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公开(公告)号：WO2011088188A1
公开(公告)日：2011-07-21
申请号：PCT/US2011/021100
申请日：2011-01-13
申请人： NOVARTIS AG , HU, Qi-Ying , KSANDER, Gary , MEREDITH, Erik , MONOVICH, Lauren G. , PAPILLON, Julien , SCHUMACHER, Christoph
发明人： HU, Qi-Ying , KSANDER, Gary , MEREDITH, Erik , MONOVICH, Lauren G. , PAPILLON, Julien , SCHUMACHER, Christoph
IPC分类号： A61P5/00 , A61K31/4188 , A61K31/55
CPC分类号： C07F9/6506 , A61K31/4188 , A61K31/55 , A61P5/00 , C07D487/04
摘要： The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or --C(O)N(R a )(R b ) wherein R a and R b are independently --(C 1 -C 4 ) alkyl, or --(C 1 -C 4 ) alkyl-(C 5 -C 7 ) aryl, wherein each of R a and R b is optionally substituted by --(C 1 -C 4 ) alkoxy; R 1 , R 2 , and R 3 , are independently hydrogen, halogen, cyano or --(C 6 -C 10 ) aryl, wherein said --(C 6 -C 10 ) aryl is optionally substituted by halogen, with the proviso that no more than one of R 1 , R 2 , and R 3 is hydrogen; and R 4 and R 5 are hydrogen; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法，包括向受试者施用治疗有效量的由式（I）表示的化合物：其中 n为1或3; 其中R a和R b独立地为 - （C 1 -C 4）烷基或 - （C 1 -C 4）烷基 - （C 5 -C 7）芳基），其中R 1为氢或-C（O）N（R a） Ra和Rb中的每一个任选被 - （C 1 -C 4）烷氧基取代; R 1，R 2和R 3独立地为氢，卤素，氰基或 - （C 6 -C 10）芳基，其中所述 - （C 6 -C 10）芳基任选被卤素取代，条件是不超过1个 ，R2和R3是氢; R4和R5是氢; 或其药学上可接受的盐。
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公开(公告)号：WO2005118557A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005052417
申请日：2005-05-27
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , SCHUMACHER CHRISTOPH , QUIRMBACH MICHAEL
IPC分类号： C07D239/00 , C07D417/04 , C07D471/04
CPC分类号： C07D471/04 , C07D417/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) in which R, R ,R , W, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译： 本申请涉及通式（I）的新型杂环化合物，其中R 1，R 1，R 2，W，X，Y，Z和n具有本说明书中定义的含义， 制剂和这些化合物作为药物的使用，特别是作为醛固酮合酶抑制剂。
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公开(公告)号：WO2006128852A3
公开(公告)日：2007-02-22
申请号：PCT/EP2006062695
申请日：2006-05-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , STOJANOVIC ALEKSANDAR , MARTI CHRISTIANE , JOTTERAND NATHALIE , SCHUMACHER CHRISTOPH , QUIRMBACH MICHAEL
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , STOJANOVIC ALEKSANDAR , MARTI CHRISTIANE , JOTTERAND NATHALIE , SCHUMACHER CHRISTOPH , QUIRMBACH MICHAEL
IPC分类号： C07D491/20 , A61P5/00 , C07D471/10 , C07D471/20 , C07D491/10
CPC分类号： C07D471/04 , C07D471/10 , C07D491/10
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R 1 , R 2 , U, V, W, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译： 该专利申请涉及通式（I）的新的杂环化合物，其中A，R，R 1，R 2，U，V，W，X，Y Z，n和p具有在描述中更详细地阐述的定义，其制备方法和这些化合物作为药物的用途，特别是作为醛固酮合酶抑制剂。
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4.发明申请
公开(公告)号：WO2005118541A3
公开(公告)日：2006-02-02
申请号：PCT/EP2005052418
申请日：2005-05-27
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , SCHUMACHER CHRISTOPH , BEHNKE DIRK , QUIRMBACH MICHAEL
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , SCHUMACHER CHRISTOPH , BEHNKE DIRK , QUIRMBACH MICHAEL
IPC分类号： C07D471/04 , A61K31/415 , C07D213/00
CPC分类号： C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) in which R, R
摘要翻译： 本申请涉及通式（I）的新型杂环化合物，其中R，R
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公开(公告)号：WO2006005725A2
公开(公告)日：2006-01-19
申请号：PCT/EP2005/053271
申请日：2005-07-08
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , SCHUMACHER, Christoph , STOJANOVIC, Aleksandar , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , SCHUMACHER, Christoph , STOJANOVIC, Aleksandar , QUIRMBACH, Michael
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I), in which L, R, R 1 , R 2 , W, X, Y, Z and n have the meanings explained in more detail in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aromatase inhibitors.
