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents
US7906552B2 (en) 2004-08-10 2011-03-15 Allergan, Inc. Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents
US20080096927A1 (en) 2004-08-24 2008-04-24 Simon Thomas J Combination Therapy for Treating Cyclooxygenase-2 Mediated Diseases or Conditions in Patients at Risk of Thrombotic Cardiovascular Events
ES2375995T3 (es) * 2004-09-17 2012-03-08 University Of Massachusetts Composiciones y sus usos para deficiencias de enzima lisosomal.
WO2006039252A2 (en) * 2004-10-01 2006-04-13 Merck & Co., Inc. Compositions and methods for treating ophthalmic diseases
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
US7612082B2 (en) * 2004-10-28 2009-11-03 Allergan, Inc. Prostaglandin EP4 antagonists
US7101906B2 (en) * 2004-11-16 2006-09-05 Allergan, Inc. 2,3,4-substituted cyclopentanones as therapeutic agents
US7183324B2 (en) 2004-11-23 2007-02-27 Allergan, Inc. 2,3,4-substituted cyclopentanones as therapeutic agents
US8148412B2 (en) 2004-12-03 2012-04-03 Novo Nordisk A/S Heteroaromatic glucokinase activators
US7091231B2 (en) * 2004-12-10 2006-08-15 Allergan, Inc. 12-Aryl prostaglandin analogs
US20080194548A1 (en) * 2005-01-06 2008-08-14 Forrest Michael J Drug Combination Therapy and Pharmaceutical Compositions for Treating Inflammatory Disorders
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
WO2006076644A2 (en) 2005-01-14 2006-07-20 Chemocentryx, Inc. Heteroaryl sulfonamides and ccr2
TWI386208B (zh) * 2005-04-18 2013-02-21 Allergan Inc 治療性的經取代環戊酮
ES2434852T3 (es) * 2005-04-21 2013-12-17 Chemocentryx, Inc. Anticuerpos que se unen a CCX-CKR2
AU2006285393A1 (en) 2005-04-27 2007-03-08 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of obesity and diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
BRPI0611257A2 (pt) * 2005-05-06 2010-08-24 Allergan Inc beta-lactamas substituÍdas e uso em medicina do mesmo
EP1721615A1 (en) 2005-05-09 2006-11-15 Komipharm International Co., Ltd. Pharmaceutical compositions comprising sodium or potassium arsenite for the treatment of urogenital cancer and its metastasis
PL1883394T3 (pl) 2005-05-23 2018-09-28 Sdg, Inc. Konstrukt lipidowy do dostarczania insuliny ssakowi
US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP1904457B1 (en) 2005-06-08 2017-09-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2612508A1 (en) * 2005-06-17 2006-12-28 Dynamis Therapeutics, Inc. Treatment of inflammatory conditions
US7777035B2 (en) 2005-06-22 2010-08-17 Chemocentryx, Inc. Azaindazole compounds and methods of use
JP2008546843A (ja) 2005-06-27 2008-12-25 アムゲン インコーポレイティッド 抗炎症性アリールニトリル化合物
WO2007005176A1 (en) * 2005-06-29 2007-01-11 Allergan, Inc. Pyrrolidinones for the treatment of glaucoma and ocular hypertension
BRPI0612996A2 (pt) 2005-07-14 2010-12-14 Novo Nordisk As ativadores de urÉia glucocinase
AU2006274509B2 (en) * 2005-07-27 2012-01-19 Alchemia Oncology Pty Limited Therapeutic protocols using hyaluronan
EP1948638B1 (en) 2005-08-12 2011-08-03 Schering Corporation Compounds for the treatment of inflammatory disorders
WO2007025166A2 (en) 2005-08-25 2007-03-01 Repair Technologies, Inc. Devices, compositions and methods for the protection and repair of cells and tissues
EP2325169B1 (en) * 2005-08-29 2015-10-07 University Of Virginia Patent Foundation Lisofylline analogues and their pharmeacuetical uses
US8871764B2 (en) 2005-08-29 2014-10-28 University Of Virginia Patent Foundation Lisofylline analogs and methods for use
CN101287475B (zh) 2005-09-07 2012-11-14 阿尔卡米亚肿瘤学股份有限公司 包含透明质酸和治疗抗体的治疗组合物以及制药用途
US20070178141A1 (en) * 2005-09-07 2007-08-02 Bebaas, Inc. Vitamin B12 compositions
US20130131007A1 (en) 2005-09-07 2013-05-23 Bebaas, Inc. Vitamin b12 compositions
EP1948245B1 (en) * 2005-10-24 2011-10-05 University of Massachusetts Compositions and their uses for gene therapy of bone conditions
ZA200804550B (en) 2005-11-09 2009-08-26 Combinatorx Inc Methods, compositions, and kits for the treatment of medical conditions
DE602006018057D1 (de) 2005-11-10 2010-12-16 Chemocentryx Inc Substituierte chinolone und verwendungsverfahren
US7585895B2 (en) * 2005-12-06 2009-09-08 Allergan, Inc. Therapeutic substituted cyclopentanes
US7427685B2 (en) 2005-12-06 2008-09-23 Allergan, Inc. Therapeutic substituted cyclopentanes
CA2634437A1 (en) * 2005-12-20 2007-07-05 Gilead Colorado, Inc. 4,7-dihydrothieno¬2,3-b|pyridine compounds and pharmaceutical compositions
US7323477B2 (en) * 2006-02-02 2008-01-29 Allergan, Inc. 7-((1H-imidazol-4-yl)methyl)-5,6,7,8-tetrahydroquinoline
WO2007098240A2 (en) * 2006-02-21 2007-08-30 Astrum Therapeutics Pty. Ltd. Compositions to reduce blood glucose levels and treat diabetes
JP2009528295A (ja) * 2006-02-24 2009-08-06 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋ経路の阻害のための組成物および方法
EP1864692A1 (en) * 2006-06-07 2007-12-12 Biotempt B.V. Use of peptides for the control of radiation injury
WO2007109578A2 (en) 2006-03-20 2007-09-27 Allergan, Inc. Substituted gamma lactams as prostaglandin ep2 agonists
US20070225246A1 (en) * 2006-03-27 2007-09-27 Denu John M O-acetyl-ADP-ribose non-hydrolyzable analogs
PE20071221A1 (es) * 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
ES2354390T3 (es) * 2006-04-11 2011-03-14 Arena Pharmaceuticals, Inc. Procedimientos de uso del receptor gpr119 para identificar compuestos útiles para aumentar la masa ósea en un individuo.
BRPI0722382A2 (pt) 2006-04-14 2012-06-05 Prana Biotechnology Ltd compostos úteis para o tratamento de cáncer
US20090016981A1 (en) 2006-05-03 2009-01-15 Allergan, Inc. Therapeutic compounds
US7439372B2 (en) 2006-05-03 2008-10-21 Allergan, Inc. Therapeutic compounds
US7476755B2 (en) 2006-05-04 2009-01-13 Allergan, Inc. Therapeutic compounds
BRPI0711352A2 (pt) 2006-05-09 2011-09-27 Merck & Co Inc composto, composição farmacêutica, e, métodos para o antagonismo de atividade receptora de cgrp em um mamìfero, e para, tratar, controlar, melhorar ou reduzir o risco de dor de cabeça, enxaqueca , ou cefaléia vascular
US7547727B2 (en) 2006-05-22 2009-06-16 Allergan, Inc. Therapeutic cyclopentane derivatives
US7550448B2 (en) * 2006-05-24 2009-06-23 Allergan, Inc. Therapeutic compounds
US7553860B2 (en) * 2006-06-14 2009-06-30 Allergan, Inc. Substituted gamma lactams as therapeutic agents
MX2008016411A (es) 2006-07-05 2009-04-28 Aventis Agriculture Compuestos derivados de 1-aril-5-alquil pirazol, procesos para hacerlos y metodos para usarlos.
