TW200412346A - Novel triazole compounds as transforming growth factor (TGF) inhibitors - Google Patents
Novel triazole compounds as transforming growth factor (TGF) inhibitors Download PDFInfo
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- TW200412346A TW200412346A TW092125634A TW92125634A TW200412346A TW 200412346 A TW200412346 A TW 200412346A TW 092125634 A TW092125634 A TW 092125634A TW 92125634 A TW92125634 A TW 92125634A TW 200412346 A TW200412346 A TW 200412346A
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- Prior art keywords
- alkyl
- group
- crc6
- phenyl
- heteroaryl
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- -1 triazole compounds Chemical class 0.000 title claims abstract description 61
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- 125000000217 alkyl group Chemical group 0.000 claims description 93
- 150000003839 salts Chemical class 0.000 claims description 43
- 125000003545 alkoxy group Chemical group 0.000 claims description 32
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 25
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 19
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- 229940002612 prodrug Drugs 0.000 claims description 16
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 125000003282 alkyl amino group Chemical group 0.000 claims description 11
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Classifications
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- 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
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- 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
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- 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
Landscapes
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
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| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| BR0314302A (pt) * | 2002-09-18 | 2005-07-05 | Pfizer Producs Inc | Compostos de pirazol como inibidores do fator de crescimento trnasformante (tgf) |
| WO2004026859A1 (en) | 2002-09-18 | 2004-04-01 | Pfizer Products Inc. | Novel imidazole compounds as transforming growth factor (tgf) inhibitors |
| AU2003256003A1 (en) | 2002-09-18 | 2004-04-08 | Pfizer Products Inc. | Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors |
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| CN101163684B (zh) | 2005-02-23 | 2012-08-29 | 盐野义制药株式会社 | 具有酪氨酸激酶抑制作用的喹唑啉衍生物 |
| AU2006272652B2 (en) * | 2005-07-25 | 2011-06-16 | Synta Pharmaceuticals Corp. | 1,2,3-triazoles inhibitors of tubulin polymerization for the treatment of proliferative disorders |
| KR20080082618A (ko) * | 2005-12-16 | 2008-09-11 | 알콘, 인코퍼레이티드 | Ａｌｋ5 조절제를 사용한 안압의 조절 |
| DE102005061840A1 (de) | 2005-12-23 | 2007-06-28 | Merck Patent Gmbh | Triazolderivate |
| WO2008009077A2 (en) * | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections |
| US9259426B2 (en) | 2006-07-20 | 2016-02-16 | Gilead Sciences, Inc. | 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
| US9782452B2 (en) | 2011-11-22 | 2017-10-10 | Cornell University | Methods for stimulating hematopoietic recovery by inhibiting TGFβ signaling |
| ES2966030T3 (es) | 2012-10-05 | 2024-04-18 | Kadmon Corp Llc | Anticuerpos anti-VEGFR-2/KDR humanos |
| CA3184040A1 (en) | 2013-03-14 | 2014-10-02 | The Brigham And Women's Hospital, Inc. | Compositions and methods for epithelial stem cell expansion comprising a wnt agonist and a histone deacetylase inhibitor |
| CA2935392C (en) | 2014-01-01 | 2022-07-26 | Medivation Technologies, Inc. | Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity |
| WO2016037016A1 (en) | 2014-09-03 | 2016-03-10 | The Brigham And Women's Hospital, Inc. | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
| AU2016216673B2 (en) | 2015-03-04 | 2017-02-02 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| 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 |
| US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| AU2017318601B2 (en) | 2016-09-02 | 2020-09-03 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| CN110392686A (zh) | 2016-12-30 | 2019-10-29 | 频率治疗公司 | 1h-吡咯-2,5-二酮化合物以及使用它们来诱导干/祖支持细胞自我更新的方法 |
| WO2019183245A1 (en) | 2018-03-20 | 2019-09-26 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| CN112867724B (zh) | 2018-07-23 | 2024-06-04 | 熙源安健医药(北京)有限公司 | 二膦酸盐药物缀合物 |
| US11162071B2 (en) | 2018-08-17 | 2021-11-02 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by upregulating JAG-1 |
| 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 |
| TW202212339A (zh) | 2019-04-17 | 2022-04-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI751516B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI879779B (zh) | 2019-06-28 | 2025-04-11 | 美商基利科學股份有限公司 | 類鐸受體調節劑化合物的製備方法 |
| CN112694477B (zh) * | 2019-10-22 | 2024-02-06 | 四川科伦博泰生物医药股份有限公司 | 吡唑并环类化合物，包含其的药物组合物，其制备方法及其用途 |
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| JPS6058981A (ja) * | 1983-09-09 | 1985-04-05 | Takeda Chem Ind Ltd | ５−ピリジル−１，３−チアゾ−ル誘導体，その製造法およびそれを含んでなる医薬組成物 |
| JPS6025142A (ja) | 1983-07-21 | 1985-02-07 | Matsushita Electric Ind Co Ltd | 表示装置の電極製造方法 |
