EA200500377A1 - Пиразольные производные как ингибиторы трансформирующего фактора роста (tgf) - Google Patents
Пиразольные производные как ингибиторы трансформирующего фактора роста (tgf)Info
- Publication number
- EA200500377A1 EA200500377A1 EA200500377A EA200500377A EA200500377A1 EA 200500377 A1 EA200500377 A1 EA 200500377A1 EA 200500377 A EA200500377 A EA 200500377A EA 200500377 A EA200500377 A EA 200500377A EA 200500377 A1 EA200500377 A1 EA 200500377A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- tgf
- growth factor
- inhibitors
- transforming growth
- pyrazol derivatives
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Abstract
Описаны новые пиразольные производные формулы (Ia), промежуточные соединения для их получения, содержащие их фармацевтические композиции и их медицинское применение. Соединения настоящего изобретения являются эффективными ингибиторами сигнального пути трансформирующего β-фактора роста (TGF). Они полезны при лечении разнообразных болезненных состояний, связанных с TGF, включая, например, рак и фиброзные заболевания.Отчет о международном поиске был опубликован 2004.07.01.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US41214602P | 2002-09-18 | 2002-09-18 | |
US48454303P | 2003-07-02 | 2003-07-02 | |
PCT/IB2003/003933 WO2004026306A2 (en) | 2002-09-18 | 2003-09-08 | Pyrazole derivatives as transforming growth factor (tgf) inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
EA200500377A1 true EA200500377A1 (ru) | 2005-08-25 |
Family
ID=32033585
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200500377A EA200500377A1 (ru) | 2002-09-18 | 2003-09-08 | Пиразольные производные как ингибиторы трансформирующего фактора роста (tgf) |
Country Status (27)
Country | Link |
---|---|
US (4) | US6958354B2 (ru) |
EP (2) | EP2165708A3 (ru) |
JP (1) | JP4519657B2 (ru) |
KR (1) | KR20050044807A (ru) |
CN (1) | CN1681501A (ru) |
AP (1) | AP2005003263A0 (ru) |
AR (1) | AR041272A1 (ru) |
AT (1) | ATE450258T1 (ru) |
AU (1) | AU2003259475A1 (ru) |
BR (1) | BR0314302A (ru) |
CA (1) | CA2496295C (ru) |
CO (1) | CO5550456A2 (ru) |
DE (1) | DE60330362D1 (ru) |
EA (1) | EA200500377A1 (ru) |
EC (1) | ECSP055679A (ru) |
ES (1) | ES2335099T3 (ru) |
HR (1) | HRP20050247A2 (ru) |
IS (1) | IS7698A (ru) |
MA (1) | MA27440A1 (ru) |
MX (1) | MXPA05002376A (ru) |
NO (1) | NO20050838L (ru) |
OA (1) | OA12929A (ru) |
PA (1) | PA8583201A1 (ru) |
PE (1) | PE20040988A1 (ru) |
PL (1) | PL375979A1 (ru) |
UY (1) | UY27985A1 (ru) |
WO (1) | WO2004026306A2 (ru) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2737737C2 (ru) * | 2016-06-13 | 2020-12-02 | Джинфлит Терапьютикс (Шанхай) Инк. | АЛЬФА- И БЕТА-НЕНАСЫЩЕННОЕ АМИДНОЕ СОЕДИНЕНИЕ - ПРОИЗВОДНОЕ БЕНЗОТРИАЗОЛА, ПРИМЕНЯЕМОЕ В КАЧЕСТВЕ ИНГИБИТОРА TGF-βRI |
RU2750702C1 (ru) * | 2017-12-13 | 2021-07-01 | Джинфлит Терапьютикс (Шанхай) Инк. | КРИСТАЛЛИЧЕСКАЯ ФОРМА И СОЛЕВАЯ ФОРМА ИНГИБИТОРА TGF-βRI И СПОСОБ ИХ ПОЛУЧЕНИЯ |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
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CN1681805A (zh) * | 2002-09-18 | 2005-10-12 | 辉瑞产品公司 | 作为转化生长因子(tgf)抑制剂的新的咪唑类化合物 |
JP4519657B2 (ja) * | 2002-09-18 | 2010-08-04 | ファイザー・プロダクツ・インク | 形質転換成長因子(tgf)阻害剤としての新規なピラゾ−ル化合物 |
DE60327443D1 (de) | 2002-09-18 | 2009-06-10 | Pfizer Prod Inc | Neue oxazolverbindungen als inhibitoren des transforming growth factor (tgf) |
CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
GB0313915D0 (en) * | 2003-06-16 | 2003-07-23 | Smithkline Beecham Corp | Compounds |
US20080171755A1 (en) * | 2004-08-31 | 2008-07-17 | Wen-Cherng Lee | Pyrimidinylpyrazoles as Tgf-Beta Inhibitors |
EP1798229A4 (en) * | 2004-09-07 | 2009-07-29 | Sankyo Co | SUBSTITUTED BIPHENYL DERIVATIVE |
