EP2038251A4 - Promédicaments hydrosolubles à charge positive de l'aspirine - Google Patents

Promédicaments hydrosolubles à charge positive de l'aspirine

Info

Publication number
EP2038251A4
EP2038251A4 EP06780025A EP06780025A EP2038251A4 EP 2038251 A4 EP2038251 A4 EP 2038251A4 EP 06780025 A EP06780025 A EP 06780025A EP 06780025 A EP06780025 A EP 06780025A EP 2038251 A4 EP2038251 A4 EP 2038251A4
Authority
EP
European Patent Office
Prior art keywords
aspirin
positive
load
water
soluble prodrugs
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
EP06780025A
Other languages
German (de)
English (en)
Other versions
EP2038251A1 (fr
Inventor
Chongxi Yu
Lina Xu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
YU, CHONGXI
Techfields Biochem Co Ltd
Original Assignee
Techfields Biochem Co Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38922980&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP2038251(A4) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Techfields Biochem Co Ltd filed Critical Techfields Biochem Co Ltd
Priority to EP13155198.8A priority Critical patent/EP2610242A1/fr
Publication of EP2038251A1 publication Critical patent/EP2038251A1/fr
Publication of EP2038251A4 publication Critical patent/EP2038251A4/fr
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C219/14—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/30—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EP06780025A 2006-07-09 2006-07-09 Promédicaments hydrosolubles à charge positive de l'aspirine Pending EP2038251A4 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP13155198.8A EP2610242A1 (fr) 2006-07-09 2006-07-09 Promédicaments hydrosolubles positivement chargés d'aspirine

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IB2006/052318 WO2008007171A1 (fr) 2006-07-09 2006-07-09 Promédicaments hydrosolubles à charge positive de l'aspirine

Publications (2)

Publication Number Publication Date
EP2038251A1 EP2038251A1 (fr) 2009-03-25
EP2038251A4 true EP2038251A4 (fr) 2010-04-21

Family

ID=38922980

Family Applications (2)

Application Number Title Priority Date Filing Date
EP13155198.8A Withdrawn EP2610242A1 (fr) 2006-07-09 2006-07-09 Promédicaments hydrosolubles positivement chargés d'aspirine
EP06780025A Pending EP2038251A4 (fr) 2006-07-09 2006-07-09 Promédicaments hydrosolubles à charge positive de l'aspirine

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP13155198.8A Withdrawn EP2610242A1 (fr) 2006-07-09 2006-07-09 Promédicaments hydrosolubles positivement chargés d'aspirine

Country Status (6)