AU2007272683B2 (en) 2006-07-10 2012-08-23 Allergan, Inc. Substituted cyclopentane derivatives as therapeutic agents
US8519135B2 (en) * 2006-07-14 2013-08-27 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2/CCR9
AU2007275873B2 (en) 2006-07-14 2012-06-14 Chemocentryx, Inc. Triazolyl phenyl benzenesulfonamides
US7700627B2 (en) * 2006-07-26 2010-04-20 Allergan, Inc. Therapeutic substituted lactams
JP5322935B2 (ja) 2006-07-31 2013-10-23 アクティベサイト ファーマシューティカルズ インコーポレイティッド 血漿カリクレインの阻害薬
WO2009137544A1 (en) * 2008-05-09 2009-11-12 Allergan, Inc. Therapeutic substituted thiazolidinones, oxazolidinones, and related compounds
US7985767B2 (en) * 2006-09-06 2011-07-26 Allergan, Inc. Therapeutic amides
US7687526B2 (en) 2006-09-07 2010-03-30 Amgen Inc. Benzo-fused compounds for use in treating metabolic disorders
EP2076525A2 (en) * 2006-10-06 2009-07-08 Wisconsin Alumni Research Foundation Colchicine neoglycosides and methods for their synthesis and use
JP2010505957A (ja) 2006-10-10 2010-02-25 アムゲン インコーポレイティッド 糖尿病に対して使用されるｎ−アリールピラゾール化合物
EP1920782A1 (en) 2006-11-10 2008-05-14 Glycotope Gmbh Carboyhdrate specific cellular immunity inducing microorganisms and fractions thereof
US8193373B2 (en) 2006-12-11 2012-06-05 Allergan, Inc. Therapeutic compounds
GB0624757D0 (en) 2006-12-12 2007-01-17 Sosei R & D Ltd Novel compounds
JP2010513569A (ja) 2006-12-19 2010-04-30 ユニバーシティ オブ バージニア パテント ファウンデーション アルコール摂取に対するトピラメートおよびオンダンセトロンの併用効果
US20080153808A1 (en) * 2006-12-22 2008-06-26 Allergan, Inc. Alpha-2 receptor pan agonist and serotonin-norepinephrine reuptake inhibitor compositions for treating chronic pain
US20080153927A1 (en) * 2006-12-22 2008-06-26 Allergan, Inc. Alpha-2b receptor agonist and relaxant compositions for treating gastrointestinal motility disorders
US20080153880A1 (en) * 2006-12-22 2008-06-26 Allergan, Inc. Pan-alpha-2 receptor agonist and acid reducer compositions for treating gastrointestinal motility disorders
US20080153832A1 (en) * 2006-12-22 2008-06-26 Allergan, Inc. Pan-alpha-2 receptor agonist and relaxant compositions for treating gastrointestinal motility disorders
US20120083508A1 (en) 2006-12-22 2012-04-05 Allergan, Inc. Alpha-2b receptor agonist and anticonvulsant compositions for treating chronic pain
US20080153874A1 (en) * 2006-12-22 2008-06-26 Allergan Inc. Alpha-2b receptor agonist and anticonvulsant compositions for treating chronic pain
US20080153825A1 (en) * 2006-12-22 2008-06-26 Allergan Inc. Alpha-2b receptor agonist and 5ht4 serotonin receptor compositions for treating gastrointestinal motility disorders
ES2526398T3 (es) 2006-12-22 2015-01-12 Allergan, Inc. Composiciones inhibidoras de la recaptación de serotonina-norepinefrina para tratar el dolor crónico
US20080153881A1 (en) * 2006-12-22 2008-06-26 Allergan, Inc. Alpha-2b receptor agonist and acid reducer compositions for treating gastrointestinal motility disorders
WO2008082217A1 (en) * 2006-12-28 2008-07-10 Lg Electronics Inc. Ice making system and method for ice making of refrigerator
AU2008204530B2 (en) 2007-01-11 2013-08-01 Vtv Therapeutics Llc Urea glucokinase activators
US20100221337A1 (en) * 2007-02-14 2010-09-02 Logical Therapeutics, Inc. Method of treating arthritis, pain or inflammation with naproxen 2(methanesulfonyl)ethyl ester and an h2 receptor antagonist
JP2010520236A (ja) 2007-02-28 2010-06-10 ユニバーシティ オブ バージニア パテント ファンデーション リソフィリンアナログとその使用法
US8563594B2 (en) * 2007-05-08 2013-10-22 Allergan, Inc. S1P3 receptor inhibitors for treating pain
PL3088384T3 (pl) 2007-05-15 2019-06-28 Merial, Inc. Związki aryloazol-2-ilo-cyjanoetyloaminowe, sposób ich wytwarzania oraz sposób ich stosowania
NZ581405A (en) 2007-05-22 2011-06-30 Chemocentryx Inc 3-(Imidazolyl)-pyrazolo[3,4-b]pyridines and their use in treating CCR1-mediated disorders
AU2008266960A1 (en) 2007-06-20 2008-12-24 Merck Sharp & Dohme Corp. Diphenyl substituted alkanes
US7776877B2 (en) 2007-06-22 2010-08-17 Chemocentryx, Inc. N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl) hetaryl arylsulfonamides
CN101820881B (zh) 2007-07-12 2013-05-01 坎莫森特里克斯公司 作为ccr2调节剂用于治疗炎症的稠合杂芳基吡啶基和苯基苯磺酰胺
WO2009012425A2 (en) * 2007-07-19 2009-01-22 Logigal Therapeutics, Inc. Compositions including leukotriene antagonists and nsaids and methods of using the same
EP2183227B1 (en) 2007-08-07 2014-09-24 Prosarix Limited 1,2,4-triazole derivatives as serotonergic modulators
US8962015B2 (en) 2007-09-28 2015-02-24 Sdg, Inc. Orally bioavailable lipid-based constructs
US8846053B2 (en) 2008-09-26 2014-09-30 Sdg, Inc. Orally bioavailable lipid-based constructs
ES2552764T3 (es) 2007-10-15 2015-12-02 The Salk Institute For Biological Studies Métodos para el tratamiento de varias enfermedades y afecciones, y compuestos útiles para los mismos
WO2009052073A2 (en) * 2007-10-18 2009-04-23 Allergan, Inc. Method of treating sensorimotor disorders with alpha-2 adrenergic receptor agonists
WO2009052075A2 (en) * 2007-10-18 2009-04-23 Allergan, Inc. Method of treating motor disorders with alpha-2b adrenergic receptor agonists
US20100216857A1 (en) * 2007-10-18 2010-08-26 Luhrs Lauren M B Method of treating motor disorders with 4-(1-(2,3-dimethylphenyl)ethyl)-1h-imidazole-2(3h)-thione
EP2222283A2 (en) * 2007-10-29 2010-09-01 University of Massachusetts Yeast cell wall protein (ycwp) encapsulated multilayered nanoparticles for nucleic acid delivery (sirna)
US8063033B2 (en) * 2008-01-18 2011-11-22 Allergan, Inc. Therapeutic beta-lactams
US7956051B2 (en) * 2008-01-24 2011-06-07 Allergan, Inc. Therapeutic amides and related compounds
US8633310B2 (en) * 2008-02-19 2014-01-21 Allergan, Inc. Therapeutic substituted lactams
US8202855B2 (en) 2008-03-04 2012-06-19 Allergan, Inc Substituted beta-lactams
US7964596B2 (en) * 2008-03-07 2011-06-21 Allergan, Inc. Therapeutic compounds
US20090233921A1 (en) * 2008-03-11 2009-09-17 Allergan, Inc. Therapeutic cyclopentane derivatives
US7960379B2 (en) * 2008-03-14 2011-06-14 Allergan, Inc. Therapeutic compounds
JP2011514385A (ja) * 2008-03-17 2011-05-06 アラーガン、インコーポレイテッド 炎症を処置するためのｓ１ｐ３受容体阻害剤
US8198318B2 (en) * 2008-03-18 2012-06-12 Allergen, Inc. Therapeutic amides
US7732443B2 (en) * 2008-03-18 2010-06-08 Yariv Donde Therapeutic substituted cyclopentanes
US7960378B2 (en) * 2008-03-18 2011-06-14 Allergan, Inc. Therapeutic compounds
US7705001B2 (en) * 2008-03-18 2010-04-27 Allergan, Inc Therapeutic substituted gamma lactams
US7956055B2 (en) * 2008-03-25 2011-06-07 Allergan, Inc. Substituted gamma lactams as therapeutic agents
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
WO2009131957A2 (en) 2008-04-21 2009-10-29 Institute For Oneworld Health Compounds, compositions and methods comprising oxadiazole derivatives
WO2009131958A2 (en) * 2008-04-21 2009-10-29 Institute For Oneworld Health Compounds, compositions and methods comprising triazine derivatives
US8236838B2 (en) * 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
US20090270398A1 (en) * 2008-04-21 2009-10-29 Institute For Oneworld Health Compounds, Compositions and Methods Comprising Pyridazine Derivatives
EP2297084A1 (en) * 2008-04-24 2011-03-23 Allergan, Inc. Therapeutic compounds
US7737140B2 (en) * 2008-04-24 2010-06-15 Allergan, Inc. Therapeutic compounds
JP2011518834A (ja) 2008-04-24 2011-06-30 アラーガン インコーポレイテッド 治療剤としての置換ガンマラクタム
US7964634B2 (en) * 2008-04-24 2011-06-21 Allergan, Inc. Therapeutic compounds
WO2009132088A1 (en) * 2008-04-24 2009-10-29 Allergan, Inc. Substituted gamma lactams as therapeutic agents
WO2010033626A1 (en) * 2008-09-19 2010-03-25 Institute For Oneworld Health Compounds, compositions and methods comprising imidazole and triazole derivatives
US7964599B2 (en) * 2008-05-09 2011-06-21 Allergan, Inc. Therapeutic compounds
WO2009137411A1 (en) * 2008-05-09 2009-11-12 Allergan, Inc. Therapeutic compounds
CA2723894A1 (en) 2008-05-09 2009-11-12 Allergan, Inc. Therapeutic substituted hydantoins, and related compounds
EP2285782A2 (en) * 2008-05-09 2011-02-23 Allergan, Inc. Therapeutic n-aryl or n-heteroaryl pyrazolidine and pyrazolidinone derivatives
CA2728227A1 (en) * 2008-05-09 2009-11-12 Allergan, Inc. Therapeutic cyclopentane derivatives
US8569349B2 (en) * 2008-05-09 2013-10-29 Allergan, Inc. Therapeutic compounds
AU2009249388B2 (en) * 2008-05-20 2014-04-03 Allergan, Inc. Therapeutic lactams
WO2009142967A1 (en) * 2008-05-20 2009-11-26 Allergan, Inc. Therapeutic prostaglandin compounds used as ocular hypotensive agents
CA2724605A1 (en) * 2008-05-27 2009-12-03 Allergan, Inc. Prostaglandin prodrugs as hypotensive agents
EP2299813B1 (en) 2008-06-12 2015-12-16 Merck Sharp & Dohme Corp. Branched 3- and 6-substituted quinolines as cgrp receptor antagonists
US20100022574A1 (en) * 2008-07-28 2010-01-28 EndogenX, Inc. Methods to Treat Pain Using an Alpha-2 Adrenergic Agonist and an Endothelin Antagonist
WO2010012650A1 (en) 2008-07-28 2010-02-04 Syddansk Universitet Compounds for the treatment of metabolic diseases
US8404736B2 (en) 2008-08-14 2013-03-26 Beta Pharma Canada Inc. Heterocyclic amide derivatives as EP4 receptor antagonists
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
EP2186521A1 (en) 2008-11-14 2010-05-19 Mergemeier Steffen Compositons for the treatment and prevention of diseases involving bacterial, viral and fungal pathogens and fragments thereof with polyvinylpyrrolidone and/or polyvinylpolypyrrolidone as therapeutically active compound
PL3050874T3 (pl) 2008-11-14 2019-07-31 Merial Inc. Wzbogacone enancjomerycznie aryloazol-2-ilocyjanoetyloaminowe związki pasożytobójcze
SG171751A1 (en) 2008-11-19 2011-07-28 Merial Ltd Compositions comprising an aryl pyrazole and/ or a formamidine methods and uses thereof
MX2011005037A (es) 2008-11-21 2011-06-16 High Point Pharmaceuticals Llc Compuestos de adamantilo benzamida.
