CO5550458A2 - Nuevos compuestos de isotiazol e isoxazol como inhibidores del factor de crecimiento transformador (tgf) - Google Patents
Nuevos compuestos de isotiazol e isoxazol como inhibidores del factor de crecimiento transformador (tgf)Info
- Publication number
- CO5550458A2 CO5550458A2 CO05025189A CO05025189A CO5550458A2 CO 5550458 A2 CO5550458 A2 CO 5550458A2 CO 05025189 A CO05025189 A CO 05025189A CO 05025189 A CO05025189 A CO 05025189A CO 5550458 A2 CO5550458 A2 CO 5550458A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- heteroaryl
- aryl
- amino
- heterocyclyl
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- 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
- 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
1.- Un compuesto de fórmula (A) o una sal, profármaco, hidrato, tautómero o solvato farmacéuticamente aceptable del mismo en el que:X es O o S;R1 es un anillo saturado, insaturado o aromático C3-C20, mono-, bi- o policíclico que contiene, opcionalmente, al menos un heteroátomo seleccionado del grupo constituido por N, O y S; R1 puede estar opcionalmente sustituido independientemente además con al menos un resto seleccionado independientemente del grupo constituido por: carbonilo, halo, haloalquilo(C1-C6), perhaloalquilo(C1-C6), perhaloalcoxi(C1-C6), alquilo(C1-C6), alquenilo(C2-C6), alquinilo (C2-C6), hidroxi, oxo, mercapto, alquil(C1-C6)tio, alcoxi(C1-C6), arilo(C5-C10) o heteroarilo(C5-C10), aril(C5-C10)oxi o heteroaril(C5-C10)oxi, aril(C5-C10)alquilo(C1-C6) o heteroaril(C5-C10)alquilo(C1-C6), aril(C5-C10)alcoxi(C1-C6) o heteroaril(C5-C10)alcoxi(C1-C6), HO-(C=O)-, éster, amido, éter, amino, aminoalquilo(C1-C6), alquil(C1-C6)aminoalquilo(C1-C6), dialquil(C1-C6)aminoalquilo(C1-C6), heterociclil(C5-C10)alquilo(C1-C6), alquil(C1-C6)- y dialquil(C1-C6)amino, ciano, nitro, carbamoílo, alquil(C1-C6)carbonilo, alcoxi(C1-C6)carbonilo, alquil(C1-C6)aminocarbonilo, dialquil(C1-C6)aminocarbonilo, aril(C5-C10)carbonilo, aril(C5-C10)oxicarbonilo, alquil(C1-C6)sulfonilo y aril( C5-C10)sulfonilo;cada R3 se selecciona independientemente del grupo constituido por hidrógeno, halo, haloalquilo(C1-C6), alquilo(C1-C6), alquenilo(C2-C6), alquinilo(C2-C6), perhaloalquilo(C1-C6), fenilo, heteroarilo(C5-C10), heterociclilo(C5-C10), cicloalquil(C3-C10), hidroxi, alcoxi(C1-C6), perhaloalcoxi(C1-C6), fenoxi, heteroaril(C5-C10)-O-, heterociclil(C5-C10)-O-, cicloalquil(C3-C10)-O-, alquil(C1-C6)-S-, alquil(C1-C6)-SO2-, alquil(C1-C6)-NH-SO2-, O2N-, NC-, amino, Ph(CH2)1-6HN-, alquil(C1-C6)-HN-, alquil(C1-C6)amino, [alquil(C1-C6)]2-amino, alquil(C1-C6)-SO2-NH-, amino(C=O)-, aminoO2S-, alquil(C1-C6)-(C=O)-NH-, alquil(C1-C6)-(C=O)-[(alquil(C1-C6))-N]-, fenil-(C=O)-NH-, fenil-(C=O)-[alquil(C1-C6)-N]-, alquil(C1-C6)-(C=O)-, fenil-(C=O)-, heteroaril(C5-C10)-(C=O)-, heterociclil(C5-C10)-(C=O)-, cicloalquil(C3 -C10)-(C=O)-, HO-(C=O)-, alquil(C1-C6)-O-(C=O)-, H2N(C=O)-, alquil(C1-C6)-NH-(C=O)-, ...
