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公开(公告)号：WO2013134085A8
公开(公告)日：2014-09-04
申请号：PCT/US2013028796
申请日：2013-03-04
发明人： BUKHTIYAROV YURI , CACATIAN SALVACION , DILLARD LAWRENCE WAYNE , DORNER-CIOSSEK CORNELIA , FUCHS KLAUS , JIA LANQI , LALA DEEPAK S , MORALES-RAMOS ANGEL , RAST GEORG , REEVES JONATHAN , SINGH SURESH B , VENKATRAMAN SHANKAR , XU ZHENRONG , YUAN JING , ZHAO YI , ZHENG YAJUN
IPC分类号： C07D235/02 , A61K31/4184 , A61P25/28 , C07C49/323 , C07D403/06 , C07D407/06
CPC分类号： A61K31/506 , A61K31/4184 , C07C49/697 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/47 , C07C313/06 , C07C331/14 , C07D235/02 , C07D403/06 , C07D405/06 , C07D407/06
摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the &bgr;-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of &bgr;-amyloid aggregates.
摘要翻译： 本发明涉及螺环酰基胍及其作为分泌酶（BACE1）活性的抑制剂，含有它们的药物组合物的用途，以及将其用作治疗神经变性疾病的治疗剂的方法，其特征在于认知 衰退，认知障碍，痴呆和以淀粉样蛋白聚集体生产为特征的疾病。
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公开(公告)号：WO2014035860A8
公开(公告)日：2015-01-15
申请号：PCT/US2013056566
申请日：2013-08-26
发明人： BUKHTIYAROV YURI , CACATIAN SALVACION , DILLARD LAWRENCE WAYNE , DORNER-CIOSSEK CORNELIA , FUCHS KLAUS , GROSS ULRIKE , HEINE NIKLAS , JIA LANQI , LALA DEEPAK S , MORALES-RAMOS ANGEL , SINGH SURESH B , SAUER ACHIM , VENKATRAMAN SHANKAR , XU ZHENRONG , YUAN JING , ZHAO YI , ZHENG YAJUN
IPC分类号： C07D235/02 , A61K31/4184 , A61P25/28 , C07D401/06 , C07D403/04
CPC分类号： C07D235/02 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/59 , C07C313/06 , C07C331/26 , C07C2603/94 , C07C2603/97 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06
摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the &bgr;- secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of &bgr;-amyloid aggregates.
摘要翻译： 本发明涉及螺环酰基胍及其作为分泌酶（BACE1）活性的抑制剂，含有它们的药物组合物的用途，以及将其用作治疗神经变性疾病的治疗剂的方法，其特征在于认知功能障碍 衰退，认知障碍，痴呆和以淀粉样蛋白聚集体生产为特征的疾病。
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公开(公告)号：WO2013138568A8
公开(公告)日：2014-08-28
申请号：PCT/US2013031250
申请日：2013-03-14
发明人： DONG CHENGGUO , FAN YI , LEFTHERIS KATERINA , LOTESTA STEPHEN , SINGH SURESH B , TICE COLIN , ZHAO WEI , ZHENG YAJUN , ZHUANG LINGHANG
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/06
CPC分类号： A61K31/506 , A61K31/4985 , C07D487/04 , C07F7/1804
摘要： Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
摘要翻译： 本文提供的是肝X受体调节剂的新化合物及其药学上可接受的盐。 还提供了包含本发明化合物和载体的组合物。 此外，进一步描述了本文的化合物的使用和与肝X受体相关的疾病或病症的治疗方法。
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公开(公告)号：WO2007117560A3
公开(公告)日：2007-12-06
申请号：PCT/US2007008521
申请日：2007-04-05
申请人： VITAE PHARMACEUTICALS INC , BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B
发明人： BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B
IPC分类号： C07D211/22 , A61K31/445 , A61P9/12 , C07D265/30
CPC分类号： C07D211/22 , C07D265/30
摘要： Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
摘要翻译： 描述的是具有口服活性并与肾素结合以抑制其活性的化合物。 它们可用于治疗或改善与肾素活性相关的疾病。 还描述了这些化合物用于治疗或改善受试者中肾素介导的病症的方法。
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公开(公告)号：WO2007117557A3
公开(公告)日：2007-11-29
申请号：PCT/US2007008518
申请日：2007-04-05
申请人： VITAE PHARMACEUTICALS INC , BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B , FLAHERTY PATRICK T
发明人： BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B , FLAHERTY PATRICK T
IPC分类号： C07D211/20 , A61K31/40 , A61K31/445 , A61K31/535 , A61P9/00 , C07D207/08 , C07D265/30
CPC分类号： C07D211/22 , C07D207/08 , C07D265/30 , C07D413/12
摘要： Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.
