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1. 发明公开

EP0189203A3 Peptidylaminodiols 失效
公开(公告)号：EP0189203A3
公开(公告)日：1989-08-23
申请号：EP86100917.3
申请日：1986-01-23
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Plattner, John Jacob , Rosenberg, Saul Howard , Fung, Anthony K.L.
IPC分类号： C07K5/06 , C07D233/64 , A61K37/64
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , C07K5/06017 , C07K5/06139 , Y02P20/55
摘要： The invention relates to renin inhibiting compounds of the formula:
wherein R 10 is
A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is O, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl.
摘要翻译：本发明涉及下式的肾素抑制化合物：其中R 10是A是氢或N-保护基; w是0或1; B是氢，羟基，NH，N-烷基，低级烷基或芳基烷基; 条件是当w为1时，B为NH且当w为0时，B为氢，羟基，低级烷基或芳基烷基; R1是低级烷基或亲脂性或芳族或亲水性氨基酸侧链; m是1-3; n是1-3; p是1-3; q是1-3; s是1-3; t是0-2; R2是氢或低级烷基; R3和R4独立地选自低级烷基，亲脂性或芳族氨基酸侧链; R5和R7独立地选自氢或低级烷基; 且R6为氢，低级烷基，乙烯基，芳基烷基或其中R8为氢或低级烷基，X为O，NH或S且R9为氢，低级烷基或烷酰基或XR9一起可为低级烷基磺酰基，N3或Cl。

2. 发明公开

EP0189203A2 Peptidylaminodiols 失效
标题翻译： Peptidylaminodiole。
公开(公告)号：EP0189203A2
公开(公告)日：1986-07-30
申请号：EP86100917.3
申请日：1986-01-23
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Plattner, John Jacob , Rosenberg, Saul Howard , Fung, Anthony K.L.
IPC分类号： C07K5/06 , C07D233/64 , A61K37/64
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , C07K5/06017 , C07K5/06139 , Y02P20/55
摘要： The invention relates to renin inhibiting compounds of the formula:
wherein R 10 is
A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is O, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl.
摘要翻译：本发明涉及下式的肾素抑制化合物：其中R 10是氢或N-保护基; w为0或1; B是氢，羟基，NH，N-烷基，低级烷基或芳基烷基; 条件是当w为1时，B为NH，当w为0时，B为氢，羟基，低级烷基或芳基烷基; R1是低级烷基或亲脂性或芳族或亲水氨基酸侧链; m为1-3; n为1-3; p为1-3; q为1-3; s是1-3; t为0-2; R2是氢或低级烷基; R3和R4独立地选自低级烷基，亲脂性或芳族氨基酸侧链; R5和R7独立地选自氢或低级烷基; 并且R 6是氢，低级烷基，乙烯基，芳烷基或其中R 8是氢或低级烷基，X是O，NH或S，R 9是氢，低级烷基或烷酰基或X R 9一起可以是低级烷基磺酰基，N 3或Cl。

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