AR074482A1 (es) 2008-12-04 2011-01-19 Merial Ltd Derivados dimericos de avermectina y milbemicina
SMT202200074T1 (it) 2008-12-22 2022-03-21 Chemocentryx Inc Antagonisti di c5ar
PL2389372T3 (pl) 2009-01-23 2016-02-29 Rigel Pharmaceuticals Inc Kompozycje i sposoby hamowania szlaku JAK
US8785468B2 (en) 2009-02-13 2014-07-22 Amgen Inc. Phenylalanine amide derivatives useful for treating insulin-related diseases and conditions
WO2010093910A1 (en) 2009-02-13 2010-08-19 Allergan, Inc. 4-(1-(3-(hydroxymethyl)-2-methylphenyl)ethyl)-1h-imidazole-2(3h)-thione
EP2395999B1 (en) 2009-02-13 2017-09-13 Allergan, Inc. Pharmaceutical compositions comprising (3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl)methanol
US8394819B2 (en) 2009-02-24 2013-03-12 Merck Sharp & Dohme Corp. Indole derivatives as CRTH2 receptor antagonists
GB0904044D0 (en) 2009-03-09 2009-04-22 Sosei R & D Ltd The treatment of inflammatory disorders and pain
WO2010103038A1 (en) 2009-03-11 2010-09-16 Novo Nordisk A/S Interleukin-21 variants having antagonistic binding to the il-21 receptor
US8511216B2 (en) * 2009-03-30 2013-08-20 Kanzaki Kokyukoki Mfg. Co., Ltd. Hydraulic actuator unit
US20100256385A1 (en) * 2009-04-02 2010-10-07 Allergan, Inc. Prostaglandin e receptor antagonists
US8343976B2 (en) * 2009-04-20 2013-01-01 Institute For Oneworld Health Compounds, compositions and methods comprising pyrazole derivatives
JP2012526133A (ja) 2009-05-05 2012-10-25 ベイポジェニックス インコーポレイテッド 炎症を低減させるための新規揮発性麻酔薬製剤およびその使用法
RU2559083C9 (ru) 2009-05-19 2016-01-20 Неуродерм Лтд Композиции для непрерывного введения ингибиторов допа-декарбоксилазы
AU2010273977A1 (en) * 2009-07-17 2012-02-02 Allergan, Inc. Compositions comprising a cholinesterase inhibitor for treating cognitive disorders
CA2768543C (en) * 2009-07-28 2017-06-20 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
BR112012003284A8 (pt) 2009-08-11 2016-05-17 Allergan Inc isotiozóis para tratar condições dos olhos
JP2013502587A (ja) * 2009-08-20 2013-01-24 ティダブリューアイ・バイオテクノロジー・インコーポレイテッド 糖尿病の診断および治療効果の決定方法
EP2470181A1 (en) 2009-08-26 2012-07-04 Allergan, Inc. Method of treating compulsive disorders with alpha-2b adrenergic receptor agonists
BR112012004335A8 (pt) 2009-09-02 2016-06-21 Merck Sharp & Dohme Composto, composição farmacêutica, e, uso do composto.
WO2011034951A2 (en) 2009-09-15 2011-03-24 The Regents Of The University Of California Assisted enzyme replacement therapy
WO2011035332A1 (en) 2009-09-21 2011-03-24 Chemocentryx, Inc. Pyrrolidinone carboxamide derivatives as chemerin-r ( chemr23 ) modulators
CA2772797C (en) 2009-09-30 2018-09-25 Transtech Pharma, Inc. Substituted imidazole derivatives
ES2549924T3 (es) 2009-11-25 2015-11-03 Cytometix, Inc. Análogos de ácido araquidónico y métodos para tratamiento analgésico usando el mismo
WO2011069143A1 (en) 2009-12-04 2011-06-09 Merial Limited Pesticidal bis-organosulfur compounds
EP2512467A1 (en) 2009-12-17 2012-10-24 Merial Limited Compositions comprising macrocyclic lactone compounds and spirodioxepinoindoles
ME02432B (me) 2009-12-17 2016-09-20 Merial Inc Antiparazitska jedinjenja dihidroazola i kompozicije koje ih sadrže
CA2784799C (en) 2009-12-30 2014-06-10 Shanghai Fochon Pharmaceutical Co Ltd Certain dipeptidyl peptidase inhibtors
US9090584B2 (en) * 2010-01-26 2015-07-28 Allergan, Inc. Therapeutic agents for treatment of ocular hypertension
US20130102591A1 (en) 2010-01-26 2013-04-25 Andrew Lurie Salzman Compositions and methods for prevention and treatment of pulmonary hypertension
US8299068B2 (en) 2010-01-29 2012-10-30 Allergan, Inc. Therapeutically active cyclopentanes
CN102791258B (zh) 2010-02-03 2018-05-08 图必制药公司 雷沙吉兰的延长释放制剂及其用途
GB201002530D0 (en) 2010-02-15 2010-03-31 Univ Wolverhampton The Di-aspirin derivatives
ES2679918T3 (es) 2010-02-18 2018-08-31 Vtv Therapeutics Llc Derivados de imidazol condensados sustituidos, composiciones farmacéuticas y métodos de uso de los mismos
TWI510241B (zh) 2010-02-18 2015-12-01 Vtv Therapeutice Llc 苯基－雜芳基衍生物及其使用方法
EP2538783B1 (en) 2010-02-22 2016-06-01 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
JP6155187B2 (ja) 2010-03-30 2017-06-28 ヴァーセオン コーポレイション トロンビンの阻害剤としての多置換芳香族化合物
UA108641C2 (uk) 2010-04-02 2015-05-25 Паразитицидна композиція, яка містить чотири активних агенти, та спосіб її застосування
WO2011130716A2 (en) 2010-04-16 2011-10-20 Access Pharmaceuticals, Inc. A nanostructures containing vitamin b12 for facilitated delivery of drugs across biological barriers
CN103068390A (zh) 2010-04-20 2013-04-24 寰宇一家健康研究所 包含哒嗪磺酰胺衍生物的化合物、组合物和方法
EP2560643A1 (en) 2010-04-20 2013-02-27 Institute for OneWorld Health Compounds, compositions and methods comprising 1,3,4-oxadiazole derivatives
EP2569307A2 (en) 2010-05-10 2013-03-20 Radikal Therapeutics Inc. Lipoic acid and nitroxide derivatives and uses thereof
US8980929B2 (en) 2010-05-21 2015-03-17 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
NZ603614A (en) 2010-05-26 2014-10-31 Transtech Pharma Llc Use of metformin in combination with a glucokinase activator and compositions comprising metformin and a glucokinase activator
ES2664872T3 (es) 2010-06-18 2018-04-23 Taiho Pharmaceutical Co., Ltd Moduladores PRPK-TPRKB y sus usos
HRP20171176T1 (hr) 2010-06-24 2017-10-06 Chemocentryx, Inc. C5ar antagonisti
CA2803920A1 (en) 2010-06-24 2011-12-29 Richard Beard Derivatives of cycloalkyl- and cycloalkenyl-1,2-dicarboxylic acid compounds having formyl peptide receptor like-1 (fprl-1) agonist or antagonist activity
US8859606B2 (en) 2010-07-01 2014-10-14 Allergan, Inc. Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response
US8492424B2 (en) 2010-07-01 2013-07-23 Allergan, Inc. Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response
US9714238B2 (en) 2010-07-02 2017-07-25 Allergan, Inc. Therapeutic agents for ocular hypertension
WO2012003145A2 (en) 2010-07-02 2012-01-05 Allergan, Inc. Therapeutic agents for ocular hypertension
HUE035574T2 (en) 2010-07-02 2018-05-28 Univ Virginia Patent Foundation Molecular genetic approach to treatment and diagnosis of alcohol and drug dependence
KR101937495B1 (ko) 2010-07-28 2019-01-10 리겔 파마슈티칼스, 인크. Ｊａｋ 경로의 억제를 위한 조성물 및 방법
US20130303497A1 (en) 2010-08-05 2013-11-14 Conrig Pharma Aps Deuterated 5-ht1a receptor agonists
EP2605771B1 (en) 2010-08-16 2018-04-04 Allergan, Inc. Method of activating regulatory t cells with alpha-2b adrenergic receptor agonists
AR082492A1 (es) 2010-08-20 2012-12-12 Allergan Inc N-alquil-2-(1-(5-sustituido-2-(3-oxo-3-(trifluorometilsulfonamido)propil)bencil)pirrolidin-2-il)oxazol-4-carboxamida y su uso para preparar un medicamento util para tratar enfermedades o afecciones mediadas por receptor dp, fp, ep, ep, tp y/o ep
WO2012032513A1 (en) 2010-09-07 2012-03-15 Bar-Ilan University Boranophosphate derivatives for the treatment of osteoarthritis
WO2012032524A1 (en) 2010-09-09 2012-03-15 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Near infrared fluorescent particles and uses thereof
GB201016880D0 (en) 2010-10-07 2010-11-17 Riotech Pharmaceuticals Ltd Phosphodiesterase inhibitors
KR101825972B1 (ko) 2010-10-15 2018-02-06 콘테라 파르마 에이피에스 운동 장애 치료를 위한 세로토닌 수용체 작용제의 조합
