公开(公告)号：US06451973B1

公开(公告)日：2002-09-17

申请号：US09214959

申请日：1999-02-01

申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

IPC分类号： C07K508

CPC分类号： C07D295/135 ,  C07C271/22 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： The invention relates to compounds of the formula I, in which R1 and R2 are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3 and R4 are, independently of each other, sec-lower alkyl or tert-lower alkyl; R5 is phenyl or cyclohexyl; and R6 and R7 are, independently of each other, lower alkyl, or, together with the linking nitrogen atom, pyrrolidino, piperidino, 4-lower alkylpiperidino, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl; or a salt thereof, provided that at least one salt-forming group is present. These compounds are inhibitors of HIV protease and are therefore suitable, for example, for treating AIDS or its preliminary stages.

摘要翻译： 本发明涉及式I化合物，其中R 1和R 2彼此独立地为低级烷基或低级烷氧基 - 低级烷基; R 3和R 4彼此独立地为低级烷基或叔 - 低级烷基; R5是苯基或环己基; R 6和R 7彼此独立地为低级烷基，或与连接氮原子一起为吡咯烷子基，哌啶子基，4-低级烷基哌啶子基，1,2,4-三唑-1-基或1,2,4-三唑 -4-基或其盐，条件是至少存在一个成盐基团。这些化合物是HIV蛋白酶的抑制剂，因此适用于例如用于治疗AIDS或其初级阶段。

公开(公告)号：US06225345B1

公开(公告)日：2001-05-01

申请号：US09068876

申请日：1998-05-21

申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang

IPC分类号： A61K3127

CPC分类号： C07C271/22 ,  Y10S514/934

摘要： The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen; or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.

摘要翻译： 本发明涉及式（I）化合物：其中R 1和R 10各自独立地为低级烷氧基羰基; R 2，R 3和R 4各自独立地为C 1 -C 4烷基，R 7，R 8和R 9各自选自氢和C 1 -C 4烷基，不超过2个基团为氢; 或R 7，R 8和R 9各自独立地为C 1 -C 4烷基，R 2，R 3和R 4各自选自氢和C 1 -C 4烷基，其中1或2个是氢; R5是苯基或环己基; R6为苯基或氰基苯基; 或其盐; 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，并且是有效的，例如针对HIV。

公开(公告)号：US06300519B1

公开(公告)日：2001-10-09

申请号：US09448328

申请日：1999-11-23

申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

IPC分类号： C07C20904

CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

摘要： There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基，R 4 是通过环碳原子键合的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，脯氨酰基的杂原子（ -SO-）和磺酰基（-SO 2 - ），并且是未取代的或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中提及的含义之一，R 6独立地为R 1，为低级烷氧基羰基 或其盐，条件是存在至少一种成盐基团。化合物是天冬氨酸逆转录病毒蛋白酶的抑制剂，并且可以用于例如AIDS的治疗。 它们具有出色的药效学性质。