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Claims for Patent: 4,567,264

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Claims for Patent: 4,567,264

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
Patent Claims: 1. A compund of the formula: ##STR14## and the pharameutically acceptable esters and acid addition salts thereof, wherein:

R1 and R5 are each methyl

R.sup.2 and R.sup.3 and R.sup.4 are each hydrogen and R.sup.6 to R.sup.12 are each hydrogen, i.e., 1-[3-phenoxy-2-hydroxypropyl]-4-[2,6-dimethylphenyl)-aminocarbonylmethyl]- piperazine, and the pharaceutically acceptable esters and acid addition salts thereof.

2. A compound of the formula: ##STR15## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:

R.sup.1 and R.sup.5 are each methyl

R.sup.2, R.sup.3, and R.sup.4 are each hydrogen, R.sup.6 is methoxy and R.sup.7 to R.sup.12 are each hydrogen, i.e., 1-[3-(2-methoxyphenoxy)-2-hydroxypropyl]-4-[(2,6,-dimethylphenyl)-aminocar bonylmethyl]-piperazine, and the pharaceutically acceptable esters and acid addition salts thereof.

3. A compound of the formula: ##STR16## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:

R.sup.1 and R.sup.5 are each methyl;

R.sup.2, R.sup.3, and R.sup.4 are each hydrogen, R.sup.6 is cyano and R.sup.7 to R.sup.12 are each hydrogen, i.e., 1-[3-(2-cyanohenoxy)-2-hydroxypropyl]-4-[2,6-dimethylphenyl)aminocarbonylm ethyl]piperazine.
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