|Title:||Cardioselective aryloxy- and arylthio- hydroxypropylene-piperazinyl acetanilides which affect calcium entry|
|Abstract:||Novel compounds of the general formula ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 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 R.sup.1 is methyl, R.sup.4 is not methyl; or R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 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 R.sup.6 and R.sup.7 together form --CH.dbd.CH--CH.dbd.CH--; R.sup.7 and R.sup.8 together form --OCH.sub.2 O--; R.sup.11 and R.sup.12 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.|
|Inventor(s):||Kluge; Arthur F. (Los Altos, CA), Clark; Robin D. (Palo Alto, CA), Strosberg; Arthur M. (Menlo Park, CA), Pascal; Jean-Claude G. (Cachan, FR), Whiting; Roger (Edinburgh, GB6)|
|Assignee:||Syntex (U.S.A.) Inc. (Palo Alto, CA)|
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