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41213102P | 2002-09-18 | 2002-09-18 | |
| US48458003P | 2003-07-02 | 2003-07-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5550458A2 true CO5550458A2 (es) | 2005-08-31 |
Family
ID=32033584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO05025189A CO5550458A2 (es) | 2002-09-18 | 2005-03-18 | Nuevos compuestos de isotiazol e isoxazol como inhibidores del factor de crecimiento transformador (tgf) |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7030125B2 (es) |
| EP (1) | EP1542995A1 (es) |
| JP (1) | JP2006506443A (es) |
| KR (1) | KR20050057441A (es) |
| CN (1) | CN1681809A (es) |
| AP (1) | AP2005003262A0 (es) |
| AR (1) | AR041275A1 (es) |
| AU (1) | AU2003263431A1 (es) |
| BR (1) | BR0314286A (es) |
| CA (1) | CA2499332A1 (es) |
| CO (1) | CO5550458A2 (es) |
| EA (1) | EA200500286A1 (es) |
| EC (1) | ECSP055685A (es) |
| HR (1) | HRP20050246A2 (es) |
| IS (1) | IS7695A (es) |
| MA (1) | MA27444A1 (es) |
| MX (1) | MXPA05002378A (es) |
| NO (1) | NO20051852L (es) |
| OA (1) | OA12925A (es) |
| PA (1) | PA8583101A1 (es) |
| PE (1) | PE20050076A1 (es) |
| PL (1) | PL375973A1 (es) |
| TW (1) | TW200410954A (es) |
| UY (1) | UY27983A1 (es) |
| WO (1) | WO2004026865A1 (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05002332A (es) | 2002-09-18 | 2005-06-08 | Pfizer Prod Inc | Nuevos compuestos de oxazol y tiazol como inhibidores del factor de crecimiento transformador (tgf). |
| CN1681501A (zh) * | 2002-09-18 | 2005-10-12 | 辉瑞产品公司 | 作为转化生长因子(tgf)抑制剂的吡唑衍生物 |
| EA200500378A1 (ru) | 2002-09-18 | 2005-08-25 | Пфайзер Продактс Инк. | Новые соединения имидазола в качестве ингибиторов трансформирующего фактора роста (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) |
| AU2005329423A1 (en) | 2004-09-20 | 2006-09-28 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| US7951805B2 (en) | 2004-09-20 | 2011-05-31 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase |
| WO2006034315A2 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes |
| AR051202A1 (es) | 2004-09-20 | 2006-12-27 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
| MX2007003321A (es) | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
| CA2580845A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase |
| CN101083994A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其用作硬脂酰CoA去饱和酶抑制剂的用途 |
| JP5123671B2 (ja) | 2005-02-17 | 2013-01-23 | シンタ ファーマシューティカルズ コーポレーション | 増殖性疾患の治療のための化合物 |
| BRPI0611187A2 (pt) | 2005-06-03 | 2010-08-24 | Xenon Pharmaceuticals Inc | derivados aminotiazàis como inibidores da estearoil-coa desaturase humana |
| ZA200804496B (en) * | 2005-12-16 | 2009-09-30 | Alcon Inc | Control of intraocular pressure using ALK5 modulation agents |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基***并吡啶，其組合物及使用其之治療方法 |
| AU2014240603B2 (en) | 2013-03-14 | 2017-11-09 | Massachusetts Institute Of Technology | Compositions and methods for epithelial stem cell expansion and culture |
| PL3089971T3 (pl) | 2014-01-01 | 2021-01-25 | Medivation Technologies Llc | Związki i sposoby ich zastosowania |
| KR102493376B1 (ko) | 2014-09-03 | 2023-01-27 | 더 브리검 앤드 우먼즈 하스피털, 인크. | 청력 손실의 치료를 위해 내이 털세포를 생성하기 위한 조성물, 시스템, 및 방법 |
| WO2016210292A1 (en) | 2015-06-25 | 2016-12-29 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
| AU2017205194A1 (en) | 2016-01-08 | 2018-07-19 | Massachusetts Institute Of Technology | Production of differentiated enteroendocrine cells and insulin producing cells |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| EP3429603B1 (en) | 2016-03-15 | 2021-12-29 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
| SG10201910821XA (en) | 2016-12-30 | 2020-01-30 | Frequency Therapeutics Inc | 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| JP2021518413A (ja) | 2018-03-20 | 2021-08-02 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物及び組成物ならびに使用方法 |
| WO2019236766A1 (en) | 2018-06-06 | 2019-12-12 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
| CN113195707A (zh) | 2018-08-17 | 2021-07-30 | 频率治疗公司 | 用于通过上调jag-1来生成毛细胞的组合物和方法 |
| WO2020037326A1 (en) | 2018-08-17 | 2020-02-20 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating foxo |
