MX2020003341A - Compuestos de imidazo-piridina como inhibidores de pad. - Google Patents

Compuestos de imidazo-piridina como inhibidores de pad.

Info

Publication number
MX2020003341A
MX2020003341A MX2020003341A MX2020003341A MX2020003341A MX 2020003341 A MX2020003341 A MX 2020003341A MX 2020003341 A MX2020003341 A MX 2020003341A MX 2020003341 A MX2020003341 A MX 2020003341A MX 2020003341 A MX2020003341 A MX 2020003341A
Authority
MX
Mexico
Prior art keywords
formula
pharmaceutically acceptable
polymorphs
prodrugs
solvates
Prior art date
Application number
MX2020003341A
Other languages
English (en)
Inventor
Gurulingappa Hallur
Athisayamani Jeyaraj Duraiswamy
Buchi Reddy Purra
N V S K Rao
Sridharan Rajagopal
Rajendra Kristam
Original Assignee
Jubilant Epipad LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Jubilant Epipad LLC filed Critical Jubilant Epipad LLC
Publication of MX2020003341A publication Critical patent/MX2020003341A/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)

Abstract

En el presente documento se describen compuestos heterocíclicos de fórmula (I), (II) y (III), junto con sus polimorfos, estereoisómeros, profármacos, solvatos, cocristales, intermedios, sales farmacéuticamente aceptables y metabolitos de los mismos. Los compuestos descritos en el presente documento, sus polimorfos, estereoisómeros, profármacos, solvatos, cocristales, intermedios, sales farmacéuticamente aceptables y metabolitos de los mismos son, por lo tanto, inhibidores de PAD4 y pueden ser útiles en el tratamiento de diversos trastornos, por ejemplo, artritis reumatoide, vasculitis, lupus eritematoso sistémico, lupus eritematoso cutáneo, colitis ulcerosa, cáncer, fibrosis quística, asma, esclerosis múltiple y psoriasis. También se describe el proceso de preparación de los compuestos de fórmula (I), (II) y (III), sus polimorfos, estereoisómeros, profármacos, solvatos, cocristales, intermedios, sales farmacéuticamente aceptables y metabolismos de los mismos, junto con una composición farmacéutica que comprende un compuesto de fórmula (I), fórmula (II), fórmula (III) o una sal farmacéuticamente aceptable de los mismos.
MX2020003341A 2017-10-18 2018-10-16 Compuestos de imidazo-piridina como inhibidores de pad. MX2020003341A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN201741037110 2017-10-18
PCT/IN2018/050671 WO2019077631A1 (en) 2017-10-18 2018-10-16 IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS

Publications (1)

Publication Number Publication Date
MX2020003341A true MX2020003341A (es) 2020-09-17

Family

ID=64051641

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2020003341A MX2020003341A (es) 2017-10-18 2018-10-16 Compuestos de imidazo-piridina como inhibidores de pad.

Country Status (20)

Country Link
US (1) US11426412B2 (es)
EP (1) EP3697785B1 (es)
JP (1) JP7307723B2 (es)
KR (1) KR102782563B1 (es)
CN (1) CN111225915B (es)
AU (1) AU2018352142B2 (es)
BR (1) BR112020007607A2 (es)
CA (1) CA3076476A1 (es)
DK (1) DK3697785T3 (es)
ES (1) ES2941512T3 (es)
FI (1) FI3697785T3 (es)
HU (1) HUE061607T2 (es)
IL (1) IL272667B (es)
MX (1) MX2020003341A (es)
PL (1) PL3697785T3 (es)
PT (1) PT3697785T (es)
RS (1) RS64104B1 (es)
SG (1) SG11202003463XA (es)
WO (1) WO2019077631A1 (es)
ZA (1) ZA202002770B (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2764243C2 (ru) 2017-09-22 2022-01-14 ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи Гетероциклические соединения в качестве ингибиторов PAD
CN111225915B (zh) 2017-10-18 2023-03-07 朱比兰特埃皮帕德有限公司 作为pad抑制剂的咪唑并吡啶化合物
US11629135B2 (en) 2017-11-06 2023-04-18 Jubilant Prodell Llc Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
RS65576B1 (sr) 2017-11-24 2024-06-28 Jubilant Episcribe Llc Heterociklična jedinjenja kao inhibitori prmt5
CN112105610B (zh) 2018-03-13 2024-01-26 朱比连特普罗德尔有限责任公司 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物
MX2021000293A (es) 2018-07-09 2021-07-15 Boehringer Ingelheim Animal Health Usa Inc Compuestos heterociclicos antihelminticos.
ES2929200T3 (es) 2018-08-08 2022-11-25 Bristol Myers Squibb Co Tienopirroles sustituidos como inhibidores de PAD4
EP3833440A1 (en) 2018-08-08 2021-06-16 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes
ES2956090T3 (es) 2018-08-08 2023-12-13 Bristol Myers Squibb Co Inhibidores de bencimidazol de enzimas PAD
WO2020085504A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法
KR20220002890A (ko) 2019-03-19 2022-01-07 뵈링거 잉겔하임 애니멀 헬스 유에스에이 인코포레이티드 구충성 아자-벤조티오펜 및 아자-벤조푸란 화합물
TW202115083A (zh) * 2019-09-27 2021-04-16 大陸商南京藥捷安康生物科技有限公司 肽醯精胺酸脫亞胺酶抑制劑及其用途
MD4051678T2 (en) 2019-10-28 2026-07-31 Merck Sharp & Dohme Llc Small molecule inhibitors of the KRAS G12C mutant
WO2021085653A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
WO2021084765A1 (en) * 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
TW202140477A (zh) * 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環pad4抑制劑
WO2021174024A1 (en) 2020-02-28 2021-09-02 First Wave Bio, Inc. Methods of treating iatrogenic autoimmune colitis
WO2021215544A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
US12702658B2 (en) 2020-04-24 2026-08-11 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C
MX2022013615A (es) 2020-04-30 2022-11-16 Gilead Sciences Inc Inhibidores de macrociclo de peptidilarginina deiminasas.
BR112022024156A2 (pt) 2020-05-29 2023-02-14 Boehringer Ingelheim Animal Health Usa Inc Compostos heterocílicos antelmínticos
BR112023002553A2 (pt) * 2020-08-12 2023-04-18 Jubilant Epipad LLC Composto, composição, uso do composto e uso da composição
WO2022109487A1 (en) 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant
TW202233174A (zh) * 2020-12-22 2022-09-01 美商基利科學股份有限公司 肽基精胺酸去亞胺酶之抑制劑
EP4267562A1 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
EP4306522A4 (en) * 2021-03-11 2025-05-21 Zhejiang University Fused ring heterocyclic compound and application thereof, and pharmaceutical composition containing same and application thereof
CN115073449A (zh) * 2021-03-11 2022-09-20 浙江大学 稠环杂环化合物及应用、含有其的药物组合物及应用
WO2022232320A1 (en) * 2021-04-27 2022-11-03 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
WO2023073641A1 (en) 2021-11-01 2023-05-04 Boehringer Ingelheim Vetmedica Gmbh Anthelmintic pyrrolopyridazine compounds
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators
KR20260096846A (ko) 2023-10-20 2026-06-24 머크 샤프 앤드 돔 엘엘씨 Kras 단백질의 소분자 억제제
WO2026020127A2 (en) 2024-07-19 2026-01-22 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad2 modulators