Country Link
EP (2) EP2610242A1 (fr)
JP (1) JP5759672B2 (fr)
CN (1) CN101484415B (fr)
AU (1) AU2006346195B2 (fr)
CA (1) CA2656858C (fr)
WO (1) WO2008007171A1 (fr)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090238763A1 (en) 2006-07-09 2009-09-24 Chongxi Yu High penetration compositions and uses thereof
US20090221703A1 (en) 2006-07-09 2009-09-03 Chongxi Yu High penetration composition and uses thereof
WO2008010025A1 (fr) * 2006-07-18 2008-01-24 Techfields Biochem Co. Ltd Pro-médicaments d'ibuprofène hydrosolubles positivement chargés à taux de pénétration cutanée très rapide
PL2084124T3 (pl) 2006-10-02 2014-08-29 Techfields Biochem Co Ltd Dodatnio naładowane rozpuszczalne w wodzie proleki prostaglandyn i związków pokrewnych o bardzo dużych szybkościach przenikania przez skórę
AU2006350707A1 (en) 2006-11-08 2008-05-15 Chongxi Yu Transdermal delivery systems of peptides and related compounds
CN101547898B (zh) 2006-12-10 2014-09-24 于崇曦 β-内酰胺类抗生素的透皮给药系统
HUE031712T2 (en) 2007-01-15 2017-08-28 Chongxi Yu Retinoids and retinoid-like compounds with positively charged water-soluble prodrugs having very high skin penetration rates
WO2008093173A1 (fr) 2007-01-31 2008-08-07 Chongxi Yu Promédicaments hydrosolubles à charge positive de 1h-imidazo[4, 5-c]quinolin-4-amines et composés associés à taux élevés de pénétration cutanée
KR20150058566A (ko) * 2007-06-04 2015-05-28 테크필즈 인크 매우 높은 피부 및 막 침투율을 가지는 ｎｓａｉａ 약물전구체 및 이들의 새로운 의약적 용도
US20100024286A1 (en) * 2008-07-31 2010-02-04 Smith Susan Jane Liquid fuel compositions
BR122021011394B1 (pt) * 2008-12-04 2021-09-28 Chongxi Yu Composição de alta penetração de um fármaco principal, e uso de uma hpc
JP2012520342A (ja) * 2009-03-16 2012-09-06 ジェンメディカ・セラピューティックス・ソシエダッド・リミターダ 代謝障害を処置するのに有用な抗炎症剤および抗酸化剤のコンジュゲート
PL2427475T3 (pl) 2009-05-08 2021-07-19 Techfields Biochem Co., Ltd. Kompozycje proleku o wysokim przenikaniu peptydów i związków powiązanych z peptydami
US9969751B2 (en) 2009-06-10 2018-05-15 Techfields Pharma Co., Ltd. High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds
WO2012137225A1 (fr) * 2011-04-08 2012-10-11 Sphaera Pharma Pvt. Ltd Réactifs de méthylformyle substitué et procédé d'utilisation de ceux-ci pour modifier des propriétés physicochimiques et/ou pharmacocinétiques de composés
CN111012914A (zh) 2012-01-18 2020-04-17 苏州泰飞尔医药有限公司 治疗肺部疾病的高穿透力前药组合物和医药组合物
CN112521305B (zh) * 2013-03-15 2023-04-25 苏州泰飞尔医药有限公司 治疗帕金森疾病的新型高穿透力药物及其药物组合物
JP5905411B2 (ja) * 2013-06-12 2016-04-20 テックフィールズ バイオケム カンパニー リミテッド アスピリンの正荷電水溶性プロドラッグ
CN104276962B (zh) * 2013-07-08 2019-04-12 浙江越甲药业有限公司 一种阿司匹林衍生物及其组合物与应用
US20150072005A1 (en) * 2013-09-10 2015-03-12 Vitalis Llc Aspirin formulation for increased efficacy
US20160168108A1 (en) 2014-12-16 2016-06-16 Adt Pharmaceuticals, Inc. Method of treating or preventing ras-mediated diseases
US9862698B2 (en) 2014-12-16 2018-01-09 Adt Pharmaceuticals, Inc. Indenyl compounds, pharmaceutical compositions, and medical uses thereof
JP6153264B2 (ja) * 2015-01-05 2017-06-28 テックフィールズ インコーポレイテッド 非常に速い皮膚及び膜浸透速度を有するｎｓａｉａプロドラッグ及びその新規医薬使用
CN106146326B (zh) * 2015-04-01 2022-10-11 浙江越甲药业有限公司 一种乙酰水杨酸衍生物晶体及其制备方法和用途
JP6289438B2 (ja) * 2015-12-03 2018-03-07 テックフィールズ バイオケム カンパニー リミテッド アスピリンの正荷電水溶性プロドラッグ
JP6588485B2 (ja) * 2017-02-21 2019-10-09 テックフィールズ バイオケム カンパニー リミテッド アスピリンの正荷電水溶性プロドラッグ
WO2019080693A1 (fr) 2017-10-26 2019-05-02 浙江越甲药业有限公司 Composition pharmaceutique stable contenant un dérivé de médicament anti-inflammatoire non stéroïdien
CN111556748B (zh) * 2017-11-17 2023-04-14 浙江越甲药业有限公司 一种局部麻醉药物
CN112020354A (zh) 2018-04-26 2020-12-01 Adt制药有限责任公司 抗癌茚类、茚满类、氮杂茚类、氮杂茚满类、药物组合物和用途
CN113677660A (zh) * 2018-12-29 2021-11-19 张婧 乙酰水杨酸衍生物及其应用
CN111925362B (zh) * 2020-08-20 2023-06-23 陕西中医药大学 一种抗癌化合物及其合成方法和应用
CN113599375B (zh) * 2021-06-21 2023-08-18 李萍 一种治疗口腔疾病的经口给药药物及用途
JP2025504448A (ja) * 2022-01-17 2025-02-12 テックフィールズ インコーポレイテッド 高透過プロドラッグによるウイルス感染症、細菌感染症、原生動物感染症、及び／又は真菌感染症の徴候、症状、及び／又は合併症の治療
AU2023206720A1 (en) * 2022-01-17 2024-08-29 Techfields Inc. Prevention or treatment of cardiovascular diseases with high penetration prodrugs of aspirin and other nsaids
CN116082439B (zh) * 2023-03-13 2025-08-15 湖北南博生物工程有限公司 一种可用于治疗冠心病的阿司匹林衍生物及其制备方法与应用

