发明名称 BISARYLAMIDES OF N,N'-DI-(1-AMINOALKYL-2)-ALKYLENE DIAMINES HAVING A CARDIOVASCULAR ACTIVITY
摘要 Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof: <CHEM> wherein: R1 and R9 are independently phenyl, phenyl C1-4 alkyl, phenyl C2-4 alkenyl or pyridyl, the aromatic moiety optionally substituted by one, two or three of halogen, trifluoromethyl, C1-4 alkoxy, C1-4 alkyl, cyano, hydroxy, nitro, NR10R11 or O2SNR10R11 wherein R10 and R11 are independently hydrogen or C1-6 alkyl or together are C3-6 polymethylene, or disubstituted at adjacent carbon atoms by C1-2 alkylenedioxy; C3-8 cycloalkyl; or aliphatic heterocyclyl having up to six ring atoms the heteroatom(s) being selected from oxygen, sulphur or nitrogen; m and n are independently integers of 0 to 3, such that m + n is 0 to 3; and R2 and R8 are independently hydrogen C1-4 alkyl or phenyl C1-4 alkyl, R3 is C1-4 alkyl optionally substituted by hydroxy or thiol or phenyl C1-4 alkyl, or together with R4 is C3-6 polymethylene, R4 is hydrogen, C1-4 alkyl, phenyl C1-4 alkyl or as defined with R3, or together with R5 is -(CH2)p-where p is an integer from 2 to 6 such that m + p is 3 to 6, R5 is hydrogen, C1-4 alkyl or as defined with R4, or together with R6 is -(CH2)q-where q is an integer from 2 to 6 such that n + q is 3 to 6, R6 is hydrogen, C1-4 alkyl, phenyl C1-4 alkyl or as defined with R5, or together with R7 is C3-6 polymethylene, and R7 is C1-4 alkyl optionally substituted by hydroxy or thiol, phenyl C1-4 alkyl or as defined with R6, in which any phenyl moiety in R2,R3,R4,R6,R7 and R8 is optionally substituted by one or two of halogen, trifluoromethyl, C1-4 alkoxy or C1-4 alkyl. Such compounds have been found to possess cardiovascular activity, in particular calcium antagonistic activity which indicates that they are of potential use in the treatment of angina.
申请公布号 ZA8505579(B) 申请公布日期 1986.09.24
申请号 ZA19850005579 申请日期 1985.07.24
申请人 BEECHAM-WUELFING GMBH. & CO. KG. 发明人 LJERKA JOZIC
分类号 C07D211/18;A61K31/16;A61K31/165;A61K31/335;A61K31/357;A61K31/395;A61K31/4402;A61K31/4406;A61K31/4409;A61K31/4427;A61K31/445;A61K31/4468;A61K31/455;A61P3/00;A61P9/06;A61P43/00;C07C67/00;C07C231/00;C07C233/12;C07C233/40;C07C233/56;C07C233/62;C07C235/50;C07C235/78;C07C237/34;C07C255/49;C07D211/26;C07D211/56;C07D211/58;C07D211/74;C07D213/75;C07D213/81;C07D213/82;C07D317/68;C07D319/18;C07D401/12 主分类号 C07D211/18
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