| AU2019419414A1 (en) | 2018-12-31 | 2023-04-06 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5095272A (es) * | 1973-12-24 | 1975-07-29 | ||
| EP0983260A2 (en) | 1997-05-22 | 2000-03-08 | G.D. Searle & Co. | 3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| US6087381A (en) | 1997-05-22 | 2000-07-11 | G. D. Searle & Company | Pyrazole derivatives as p38 kinase inhibitors |
| DE60001229T2 (de) | 1999-04-09 | 2003-10-30 | Smithkline Beecham Corp | Triarylimidazole |
| AR029803A1 (es) | 2000-02-21 | 2003-07-16 | Smithkline Beecham Plc | Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden |
| 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 |
| GB0027987D0 (en) * | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
| JP2004517068A (ja) | 2000-11-16 | 2004-06-10 | スミスクライン・ビーチャム・コーポレイション | 化合物 |
| GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
| US20040097502A1 (en) * | 2001-02-02 | 2004-05-20 | Gellibert Francoise Jeanne | Pyrazoles as tgf inhibitors |
| GB0102668D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| GB0102672D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| ATE291020T1 (de) * | 2001-02-02 | 2005-04-15 | Smithkline Beecham Corp | Pyrazolderivate gegen tgf überexprimierung |
| US6673818B2 (en) * | 2001-04-20 | 2004-01-06 | Pharmacia Corporation | Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation |
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| WO2004013135A1 (en) | 2002-07-31 | 2004-02-12 | Smithkline Beecham Corporation | 2-phenylpyridin-4-yl derivatives as alk5 inhibitors |
-
2003
- 2003-09-12 BR BR0314286-8A patent/BR0314286A/pt not_active IP Right Cessation
- 2003-09-12 EP EP03797466A patent/EP1542995A1/en not_active Withdrawn
- 2003-09-12 EA EA200500286A patent/EA200500286A1/ru unknown
- 2003-09-12 AU AU2003263431A patent/AU2003263431A1/en not_active Abandoned
- 2003-09-12 WO PCT/IB2003/004005 patent/WO2004026865A1/en active Application Filing
- 2003-09-12 KR KR1020057004662A patent/KR20050057441A/ko not_active Application Discontinuation
- 2003-09-12 CA CA002499332A patent/CA2499332A1/en not_active Abandoned
- 2003-09-12 JP JP2004568905A patent/JP2006506443A/ja not_active Withdrawn
- 2003-09-12 CN CNA038222043A patent/CN1681809A/zh active Pending
- 2003-09-12 PL PL03375973A patent/PL375973A1/xx not_active Application Discontinuation
- 2003-09-12 MX MXPA05002378A patent/MXPA05002378A/es active IP Right Grant
- 2003-09-12 AP AP2005003262A patent/AP2005003262A0/xx unknown
- 2003-09-12 OA OA1200500074A patent/OA12925A/en unknown
- 2003-09-15 TW TW092125380A patent/TW200410954A/zh unknown
- 2003-09-16 AR ARP030103359A patent/AR041275A1/es unknown
- 2003-09-16 UY UY27983A patent/UY27983A1/es not_active Application Discontinuation
- 2003-09-17 PA PA20038583101A patent/PA8583101A1/es unknown
- 2003-09-17 US US10/667,167 patent/US7030125B2/en not_active Expired - Fee Related
- 2003-09-17 PE PE2003000951A patent/PE20050076A1/es not_active Application Discontinuation
-
2005
- 2005-02-14 IS IS7695A patent/IS7695A/is unknown
- 2005-03-16 HR HR20050246A patent/HRP20050246A2/hr not_active Application Discontinuation
- 2005-03-17 EC EC2005005685A patent/ECSP055685A/es unknown
- 2005-03-18 MA MA28158A patent/MA27444A1/fr unknown
- 2005-03-18 CO CO05025189A patent/CO5550458A2/es not_active Application Discontinuation
- 2005-04-15 NO NO20051852A patent/NO20051852L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PL375973A1 (en) | 2005-12-12 |
| TW200410954A (en) | 2004-07-01 |
| MXPA05002378A (es) | 2005-05-23 |
| EA200500286A1 (ru) | 2005-08-25 |
| US7030125B2 (en) | 2006-04-18 |
| NO20051852L (no) | 2005-06-16 |
| CN1681809A (zh) | 2005-10-12 |
| OA12925A (en) | 2006-10-13 |
| IS7695A (is) | 2005-02-14 |
| JP2006506443A (ja) | 2006-02-23 |
| UY27983A1 (es) | 2004-04-30 |
| AR041275A1 (es) | 2005-05-11 |
| MA27444A1 (fr) | 2005-07-01 |
| PE20050076A1 (es) | 2005-03-26 |
| HRP20050246A2 (en) | 2005-10-31 |
| EP1542995A1 (en) | 2005-06-22 |
| ECSP055685A (es) | 2005-05-30 |
| WO2004026865A1 (en) | 2004-04-01 |
| BR0314286A (pt) | 2005-08-02 |
| PA8583101A1 (es) | 2004-04-23 |
| CA2499332A1 (en) | 2004-04-01 |
| KR20050057441A (ko) | 2005-06-16 |
| AU2003263431A1 (en) | 2004-04-08 |
| AP2005003262A0 (en) | 2005-03-31 |
| US20040116473A1 (en) | 2004-06-17 |
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