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公开(公告)号:EP1158986A1
公开(公告)日:2001-12-05
申请号:EP99963112.0
申请日:1999-12-21
发明人: MARQUIS, Robert, Wells, Jr. , RU, Yu , VEBER, Daniel, Frank , CUMMINGS, Maxwell, David , THOMPSON, Scott, Kevin , YAMASHITA, Dennis
IPC分类号: A61K31/55 , C07D223/08 , C07D401/02 , C07D403/02 , C07D405/02 , C07D409/02 , C07D411/02 , C07D413/02 , C07D417/02 , C07D419/02
CPC分类号: C07D405/14 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04
摘要: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
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公开(公告)号:EP3760623A1
公开(公告)日:2021-01-06
申请号:EP20184866.0
申请日:2015-12-17
发明人: GOODACRE, Simon Charles , LABADIE, Sharada , LIANG, Jun , ORTWINE, Daniel Fred , RAY, Nicholas Charles , WANG, Xiaojing , ZBIEG, Jason , ZHANG, Birong
IPC分类号: C07D401/14 , A61K31/397 , A61K31/4025 , C07D403/02 , C07D403/14 , C07D409/02 , C07D413/02 , C07D417/02 , C07D417/14 , C07D205/04 , C07D207/08 , C07D493/04 , C07D411/02 , A61P35/00
摘要: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure:
and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.-
公开(公告)号:EP1320370A1
公开(公告)日:2003-06-25
申请号:EP01966474.7
申请日:2001-08-31
IPC分类号: A61K31/55 , C07D223/08 , C07D401/02 , C07D403/02 , C07D405/02 , C07D409/02 , C07D411/02 , C07D413/02 , C07D417/02 , C07D419/02
CPC分类号: C07D401/12 , A61K31/55 , A61K38/00 , C07D223/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04 , C07K5/06139 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/422 , Y02A50/491
摘要: The present invention relates to methods of treating parasitic diseases which are mediated by cysteine proteases by administration of 4-amino-azepan-3-one protease inhibitors. In particular, the present invention relates to a method of treating malaria by inhibiting the cysteine protease falcipain.
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公开(公告)号:EP3233828A1
公开(公告)日:2017-10-25
申请号:EP15810659.1
申请日:2015-12-17
发明人: SMITH, Nicholas D. , LIANG, Jun , ORTWINE, Daniel Fred , WANG, Xiaojing , KAHRAMAN, Mehmet , NAGASAWA, Johnny Y. , GOODACRE, Simon Charles , RAY, Nicholas Charles , GOVEK, Steven P.
IPC分类号: C07D401/14 , A61K31/397 , A61K31/4025 , C07D403/02 , C07D403/14 , C07D409/02 , C07D413/02 , C07D417/02 , C07D417/14 , C07D205/04 , C07D207/08 , C07D493/04 , C07D411/02
摘要: Described herein are compounds that are estrogen receptor modulators of Formula (I) and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
摘要翻译: 本文描述的是式(I)的雌激素受体调节剂及其立体异构体,互变异构体或药学上可接受的盐的化合物,其中SERMF是选择性雌激素受体调节剂片段并且具有本文所述的取代基和结构特征。 还描述了包含本文所述化合物的药物组合物和药物,以及单独使用此类雌激素受体调节剂并与其他化合物一起使用以治疗介导或依赖于雌激素受体的疾病或病症的方法。
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公开(公告)号:EP0948327B1
公开(公告)日:2006-03-08
申请号:EP97952573.0
申请日:1997-12-19
申请人: Merck & Co., Inc.