WO2012058532A2 (en) 2010-10-28 2012-05-03 Yale University Methods and compositions for assessing and treating cancer
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
TWI522355B (zh) 2010-11-12 2016-02-21 默沙東藥廠 六氫吡啶酮甲醯胺氮雜茚滿ｃｇｒｐ受體拮抗劑
CN110123743A (zh) 2010-11-15 2019-08-16 纽罗德姆有限公司 L-多巴、多巴脱羧酶抑制剂、儿茶酚-o-甲基转移酶抑制剂及其组合物的连续施用
DK2640728T3 (en) 2010-11-16 2016-11-28 Merial Inc NEW MONENSINDERIVATER FOR TREATMENT AND PREVENTION OF protozoal INFECTIONS
DK2643470T3 (en) 2010-11-24 2016-05-17 Univ Yale Preparations and methods for treating ischemic injury with D-DT
WO2012070040A1 (en) 2010-11-26 2012-05-31 Technion Research And Development Foundation Ltd Compositions and methods for ameliorating renal dysfunction induced by renal hypoperfusion or acute kidney injury
CA2819457A1 (en) 2010-12-03 2012-06-07 Allergan, Inc. Pharmaceutical compositions comprising 3,4-dihydroisoquinolin-2(1h)-yl-3-phenylurea derivatives having formyl peptide receptor like-1 (fprl-1) agonist or antagonist activity
US8435993B2 (en) 2010-12-07 2013-05-07 Philadelphia Health And Education Corporation Methods of inhibiting metastasis from cancer
GB201020860D0 (en) 2010-12-09 2011-01-26 Univ Wolverhampton Disulfiram formulation and uses thereof
JP6144627B2 (ja) 2010-12-15 2017-06-07 コントラヴィア ファーマシューティカルズ、インク． アミノ酸１および３で修飾されたシクロスポリン類似体分子
WO2012087777A1 (en) 2010-12-22 2012-06-28 Merck Sharp & Dohme Corp. Fused heterocyclic indane carboxamide cgrp receptor antagonists
WO2012093383A1 (en) 2011-01-04 2012-07-12 Radikal Therapeutics Inc. Compositions and methods for treatment of sepsis and related conditions
US11759441B2 (en) 2011-01-07 2023-09-19 Anji Pharmaceuticals Inc. Biguanide compositions and methods of treating metabolic disorders
US9572784B2 (en) 2011-01-07 2017-02-21 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
PT2661266T (pt) 2011-01-07 2020-11-30 Anji Pharma Us Llc Terapias com base em ligandos do recetor quimiossensorial
US9480663B2 (en) 2011-01-07 2016-11-01 Elcelyx Therapeutics, Inc. Biguanide compositions and methods of treating metabolic disorders
US11974971B2 (en) 2011-01-07 2024-05-07 Anji Pharmaceuticals Inc. Compositions and methods for treating metabolic disorders
US8796338B2 (en) 2011-01-07 2014-08-05 Elcelyx Therapeutics, Inc Biguanide compositions and methods of treating metabolic disorders
US9211263B2 (en) 2012-01-06 2015-12-15 Elcelyx Therapeutics, Inc. Compositions and methods of treating metabolic disorders
KR20140026396A (ko) 2011-03-08 2014-03-05 어섹스 팔마큐티칼스 인코포레이티드 생물학적 막을 가로질러 활성물질의 전달을 위한 표적화된 나노담체 시스템
HRP20181286T1 (hr) 2011-03-10 2018-10-05 Rigel Pharmaceuticals, Inc. 2,4 supstituirani pirimidindiamini za uporabu kod diskoidnog lupusa
US8476221B2 (en) 2011-03-18 2013-07-02 Halimed Pharmaceuticals, Inc. Methods and compositions for the treatment of metabolic disorders
DK2937349T3 (en) 2011-03-23 2017-02-20 Amgen Inc CONDENSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3
GEP20166444B (en) 2011-04-06 2016-03-10 Medical College Of Wisconsin Epoxyeicosatrienoic acid analogs and methods of making and using the same
CN104470886A (zh) 2011-04-08 2015-03-25 赛丹思科大学 用于治疗代谢疾病的邻-氟取代的化合物
US9480751B2 (en) 2011-04-11 2016-11-01 Yeda Research And Development Co. Ltd. Albumin binding probes and drug conjugates thereof
WO2012142308A1 (en) 2011-04-13 2012-10-18 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
ES2647072T3 (es) 2011-04-18 2017-12-19 Max-Delbrück-Centrum Für Molekulare Medizin In Der Helmholtz-Gemeinschaft Niclosamida para el tratamiento de la metástasis en el cáncer
ES2579319T3 (es) 2011-05-04 2016-08-09 Balance Therapeutics, Inc. Derivados de pentilenotetrazol
US20140161827A1 (en) 2011-05-09 2014-06-12 University Of Virginia Patent Foundation Compositions and methods for treating cancer
AU2012262533A1 (en) 2011-05-27 2013-12-19 Allergan, Inc. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of visual system disorders
WO2012163365A1 (en) 2011-06-01 2012-12-06 Concit Pharma Aps Combinations of serotonin receptor agonists for treatment of movement disorders
US20120329873A1 (en) 2011-06-17 2012-12-27 Li yong-xin D-serine for the treatment of visual system disorders
WO2013003168A1 (en) 2011-06-27 2013-01-03 Merial Limited Novel insect-repellent coumarin derivatives, syntheses, and methods of use
US8946270B2 (en) 2011-06-27 2015-02-03 Merial Limited Amido-pyridyl ether compounds and compositions and their use against parasites
WO2013005216A1 (en) 2011-07-05 2013-01-10 Radikal Therapeutics Inc. Compositions and methods for treatment of renal ischemia-reperfusion injury
AU2012287338A1 (en) 2011-07-25 2014-02-27 Allergan, Inc. N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives as modulators of alpha 2 adrenergic receptors
US8609658B2 (en) 2011-07-27 2013-12-17 Allergan, Inc. N,N-dialkylalkylenyl esters, compositions thereof, and methods for use thereof
WO2013019169A1 (en) 2011-08-01 2013-02-07 Institute For Oneworld Health Phosphate prodrugs
WO2013036290A1 (en) 2011-09-09 2013-03-14 Yale University Compositions and methods for assessing and treating inflammatory diseases and disorders
US20130096173A1 (en) 2011-09-09 2013-04-18 Bankole A. Johnson Molecular genetic approach to treatment and diagnosis of alcohol and drug dependence
EP2758389B1 (en) 2011-09-22 2017-06-07 Merck Sharp & Dohme Corp. Pyrazole carboxamides as janus kinase inhibitors
EP2763535B1 (en) 2011-10-03 2017-06-07 Merck Sharp & Dohme Corp. Azaindoles as janus kinase inhibitors
US10980798B2 (en) 2011-11-03 2021-04-20 Taiwan Liposome Company, Ltd. Pharmaceutical compositions of hydrophobic camptothecin derivatives
CA2850955C (en) 2011-11-03 2019-11-19 Taiwan Liposome Company, Ltd. Pharmaceutical compositions of hydrophobic camptothecin derivatives
JP6249568B2 (ja) 2011-11-17 2017-12-20 メリアル インコーポレイテッド アリールピラゾールと置換イミダゾールを含む組成物、その使用方法
CN103202863A (zh) 2011-11-18 2013-07-17 善笙生物科技股份有限公司 一种用于预防或改善关节炎症状的药物组合物及其应用
WO2013078151A1 (en) 2011-11-21 2013-05-30 Allergan, Inc. Pharmaceutical compositions comprising 4-[1-(2,3-dimethylphenyl)ethyl]-3h-imidazole derivatives for treating retinal diseases
ES2648340T3 (es) 2011-12-01 2018-01-02 Chemocentryx, Inc. Benzoimidazoles y benzopirazoles substituidos como antagonistas de CCR(4)
JP6141864B2 (ja) 2011-12-01 2017-06-07 ケモセントリックス，インコーポレイティド Ｃｃｒ（４）アンタゴニストとしての置換アニリン
BR122020002199B1 (pt) 2011-12-02 2021-01-19 Merial, Inc. formulações de moxidectina injetável de ação prolongada e novas formas de cristal de moxidectina
WO2013085802A1 (en) 2011-12-06 2013-06-13 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
US9567328B2 (en) 2011-12-21 2017-02-14 Allergan, Inc. Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response
EP2794574B1 (en) 2011-12-21 2017-11-08 Allergan, Inc. Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response
EP2966064A1 (en) 2011-12-27 2016-01-13 Allergan, Inc. Pyrazole-3-carboxylic acid compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response
CA2862263C (en) 2011-12-27 2016-09-06 Allergan, Inc. Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response
MX2014008190A (es) 2012-01-06 2015-02-04 Elcelyx Therapeutics Inc Composiciones de biguanida y métodos para tratar transtornos metabólicos.
