;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."/> Azahexane derivatives as substrate isosters of retroviral asparate proteases
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Azahexane derivatives as substrate isosters of retroviral asparate proteases

机译:氮杂己烷衍生物作为逆转录病毒天冬氨酸蛋白酶的底物等排体

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.
机译:本发明涉及式(I)的化合物:<化学ID =“ CHEM-US-00001”> <图像文件=“ US06225345-20010501-C00001.GIF” imgContent =“ undefined” imgFormat =“ GIF” /> ;其中R < Sub> 1 和R 10 各自独立于另一个低级烷氧羰基; R 2 ,R 3 和R 4 各自独立于另一个C 1 -C 4 烷基和R 7 ,R 8 和R 9 分别选自氢和C 1 -C 4 烷基,其中不超过2个基团为氢;或R 7 ,R 8 和R 9 各自独立于另一个C 1 -C 4 烷基和R 2 ,R 3 和R 4 分别选自氢和C 1 -C 4 烷基,其中1或2个基团为氢; R 5 是苯基或环己基;和R 6 是苯基或氰基苯基;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,并且例如对HIV有效。

著录项

  • 公开/公告号US6225345B1

    专利类型

  • 公开/公告日2001-05-01

    原文格式PDF

  • 申请/专利权人 NOVARTIS AG;

    申请/专利号US19980068876

  • 申请日1998-05-21

  • 分类号A61K312/70;C07C2711/00;C07C2690/40;

  • 国家 US

  • 入库时间 2022-08-22 01:04:27

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