| DE3486009T2 (de) * | 1983-09-09 | 1993-04-15 | Takeda Chemical Industries Ltd | 5-pyridyl-1,3-thiazol-derivate, ihre herstellung und anwendung. |
| GB9201692D0 (en) * | 1992-01-27 | 1992-03-11 | Smithkline Beecham Intercredit | Compounds |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| CA2288787A1 (en) | 1997-05-22 | 1998-11-26 | G.D. Searle And Co. | Pyrazole derivatives as p38 kinase inhibitors |
| RU2249591C2 (ru) | 1997-05-22 | 2005-04-10 | Дж.Д. Серл Энд Ко. | 3(5)-гетероарилзамещенные пиразолы в качестве ингибиторов киназы p38 |
| DE69821132T2 (de) * | 1997-10-27 | 2004-10-21 | Takeda Chemical Industries Ltd | 1,3-thiazole als adenosine a3 rezeptor antagonisten zur behandlung von asthma, allergien und diabetes |
| DE60001229T2 (de) | 1999-04-09 | 2003-10-30 | Smithkline Beecham Corp., Philadelphia | Triarylimidazole |
| JP2000302680A (ja) * | 1999-04-23 | 2000-10-31 | Takeda Chem Ind Ltd | 脳保護剤 |
| CA2381215A1 (en) * | 1999-08-06 | 2001-02-15 | Takeda Chemical Industries, Ltd. | P38map kinase inhibitors |
| 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 |
| WO2002040468A1 (en) | 2000-11-16 | 2002-05-23 | Smithkline Beecham Corporation | Compounds |
| CA2436739A1 (en) * | 2000-12-26 | 2002-07-04 | Takeda Chemical Industries, Ltd. | Combination agent |
| GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
| US20040077697A1 (en) * | 2001-02-02 | 2004-04-22 | Hiroyuki Koshio | 2-Acylaminothiazole derivative or its salt |
| US20040097502A1 (en) | 2001-02-02 | 2004-05-20 | Gellibert Francoise Jeanne | Pyrazoles as tgf inhibitors |
| GB0102672D0 (en) | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| DE60203263T2 (de) | 2001-02-02 | 2006-02-09 | Smithkline Beecham Corp. | Pyrazolderivate gegen tgf überexprimierung |
| GB0102673D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| GB0102668D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| GB0102665D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| US20050080113A1 (en) * | 2001-06-11 | 2005-04-14 | Shigenori Ohkawa | Medicinal compositions |
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| GB0217780D0 (en) | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
| TW200417547A (en) | 2002-07-31 | 2004-09-16 | Smithkline Beecham Corp | Compounds |
-
2003
- 2003-09-08 KR KR1020057004575A patent/KR20050057393A/ko not_active Ceased
- 2003-09-08 MX MXPA05002982A patent/MXPA05002982A/es unknown
- 2003-09-08 HR HR20050251A patent/HRP20050251A2/hr not_active Application Discontinuation
- 2003-09-08 PL PL03375974A patent/PL375974A1/xx not_active Application Discontinuation
- 2003-09-08 OA OA1200500076A patent/OA12927A/en unknown
- 2003-09-08 JP JP2004568900A patent/JP2006502236A/ja not_active Abandoned
- 2003-09-08 AP AP2005003260A patent/AP2005003260A0/xx unknown
- 2003-09-08 BR BR0314577-8A patent/BR0314577A/pt not_active IP Right Cessation
- 2003-09-08 AU AU2003260810A patent/AU2003260810A1/en not_active Abandoned
- 2003-09-08 EP EP03797428A patent/EP1542685A1/en not_active Withdrawn
- 2003-09-08 CN CNA038221594A patent/CN1681502A/zh active Pending
- 2003-09-08 EA EA200500376A patent/EA200500376A1/ru unknown
- 2003-09-08 WO PCT/IB2003/003825 patent/WO2004026307A1/en not_active Ceased
- 2003-09-08 CA CA002497971A patent/CA2497971A1/en not_active Abandoned
- 2003-09-16 AR ARP030103360A patent/AR041276A1/es unknown
- 2003-09-16 PE PE2003000947A patent/PE20050074A1/es not_active Application Discontinuation
- 2003-09-16 UY UY27981A patent/UY27981A1/es not_active Application Discontinuation
- 2003-09-17 TW TW092125634A patent/TW200412346A/zh unknown
- 2003-09-17 PA PA20038583401A patent/PA8583401A1/es unknown
- 2003-09-17 US US10/667,183 patent/US7053095B2/en not_active Expired - Fee Related
-
2005
- 2005-02-24 NO NO20051010A patent/NO20051010L/no unknown
- 2005-02-24 IS IS7713A patent/IS7713A/is unknown
- 2005-03-16 CO CO05024528A patent/CO5540390A2/es not_active Application Discontinuation
- 2005-03-17 EC EC2005005681A patent/ECSP055681A/es unknown
- 2005-03-18 MA MA28156A patent/MA27442A1/fr unknown
-
2006
- 2006-02-07 US US11/349,481 patent/US20060128761A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004026307A1 (en) | 2004-04-01 |
| CN1681502A (zh) | 2005-10-12 |
| NO20051010L (no) | 2005-05-31 |
| US20040110798A1 (en) | 2004-06-10 |
| UY27981A1 (es) | 2004-04-30 |
| PA8583401A1 (es) | 2004-04-23 |
| MA27442A1 (fr) | 2005-07-01 |
| US20060128761A1 (en) | 2006-06-15 |
| ECSP055681A (es) | 2005-05-30 |
| AU2003260810A1 (en) | 2004-04-08 |
| MXPA05002982A (es) | 2005-06-22 |
| EA200500376A1 (ru) | 2005-08-25 |
| CA2497971A1 (en) | 2004-04-01 |
| US7053095B2 (en) | 2006-05-30 |
| KR20050057393A (ko) | 2005-06-16 |
| PL375974A1 (en) | 2005-12-12 |
| PE20050074A1 (es) | 2005-03-21 |
| EP1542685A1 (en) | 2005-06-22 |
| JP2006502236A (ja) | 2006-01-19 |
| HRP20050251A2 (en) | 2005-10-31 |
| OA12927A (en) | 2006-10-13 |
| IS7713A (is) | 2005-02-24 |
| BR0314577A (pt) | 2005-08-09 |
| CO5540390A2 (es) | 2005-07-29 |
| AR041276A1 (es) | 2005-05-11 |
| AP2005003260A0 (en) | 2005-03-31 |
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