SG10201901922VA (en) 2012-01-06 2019-04-29 Elcelyx Therapeutics Inc Compositions and methods for treating metabolic disorders
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
RU2627268C2 (ru) 2012-02-29 2017-08-04 Хемоцентрикс, Инк. Аза-арил-1Н-пиразол-1-ил-сульфонамиды
NZ629898A (en) 2012-03-23 2016-04-29 Oxigene Inc Compositions and methods for inhibition of cathepsins
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
US20150057220A1 (en) 2012-04-16 2015-02-26 Kaneq Pharma Inc. Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors
EP2838520B1 (en) 2012-04-17 2017-12-13 University College Dublin National University Of Ireland, Dublin Thromboxane receptor antagonists
US9718781B2 (en) 2012-04-17 2017-08-01 University College Dublin, National University Of Ireland, Dublin Methods and compounds for treating proliferative disorders and viral infections
PT2838517T (pt) 2012-04-18 2018-01-04 Contera Pharma Aps Formulação farmacêutica disponível sob forma oral adequada para a melhoria da gestão dos distúrbios da mobilidade
WO2013169574A2 (en) 2012-05-09 2013-11-14 Merck Sharp & Dohme Corp. Aliphatic spirolactam cgrp receptor antagonists
US9227973B2 (en) 2012-05-09 2016-01-05 Merck Sharp & Dohme Corp. Pyridine CGRP receptor antagonists
EP2846799B1 (en) 2012-05-09 2017-11-15 Merck Sharp & Dohme Corp. Spirolactam cgrp receptor antagonists
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
WO2013190497A2 (en) 2012-06-21 2013-12-27 Radikal Therapeutics Inc. Compositions and methods for treatment of inflammatory diseases of the lung
US20140024621A1 (en) 2012-07-23 2014-01-23 Ms Therapeutics Limited Aminopyridine compounds and their uses
US9315508B2 (en) 2012-07-23 2016-04-19 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-IV inhibitors
CN104768544B (zh) 2012-08-09 2017-06-16 迪纳米斯治疗公司 包括葡甲胺或其盐的组合物在制备减少或预防甘油三酯水平增加的药物中的应用
EP2890696A1 (en) 2012-08-29 2015-07-08 Amgen, Inc. Quinazolinone compounds and derivatives thereof
JP2015528501A (ja) 2012-09-12 2015-09-28 ライジェル ファーマシューティカルズ， インコーポレイテッド 白斑の治療法
WO2014060606A1 (en) 2012-10-19 2014-04-24 Txp Pharma Gmbh Alpha- and gamma-msh analogues
JP6322200B2 (ja) 2012-11-16 2018-05-09 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤
CA2891926A1 (en) 2012-11-20 2014-05-30 Merial, Inc. Anthelmintic compounds and compositions and method of using thereof
AU2013355054B2 (en) 2012-12-07 2017-08-24 Chemocentryx, Inc. Diazole lactams
US9169248B2 (en) 2012-12-21 2015-10-27 Chemocentryx, Inc. Diazole amides
EP2945932B1 (en) 2013-01-21 2018-11-21 Allergan, Inc. Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response
JP2016506930A (ja) 2013-01-25 2016-03-07 ライジェル ファーマシューティカルズ， インコーポレイテッド 炎症性腸疾患を処置するための化合物および方法
WO2014134774A1 (en) 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
HRP20180459T1 (hr) 2013-03-05 2018-05-04 Salzman Group, Inc. Prolijekovi multifunkcionalnih nitroksidnih derivata i njihova primjena
RU2677278C2 (ru) 2013-03-13 2019-01-16 Неуродерм Лтд Способ лечения болезни паркинсона
CN105452213B (zh) 2013-03-14 2017-09-22 阿尔克梅斯制药爱尔兰有限公司 富马酸酯前体药物及其在治疗多种疾病中的应用
ES2791749T3 (es) 2013-03-15 2020-11-05 Verseon Corp Halogenopirazoles como inhibidores de la trombina
WO2014145986A1 (en) 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors
US9051294B2 (en) 2013-04-30 2015-06-09 Allergan, Inc. Therapeutic agents
US9000032B2 (en) 2013-05-31 2015-04-07 Allergan, Inc. Substituted cyclopentenes as therapeutic agents
CA2917149C (en) 2013-07-02 2021-02-02 Cineole Corp., Llc Antimicrobial formulation comprising isoamyl hexanoates together with propanoic acid and/or isobutyric acid
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US9718818B2 (en) 2013-08-22 2017-08-01 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
TWI622406B (zh) 2013-10-23 2018-05-01 善笙生物科技股份有限公司 來自牛樟芝菌絲體的化合物及混合物的用途
US9315486B2 (en) 2013-10-29 2016-04-19 Allergan, Inc. Therapeutic cyclopentanols, compositions thereof, and methods for use thereof
CN105873925B (zh) 2013-11-01 2019-09-10 勃林格殷格翰动物保健美国公司 抗寄生物的和杀虫的异噁唑啉化合物
US9809568B2 (en) 2013-11-14 2017-11-07 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
EA029826B1 (ru) 2013-12-02 2018-05-31 Кемосентрикс, Инк. Соединения против ccr6
US9388153B2 (en) 2013-12-20 2016-07-12 Allergan, Inc. Secondary amines as therapeutic agents
EP3099667B1 (en) 2014-01-27 2017-11-01 Allergan, Inc. Antagonists acting at multiple prostaglandin receptors for the treatment of inflammation
EP3102564A4 (en) 2014-02-05 2017-10-18 Merck Sharp & Dohme Corp. Tablet formulation for cgrp-active compounds
US12168004B2 (en) 2014-02-05 2024-12-17 Merck Sharp & Dohme Llc Treatment of migraine
US10258585B2 (en) 2014-03-13 2019-04-16 Neuroderm, Ltd. DOPA decarboxylase inhibitor compositions
EP3116475B1 (en) 2014-03-13 2020-11-04 Neuroderm Ltd Dopa decarboxylase inhibitor compositions
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2015162483A1 (en) 2014-04-22 2015-10-29 Txp Pharma Gmbh Alpha- and gamma-msh analogues
WO2015162486A1 (en) 2014-04-22 2015-10-29 Txp Pharma Gmbh Linear gamma msh with c- and / or n-terminal extensions of lysine and / or glutamic acid residues
WO2015162485A1 (en) 2014-04-22 2015-10-29 Txp Pharma Gmbh Peptide analogues with branched amino acid probe(s)
US9394273B2 (en) 2014-05-15 2016-07-19 Allergan, Inc. Therapeutic prostaglandin receptor agonists
MX375153B (es) 2014-05-19 2025-03-06 Boehringer Ingelheim Animal Health Usa Inc Compuestos antihelminticos.
WO2015179815A1 (en) 2014-05-22 2015-11-26 Allergan, Inc. Amidoalkylenyl and amidoaryl esters, compositions thereof, and methods for their use
ES2721525T3 (es) 2014-06-06 2019-08-01 Allergan Inc Novedosos agonistas de EP4 como compuestos terapéuticos
US9908923B2 (en) 2014-06-11 2018-03-06 The Medical College Of Wisconsin, Inc. Monomeric CXCL121 peptide and methods of use thereof
WO2016009341A1 (en) 2014-07-14 2016-01-21 Radikal Therapeutics Inc. Thioredoxin mimetic prodrugs and uses thereof
GB201417828D0 (en) 2014-10-08 2014-11-19 Cereno Scient Ab New methods and compositions
WO2016036586A1 (en) 2014-09-03 2016-03-10 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
KR20170048410A (ko) 2014-09-17 2017-05-08 베르선 코포레이션 세린 프로테아제 저해제로서의 피라졸릴-치환된 피리돈 화합물
IL292655B2 (en) 2014-10-06 2024-03-01 Chemocentryx Inc Ccr9 chemokine receptor inhibitor for use in a method of treating or reducing the development of inflammatory bowel disease
EP3227292B1 (en) 2014-12-02 2022-03-09 Alterity Therapeutics Limited 4H-PYRIDO[1,2-a]PYRIMIDIN-4-ONE COMPOUNDS
DK3230255T3 (da) 2014-12-09 2020-06-22 Ezekiel Golan Regulatorer af uhæmmet adfærd
US9899696B2 (en) * 2015-01-21 2018-02-20 Lockheed Martin Advanced Energy Storage, Llc Solid buffer materials for electrolyte solutions and flow batteries utilizing same
MA41558B1 (fr) 2015-02-20 2023-02-28 Univ Leland Stanford Junior Compositions d'allergènes mélangés et leurs procédés d'utilisation
AU2016224974B2 (en) 2015-02-27 2019-09-26 Verseon Corporation Substituted pyrazole compounds as serine protease inhibitors
HK1249847A1 (zh) 2015-03-09 2018-11-16 Intekrin Therapeutics, Inc. 用於治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法
ES2983910T3 (es) 2015-05-19 2024-10-28 Univ Yale Composiciones para tratar afecciones patológicas de calcificación y métodos que usan las mismas
AU2016263564B2 (en) 2015-05-20 2019-12-05 Amgen Inc. Triazole agonists of the APJ receptor
CN107835818B (zh) 2015-05-20 2022-04-29 勃林格殷格翰动物保健美国公司 驱虫缩酚酸肽化合物
EP3666282A1 (en) 2015-06-03 2020-06-17 The Medical College of Wisconsin, Inc. An engineered ccl20 locked dimer polypeptide
US11571462B2 (en) 2015-06-03 2023-02-07 The Medical College Of Wisconsin, Inc. Engineered CCL20 locked dimer polypeptide
ES2902467T3 (es) 2015-06-15 2022-03-28 Univ Leland Stanford Junior TIMP2 para su uso en el tratamiento de afecciones asociadas al envejecimiento
ES2858551T3 (es) 2015-06-16 2021-09-30 Atxa Therapeutics Ltd Antagonistas del receptor de tromboxano
JP6871919B2 (ja) 2015-06-16 2021-05-19 ナノファギックス エルエルシー 薬物送達及びイメージング化学コンジュゲート、製剤及びその使用方法
US10744070B2 (en) 2015-06-19 2020-08-18 University Of Southern California Enteral fast access tract platform system
US10631564B2 (en) 2015-06-19 2020-04-28 University Of Southern California Enterically coated microparticle compositions and methods for modified nutrient delivery
NO346258B1 (en) 2015-06-30 2022-05-16 Neurad Ltd Novel breathing control modulating compounds, and methods of making and using same
US11173197B2 (en) 2015-07-07 2021-11-16 Bluewillow Biologics, Inc. Methods and compositions for nanoemulsion vaccine formulations
EP3334706B1 (en) 2015-08-10 2020-09-30 Ramot at Tel-Aviv University Ltd. Pillararenes and uses thereof
EP3371203B1 (en) 2015-11-02 2020-02-26 University Of Rochester Bortezomib conjugates and methods using same
WO2017077528A2 (en) 2015-11-02 2017-05-11 Salzman Lovelace Investments, Ltd. Methods and pharmaceutical compositions for treatment of lung inflammation
WO2017079260A1 (en) 2015-11-02 2017-05-11 University Of Rochester Phosphonate-chloroquine conjugates and methods using same
TWI734715B (zh) 2015-11-19 2021-08-01 美商卡默森屈有限公司 趨化因子受體調節劑
TWI724056B (zh) 2015-11-19 2021-04-11 美商卡默森屈有限公司 Ｃｘｃｒ２抑制劑
US20180371434A1 (en) 2015-11-20 2018-12-27 Yale University Compositions for Treating Ectopic Calcification Disorders, and Methods Using Same
MX2022006069A (es) 2016-01-14 2023-01-12 Chemocentryx Inc Metodo para tratar glomerulopatia c3.