JP2008516962A (ja) * | 2004-10-15 | 2008-05-22 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | 血管傷害を治療する方法 |
TW200639163A (en) | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
WO2007070866A2 (en) * | 2005-12-16 | 2007-06-21 | Alcon, Inc. | Control of intraocular pressure using alk5 modulation agents |
UA92670C2 (ru) | 2006-10-31 | 2010-11-25 | Пфайзер Продактс Инк. | Пиразолиновые соединения и их фармацевтическое применение, композиция на их основе |
AU2008281543A1 (en) * | 2007-08-01 | 2009-02-05 | Pfizer Inc. | Pyrazole compounds and their use as Raf inhibitors |
ES2813875T3 (es) | 2014-01-01 | 2021-03-25 | Medivation Tech Llc | Compuestos y procedimientos de uso |
WO2016160881A1 (en) | 2015-04-01 | 2016-10-06 | Rigel Pharmaceuticals, Inc. | TGF-β INHIBITORS |
EP3313420B1 (en) | 2015-06-25 | 2024-03-13 | The Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
EP3429603B1 (en) | 2016-03-15 | 2021-12-29 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
US11266647B2 (en) * | 2016-10-26 | 2022-03-08 | Icahn School Of Medicine At Mount Sinai | Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition |
EP3539957A4 (en) * | 2016-11-14 | 2020-05-13 | Jiangsu Hengrui Medicine Co., Ltd. | 3,4-BIPYRIDYL-PYRAZOLE DERIVATIVE AND PRODUCTION METHOD THEREFOR AND MEDICAL USE THEREOF |
CA3084581A1 (en) | 2017-11-20 | 2019-05-23 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
AU2019205944A1 (en) | 2018-01-05 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
AU2019240065A1 (en) | 2018-03-20 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
TW202012390A (zh) * | 2018-06-29 | 2020-04-01 | 日商日本歐愛特農業科技股份有限公司 | 新穎之經取代吡唑衍生物 |
CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
EP3894401A2 (en) | 2018-12-11 | 2021-10-20 | Theravance Biopharma R&D IP, LLC | Naphthyridine and quinoline derivatives useful as alk5 inhibitors |
CN110467601B (zh) * | 2019-08-29 | 2021-07-02 | 杭州市西溪医院 | 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用 |
IL293084A (en) | 2019-11-22 | 2022-07-01 | Theravance Biopharma R& D Ip Llc | 5,1-Converted naphthyridines or quinolines as alk5 inhibitors |
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US3492397A (en) | 1967-04-07 | 1970-01-27 | Warner Lambert Pharmaceutical | Sustained release dosage in the pellet form and process thereof |
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US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
WO2000061576A1 (en) | 1999-04-09 | 2000-10-19 | Smithkline Beecham Corporation | Triarylimidazoles |
CO5271680A1 (es) | 2000-02-21 | 2003-04-30 | Smithkline Beecham Corp | Compuestos |
GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
PE20020506A1 (es) | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
WO2002040468A1 (en) | 2000-11-16 | 2002-05-23 | Smithkline Beecham Corporation | Compounds |
GB0027987D0 (en) | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
JP2004521901A (ja) * | 2001-02-02 | 2004-07-22 | グラクソ グループ リミテッド | Tgf阻害剤としてのピラゾール |
US20040087623A1 (en) * | 2001-02-02 | 2004-05-06 | Gellibert Francoise Jeanne | Pyrazole derivatives against tgf overexpression |
GB0102672D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
MXPA03008142A (es) | 2001-03-09 | 2003-12-12 | Pfizer Prod Inc | Nuevos compuestos antiinflamatorios de bencimidazol. |
EP1382603B1 (en) | 2001-04-26 | 2008-07-23 | Eisai R&D Management Co., Ltd. | Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof |
AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
JP2005539000A (ja) | 2002-07-31 | 2005-12-22 | スミスクライン・ビーチャム・コーポレイション | Alk5阻害剤としての2−フェニルピリジン−4−イル誘導体 |
EA200500286A1 (ru) | 2002-09-18 | 2005-08-25 | Пфайзер Продактс Инк. | Новые изотиазольные и изоксазольные соединения в качестве ингибиторов трансформирующего фактора роста (тфр) |