Family Cites Families (279)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1230663A (es) 1968-12-10 1971-05-05
GB1356789A (en) 1970-08-06 1974-06-12 Prodotti Antibiotici Spa Derivatives of theophylline
DE2050657C3 (de) 1970-10-15 1974-06-20 Basf Ag, 6700 Ludwigshafen Azofarbstoffe, Verfahren zu ihrer Herstellung und deren Verwendung
US3970753A (en) 1973-06-12 1976-07-20 Smith Kline & French Laboratories Limited Imidazo[1,2-a]pyridines
DE2361390A1 (de) 1973-12-10 1975-06-19 Merck Patent Gmbh Isochinolinderivate und verfahren zu ihrer herstellung
US4246274A (en) 1978-05-10 1981-01-20 Bayer Aktiengesellschaft Antimycotic hydroxypropyl-imidazoles
DE2832677A1 (de) 1978-07-26 1980-02-07 Bayer Ag Hydroxypropyl-imidazole, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
DE3210570A1 (de) 1982-03-23 1983-10-06 Hoechst Ag 3-azolyl-1,2-diaryl-1-halogen-1-propene, ihre herstellung, ihre verwendung als pflanzenschutzmittel und diese verbindungen enthaltende praeparate
WO1984002907A1 (en) 1983-01-21 1984-08-02 Alkaloida Vegyeszeti Gyar New alkyl diamine derivatives
JP2528107B2 (ja) 1985-03-15 1996-08-28 サマ−トン,ジエ−ムス ポリヌクレオチド測定試薬と方法
DE3628545A1 (de) 1985-09-23 1987-04-23 Hoechst Ag Arylmethylazole und deren salze, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung
JPH07100688B2 (ja) 1986-02-12 1995-11-01 大日本製薬株式会社 環状アミン誘導体
JPH07121911B2 (ja) 1986-03-26 1995-12-25 クミアイ化学工業株式会社 4(1h)−ピリジノン誘導体および農園芸用殺菌剤
DE3631013A1 (de) 1986-09-12 1988-03-24 Thomae Gmbh Dr K Neue naphthylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
EP0301751B1 (en) 1987-07-31 1993-03-10 Takeda Chemical Industries, Ltd. Pyridinium derivatives, their production and use
US5210266A (en) 1987-12-03 1993-05-11 Dainippon Pharmaceutical Co., Ltd. N-substituted mercaptopropanamide derivatives
US5179125A (en) 1987-12-03 1993-01-12 Dainippon Pharmaceutical Co., Ltd. N-substituted mercaptopropanamide derivatives
GB8820231D0 (en) * 1988-08-25 1988-09-28 Fujisawa Pharmaceutical Co New benzazole compounds processes for preparation thereof & pharmaceutical composition comprising same
FR2638747B1 (fr) 1988-11-08 1993-12-24 Synthelabo Derives de phenyloxypropanolamines, leur preparation et leur application en therapeutique
DE3901723A1 (de) 1989-01-21 1990-07-26 Bayer Ag Azolyl-derivate
JP2769711B2 (ja) 1989-02-17 1998-06-25 昭和電工株式会社 オレフィン重合用触媒成分の製造方法及びオレフィンの重合方法
AU6143790A (en) 1989-07-04 1991-01-17 Kumpf, Ursula Process and device for drawing optical fibre cables into protective pipes
US5420289A (en) 1989-10-27 1995-05-30 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
US5229516A (en) 1989-10-27 1993-07-20 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
PT95692A (pt) 1989-10-27 1991-09-13 American Home Prod Processo para a preparacao de derivados de acidos indole-,indeno-,piranoindole- e tetra-hidrocarbazole-alcanoicos, ou quais sao uteis como inibidores de pla2 e da lipoxigenase
CA2048110C (en) 1990-07-30 2002-06-25 Muneo Takatani Imidazopyridine derivatives and their use
DE69213184T2 (de) 1991-07-03 1997-01-09 Shionogi & Co Phospholipase a2 inhibitor
EP0533056A3 (en) 1991-09-14 1993-06-16 Hoechst Aktiengesellschaft Substituted aminopropanes, process for their preparation and their use as antimycotic agents
CA2079374C (en) 1991-09-30 2003-08-05 Merck Frosst Canada Incorporated (bicyclic-azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5273980A (en) 1991-09-30 1993-12-28 Merck Frosst Canada Inc. Bicyclic-azaarylmethoxy) indoles as inhibitors of leukotriene biosynthesis
US5330989A (en) 1991-10-24 1994-07-19 American Home Products Corporation Heterocycles substituted with biphenyl-3-cyclobutene-1,2-dione derivatives
AU2945392A (en) 1991-12-10 1993-07-19 Hoechst Schering Agrevo Gmbh Pyrimidinyl- or triazinyl-oxy(or thio)aldehyde derivatives and their use as herbicides or plant-growth regulators
GB9206757D0 (en) 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
DE4227522A1 (de) 1992-08-20 1994-02-24 Bayer Ag Lichtpolarisierende Folien und neue dichroitische Farbstoffe hierfür
JP3298954B2 (ja) 1992-12-16 2002-07-08 三共株式会社 新規n,n’−ジベンゾイルヒドラジン誘導体及び殺虫組成物
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
DK0691959T3 (da) 1993-03-29 1999-04-26 Zeneca Ltd Heterocykliske derivater som blodpladeaggregations-inhibitorer
IL109220A0 (en) 1993-04-05 1994-07-31 Synaptic Pharma Corp Dihydropyridines and new uses thereof
JPH09501405A (ja) 1993-05-27 1997-02-10 スミスクライン・ビーチャム・ラボラトワール・ファルマソーティク 抗不整脈用n−置換3−ベンズアゼピンまたはイソキノリン
FR2706895A1 (en) 1993-06-22 1994-12-30 Synthelabo Tetrahydroisoquinoline derivatives, their preparation and their application in therapeutics
JPH07179402A (ja) 1993-10-20 1995-07-18 Ishihara Sangyo Kaisha Ltd 置換ベンゼン誘導体、その製造方法及びそれを含有する有害生物防除剤
US5461154A (en) 1994-02-02 1995-10-24 Eli Lilly And Company Intermediate and process for making
TW281667B (es) 1994-02-03 1996-07-21 Synthelabo
GB9402807D0 (en) 1994-02-14 1994-04-06 Xenova Ltd Pharmaceutical compounds
JPH07304770A (ja) 1994-05-11 1995-11-21 Kanebo Ltd 新規ベンゾアゼピノン誘導体