SG11201806153QA (en) 2016-01-20 2018-08-30 Chemocentryx Inc 2-oxindole compounds
KR20180105701A (ko) 2016-02-11 2018-09-28 모데차이 체비온 신경변성의 치료를 위한 방법 및 약학 조성물
UY37137A (es) 2016-02-24 2017-09-29 Merial Inc Compuestos antiparasitarios de isoxazolina, formulaciones inyectables de acción prolongada que los comprenden, métodos y usos de los mismos
WO2017153977A1 (en) 2016-03-08 2017-09-14 Salzman Lovelace Investments, Ltd. Solid formulations of resolvins and uses thereof
WO2017176620A2 (en) 2016-04-04 2017-10-12 Chemocentryx, Inc. SOLUBLE C5aR ANTAGONISTS
US10946020B2 (en) 2016-04-06 2021-03-16 University Of Virginia Patent Foundation Compositions and methods for treating cancer
US9988369B2 (en) 2016-05-03 2018-06-05 Amgen Inc. Heterocyclic triazole compounds as agonists of the APJ receptor
US11173207B2 (en) 2016-05-19 2021-11-16 The Regents Of The University Of Michigan Adjuvant compositions
US10036024B2 (en) 2016-06-03 2018-07-31 Purdue Research Foundation siRNA compositions that specifically downregulate expression of a variant of the PNPLA3 gene and methods of use thereof for treating a chronic liver disease or alcoholic liver disease (ALD)
WO2017210566A1 (en) 2016-06-03 2017-12-07 Novacyte, Inc. Polymer linkers and their uses
KR102401963B1 (ko) 2016-06-27 2022-05-25 케모센트릭스, 인크. 면역조절제 화합물
CA3030089C (en) 2016-07-11 2024-04-23 Contera Pharma Aps Pulsatile drug delivery system for treating morning akinesia
WO2018026764A1 (en) 2016-08-01 2018-02-08 University Of Rochester Nanoparticles for controlled release of anti-biofilm agents and methods of use
WO2018039508A1 (en) 2016-08-25 2018-03-01 Merial, Inc. Method for reducing unwanted effects in parasiticidal treatments
US10449230B2 (en) 2016-10-06 2019-10-22 The Regents Of The University Of California Polymyxin derived cell penetrating scaffolds
CN110381738B (zh) 2016-10-14 2021-07-16 勃林格殷格翰动物保健美国公司 农药的和杀寄生物的乙烯基异噁唑啉化合物
WO2018085307A1 (en) 2016-11-03 2018-05-11 Wu Laurence I Prodrugs of clofarabine
CN116751200A (zh) 2016-11-07 2023-09-15 爱彼特生物制药公司 含有取代的吡啶酮的三环化合物以及使用其的方法
WO2018093577A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Cycloalkyl substituted triazole compounds as agonists of the apj receptor
WO2018097944A1 (en) 2016-11-16 2018-05-31 Amgen Inc. Triazole furan compounds as agonists of the apj receptor
US11046680B1 (en) 2016-11-16 2021-06-29 Amgen Inc. Heteroaryl-substituted triazoles as APJ receptor agonists
US11191762B2 (en) 2016-11-16 2021-12-07 Amgen Inc. Alkyl substituted triazole compounds as agonists of the APJ Receptor
US10689367B2 (en) 2016-11-16 2020-06-23 Amgen Inc. Triazole pyridyl compounds as agonists of the APJ receptor
EP3541789A1 (en) 2016-11-16 2019-09-25 Boehringer Ingelheim Animal Health USA Inc. Anthelmintic depsipeptide compounds
US10906890B2 (en) 2016-11-16 2021-02-02 Amgen Inc. Triazole phenyl compounds as agonists of the APJ receptor
EP4134080B1 (en) 2016-11-23 2024-11-13 ChemoCentryx, Inc. Ccr2 inhibitors for use in treating renal diseases
WO2018106928A1 (en) 2016-12-08 2018-06-14 Contravir Pharmaceuticals, Inc. Treatment and prevention of hbv diseases by cyclosporine analogue molecules modified at amino acides 1 and 3
AU2017376398B2 (en) 2016-12-14 2021-07-15 Intervet International B.V. Aminopyrazoles as selective janus kinase inhibitors
US11098010B2 (en) 2017-03-21 2021-08-24 Arbutus Biopharma Corporation Substituted dihydroindene-4-carboxamides and analogs thereof, and methods using same
KR20200036808A (ko) 2017-04-03 2020-04-07 코히러스 바이오사이언시스, 인크. 진행성 핵상 마비 치료를 위한 PPARγ 작용제
AR111464A1 (es) 2017-04-14 2019-07-17 Contravir Pharmaceuticals Inc Terapia combinada para el tratamiento de infecciones virales
DE202017002464U1 (de) 2017-05-09 2017-06-12 St. Lotus Biotech Corp. Pflanzliche Zusammensetzung zur Vorbeugung oder Linderung von ischämischem Schlaganfall
US11484543B2 (en) 2017-05-18 2022-11-01 The Rockefeller University Compositions and methods for diagnosing and treating diseases and disorders associated with mutant KCNJ5
WO2018236745A1 (en) 2017-06-20 2018-12-27 Carnot, Llc COMPOSITIONS AND METHODS FOR INCREASING THE EFFICACY OF CARDIAC METABOLISM
CN111225665B (zh) 2017-08-08 2023-12-08 凯莫森特里克斯股份有限公司 大环免疫调节剂
ES2944616T3 (es) 2017-08-14 2023-06-22 Boehringer Ingelheim Animal Health Usa Inc Compuestos de pirazol-isoxazolina plaguicidas y parasiticidas
CA3073802A1 (en) 2017-08-23 2019-02-28 Gavish-Galilee Bio Applications Ltd. Compositions and methods for treating atherosclerotic cardiovascular disease
MA50665A (fr) 2017-09-25 2020-08-05 Chemocentryx Inc Polythérapie utilisant un antagoniste du récepteur 2 de la chimiokine (ccr2) et un inhibiteur pd-1/pd-l1
US10758540B2 (en) 2017-10-11 2020-09-01 Chemocentryx, Inc. Treatment of focal segmental glomerulosclerosis with CCR2 antagonists
US20190134020A1 (en) 2017-10-31 2019-05-09 Chemocentryx, Inc. C5aR INHIBITOR REDUCTION OF URINARY sCD163
MA50509A (fr) 2017-11-03 2021-06-02 Amgen Inc Agonistes de triazole fusionnés du récepteur apj
CN111818929A (zh) 2017-11-27 2020-10-23 由卫生与公众服务部部长代表的美利坚合众国 用于治疗和/或预防牙周疾病的化合物、组合物和方法
CN111788184B (zh) 2017-12-22 2023-12-22 凯莫森特里克斯股份有限公司 用作C5aR抑制剂的二芳基取代的5,5-稠合环化合物
WO2019126424A1 (en) 2017-12-22 2019-06-27 Chemocentryx, Inc. DIARYL SUBSTITUTED 6,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS
US11207294B2 (en) 2018-01-08 2021-12-28 Chemocentryx, Inc. Methods of treating generalized pustular psoriasis with an antagonist of CCR6 or CXCR2
WO2019141957A1 (en) 2018-01-19 2019-07-25 Cado Biotechnology Ivs N-pyrimidinyl hydroxy pyrazole derivatives and uses thereof
CN117643587A (zh) 2018-02-05 2024-03-05 深圳市原力生命科学有限公司 用于治疗癌症的杂二环羧酸
EP3749096A1 (en) 2018-02-08 2020-12-16 Boehringer Ingelheim Animal Health USA Inc. Parasiticidal compositions comprising eprinomectin and praziquantel, methods and uses thereof
JP2021513553A (ja) 2018-02-13 2021-05-27 ビートルバング ファーマ リミテッド カンナビノイド誘導体並びにそのコンジュゲート及びその使用
US10568874B2 (en) 2018-02-22 2020-02-25 Chemocentryx, Inc. Indane-amines as PD-L1 antagonists
EP3759225A1 (en) 2018-03-02 2021-01-06 Sixfold Bioscience Ltd. Compositions for delivery of cargo to cells
JP2021519334A (ja) 2018-03-26 2021-08-10 クリア クリーク バイオ， インコーポレイテッド ジヒドロオロト酸デヒドロゲナーゼを阻害するための組成物および方法
WO2019190822A1 (en) 2018-03-28 2019-10-03 Vtv Therapeutics Llc Crystalline forms of [3-(4- {2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1h-imidazol-4-yl} -phenoxy)-propyl]-diethyl-amine
WO2019190823A1 (en) 2018-03-28 2019-10-03 Vtv Therapeutics Llc Pharmaceutically acceptable salts of [3-(4- {2-butyl-1-[4-(4-chlorophenoxy)-phenyl]-1h-imidazol-4-yl} -phenoxy)-propyl]-diethyl-amine
ES2993034T3 (en) 2018-04-02 2024-12-20 Chemocentryx Inc Prodrugs of fused-bicyclic c5ar antagonists
EP3552605A1 (en) 2018-04-11 2019-10-16 Univerzita Palackého V Olomouchi Mcoppb for use as medicament
MA52487A (fr) 2018-05-01 2021-03-10 Amgen Inc Pyrimidinones substituées en tant qu'agonistes du récepteur apj
KR20210015892A (ko) 2018-05-29 2021-02-10 세르시 테라퓨틱스 인코포레이티드 통증 치료를 위한 화합물, 이를 포함하는 조성물 및 이를 사용하는 방법
US12383545B1 (en) 2018-06-08 2025-08-12 Allergan Pharmaceuticals International Limited Treatment of migraine
US20190374607A1 (en) 2018-06-08 2019-12-12 The Medical College Of Wisconsin, Inc. Methods of treating vascular leakage using cxcl12 peptides
MX2021000293A (es) 2018-07-09 2021-07-15 Boehringer Ingelheim Animal Health Usa Inc Compuestos heterociclicos antihelminticos.
