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1. 发明申请

WO1996000732A1 PHOSPHINIC ACID DERIVATIVES 审中-公开
标题翻译：磷酸衍生物
公开(公告)号：WO1996000732A1
公开(公告)日：1996-01-11
申请号：PCT/US1995007128
申请日：1995-06-19
申请人： SCHERING CORPORATION
发明人： SCHERING CORPORATION , MCKITTRICK, Brian, A. , CZARNIECKI, Michael, F. , CHACKALAMANNIL, Samuel , CHUNG, Shin , DEFREES, Shawn , STAMFORD, Andrew, W.
IPC分类号： C07F09/30
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728
摘要： Phosphinic acid derivatives of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene; R1, R2, R3 and R4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R1 and R2 form a cycloalkyl ring of 3-8 members and R3 and R4 are as defined; or R3 and R4 form a cycloalkyl ring of 3-7 members and R1 and R2 are as defined; or R1 and R2 together, and R3 and R4 together, each form a cycloalkyl ring; R5 is -OR9 or -NHR9, wherein R9 is hydrogen or alkyl; n is 0 or 1; A1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A1 and R5 together form a radical of an alpha -aminoacyl derivative; and R6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or -A2-R7, wherein A2 is a divalent alpha -iminoacyl radical, and R7 is a substituent on the alpha -imino atom selected from H, R8OCO-, R8SO2- and R8NHCO-, wherein R8 is aryl, arylmethyl or (C1-C8)alkyl; are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R and R form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.
摘要翻译：结构式（I）的亚磷酸衍生物或其药学上可接受的盐，其中R是H，烷基或烷酰氧基亚甲基; R 1，R 2，R 3和R 4是H，烷基，烯基，烯基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，羟基烷基，羧基烷基，硫代烷基，烷氧基硫代烷基，氨基烷基，烷基氨基烷基，环烷基取代的烷基或杂环烷基。或R 1和R 2形成3-8成员的环烷基环，并且R 3和R 4如所定义; 或R 3和R 4形成3-7成员的环烷基环，并且R 1和R 2如所定义; 或R 1和R 2一起，并且R 3和R 4一起形成环烷基环; R5是-OR9或-NHR9，其中R9是氢或烷基; n为0或1; A1是对氨基苯甲酰基或对氨基苯磺酰基，或者A1和R5一起形成α-氨基酰基衍生物的基团; R6为苯基甲氧基羰基，芳基羰基，杂芳基羰基或-A2-R7，其中A2为二价α-亚氨酰基，R7为选自H，R8OCO-，R8SO2-和R8NHCO-的α-亚氨基原子上的取代基，其中R8 是芳基，芳甲基或（C1-C8）烷基; 被公开用作内皮素转化酶抑制剂; 还公开了其中R 3和R 4形成环烷基环的新化合物的属，以及包含所述新化合物的药物组合物。

2. 发明公开

EP0767794A1 PHOSPHINIC ACID DERIVATIVES 失效
标题翻译：膦衍生物
公开(公告)号：EP0767794A1
公开(公告)日：1997-04-16
申请号：EP95924573.0
申请日：1995-06-19
申请人： SCHERING CORPORATION
发明人： MCKITTRICK, Brian, A. , CZARNIECKI, Michael, F. , CHACKALAMANNIL, Samuel , CHUNG, Shin , DEFREES, Shawn , STAMFORD, Andrew, W.
IPC分类号： A61K31 , A61P1 , A61P3 , A61P9 , A61P11 , A61P13 , A61P15 , A61P35 , A61P43 , C07F9
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728
摘要： Phosphinic acid derivatives of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene; R1, R2, R3 and R4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R1 and R2 form a cycloalkyl ring of 3-8 members and R3 and R4 are as defined; or R3 and R4 form a cycloalkyl ring of 3-7 members and R1 and R2 are as defined; or R1 and R2 together, and R3 and R4 together, each form a cycloalkyl ring; R5 is -OR9 or -NHR9, wherein R9 is hydrogen or alkyl; n is 0 or 1; A1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A1 and R5 together form a radical of an α-aminoacyl derivative; and R6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or -A2-R7, wherein A2 is a divalent α-iminoacyl radical, and R7 is a substituent on the α-imino atom selected from H, R8OCO-, R8SO2- and R8NHCO-, wherein R8 is aryl, arylmethyl or (C1-C8)alkyl; are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R?3 and R4¿ form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.

3. 发明授权

EP0767794B1 PHOSPHINIC ACID DERIVATIVES 失效
标题翻译：膦衍生物
公开(公告)号：EP0767794B1
公开(公告)日：2000-02-02
申请号：EP95924573.9
申请日：1995-06-19
申请人： SCHERING CORPORATION
发明人： MCKITTRICK, Brian, A. , CZARNIECKI, Michael, F. , CHACKALAMANNIL, Samuel , CHUNG, Shin , DEFREES, Shawn , STAMFORD, Andrew, W.
IPC分类号： C07F9/30 , A61K31/66 , C07F9/572 , C07F9/6558
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728

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