US5593994A (en) 1994-09-29 1997-01-14 The Dupont Merck Pharmaceutical Company Prostaglandin synthase inhibitors
EP0793653A1 (en) 1994-11-23 1997-09-10 Neurogen Corporation Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands
US5541033A (en) 1995-02-01 1996-07-30 Ocg Microelectronic Materials, Inc. Selected o-quinonediazide sulfonic acid esters of phenolic compounds and their use in radiation-sensitive compositions
US5554621A (en) 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives
US20030018025A1 (en) 1995-06-07 2003-01-23 Neurogen Corporation, Corporation Of The State Of Delaware Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives: new classes of dopamine receptor subtype specific ligands
EP0848957A1 (en) 1995-09-08 1998-06-24 Kanebo Ltd. Fas LIGAND SOLUBILIZATION INHIBITOR
CN1209744A (zh) 1995-12-29 1999-03-03 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
US6235731B1 (en) 1996-04-24 2001-05-22 Takeda Chemical Industries, Ltd. Fused imidazopyridine derivatives as antihyperlipidemic agents
EP0819977B1 (en) 1996-07-17 2006-01-04 Fuji Photo Film Co., Ltd. Oxonol compound and silver halide photographic material
GB9717576D0 (en) 1997-08-19 1997-10-22 Xenova Ltd Pharmaceutical compounds
HN1997000027A (es) 1996-12-06 1997-06-05 Pfizer Prod Inc Derivados de 6-fenil piridil - 2 amina
HUP9700392A1 (hu) 1997-02-10 1999-09-28 ICN Magyarország Részvénytársaság Egy vagy két hatóanyagot tartalmazó kardioprotektív hatású gyógyszerkészítmények
US6048877A (en) 1997-02-21 2000-04-11 Bristol-Myers Squibb Company Tetralone derivatives as antiarrhythmic agents
WO1998038156A1 (en) 1997-02-27 1998-09-03 Takeda Chemical Industries, Ltd. Amine compounds, their production and use as amyloid-beta production inhibitors
DE19717371A1 (de) 1997-04-24 1998-10-29 Basf Ag Propargyl-terminierte, nematische oder cholesterische Polymere
ID24525A (id) 1997-07-31 2000-07-20 Hoffmann La Roche Turunan-turunan hidroksikumaranon tersubstitusi-0 sebagai zat anti tumor dan zat antimetastatik
JPH11119379A (ja) 1997-10-08 1999-04-30 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料および画像形成方法
WO1999032447A2 (en) 1997-12-11 1999-07-01 American Home Products Corporation 2,4,6-trisubstituted pyridines with estrogenic activity and methods for the solid phase synthesis thereof
TW555757B (en) 1998-07-31 2003-10-01 Akzo Nobel Nv Aminomethylcarboxylic acid derivatives
DE19834751A1 (de) 1998-08-01 2000-02-03 Boehringer Ingelheim Pharma Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel
EP1123918B1 (en) 1998-10-20 2005-03-09 Takeda Pharmaceutical Company Limited Aromatic amine derivatives, process for the preparation thereof and agents containing the same
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
US6357758B1 (en) 1999-06-30 2002-03-19 Federal-Mogul World Wide, Inc. Metal gasket and method of manufacturing
JP4603679B2 (ja) 1999-12-14 2010-12-22 日本化薬株式会社 害虫防除剤
GB0007108D0 (en) 2000-03-23 2000-05-17 Novartis Ag Organic compounds
US6534651B2 (en) 2000-04-06 2003-03-18 Inotek Pharmaceuticals Corp. 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof
AU2001258771A1 (en) 2000-05-19 2001-11-26 Takeda Chemical Industries Ltd. -secretase inhibitors
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
CA2410680A1 (en) 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
CA2425288A1 (en) 2000-10-11 2002-05-02 Sander G. Mills Pyrrolidine modulators of ccr5 chemokine receptor activity
US20020094989A1 (en) 2000-10-11 2002-07-18 Hale Jeffrey J. Pyrrolidine modulators of CCR5 chemokine receptor activity
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
FR2822153B1 (fr) 2001-03-19 2003-10-31 Servier Lab Nouveaux derives d'indenoindolones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP2004529132A (ja) 2001-03-27 2004-09-24 アクテリオン ファマシューティカルズ リミテッド 1,2,3,4−テトラヒドロイソキノリン誘導体
FR2822827B1 (fr) 2001-03-28 2003-05-16 Sanofi Synthelabo Nouveaux derives de n-(arylsulfonyl) beta-aminoacides comportant un groupe aminomethyle substitue, leur procede de preparation et les compositions pharmaceutiques en contenant
MXPA03009239A (es) 2001-04-10 2004-11-12 Johnson & Johnson Derivados de 1,3,8-triazapiro[4,5]decan-4-ona utiles para el tratamiento de trastornos mediados por el receptor orl-1.
WO2002088089A1 (en) 2001-04-19 2002-11-07 Banyu Pharmaceutical Co., Ltd. Spiropiperidine derivatives, nociceptin receptor antagonists containing the same as the active ingredient and medicinal compositions
ATE338035T1 (de) 2001-06-05 2006-09-15 Boehringer Ingelheim Pharma 1,4-disubstituierte benzokondensierte cycloalkyl harnstoffverbindungen
CN1543451A (zh) 2001-06-07 2004-11-03 过氧化物酶体增生剂激活的受体的调节剂
BR0212676A (pt) 2001-09-21 2006-05-23 Upjohn Co compostos terapêuticos ligantes de 5-ht, composições farmacêuticas compreendendo tais compostos e seus usos
CA2463975A1 (en) 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
SE0103644D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic isoquinoline compounds