TWI826492B (zh) 2018-07-27 2023-12-21 加拿大商愛彼特生物製藥公司 經取代四氫環戊[c]吡咯、經取代二氫吡咯，其類似物及使用其之方法
US10966943B2 (en) 2018-09-06 2021-04-06 Innopharmascreen Inc. Methods and compositions for treatment of asthma or parkinson's disease
JP7464591B2 (ja) 2018-10-10 2024-04-09 ブイティーブイ・セラピューティクス・エルエルシー ［３－（４－｛２－ブチル－１－［４－（４－クロロ－フェノキシ）－フェニル］－１ｈ－イミダゾール－４－イル｝－フェノキシ）－プロピル］－ジエチル－アミンの代謝産物
EP4497474A3 (en) 2018-10-17 2025-04-23 Imbria Pharmaceuticals, Inc. Methods of treating rheumatic diseases using trimetazidine-based compounds
WO2020092136A1 (en) 2018-10-31 2020-05-07 Merck Sharp & Dohme Corp. N-heteroaryl indazole derivatives as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
WO2020092845A1 (en) 2018-11-01 2020-05-07 Rigel Pharmaceuticals, Inc. Method and composition embodiments for treating acute myeloid leukemia
EP3883648A1 (en) 2018-11-20 2021-09-29 Boehringer Ingelheim Animal Health USA Inc. Indazolylcyanoethylamino compound, compositions of same, method of making, and methods of using thereof
TW202415643A (zh) 2018-12-12 2024-04-16 加拿大商愛彼特生物製藥公司 經取代之芳基甲基脲類及雜芳基甲基脲類、其類似物及其使用方法
WO2020159565A1 (en) 2019-02-01 2020-08-06 Cersci Therapeutics, Inc. Methods of treating post-surgical pain with a thiazoline anti-hyperalgesic agent
WO2020159588A1 (en) 2019-02-01 2020-08-06 Cersci Therapeutics, Inc. Methods of treating diabetic neuropathy with a thiazoline anti-hyperalgesic agent
JP7637630B2 (ja) 2019-03-19 2025-02-28 ベーリンガー インゲルハイム フェトメディカ ゲーエムベーハー 駆虫性アザベンゾチオフェンおよびアザベンゾフラン化合物
US11684652B2 (en) 2019-05-09 2023-06-27 The Feinstein Institutes For Medical Research HMGB1 antagonist treatment of acute lung injury
US20200377518A1 (en) 2019-05-29 2020-12-03 Rigel Pharmaceuticals, Inc. Method of preventing and treating thrombosis
EP3976101A4 (en) 2019-05-31 2023-06-21 Imbria Pharmaceuticals, Inc. FIBROSIS TREATMENT METHODS USING COMPOUNDS THAT PROMOTE GLUCOSE OXIDATION
WO2020247298A2 (en) 2019-06-06 2020-12-10 Merck Sharp & Dohme Corp. 1-pyrazolyl, 5-, 6- disubstituted indazole derivatives as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
CN114502531B (zh) 2019-07-08 2024-05-24 雷佐鲁特公司 制备血浆激肽释放酶抑制剂的方法
US11872217B2 (en) 2019-07-10 2024-01-16 Chemocentryx, Inc. Indanes as PD-L1 inhibitors
BR112022001418A2 (pt) 2019-08-08 2022-06-07 Rigel Pharmaceuticals Inc Compostos e método para tratar a síndrome de liberação de citocinas
WO2021030526A1 (en) 2019-08-14 2021-02-18 Rigel Pharmaceuticals, Inc. Method of blocking or ameliorating cytokine release syndrome
CR20220216A (es) 2019-10-16 2023-01-09 Chemocentryx Inc Aminas de heteroaril-bifenilo para el tratamiento de enfermedades pd-l1
US11713307B2 (en) 2019-10-16 2023-08-01 Chemocentryx, Inc. Heteroaryl-biphenyl amides for the treatment of PD-L1 diseases
AU2020371556A1 (en) 2019-10-25 2022-05-05 Merck Sharp & Dohme Llc N-(heteroaryl) quinazolin-2-amine derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof
CN118908883A (zh) 2019-11-08 2024-11-08 凯莫森特里克斯股份有限公司 补体成分c5a受体的盐形式
US10792360B1 (en) 2019-11-21 2020-10-06 Chemocentryx, Inc. Compositions and methods for treating inflammatory bowel disease using CCR9 inhibitor and anti-TNF-alpha blocking antibodies
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
US20210300873A1 (en) 2020-03-20 2021-09-30 Clear Creek Bio, Inc. Stable polymorphic compositions of brequinar sodium and methods of use and manufacture thereof
BR112022019349A2 (pt) 2020-03-27 2022-11-16 Aclaris Therapeutics Inc Forma cristalina, composição farmacêutica, comprimido e método para isolar um composto
TWI904146B (zh) 2020-03-31 2025-11-11 美商卡默森屈有限公司 使用ｃｃｒ９抑制劑及抗ｉｌ-２３阻斷抗體治療發炎性腸道疾病的組成物及方法
IL297489A (en) 2020-04-23 2022-12-01 Aztherapies Inc Cellular ablation of hla-class i mhc
EP3901160A1 (en) 2020-04-25 2021-10-27 Nuvamid SA Nicotinamide mononucleotide and nicotinamide riboside derivatives and use thereof in the treatment of viral infections and respiratory complications, in particular caused by influenzavirus or coronavirus
US20230150984A1 (en) 2020-04-24 2023-05-18 Nuvamid Sa Nicotinamide mononucleotide and nicotinamide riboside derivatives and use thereof in the treatment of viral infections and respiratory complications, in particular caused by influenzavirus or coronavirus
JP2023523345A (ja) 2020-04-27 2023-06-02 シックスフォールド バイオサイエンス リミテッド モジュール官能基を有する核酸ナノ粒子を含有する組成物
US20230172878A1 (en) 2020-04-30 2023-06-08 Annette M. Tobia Compositions and methods for treating cytokine storms
WO2021243275A2 (en) 2020-05-28 2021-12-02 Aztherapies, Inc. Car-treg-based therapies for treating neurgdegenerative diseases
PH12022553222A1 (en) 2020-05-29 2024-02-12 Boehringer Ingelheim Animal Health Usa Inc Anthelmintic heterocyclic compounds
US11530184B2 (en) 2020-06-30 2022-12-20 Imbria Pharmaceuticals, Inc. Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate
US11780811B2 (en) 2020-06-30 2023-10-10 Imbria Pharmaceuticals, Inc. Methods of synthesizing 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate
MX2023000447A (es) 2020-07-07 2023-04-20 Atxa Therapeutics Ltd Antagonista de receptor de tromboxano formulaciones.
WO2022013430A1 (en) 2020-07-17 2022-01-20 Université De Bretagne Occidentale New glycolipids and use thereof as sk3 ion channel modulators
EP4188375A4 (en) 2020-07-29 2024-07-24 Allergan Pharmaceuticals International Limited MIGRAINE TREATMENT
WO2022029275A1 (en) 2020-08-06 2022-02-10 Nuvamid Sa Combination of nicotinamide mononucleotide derivatives and other therapeutic agents for use in the treatment of coronavirus infections and covid-19
JP7842734B2 (ja) 2020-08-07 2026-04-08 ヌバミッド エスエー 抗悪性腫瘍薬誘発毒性の処置および防止におけるニコチンアミドモノヌクレオチド誘導体およびその使用
CA3190959A1 (en) 2020-08-12 2022-02-17 Txp Pharma Ag Exendin-4 peptide analogues
WO2022060764A1 (en) 2020-09-18 2022-03-24 Merck Sharp & Dohme Corp. Modified benzofuran-carboxamides as glucosylceramide synthase inhibitors
CN116546984A (zh) 2020-09-28 2023-08-04 耶鲁大学 5-ht2a受体的选择性激动剂及其使用方法
US12178853B2 (en) 2020-10-13 2024-12-31 Betavive Ltd. Method and compounds for treating diabetes and associated metabolic diseases
CA3195193A1 (en) 2020-10-29 2022-05-05 Peter H. Fuller N-linked isoquinoline amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof
GB202017251D0 (en) 2020-10-30 2020-12-16 Queens Univ Of Belfast Neurodegenerative treatment
GB202017255D0 (en) 2020-10-30 2020-12-16 Queens Univ Of Belfast Immunomodulatory agent
US11844754B2 (en) 2020-11-17 2023-12-19 Neuroderm, Ltd. Methods for treatment of Parkinson's disease
US11331293B1 (en) 2020-11-17 2022-05-17 Neuroderm, Ltd. Method for treatment of Parkinson's disease
US11213502B1 (en) 2020-11-17 2022-01-04 Neuroderm, Ltd. Method for treatment of parkinson's disease
WO2022115921A1 (en) 2020-12-04 2022-06-09 Cymra Life Sciences Limited Antiinflammatory compositions comprising cannabidiol, delta-9- tetrahydrocannabinol and linalool
US12076318B2 (en) 2020-12-10 2024-09-03 Imbria Pharmaceuticals, Inc. Methods of treating heart failure with hibernating myocardium using modified forms of trimetazidine
US11730733B2 (en) 2020-12-10 2023-08-22 Imbria Pharmaceuticals, Inc. Methods of treating non-obstructive hypertrophic cardiomyopathy using modified forms of trimetazidine
US11793807B2 (en) 2020-12-10 2023-10-24 Imbria Pharmaceuticals, Inc. Methods of treating heart failure with preserved ejection fraction using modified forms of trimetazidine
US11969422B2 (en) 2020-12-10 2024-04-30 Imbria Pharmaceuticals, Inc. Methods of treating heart failure with reduced ejection fraction using modified forms of trimetazidine
CA3206030A1 (en) 2020-12-18 2022-06-23 Nuvamid Sa Nicotinamide mononucleotide derivatives and use thereof in the treatment and prevention of a red blood cell disorder
AU2021409718A1 (en) 2020-12-22 2023-07-13 Allergan Pharmaceuticals International Limited Treatment of migraine
MX2023009249A (es) 2021-02-08 2023-10-23 Bausch Health Ireland Ltd Método para prevenir, tratar o mejorar la colitis ulcerosa.