IPC分类号: A61K31/135 , C07D413/04 , C07D411/02 , C07D213/56 , C07D405/12 , C07D413/12 , C07D209/18 , C07D307/80 , C07D407/12 , C07D307/92 , C07D403/12 , A61K31/47 , A61K31/41 , A61K31/40 , A61K31/395 , A61K31/415 , C07D409/12 , C07D209/12
CPC分类号: A61K31/135 , A61K31/343 , A61K31/395 , A61K31/40 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/423 , A61K31/47 , A61K31/4709 , A61K31/517 , C07D209/12 , C07D209/18 , C07D213/56 , C07D307/80 , C07D307/83 , C07D307/92 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D411/02 , C07D413/04 , C07D413/12
摘要: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compound which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
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公开(公告)号:EP1320370A4
公开(公告)日:2008-10-22
申请号:EP01966474
申请日:2001-08-31
发明人: TEW DAVID G , THOMPSON SCOTT K , VEBER DANIEL F
IPC分类号: A61K31/55 , A61K38/00 , A61P33/00 , A61P33/06 , A61P43/00 , C07D223/08 , C07D223/12 , C07D401/02 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/12 , C07D405/02 , C07D405/12 , C07D405/14 , C07D409/02 , C07D409/12 , C07D409/14 , C07D411/02 , C07D413/02 , C07D413/14 , C07D417/02 , C07D417/14 , C07D419/02 , C07D471/04 , C07D495/04 , C07K5/078
CPC分类号: C07D401/12 , A61K31/55 , A61K38/00 , C07D223/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04 , C07K5/06139
摘要: The present invention relates to methods of treating parasitic diseases which are mediated by cysteine proteases by administration of 4-amino-azepan-3-one protease inhibitors. In particular, the present invention relates to a method of treating malaria by inhibiting the cysteine protease falcipain.
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公开(公告)号:EP1158986A4
公开(公告)日:2002-03-27
申请号:EP99963112
申请日:1999-12-21
发明人: MARQUIS ROBERT WELLS JR , RU YU , VEBER DANIEL FRANK , CUMMINGS MAXWELL DAVID , THOMPSON SCOTT KEVIN , YAMASHITA DENNIS
IPC分类号: A61K31/4375 , A61K31/55 , A61P1/02 , A61P3/14 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/00 , A61P31/04 , A61P33/00 , A61P33/06 , A61P33/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07D223/08 , C07D401/02 , C07D403/02 , C07D405/02 , C07D409/02 , C07D411/02 , C07D413/02 , C07D417/02 , C07D419/02
CPC分类号: C07D405/14 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04
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公开(公告)号:EP3233828B1
公开(公告)日:2020-03-04
申请号:EP15810659.1
申请日:2015-12-17
发明人: SMITH, Nicholas D. , LIANG, Jun , ORTWINE, Daniel Fred , WANG, Xiaojing , KAHRAMAN, Mehmet , NAGASAWA, Johnny Y. , GOODACRE, Simon Charles , RAY, Nicholas Charles , GOVEK, Steven P.
IPC分类号: C07D401/14 , A61K31/397 , A61K31/4025 , C07D403/02 , C07D403/14 , C07D409/02 , C07D413/02 , C07D417/02 , C07D417/14 , C07D205/04 , C07D207/08 , C07D493/04 , C07D411/02
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公开(公告)号:EP1828169A2
公开(公告)日:2007-09-05
申请号:EP05853144.3
申请日:2005-12-07
发明人: MICHELOTTI, Enrique Luis Four Valley Square , SPRINGMAN, Eric Bruce Four Valley Square , NGUYEN, Duyan Four Valley Square , SHETTY, Rupa S. Four Valley Square , LEE, Younghee Four Valley Square , MOFFETT, Kristofer Kent Four Valley Square , LUDINGTON, Jennifer Lee Four Valley Square , FUJIMOTO, Ted Tsutomu Four Valley Square , KONTEATIS, Zenon D. Four Valley Square , LIU, Bin Four Valley Square , HOLLINGER, Frank Four Valley Square , DORSEY, Bruce D. Four Valley Square
IPC分类号: C07D403/02 , C07D403/14 , C07D405/02 , C07D405/14 , C07D407/02 , C07D407/14 , C07D411/02 , C07D411/14 , C07D413/02 , C07D413/14 , A61K31/381 , A61K31/4155 , A61K31/445 , A61P19/02 , A61P35/00
CPC分类号: C07D333/38 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/56 , C07D295/192 , C07D333/36 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D495/04
摘要: The present invention is directed to a compound having the formula (I) wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP Kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
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公开(公告)号:EP1824843A2
公开(公告)日:2007-08-29
申请号:EP05853146.8
申请日:2005-12-07
IPC分类号: C07D403/02 , C07D403/14 , C07D405/02 , C07D405/14 , C07D407/02 , C07D411/02 , C07D411/14 , C07D413/02 , C07D413/04 , C07D417/02 , C07D417/14 , A61K31/4155 , A61K31/445 , A61P19/02 , A61P35/00
CPC分类号: C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
摘要: The present invention is directed to a compound having the formula (I) wherein R1, R2, R3, R4, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The present invention is also directed to compounds that stabilize the open conformation of a protein kinase, a crystallized protein kinase in the open conformation, and uses thereof. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease.
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