JP2005514366A (ja) 2001-11-20 2005-05-19 イーライ・リリー・アンド・カンパニー 3−置換オキシインドールβ3アゴニスト
DE60225174T2 (de) 2001-11-20 2009-02-12 Eli Lilly And Co., Indianapolis Beta-3 adrenergische agonisten
GB0202873D0 (en) 2002-02-07 2002-03-27 Novartis Ag Organic compounds
JP2005523288A (ja) 2002-02-19 2005-08-04 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 疾病治療用の縮合した二環式−n−架橋−複素環式芳香族カルボキサミド
US6875780B2 (en) 2002-04-05 2005-04-05 Warner-Lambert Company Compounds that modulate PPAR activity and methods for their preparation
AU2003248122A1 (en) 2002-07-25 2004-02-16 Kotobuki Pharmaceutical Co., Ltd. Sodium channel inhibitor
EP1388342A1 (en) 2002-08-07 2004-02-11 Aventis Pharma Deutschland GmbH Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
UA80296C2 (en) 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
AU2003268512A1 (en) 2002-09-09 2004-03-29 Janssen Pharmaceutica N.V. Hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives useful for the treatment of ORL-1 receptor mediated disorders
WO2004035579A1 (ja) 2002-10-15 2004-04-29 Takeda Pharmaceutical Company Limited イミダゾピリジン誘導体、その製造法および用途
US20070004736A1 (en) 2002-11-22 2007-01-04 Keiji Kubo Imidazole derivative, process for producing the same, and use
CA2508618C (en) 2002-12-06 2012-02-21 Bayer Healthcare Ag Tetrahydro-naphthalene derivatives
US6936638B2 (en) 2002-12-20 2005-08-30 Migenix Corp. Ligands of adenine nucleotide translocase (ANT) and compositions and methods related thereto
WO2004078731A1 (en) 2003-03-06 2004-09-16 'chemical Diversity Research Institute', Ltd. Quinoline-carboxylic acids and the derivatives thereof, a focused library
US7195849B2 (en) 2003-03-11 2007-03-27 Arch Specialty Chemicals, Inc. Photosensitive resin compositions
JP4226395B2 (ja) 2003-06-16 2009-02-18 アルパイン株式会社 音声補正装置
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2005058823A1 (ja) 2003-12-17 2005-06-30 Takeda Pharmaceutical Company Limited ウレア誘導体、その製造法及び用途
US20050159334A1 (en) 2004-01-16 2005-07-21 Gluck Oscar S. Method for treating rheumatoid arthritis by inhibiting peptidylarginine deiminase
AU2005225471B2 (en) 2004-03-26 2011-05-12 Methylgene Inc. Inhibitors of histone deacetylase
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
RU2266906C1 (ru) 2004-04-29 2005-12-27 Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека
GB0413605D0 (en) 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
US7488745B2 (en) 2004-07-16 2009-02-10 Schering Corporation Compounds for the treatment of inflammatory disorders
EP1655283A1 (en) 2004-11-08 2006-05-10 Evotec OAI AG 11beta-HSD1 Inhibitors
JP2008007405A (ja) 2004-12-07 2008-01-17 Takeda Chem Ind Ltd カルボキサミド誘導体
ATE469897T1 (de) 2004-12-22 2010-06-15 Theravance Inc Indazolcarbonsäureamidverbindungen
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
DE102005016547A1 (de) 2005-04-08 2006-10-12 Grünenthal GmbH Substituierte 5,6,7,8-Tetrahydro-imidazo(1,2-a)pyridin-2-ylamin-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
AR054363A1 (es) 2005-05-23 2007-06-20 Astrazeneca Ab Compuestos que exhiben actividad moduladora en el receptor 5-hidroxi-triptamina 6
US7800123B2 (en) 2005-05-25 2010-09-21 Koninklijke Philips Electronics N.V. Electroluminescence device
NZ564130A (en) 2005-06-02 2009-12-24 Jenrin Discovery N-propargyl-1-aminoindan compounds useful for treating obesity
US7317022B2 (en) 2005-06-07 2008-01-08 Theravance, Inc. Benzoimidazolone-carboxamide compounds as 5-HT4 receptors agonists
US7592461B2 (en) 2005-12-21 2009-09-22 Bristol-Myers Squibb Company Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
EP1962855B1 (en) 2005-12-22 2013-08-21 Hydra Biosciences, Inc. Trpa1 inhibitors for treating pain
KR101062583B1 (ko) 2006-01-17 2011-09-06 에프. 호프만-라 로슈 아게 Gaba 수용체에 의해 알츠하이머병의 치료에 유용한아릴-아이속사졸-4-일-이미다조[1,2-a]피리딘
WO2007087548A2 (en) 2006-01-25 2007-08-02 Smithkline Beecham Corporation Chemical compounds
US20070191371A1 (en) 2006-02-14 2007-08-16 Kalypsys, Inc. Heterocyclic modulators of ppar
AU2007225208A1 (en) 2006-03-14 2007-09-20 Amgen Inc. Bicyclic carboxylic acid derivatives useful for treating metabolic disorders
RU2302417C1 (ru) 2006-03-14 2007-07-10 Иващенко Андрей Александрович 1-оксо-3-(1н-индол-3-ил)-1,2,3,4-тетрагидроизохинолины, способы их получения, комбинаторная библиотека и фокусированная библиотека
CA2540218A1 (en) 2006-03-17 2007-09-17 Tenxc Wireless Inc. Asymmetric beams for spectrum efficiency
DE102006015449A1 (de) 2006-03-31 2007-10-04 Eads Deutschland Gmbh Selbstleuchtender Körper und Verfahren zu seiner Herstellung
RU2303597C1 (ru) 2006-05-12 2007-07-27 Иващенко Андрей Александрович Фармацевтическая композиция, способы ее получения и применения
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
JP5352454B2 (ja) 2006-06-28 2013-11-27 サノフイ Cxcr2アンンタゴニスト
WO2008008059A1 (en) 2006-07-12 2008-01-17 Locus Pharmaceuticals, Inc. Anti-cancer agents ans uses thereof
DE102006039003A1 (de) 2006-08-19 2008-02-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Verbindungen