AP2005003260A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Novel triazole compounds as transforming growth factor (TGF) inhibitors. |
CN1681805A (zh) | 2002-09-18 | 2005-10-12 | 辉瑞产品公司 | 作为转化生长因子(tgf)抑制剂的新的咪唑类化合物 |
JP4519657B2 (ja) * | 2002-09-18 | 2010-08-04 | ファイザー・プロダクツ・インク | 形質転換成長因子(tgf)阻害剤としての新規なピラゾ−ル化合物 |
DE60327443D1 (de) | 2002-09-18 | 2009-06-10 | Pfizer Prod Inc | Neue oxazolverbindungen als inhibitoren des transforming growth factor (tgf) |
PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
-
2003
- 2003-09-08 JP JP2004568904A patent/JP4519657B2/ja not_active Expired - Fee Related
- 2003-09-08 CA CA2496295A patent/CA2496295C/en not_active Expired - Fee Related
- 2003-09-08 EP EP09177298A patent/EP2165708A3/en not_active Withdrawn
- 2003-09-08 KR KR1020057004598A patent/KR20050044807A/ko not_active Application Discontinuation
- 2003-09-08 BR BR0314302-3A patent/BR0314302A/pt not_active IP Right Cessation
- 2003-09-08 WO PCT/IB2003/003933 patent/WO2004026306A2/en active Application Filing
- 2003-09-08 CN CNA038222655A patent/CN1681501A/zh active Pending
- 2003-09-08 EA EA200500377A patent/EA200500377A1/ru unknown
- 2003-09-08 OA OA1200500078A patent/OA12929A/en unknown
- 2003-09-08 AU AU2003259475A patent/AU2003259475A1/en not_active Abandoned
- 2003-09-08 AP AP2005003263A patent/AP2005003263A0/xx unknown
- 2003-09-08 EP EP03797443A patent/EP1542684B1/en not_active Expired - Lifetime
- 2003-09-08 MX MXPA05002376A patent/MXPA05002376A/es active IP Right Grant
- 2003-09-08 DE DE60330362T patent/DE60330362D1/de not_active Expired - Lifetime
- 2003-09-08 ES ES03797443T patent/ES2335099T3/es not_active Expired - Lifetime
- 2003-09-08 AT AT03797443T patent/ATE450258T1/de not_active IP Right Cessation
- 2003-09-08 PL PL03375979A patent/PL375979A1/xx not_active Application Discontinuation
- 2003-09-15 PE PE2003000940A patent/PE20040988A1/es not_active Application Discontinuation
- 2003-09-16 UY UY27985A patent/UY27985A1/es not_active Application Discontinuation
- 2003-09-16 AR ARP030103356A patent/AR041272A1/es unknown
- 2003-09-17 US US10/667,189 patent/US6958354B2/en not_active Expired - Fee Related
- 2003-09-17 PA PA20038583201A patent/PA8583201A1/es unknown
-
2005
- 2005-02-16 NO NO20050838A patent/NO20050838L/no unknown
- 2005-02-17 IS IS7698A patent/IS7698A/is unknown
- 2005-03-16 HR HR20050247A patent/HRP20050247A2/hr not_active Application Discontinuation
- 2005-03-16 EC EC2005005679A patent/ECSP055679A/es unknown
- 2005-03-16 CO CO05024529A patent/CO5550456A2/es not_active Application Discontinuation
- 2005-03-18 MA MA28154A patent/MA27440A1/fr unknown
- 2005-09-23 US US11/234,564 patent/US7151110B2/en not_active Expired - Fee Related
-
2006
- 2006-11-08 US US11/557,638 patent/US7638537B2/en not_active Expired - Fee Related
-
2009
- 2009-11-12 US US12/617,027 patent/US20100056571A1/en not_active Abandoned
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2737737C2 (ru) * | 2016-06-13 | 2020-12-02 | Джинфлит Терапьютикс (Шанхай) Инк. | АЛЬФА- И БЕТА-НЕНАСЫЩЕННОЕ АМИДНОЕ СОЕДИНЕНИЕ - ПРОИЗВОДНОЕ БЕНЗОТРИАЗОЛА, ПРИМЕНЯЕМОЕ В КАЧЕСТВЕ ИНГИБИТОРА TGF-βRI |
RU2750702C1 (ru) * | 2017-12-13 | 2021-07-01 | Джинфлит Терапьютикс (Шанхай) Инк. | КРИСТАЛЛИЧЕСКАЯ ФОРМА И СОЛЕВАЯ ФОРМА ИНГИБИТОРА TGF-βRI И СПОСОБ ИХ ПОЛУЧЕНИЯ |
US11236112B2 (en) | 2017-12-13 | 2022-02-01 | Genfleet Therapeutics (Shanghai) Inc. | Crystal form and salt form of TGF-βRI inhibitor and preparation method therefor |
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EA200500286A1 (ru) | Новые изотиазольные и изоксазольные соединения в качестве ингибиторов трансформирующего фактора роста (тфр) | |
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