发明公开
- 专利标题: PYRROLE DERIVATIVES FOR TREATING AIDS
- 专利标题(中): PRRROLDERIVATE用于治疗艾滋病
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申请号: EP01938137.5申请日: 2001-04-30
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公开(公告)号: EP1301481A1公开(公告)日: 2003-04-16
- 发明人: DYMOCK, Brian William , JONES, Philip Stephen , MERRETT, John, Herbert , PARRATT, Martin John
- 申请人: F. HOFFMANN-LA ROCHE AG
- 申请人地址: 124 Grenzacherstrasse 4070 Basel CH
- 专利权人: F. HOFFMANN-LA ROCHE AG
- 当前专利权人: F. HOFFMANN-LA ROCHE AG
- 当前专利权人地址: 124 Grenzacherstrasse 4070 Basel CH
- 代理机构: Rauber, Beat
- 优先权: GB0016453 20000704
- 国际公布: WO02002524 20020110
- 主分类号: C07D207/36
- IPC分类号: C07D207/36 ; C07D401/06 ; A61K31/44 ; A61K31/40 ; A61K31/18
摘要:
The invention is concerned with novel pyrrole derivatives, a prcess for their manufacture, pharmaceutical compositions and the use of such compounds in medecine. In particular, the compounds of formula (I) are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV mediated process. The invention describes novel compounds of formula (I) wherein R1 is alkyl, cycloalkyl, aryl or heterocyclyl; R2 is alkyl, cycloalkyl, aryl or heterocyclyl; R3 is hydrogen, alkyl, cycloalkyl, aryl or heterocyclyl; R4 is hydrogen, alkyl, carboxyl, C(=O)R, CONR'R'', cyano or alkenyl, wherein R is hydrogen, alkyl, alkoxy, trifluoromethyl, methyl-oxy-carbonyl or ethyl-oxy-carbonyl, and wherein R' and R'', are independantly of each other, hydrogen, alkyl or aryl; R5 is alkyl, aryl or a group -Z-C(=O)R''', wherein Z is a single bond or -CH=CH-, and wherein R''' is hydrogen or alkyl; X represents S, S(O), S(O)¿2?, O, N(alkyl) or X-R?2¿ together CH¿2?-aryl or CH2-heterocyclyl; and with the proviso that only one of R?3 and R4¿ is hydrogen and alkyl in R3 is not CF¿3?; and hydrolyzable esters or ethers thereof or a pharmaceutically acceptable salt thereof.
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