EP2076513A1 (en) 2006-10-20 2009-07-08 Irm Llc Compositions and methods for modulating c-kit and pdgfr receptors
JP2010510250A (ja) 2006-11-21 2010-04-02 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 スフィンゴシン=1−燐酸受容体アゴニスト活性を有するヒドリンダンアナログ
CA2670636A1 (en) 2006-11-27 2008-06-05 H. Lundbeck A/S Heteroaryl amide derivatives
WO2008065500A2 (en) 2006-11-30 2008-06-05 Pfizer Products Inc. Heteroaryl amides as type i glycine transport inhibitors
CA2673003A1 (en) 2006-12-22 2008-07-03 Novartis Ag Quinazolines for pdk1 inhibition
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
EP2073799A4 (en) 2007-03-12 2009-08-19 Vm Discovery Inc NOVEL ACTIVE SUBSTANCES FROM CALCIUMIONAL CHANNEL MODULATORS
JP2010522765A (ja) 2007-03-28 2010-07-08 アレイ バイオファーマ、インコーポレイテッド 受容体チロシンキナーゼとしてのイミダゾ[1,2−a]ピリジン化合物
JP5313881B2 (ja) 2007-04-04 2013-10-09 興和株式会社 テトラヒドロイソキノリン化合物
JP2008280344A (ja) 2007-04-12 2008-11-20 Sumitomo Chemical Co Ltd ヒドラジド化合物及びそれを含有する有害節足動物防除剤
AR066379A1 (es) 2007-05-02 2009-08-12 Boehringer Ingelheim Int Amidas de acido carboxilico su preparacion y su uso como medicamentos
CA2692004C (en) 2007-06-15 2013-04-09 Board Of Regents, The University Of Texas System Methods and compositions to inhibit edema factor and adenylyl cyclase
ES2442003T3 (es) 2007-06-20 2014-02-07 Mitsubishi Tanabe Pharma Corporation Nuevo derivado de sulfonamida de ácido malónico y uso farmacéutico del mismo
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
CN101842098A (zh) 2007-08-10 2010-09-22 基因实验室技术有限公司 用于治疗病毒感染的含氮的二环化学实体
WO2009048152A2 (en) 2007-10-11 2009-04-16 Sumitomo Chemical Company, Limited Unsaturated imine compound and use thereof for pest control
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
CA2702984C (en) 2007-10-19 2017-04-11 Sarcode Corporation Compositions and methods for treatment of diabetic retinopathy
EP2072050A1 (en) 2007-12-21 2009-06-24 Santhera Pharmaceuticals (Schweiz) AG Compounds with anti-emetic effect
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
FR2925902B1 (fr) 2008-01-02 2011-01-07 Sanofi Aventis DERIVES D'IMIDAZO°1,2-a!PYRIDINE-2-CARBOXAMIDES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
RU2371444C1 (ru) 2008-01-24 2009-10-27 Андрей Александрович Иващенко ФУРО- И ТИЕНО[2,3-b]-ХИНОЛИН-2-КАРБОКСАМИДЫ, СПОСОБ ПОЛУЧЕНИЯ И ПРОТИВОТУБЕРКУЛЕЗНАЯ АКТИВНОСТЬ
PL2254873T3 (pl) 2008-02-22 2014-10-31 Otsuka Pharma Co Ltd Związek benzodiazepinowy i kompozycja farmaceutyczna
JP2009209090A (ja) 2008-03-04 2009-09-17 Mitsui Chemicals Inc 殺虫剤及び該殺虫剤に含まれる化合物、並びに該化合物の使用方法
US20090276250A1 (en) 2008-05-01 2009-11-05 Travel Tech Systems, Llc Process and system to determine commercial airline arrivals
US8148408B2 (en) 2008-05-09 2012-04-03 Abbott Laboratories Selective substituted pyridine ligands for neuronal nicotinic receptors
WO2009140101A2 (en) 2008-05-12 2009-11-19 Boehringer Ingelheim International Gmbh Imidazopyridine compounds useful as mmp-13 inhibitors
JP2009274984A (ja) 2008-05-14 2009-11-26 Sumitomo Chemical Co Ltd 化合物、光学フィルムおよび光学フィルムの製造方法
US20100121052A1 (en) 2008-06-20 2010-05-13 Rama Jain Novel compounds for treating proliferative diseases
EA022417B1 (ru) 2008-10-21 2015-12-30 Саймабэй Терапевтикс, Инк. Арильные агонисты рецептора gpr120 и их применение
DE102008060958A1 (de) 2008-12-06 2010-07-08 Saltigo Gmbh Hydroxytetralone
RU2016116516A (ru) 2008-12-08 2018-12-07 Мандифарма Интернэшнл Корпорейшн Лимитед Композиции ингибиторов тирозинкиназных рецепторов белков
US8367700B2 (en) 2008-12-17 2013-02-05 Gruenenthal Gmbh Substituted 4-(1.2,3,4-tetrahydroisoquinolin-2-yl)-4-oxobutyric acid amide as KCNQ2/3 modulators
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
JP2012051806A (ja) 2009-02-26 2012-03-15 Eisai R & D Management Co Ltd イミダゾリルピラジン誘導体
KR101641385B1 (ko) 2009-03-16 2016-07-20 스미또모 가가꾸 가부시끼가이샤 화합물, 광학 필름 및 광학 필름의 제조 방법
JP5899607B2 (ja) 2009-03-16 2016-04-06 住友化学株式会社 化合物、光学フィルム及び光学フィルムの製造方法
AU2010232729A1 (en) 2009-03-31 2011-10-20 Arqule, Inc. Substituted indolo-pyridinone compounds
WO2010151799A2 (en) 2009-06-26 2010-12-29 University Of Massachusetts Compounds for modulating rna binding proteins and uses therefor
JP5669481B2 (ja) 2009-08-21 2015-02-12 大塚製薬株式会社 医薬組成物
GB0914767D0 (en) 2009-08-24 2009-09-30 Sterix Ltd Compound
EP2357176A1 (en) 2010-01-15 2011-08-17 Hybrigenics S.A. Amidoacridine derivatives useful as selective inhibitors of ubiquitin specific protease 7
SG183257A1 (en) 2010-02-11 2012-09-27 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US8697911B2 (en) 2010-07-07 2014-04-15 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
BR112013003864B1 (pt) 2010-08-20 2021-08-31 Hutchison Medipharma Limited Compostos de pirrolpirimidina, composição e uso dos mesmos
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
US20130203756A1 (en) 2010-10-29 2013-08-08 Jamie L. Bunda Isoindoline pde10 inhibitors
WO2012087833A1 (en) 2010-12-22 2012-06-28 Abbott Laboratories Hepatitis c inhibitors and uses thereof