WO2022184685A1 (en) 2021-03-01 2022-09-09 Nuvamid Sa Nicotinamide mononucleotide derivatives and use thereof for the treatment and/or prevention of long covid-19
EP4070799A1 (en) 2021-04-08 2022-10-12 Nuvamid SA Compositions for the improvement of sport performance
EP4079311B1 (en) 2021-04-20 2025-10-01 Nuvamid SA Nmn and derivatives for use in the treatment of depression and/or anxiety in patients having a form of parkinsonism
EP4079310A1 (en) 2021-04-20 2022-10-26 Nuvamid SA Nmn and derivatives for its use in the treatment of alpha-synucleinopathies
US11883396B2 (en) 2021-05-03 2024-01-30 Imbria Pharmaceuticals, Inc. Methods of treating kidney conditions using modified forms of trimetazidine
US20240285702A1 (en) 2021-05-31 2024-08-29 Cannabotech Ltd. Compositions comprising a cannabinoid and uses thereof
WO2022263625A1 (en) 2021-06-17 2022-12-22 Nuvamid Sa Nicotinamide mononucleotide derivatives and use thereof for the treatment of heart failure with preserved ejection fraction
EP4355743A1 (en) 2021-06-18 2024-04-24 University of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
WO2023012182A1 (en) 2021-08-02 2023-02-09 Nuvamid Sa Nicotinamide mononucleotide derivatives for use in the treatment of sapho syndrome
WO2023023532A2 (en) 2021-08-18 2023-02-23 Chemocentryx, Inc. Aryl sulfonyl (hydroxy) piperidines as ccr6 inhibitors
MX2024003952A (es) 2021-09-27 2024-05-27 Allergan Pharmaceuticals Int Ltd Combinación que comprende atogepant para tratar la migraña.
US12447198B2 (en) 2021-10-12 2025-10-21 Betavive Ltd. Peptides and fragments for treating diabetes and associated metabolic diseases
KR20250053961A (ko) 2022-09-02 2025-04-22 머크 샤프 앤드 돔 엘엘씨 엑사테칸-유래 토포이소머라제-1 억제제 제약 조성물 및 그의 용도
IL319372A (en) 2022-09-06 2025-05-01 Hadasit Med Res Service Combinations involving psychedelic drugs for the treatment of chronic schizophrenia and other neuropsychiatric and neurological disorders
TW202432099A (zh) 2022-10-25 2024-08-16 美商默沙東有限責任公司 源自依克沙替康(exatecan)之adc連接子-載藥(payload)、醫藥組合物及其用途
IL321395A (en) 2022-12-14 2025-08-01 Merck Sharp & Dohme Llc Auristatin cargo-linkers, pharmaceutical compounds, and their uses
US12091400B2 (en) 2023-01-20 2024-09-17 Epics Therapeutics Piperidine derivatives as METTL3 inhibitors
EP4680606A1 (en) 2023-03-17 2026-01-21 AtmosR Adenine derivatives as hsp90 inhibitors
US12161612B2 (en) 2023-04-14 2024-12-10 Neuroderm, Ltd. Methods and compositions for reducing symptoms of Parkinson's disease
WO2025011733A1 (en) 2023-07-07 2025-01-16 Nuvamid Sa Nicotinamide mononucleotide and derivatives thereof and use thereof in the treatment and prevention of polycythemia
KR20260053367A (ko) 2023-08-14 2026-04-21 뉴림 파머슈티칼스(1991) 리미티드 Gal475 조성물 및 그의 사용 방법
WO2025064408A1 (en) 2023-09-18 2025-03-27 The Broad Institute, Inc. Compositions and methods for treating cardiovascular disease
WO2025099725A1 (en) 2023-11-09 2025-05-15 Hadasit Medical Research Services And Development Ltd. Conjugates and uses thereof
GB2636364A (en) 2023-12-07 2025-06-18 Aramune Tech Limited Arabinogalactan
WO2025134072A1 (en) 2023-12-21 2025-06-26 Bausch Health Ireland Limited Methods for preventing, treating, or ameliorating ulcerative colitis in certain patient populations with amiselimod
WO2025176994A1 (en) 2024-02-20 2025-08-28 Analytical Services For Art & Archaeology (Scotland) Ltd Composition and method of use
WO2025219976A1 (en) 2024-04-19 2025-10-23 Betavive Ltd. Peptides and fragments for treating diabetes and associated metabolic diseases
GB202405650D0 (en) 2024-04-22 2024-06-05 Royal College Surgeons Ireland Hdac6 protacs
US12599544B2 (en) 2024-05-09 2026-04-14 Alsteni Medical, Inc. Intraoral gastrointestinal access device and related methods
WO2026017846A1 (en) 2024-07-19 2026-01-22 Epics Therapeutics Piperidine derivatives as mettl3 inhibitors for the treatment of carcinomas
WO2026027787A1 (en) 2024-08-02 2026-02-05 The University Court Of The University Of Edinburgh Cyclophilin modulators

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US536155A (en) * 1895-03-19 Pill or tablet
US2211485A (en) * 1940-08-13 Effervescent acetyl salicylic acid
US2312381A (en) * 1940-10-24 1943-03-02 Frank J Bickenheuser Medicinal tablet
US3062715A (en) * 1953-11-18 1962-11-06 George S Pfaus Vaginal tablet
GB917456A (en) * 1958-10-30 1963-02-06 Casco Lab Inc Suppository composition and preparation thereof
US3131123A (en) * 1959-03-13 1964-04-28 Lab Francais De Therapeutique Enteric tablets and manufacture thereof
US3136692A (en) * 1961-06-30 1964-06-09 Strong Cobb Arner Inc Effervescent composition containing polyvinylpyrrolidone
GB1093286A (en) * 1965-02-15 1967-11-29 Biorex Laboratories Ltd Improvements in or relating to dosage unit forms for the administration of medicaments and diagnostic agents
FR5391M (ja) * 1965-11-04 1967-10-23
GB1123316A (en) * 1966-12-09 1968-08-14 Wynlit Pharmaceuticals Trust R Improvements in suppositories
US3495001A (en) * 1968-05-27 1970-02-10 Miles Lab Effervescent compositions of acetylsalicylic acid
US3887700A (en) * 1969-11-28 1975-06-03 Aspro Nicholas Ltd Analgesic formulations
US3764668A (en) * 1970-09-30 1973-10-09 Interx Research Corp Compositions of salts of salicylamide
US3676549A (en) * 1970-09-30 1972-07-11 Alza Corp Administration of alkali metal salts of salicylamide
GB1359614A (en) * 1971-04-06 1974-07-10 Dev Et De Rech Soc Fr De Method for the manufacture of effervescent tablets
US3845770A (en) * 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) * 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
GB1478759A (en) * 1974-11-18 1977-07-06 Alza Corp Process for forming outlet passageways in pills using a laser
US4036228A (en) * 1975-09-11 1977-07-19 Alza Corporation Osmotic dispenser with gas generating means
US4008719A (en) * 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4111201A (en) * 1976-11-22 1978-09-05 Alza Corporation Osmotic system for delivering selected beneficial agents having varying degrees of solubility
US4160452A (en) * 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20150137871A (ko) * 2014-05-30 2015-12-09 디씨에스이엔지 주식회사 회전속도비를 이용하여 회전체내 절삭툴을 제어할 수 있는 오비탈식 파이프 절삭장치

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Publication number Publication date
IE810765L (en) 1981-10-25
EP0040899A3 (en) 1982-08-11
DK184681A (da) 1981-10-26
ATE9267T1 (de) 1984-09-15
ES8307092A1 (es) 1983-06-16
ES267593U (es) 1983-05-16
PT72796B (fr) 1982-03-30
DK152482C (da) 1988-08-01
EP0040899A2 (en) 1981-12-02
US4265874A (en) 1981-05-05
IE51216B1 (en) 1986-11-12
DK152482B (da) 1988-03-07
EP0040899B1 (en) 1984-09-12
ES510822A0 (es) 1983-06-16
JPS56167617A (en) 1981-12-23
GR73519B (ja) 1984-03-09
NZ196561A (en) 1983-05-10
ES267593Y (es) 1983-11-16
DE3165901D1 (en) 1984-10-18
PT72796A (fr) 1981-05-01

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