摘要翻译： 本申请涉及通式（I）的新型杂环化合物，其中L，R，R
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公开(公告)号：WO2009127251A1
公开(公告)日：2009-10-22
申请号：PCT/EP2008/054586
申请日：2008-04-16
IPC分类号： A61K31/538 , A61K45/06 , A61P9/12 , A61P3/10 , A61P3/06
CPC分类号： A61K45/06 , A61K31/538 , A61K2300/00
摘要： The invention relates to drug combinations comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof with specific cardiovascular treatment agents of complementary pharmacological mechanism to generate a synergistic therapeutic effect.
摘要翻译： 本发明涉及包含式（I）的肾素抑制剂或其药学上可接受的盐与具有互补的药理学机制的特定心血管治疗剂的药物组合，以产生协同治疗效果。
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公开(公告)号：WO2008077916A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/064404
申请日：2007-12-21
IPC分类号： A61K31/165 , A61K31/506 , A61P13/12 , A61P9/08
CPC分类号： A61K31/165 , A61K31/506
摘要： The present invention relates to a pharmaceutical composition and method of achieving a therapeutic effect including, but not limited to, the treatment of hypertension, kidney or heart disease in an animal, preferably a mammal including a human subject, using (i) SPP100/aliskiren or a pharmaceutically acceptable salt thereof in combination with (ii) SPP301/avosentan or a pharmaceutically acceptable salt thereof and (iii) a pharmaceutically acceptable carrier.
摘要翻译： 本发明涉及使用（i）SPP100 /阿利吉仑来实现治疗效果的药物组合物和方法，所述药物组合物和方法包括但不限于在动物，优选包括人受试者的哺乳动物中治疗高血压，肾脏或心脏病 或其药学上可接受的盐与（ii）SPP301 /阿泊生坦或其药学上可接受的盐组合，和（iii）药学上可接受的载体。
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公开(公告)号：WO2007031501A3
公开(公告)日：2007-03-22
申请号：PCT/EP2006/066250
申请日：2006-09-11
IPC分类号： A61P9/00 , A61K31/505 , A61K31/506
摘要： The present invention relates to the use of a compound of formula (I), wherein R 1 is pyridyl or thiazolyl, any of which may optionally be substituted with C 1-8 alkyl or C 2-8 alkenyl; and a) R 2 is methoxy and n is zero or one; or b) R 2 is chlorine and n is zero; and pharmaceutically acceptable salts thereof for the prevention of blood vessel graft failure in patients undergoing artery bypass graft surgery.
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公开(公告)号：WO2005118541A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005/052418
申请日：2005-05-27
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , SCHUMACHER, Christoph , BEHNKE, Dirk , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , SCHUMACHER, Christoph , BEHNKE, Dirk , QUIRMBACH, Michael
IPC分类号： C07D213/00
CPC分类号： C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译： 本申请涉及通式（I）的新型杂环化合物，其中R 1，R 2，R 2，X，Y，Z和n具有本说明书中定义的含义，其制备方法和 使用这些化合物作为药物，特别是作为醛固酮合酶抑制剂。
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公开(公告)号：WO2006128852A2
公开(公告)日：2006-12-07
申请号：PCT/EP2006/062695
申请日：2006-05-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JOTTERAND, Nathalie , SCHUMACHER, Christoph , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JOTTERAND, Nathalie , SCHUMACHER, Christoph , QUIRMBACH, Michael
IPC分类号： C07D491/20 , C07D491/10 , C07D471/20 , C07D471/10 , A61P5/00
CPC分类号： C07D471/04 , C07D471/10 , C07D491/10
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R 1 , R 2 , U, V, W, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译： 该专利申请涉及通式（I）的新的杂环化合物，其中A，R，R 1，R 2，U，V，W，X，Y Z，n和p具有在说明书中更详细阐述的定义，其制备方法和这些化合物作为药物，特别是醛固酮合酶抑制剂的用途。
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