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Generated: September 24, 2017

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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)
Application Number:06/495,904
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International Patent Family for Patent: ► Subscribe

Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Hungary192404► Subscribe
HungaryT34177► Subscribe
Finland78479► Subscribe
Hong Kong91989► Subscribe
Finland841989► Subscribe
Denmark248384► Subscribe
Denmark168535► Subscribe
European Patent Office0126449► Subscribe
Spain532565► Subscribe
Spain8601947► Subscribe
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The estimated expiration dates shown above are derived by simply adding 20 years to the priority date.
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