摘要翻译： 描述其二氨基丙醇是口服活性的并且结合肾素以抑制其活性。 它们可用于治疗或改善与升高相关的疾病。 肾素活性水平或治疗天冬氨酸蛋白酶介导的病症。 还描述了在有需要的受试者中使用二氨基丙醇来改善或治疗肾素相关疾病的方法。
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公开(公告)号：WO2008156831A3
公开(公告)日：2009-06-18
申请号：PCT/US2008007704
申请日：2008-06-20
申请人： VITAE PHARMACEUTICALS INC , SMITHKLINE BEECHAM CORP , BALDWIN JOHN J , CACATIAN SALVACION , CLAREMON DAVID A , DILLARD LAWRENCE W , FLAHERTY PATRICK T , ISHCHENKO ALEXEY V , JIA LANQI , MCGEEHAN GERARD , SIMPSON ROBERT D , SINGH SURESH B , TICE COLIN M , XU ZHENRONG , YUAN JING , ZHAO WEI , ZHUANG LINGHANG , ZHANG JING
发明人： BALDWIN JOHN J , CACATIAN SALVACION , CLAREMON DAVID A , DILLARD LAWRENCE W , FLAHERTY PATRICK T , ISHCHENKO ALEXEY V , JIA LANQI , MCGEEHAN GERARD , SIMPSON ROBERT D , SINGH SURESH B , TICE COLIN M , XU ZHENRONG , YUAN JING , ZHAO WEI , ZHUANG LINGHANG , ZHANG JING
IPC分类号： C07C237/24 , A61K31/165 , A61P9/00 , A61P9/04 , A61P9/12 , C07C237/32
CPC分类号： C07C237/24 , C07C237/32 , C07C2601/08
摘要： The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
摘要翻译： 本发明涉及天冬氨酸蛋白酶抑制剂。 本发明还涉及包含所公开的天冬氨酸蛋白酶抑制剂的药物组合物。 本发明还涉及在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用所公开的天冬氨酸蛋白酶抑制剂治疗受试者中天冬氨酸蛋白酶介导的病症的方法。
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公开(公告)号：WO2008024497A3
公开(公告)日：2008-07-24
申请号：PCT/US2007018789
申请日：2007-08-24
申请人： VITAE PHARMACEUTICALS INC , CLAREMON DAVID A , SINGH SURESH B , TICE COLIN M , YE YUANJIE , CACATIAN SALVACION , HE WEI , SIMPSON ROBERT , XU ZHENRONG , ZHAO WEI
发明人： CLAREMON DAVID A , SINGH SURESH B , TICE COLIN M , YE YUANJIE , CACATIAN SALVACION , HE WEI , SIMPSON ROBERT , XU ZHENRONG , ZHAO WEI
IPC分类号： C07D221/20 , A61K31/438 , A61P3/10 , C07D401/06 , C07D413/06 , C07D471/10 , C07D491/107
CPC分类号： C07D221/20 , C07D211/16 , C07D211/22 , C07D211/26 , C07D211/34 , C07D401/06 , C07D401/08 , C07D413/06 , C07D471/10 , C07D491/107
摘要： This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11ß- HSDl in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
摘要翻译： 本发明涉及新的式（I *）化合物，其药学上可接受的盐及其药物组合物，其可用于治疗性治疗与哺乳动物中调节或抑制11β-HSD1相关的疾病。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇产生或抑制细胞中可的松向皮质醇转化的方法。
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公开(公告)号：WO2008036247A8
公开(公告)日：2008-06-26
申请号：PCT/US2007020164
申请日：2007-09-18
申请人： VITAE PHARMACEUTICALS INC , BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B , JIA LANQI , FLAHERTY PATRICK T
发明人： BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B , JIA LANQI , FLAHERTY PATRICK T
IPC分类号： C07D309/04 , A61K31/435 , A61P9/00 , C07D405/12
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.