EP3345901A3 (en) 2011-06-29 2018-09-12 President and Fellows of Harvard College Small molecules as antiaging agents
EP2726601B1 (en) 2011-06-29 2018-12-26 The General Hospital Corporation Compositions and methods for enhancing bioenergetic status in female germ cells
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
JP2014198669A (ja) 2011-08-03 2014-10-23 杏林製薬株式会社 ビアリールエステル誘導体、及びそれらを有効成分とする医薬
EP2744807A4 (en) 2011-08-15 2015-03-04 Intermune Inc COMPOUNDS AS LYSOPHOSPHIC ACID RECEPTOR ANTAGONISTS
US20130116241A1 (en) 2011-11-09 2013-05-09 Abbvie Inc. Novel inhibitor compounds of phosphodiesterase type 10a
ES2647486T3 (es) 2011-12-22 2017-12-21 Gilead Sciences, Inc. Pirazolo[1,5-a]pirimidinas como agentes antivirales
AU2012355624A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
AU2012355623A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
EA201491265A1 (ru) 2011-12-23 2014-11-28 Новартис Аг Соединения для ингибирования взаимодействия bcl-2 с партнерами по связыванию
AU2012355613A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
CZ2012114A3 (cs) 2012-02-17 2013-02-20 Zentiva, K.S. Zpusob prípravy rivaroxabanu zalozený na úspore 1,1´ -karbonyldiimidazolu
US8859541B2 (en) 2012-02-27 2014-10-14 Boehringer Ingelheim International Gmbh 6-alkynylpyridines
US9296725B2 (en) 2012-05-24 2016-03-29 Cellzome Limited Heterocyclyl pyrimidine analogues as TYK2 inhibitors
EP2669276A1 (en) 2012-05-31 2013-12-04 Université de Strasbourg Ornithine- and lysine-derivatives for the treatment of pain
WO2013192430A2 (en) 2012-06-20 2013-12-27 The Regents Of The University Of California Dynamic biomimetic synzyme catalyst, catalysis, and catalytic systems
FR2993564B1 (fr) 2012-07-20 2014-08-22 Metabrain Res Derives d'imidazopyridine utiles dans le traitement du diabete
RU2611010C2 (ru) * 2012-07-26 2017-02-17 Глаксо Груп Лимитед 2-(Азаиндол-2-ил)бензимидазолы в качестве ингибиторов PAD4
WO2014031872A2 (en) 2012-08-23 2014-02-27 The Broad Institute, Inc. Small molecule inhibitors for treating parasitic infections
EP2887803A4 (en) 2012-08-24 2016-08-03 Univ Texas PRO-NEUROGENIC COMPOUNDS
EP2921229A1 (en) 2012-11-15 2015-09-23 Takasago International Corporation Aluminum catalyst
US9604930B2 (en) 2012-12-21 2017-03-28 Epizyme, Inc. Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof
WO2014100764A2 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Methods of inhibiting prmt5
EP2968303B1 (en) 2013-03-14 2018-07-04 The Trustees of Columbia University in the City of New York Octahydrocyclopentapyrroles, their preparation and use
FR3008976A1 (fr) 2013-07-23 2015-01-30 Servier Lab "nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent"
EA029981B1 (ru) 2013-08-27 2018-06-29 Бристол-Майерс Сквибб Компани Ингибиторы ido
MX2016002544A (es) 2013-09-04 2016-06-17 Squibb Bristol Myers Co Compuestos utiles como inmunomoduladores.
GB201321730D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321746D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
WO2015108038A1 (ja) 2014-01-17 2015-07-23 第一三共株式会社 エチレングリコール化合物
JP6569661B2 (ja) 2014-02-27 2019-09-04 小野薬品工業株式会社 選択的ep2アゴニスト活性を有する化合物
US9067898B1 (en) 2014-03-07 2015-06-30 Janssen Pharmaceutica Nv Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes
ES2738416T3 (es) 2014-03-19 2020-01-22 Boehringer Ingelheim Int Inhibidores heteroarílicos de SYK
CN106065009B (zh) 2014-06-28 2019-03-01 广东东阳光药业有限公司 作为丙型肝炎抑制剂的化合物及其在药物中的应用
DK3169671T3 (da) 2014-07-17 2019-09-23 Sunshine Lake Pharma Co Ltd 1-(5-(tert.-butyl)isoxazol-3-yl)-3-(4-((phenyl)ethynyl)phenyl)ureaderivater og relaterede forbindelser som flt3-inhibitorer til behandling af kræft
EP3187497A4 (en) 2014-08-26 2018-02-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
GB201415573D0 (en) 2014-09-03 2014-10-15 Cancer Therapeutics Crc Pty Ltd Compounds
EP3188730B1 (en) 2014-09-05 2019-05-01 Merck Sharp & Dohme Corp. Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
CN105461693B (zh) 2014-09-26 2019-10-25 广东东阳光药业有限公司 Crth2拮抗剂化合物及其用途
US10561748B2 (en) 2014-10-03 2020-02-18 Divya MAHESHWARI Anthranilic acid derivatives
ES2578377B1 (es) 2014-12-22 2017-05-04 Consejo Superior De Investigaciones Científicas (Csic) Compuestos moduladores del sensor neuronal de calcio dream y sus usos terapéuticos.
WO2016185279A1 (en) 2015-05-21 2016-11-24 Glaxosmithkline Intellectual Property Development Limited Benzoimidazole derivatives as pad4 inhibitors
CA2994798A1 (en) 2015-07-03 2017-01-12 Anca CATRINA Methods and compounds for the alleviation and/or prevention of bone loss
US10246429B2 (en) 2015-08-06 2019-04-02 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
EA035584B1 (ru) 2015-08-12 2020-07-10 Зингента Партисипейшнс Аг Микробиоцидные гетеробициклические производные
US10065970B2 (en) 2015-09-08 2018-09-04 Genentech, Inc. Tricyclic PI3K inhibitor compounds and methods of use
WO2017068412A1 (en) 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