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GB958186A (en) * 1962-10-02 1964-05-21 Biosedra Lab Salicylamide derivatives
EP0152379A2 (fr) * 1984-02-15 1985-08-21 Ciba-Geigy Ag Procédé pour la préparation de compositions pharmaceutiques contenant des liposomes unilamellaires

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Publication number Priority date Publication date Assignee Title
GB958186A (en) * 1962-10-02 1964-05-21 Biosedra Lab Salicylamide derivatives
EP0152379A2 (fr) * 1984-02-15 1985-08-21 Ciba-Geigy Ag Procédé pour la préparation de compositions pharmaceutiques contenant des liposomes unilamellaires

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Title
CHANAL, J. L. ET AL: "Study on the distribution and elimination of dimethylaminoethyl acetylsalicylate in the rat. Effect of the carbon-14 labeling position", BOLLETTINO CHIMICO FARMACEUTICO , 119(6), 331-8 CODEN: BCFAAI; ISSN: 0006-6648, 1980, XP008119887 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1966, MACHON, ZDZISLAW ET AL: "Synthesis of benzoylcholine derivatives", XP002571761, retrieved from STN Database accession no. 1966:412012 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1981, WOLINSKI, JERZY ET AL: "Search for anticholinergic compounds. XX. Synthesis of aminoalkyl o-, m-, and p-hydroxybenzoates and o-, m-, and p-acetoxybenzoates", XP002571760, retrieved from STN Database accession no. 1981:424459 *
MACHON, ZDZISLAW ET AL: "Synthesis of benzoylcholine derivatives", DISSERTATIONES PHARMACEUTICAE , 17(4), 491-6 CODEN: DIPHAH; ISSN: 0301-1615, 1965 *
See also references of WO2008007171A1 *
WOLINSKI, JERZY ET AL: "Search for anticholinergic compounds. XX. Synthesis of aminoalkyl o-, m-, and p-hydroxybenzoates and o-, m-, and p-acetoxybenzoates", ACTA POLONIAE PHARMACEUTICA , 37(3), 275-80 CODEN: APPHAX; ISSN: 0001-6837, 1980, XP008119888 *

Also Published As

Publication number Publication date
EP2610242A1 (fr) 2013-07-03
JP5759672B2 (ja) 2015-08-05
EP2038251A1 (fr) 2009-03-25
CA2656858C (fr) 2016-01-19
JP2009542797A (ja) 2009-12-03
AU2006346195B2 (en) 2013-03-07
CN101484415B (zh) 2013-08-14
CA2656858A1 (fr) 2008-01-17
CN101484415A (zh) 2009-07-15
AU2006346195A1 (en) 2008-01-17
WO2008007171A1 (fr) 2008-01-17

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