36292-29-2Relevant articles and documents
Cardioselective aryloxy- and arylthio- hydroxypropylene-piperazinyl acetanilides which affect calcium entry
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, (2008/06/13)
Novel compounds of the general formula STR1 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 --OCH2 O--; 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 --OCH2 O--; 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.
Primary aminoacylanilides, methods of making the same and use as antiarrhythmic drugs
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, (2008/06/13)
Primary amino acylanilides of the formula, wherein R1 is selected from the group consisting of hydrogen, methyl, ethyl and propyl, R2 is selected from the group consisting of methyl, ethyl, chlorine, methoxy and ethoxy, R3 is selected from the group consisting of hydrogen and methyl, R4 is selected from the group consisting of hydrogen, methyl, and a C1 -C4 alkoxy group, R6 is selected from the group consisting of methyl, ethyl, chlorine, methoxy and ethoxy, R7 is hydrogen, methyl or ethyl, R8 is hydrogen, R9 is hydrogen, methyl or ethyl, R10 is hydrogen, and n is 0 or 1, with the provisions that (a) when n is 0, R8 can also be methyl; (b) when n is 1, and R7 is hydrogen, and R9 is hydrogen or methyl, then R10 can also be methyl; (c) when R1 is hydrogen, R2 is methyl, R3 is hydrogen, R6 is methyl, R7 is hydrogen, R8 is hydrogen, and n is 0, then R4 can be ethoxy or propoxy only; (d) when R1 is hydrogen, R2 is methyl, R3, R4, R7 and R8 are hydrogen, and n is 0, then R6 is methoxy, ethoxy, or ethyl only; and the therapeutically acceptable salts thereof. Compounds of this type have been found to be effective longlasting cardiac antiarrhythmic agents, especially when administered by the oral route