US10280159B2 (en) 2015-12-22 2019-05-07 AbbVie Deutschland GmbH & Co. KG Fused (hetero)cyclic compounds as S1P modulators
EP3190103A1 (en) 2016-01-08 2017-07-12 Rijksuniversiteit Groningen Inhibitors of the pd-1/pd-l1 protein/protein interaction
SG11201807021UA (en) 2016-02-23 2018-09-27 Padlock Therapeutics Inc Heteroaryl inhibitors of pad4
MA45377A (fr) 2016-06-16 2019-04-24 Janssen Sciences Ireland Unlimited Co Composés hétérocycliques en tant qu'agents antibacteriens
EP3478662B1 (en) 2016-06-30 2020-09-16 ViiV Healthcare UK (No.5) Limited Azadecalin derivatives as inhibitors of human immunodeficiency virus replication
CN110818690B (zh) 2016-07-26 2021-08-10 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
WO2018026971A1 (en) 2016-08-03 2018-02-08 Arising International, Llc Symmetric or semi-symmetric compounds useful as immunomodulators
TWI795381B (zh) 2016-12-21 2023-03-11 比利時商健生藥品公司 作為malt1抑制劑之吡唑衍生物
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
WO2018121610A1 (zh) 2016-12-27 2018-07-05 山东大学 针对Smoothened突变株的刺猬通路抑制剂
CN107056630B (zh) 2017-01-23 2020-01-17 合肥工业大学 一种茚满类衍生物及其合成方法和在医药上的用途
US12012467B2 (en) 2017-03-28 2024-06-18 Regents Of The University Of Michigan Small molecule DCN1 inhibitors and therapeutic methods using the same
EP3621962A4 (en) 2017-05-10 2020-12-09 Forge Therapeutics, Inc. ANTIBACTERIAL COMPOUNDS
CN107163044B (zh) 2017-06-19 2021-04-23 广东药科大学 一类具有蛋白酶修饰活性的萘乙二酮化合物及其衍生物
CN110785418A (zh) 2017-06-21 2020-02-11 豪夫迈·罗氏有限公司 作为irak4调节剂的异二氢吲哚酮衍生物
GB201710851D0 (en) 2017-07-06 2017-08-23 Galápagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
RU2764243C2 (ru) 2017-09-22 2022-01-14 ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи Гетероциклические соединения в качестве ингибиторов PAD
CN111225915B (zh) 2017-10-18 2023-03-07 朱比兰特埃皮帕德有限公司 作为pad抑制剂的咪唑并吡啶化合物
JP7270989B2 (ja) 2017-10-20 2023-05-11 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
US11629135B2 (en) 2017-11-06 2023-04-18 Jubilant Prodell Llc Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
RS65576B1 (sr) 2017-11-24 2024-06-28 Jubilant Episcribe Llc Heterociklična jedinjenja kao inhibitori prmt5
WO2019126081A1 (en) 2017-12-19 2019-06-27 Bristol-Myers Squibb Company Amide substituted indole compounds useful as tlr inhibitors
CN110117278B (zh) 2018-02-07 2022-07-19 石家庄以岭药业股份有限公司 烷氧基苯并五元(六元)杂环胺类化合物及其药物用途
WO2019160014A1 (ja) 2018-02-14 2019-08-22 富士フイルム株式会社 重合性液晶組成物、光学異方性膜、光学フィルム、偏光板および画像表示装置
CN112105610B (zh) 2018-03-13 2024-01-26 朱比连特普罗德尔有限责任公司 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物
JP6956033B2 (ja) 2018-03-14 2021-10-27 日本化薬株式会社 ベンゾアゾール化合物、並びにこれを含んだ顔料組成物
CN108358917B (zh) 2018-04-24 2020-06-19 北京市结核病胸部肿瘤研究所 含有碱性稠环片段的咪唑并[1,2-a]吡啶-3-酰胺类化合物及其制备方法
WO2019205147A1 (zh) 2018-04-28 2019-10-31 上海璃道医药科技有限公司 包含苯并含氧脂肪环结构的氨基乙酰胺类化合物及其用途
WO2019213234A1 (en) 2018-05-01 2019-11-07 The Trustees Of Columbia University In The City Of New York Triazolopyrimidines, their preparation and use
US12440486B2 (en) 2018-08-01 2025-10-14 The Trustees Of Columbia University In The City Of New York RBP4 antagonists for treatment and prevention of non-alcoholic fatty liver disease and gout
AU2019316858B2 (en) 2018-08-06 2024-03-28 Moexa Pharmaceuticals Limited Smad3 inhibitors
CN112654903B (zh) 2018-08-28 2022-09-27 富士胶片株式会社 层叠体及图像显示装置
CN110963997A (zh) 2018-09-28 2020-04-07 四川科伦博泰生物医药股份有限公司 杂环酰胺类化合物、包含其的药物组合物及其制备方法和用途
EP3643711A1 (en) 2018-10-24 2020-04-29 Bayer Animal Health GmbH New anthelmintic compounds
WO2020092394A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Imidazopyridine derivatives as alpha4beta7 integrin inhibitors
CN110105299B (zh) 2019-01-23 2023-01-03 中山大学 一种含芳醚取代恶唑烷酮羧酸酯类衍生物及其制备方法和应用
WO2020201773A1 (en) 2019-04-05 2020-10-08 Storm Therapeutics Ltd Mettl3 inhibitory compounds
RU2717101C1 (ru) 2019-06-03 2020-03-18 Андрей Александрович Иващенко Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2Н-пиридо[1,2-a]пиразин-7-карбоксамиды - ингибиторы интегразы ВИЧ, способы их получения и применения
JP7420502B2 (ja) 2019-07-24 2024-01-23 住友化学株式会社 重合性液晶混合組成物、位相差板、楕円偏光板および有機el表示装置
AR119494A1 (es) 2019-07-29 2021-12-22 Servier Lab DERIVADOS DE 6,7-DIHIDRO-5H-PIRIDO[2,3-c]PIRIDAZIN-8-ILO, COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SUS USOS COMO AGENTES PROAPOPTÓTICOS
WO2021028810A1 (en) 2019-08-09 2021-02-18 Inorbit Therapeutics Ab Sulfinic acid compounds as free fatty acid receptor agonists
JP7182533B2 (ja) 2019-09-27 2022-12-02 富士フイルム株式会社 液晶組成物、光学異方性層、光学フィルム、偏光板および画像表示装置
JP7265024B2 (ja) 2019-09-27 2023-04-25 富士フイルム株式会社 液晶組成物、光学異方性層、光学フィルム、偏光板および画像表示装置
ES3058346T3 (es) 2019-11-15 2026-03-10 Yuhan Corp Derivados que tienen un resto 2,3-dihidro-1H-indeno o 2,3-dihidrobenzofurano o una sal farmacéuticamente aceptable de mismo y composiciones farmacéuticas que comprenden los mismos
US11811624B2 (en) 2019-11-15 2023-11-07 Mitsubishi Electric Corporation Edge device linking system, edge device linking method, and recording medium
CN111606904B (zh) 2020-04-07 2021-10-15 广州医科大学 氮杂吲哚类化合物及其应用