摘要翻译： 本发明涉及由以下结构式（I）表示的天冬氨酸蛋白酶抑制剂或其药学上可接受的盐。 本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。 还公开了在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。
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公开(公告)号：WO2007117482A3
公开(公告)日：2007-11-22
申请号：PCT/US2007008339
申请日：2007-04-05
申请人： VITAE PHARMACEUTICALS INC , SMITHKLINE BEECHAM CORP , BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B , FLAHERTY PATRICK T , KALLANDER LARA S , LEACH COLIN A , LAWHORN BRIAN , LU QING , TERRELL LAMONT R , GHAVINI-ALAGHA BAHMAN , ZHANG JING , GHIRLANDA DAMIANO , HOU XIAOPING , SEMUS SIMON
发明人： BALDWIN JOHN J , CLAREMON DAVID A , TICE COLIN M , CACATIAN SALVACION , DILLARD LAWRENCE W , ISHCHENKO ALEXEY V , YUAN JING , XU ZHENRONG , MCGEEHAN GERARD , ZHAO WEI , SIMPSON ROBERT D , SINGH SURESH B , FLAHERTY PATRICK T , KALLANDER LARA S , LEACH COLIN A , LAWHORN BRIAN , LU QING , TERRELL LAMONT R , GHAVINI-ALAGHA BAHMAN , ZHANG JING , GHIRLANDA DAMIANO , HOU XIAOPING , SEMUS SIMON
IPC分类号： C07D211/22 , A61K31/44 , A61K31/5375 , A61P9/12 , C07D265/30 , C07D401/06
CPC分类号： C07D211/22 , C07D265/30 , C07D401/06
摘要： Disclosed are compounds according to Formula (I): wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula (I).
摘要翻译： 公开了根据式（I）的化合物：其中变量在本文中定义。 这些化合物可以结合天冬氨酸蛋白酶以抑制其活性。 它们可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 本文还描述了在有需要的受试者中拮抗天冬氨酸蛋白酶抑制剂的方法，包括向受试者施用治疗有效量的根据式（I）的化合物。
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10.发明申请CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 审中-公开11BETA-羟基脱氢酶脱氢酶的碳酸盐和尿素抑制剂1
公开(公告)号：WO2009131669A3
公开(公告)日：2010-04-01
申请号：PCT/US2009002478
申请日：2009-04-21
申请人： VITAE PHARMACEUTICALS INC , CLAREMON DAVID A , ZHUANG LINGHANG , YE YUANJIE , SINGH SURESH B , TICE COLIN M
发明人： CLAREMON DAVID A , ZHUANG LINGHANG , YE YUANJIE , SINGH SURESH B , TICE COLIN M
IPC分类号： C07D205/04 , A61K31/397 , A61K31/40 , A61K31/407 , A61K31/433 , A61K31/4406 , A61K31/4995 , A61K31/506 , C07D207/16 , C07D211/56 , C07D401/12 , C07D403/12 , C07D417/12 , C07D487/04 , C07D487/08
CPC分类号： C07D487/08 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/56 , C07D401/12 , C07D403/12 , C07D417/12 , C07D487/04
摘要： This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 Vl, Vla, VIb, VII, Vila, VIIb, VIII, Vllla, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ß-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
摘要翻译： 本发明涉及式I，II，III，IIIa，NIb，IV，IVa，IVb，IVc，IVd，IVe，V，Va，Vb1 VI，Vla，VIb，VII，VIIa，VIIb， VIIIa，VIIIb，IX，IXa，X和Xa，其药学上可接受的盐及其药物组合物，其可用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇生产或抑制细胞中可的松转化为皮质醇的方法。
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