发明名称 CARDIOSELECTIVE ARYLOXY-AND ARYLTHIO-HYDROXYPROPYLENI-PIPERAZINYL ACETANILIDES WHICH AFFECT CALCIUM ENTRY
摘要 Novel compounds of the general formula <IMAGE> (I) and the pharmaceutically acceptable esters and acid addition salts thereof, wherein: R1, R2, R3, R4 and R5 are each independently hydrogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, N-optionally substituted alkylamido, except that when R1 is methyl, R4 is not methyl; or R2 and R3 together form -OCH2O-; R6, R7, R8, R9 and R10 are each independently hydrogen, lower acyl, aminocarbonylmethyl, cyano, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, di-lower alkyl amino; or R6 and R7 together form -CH=CH-CH=CH-; R7 and R8 together form -OCH2O-; R11 and R12 are each independently hydrogen or lower alkyl; and W is oxygen or sulfur. These cardioselective compounds have calcium entry blockade properties and therefore are useful in therapy in the treatment of cardiovascular diseases, including arrhythmias, variant and exercise induced angina and myocardial infarction.
申请公布号 ZA8403746(B) 申请公布日期 1986.01.29
申请号 ZA19840003746 申请日期 1984.05.17
申请人 SYNTEX (USA) INC. 发明人 ARTHUR FREDERICK KLUGE;ROBIN DOUGLAS CLARK;ARTHUR MARTIN STROSBERG;JEAN CLAUDE PASCAL;ROGER LEWIS WHITING
分类号 C07D295/14;A61K31/495;A61P9/00;A61P9/06;A61P9/08;A61P9/10;A61P43/00;C07D295/04;C07D295/08;C07D295/092;C07D295/10;C07D295/15;C07D303/22;C07D317/66 主分类号 C07D295/14
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