Invention Grant
- Patent Title: Active compounds
- Patent Title (中): 活性化合物
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Application No.: US231183Application Date: 1988-08-11
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Publication No.: US4987138APublication Date: 1991-01-22
- Inventor: Frederick Cassidy , Geoffrey Stemp
- Applicant: Frederick Cassidy , Geoffrey Stemp
- Applicant Address: GB2
- Assignee: Beecham Group p.l.c.
- Current Assignee: Beecham Group p.l.c.
- Current Assignee Address: GB2
- Priority: GBX8522492 19850911; GBX8523051 19850918
- Main IPC: C07C49/245
- IPC: C07C49/245 ; A61K31/165 ; A61K31/215 ; A61K31/22 ; A61K31/265 ; A61K31/275 ; A61K31/35 ; A61K31/352 ; A61K31/443 ; A61K31/445 ; A61K31/47 ; A61P1/00 ; A61P9/00 ; A61P9/12 ; A61P11/00 ; A61P25/02 ; C07C45/00 ; C07C49/252 ; C07C49/255 ; C07C49/83 ; C07C49/84 ; C07C67/00 ; C07C201/00 ; C07C239/00 ; C07C301/00 ; C07C303/26 ; C07C303/30 ; C07C303/36 ; C07C303/40 ; C07C309/28 ; C07C313/00 ; C07C313/04 ; C07C313/06 ; C07C317/24 ; C07C317/46 ; C07C323/25 ; C07D215/20 ; C07D215/48 ; C07D311/58 ; C07D405/04
Abstract:
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl(NOH) or --C(C.sub.1-6 alkyl)NNH.sub.2 or, when Y is oxygen, one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.2 and R.sub.3 together are C.sub.2-5 polymethylene;R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy;R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.7 is NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently C.sub.1-6 alkyl, R.sub.8 is hydrogen and R.sub.9 is C.sub.1-6 alkyl or R.sub.8 and R.sub.9 together are C.sub.4-5 polymethylene; or R.sub.6 and R.sub.8 together are --(CH.sub.2).sub.n --wherein n is 2 or 3, and R.sub.9 is hydrogen or C.sub.1-6 alkyl; or R.sub.7 is CH.sub.2 R.sub.10 wherein R.sub.10 is hydrogen or C.sub.1-5 alkyl optionally substituted by halo, hydroxy or C.sub.1-6 alkoxy; or R.sub.6 and R.sub.10 are ---(CH.sub.2).sub.m -- wherein m is 2 or 3;X is oxygen or sulphur; andY is oxygen, CH.sub.2 or NH;the R.sub.6 --CH--CX--R.sub.7 group being trans to the R.sub.5 group; having blood pressure lowering activity, a process for their preparation and their use as pharmaceuticals.
Public/Granted literature
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