Also Published As

Publication number Publication date
SG11202003463XA (en) 2020-05-28
IL272667B (en) 2022-09-01
BR112020007607A2 (pt) 2020-09-29
IL272667A (en) 2020-03-31
HUE061607T2 (hu) 2023-07-28
EP3697785B1 (en) 2022-12-28
US20200237771A1 (en) 2020-07-30
KR102782563B1 (ko) 2025-03-14
AU2018352142B2 (en) 2022-08-25
ES2941512T3 (es) 2023-05-23
PT3697785T (pt) 2023-04-03
JP2021500330A (ja) 2021-01-07
RU2020114991A (ru) 2021-11-18
CA3076476A1 (en) 2019-04-25
CN111225915B (zh) 2023-03-07
PL3697785T3 (pl) 2023-08-07
JP7307723B2 (ja) 2023-07-12
RU2020114991A3 (es) 2022-03-30
RS64104B1 (sr) 2023-04-28
DK3697785T3 (da) 2023-04-03
WO2019077631A1 (en) 2019-04-25
KR20200071752A (ko) 2020-06-19
FI3697785T3 (fi) 2023-04-03
EP3697785A1 (en) 2020-08-26
ZA202002770B (en) 2021-10-27
CN111225915A (zh) 2020-06-02
US11426412B2 (en) 2022-08-30
AU2018352142A1 (en) 2020-03-05

Similar Documents

Publication Publication Date Title
MX2020003242A (es) Compuestos heterociclicos como inhibidores de pad.
MX2020005363A (es) Compuestos heterociclicos como inhibidores de prmt5.
ZA202206810B (en) Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
PH12020500529A1 (en) Bicyclic heterocyclyl derivatives as irak4 inhibitors
PH12018502227A1 (en) Macrocyclic mcl1 inhibitors for treating cancer
SA519401446B1 (ar) مُعدِّل منظم التوصيل عبر الأغشية للتليف الكيسي، تركيبات صيدلية، طرق علاج، وعملية لتحضير المُعدِّل
PH12018500765A1 (en) N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use
PH12016501338A1 (en) Indazole compounds as irak4 inhibitors
MX418519B (es) Inhibidores selectivos de jak1
MX387321B (es) Derivados de benzoimidazol como inhibidores de peptidil arginina deiminasa 4 (pad4).
MX2016010056A (es) 6-heteroariloxi o 6-ariloxi-quinolina-2-carboxamidas y metodos de uso.
WO2016087665A3 (en) Compounds for treating cystic fibrosis
NZ721645A (en) Compounds for use as gpr120 agonists
MX2020001717A (es) Inhibidores macrociclicos de mcl-1 y metodos de uso.
PH12017501652B1 (en) Kv1.3 inhibitors and their medical application
PH12019500569A1 (en) Blood-brain barrier-penetrant dopamine-b-hydroxylase inhibitors
MX2019010096A (es) Derivados de 1, 4, 6-trisustituidos-2-alquil-1h-benzo[d]imidazol como inhibidores de dihidroorotato oxigenasa.
TN2016000489A1 (en) Carboxamide derivatives.
MX2020008746A (es) Compuestos de sulfonimidoilpurinona 7-sustituidos y sus derivados para el tratamiento y prevencion del cancer de higado.
PH12020500542A1 (en) Dopamine-b-hydroxylase inhibitors
TN2017000342A1 (en) Novel cyclopropabenzofuranyl pyridopyrazinediones
WO2008087514A3 (en) Hdac inhibitors
MX2017003458A (es) Indazol ureas y metodo de uso.
WO2019195641A3 (en) 1,3,4-oxadiazoles as inhibitors of rho/mrtf/srf-mediated gene transcription and methods for use of the same
NZ748942A (en) Pyrazolylaminobenzimidazole derivatives as jak inhibitors