发明名称 Anti-hypertensive chromanol derivatives
摘要 Compounds of formula (I): <IMAGE> (I) wherein: either one of R1 and R2 is hydrogen and the other is selected from the class of C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, C1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkoxysulphinylamino, C1-6 alkoxysulphonylamino C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl groups or by C2-7 alkanoyl; one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R3 and R4 together are C2-5 polymethylene; either R5 is hydrogen, hydroxy, C1-6 alkoxy or C1-7 acyloxy and R6 is hydrogen or R5 and R6 together are a bond; R7 is selected from the class consisting of C1-6 alkyl substituted by amino optionally substituted by one or two C1-6 alkyl groups which may be the same or different; amino optionally substituted by a C1-6 alkyl or C1-6 alkenyl group or a C1-6 alkanoyl group optionally substituted by up to three halo atoms or by a phenyl group optionally substituted by C1-6 alkyl, C1-6 alkoxy or halogen; or C1-6 alkoxy, or phenoxy optionally substituted by C1-6 alkyl, C1-6 alkoxy or halogen; or, when X is oxygen, R7 is further selected from the class of carboxy, C1-6 alkoxycarbonyl, or aminocarbonyl optionally substituted by one or two C1-6 alkyl groups which may be the same or different; R8 is hydrogen or C1-6 alkyl; and X is oxygen or sulphur; the R8-N-CX-R7 group being trans to the R5 group when R5 and R6 together are not a bond; or when the compound of formula (I) contains a salifiable group, pharmaceutically acceptable salts thereof, having pharmacological activity, a process for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.
申请公布号 US4575511(A) 申请公布日期 1986.03.11
申请号 US19840610626 申请日期 1984.05.16
申请人 BEECHAM GROUP P.L.C. 发明人 EVANS, JOHN M.;CASSIDY, FREDERICK
分类号 A61K31/35;A61K31/352;A61P9/12;C07D311/68;(IPC1-7):A61K31/35;C07D311/02 主分类号 A61K31/35
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