Cardioselective aryloxy and arylthio-hydroxypropyl...

C - Chemistry – Metallurgy – 07 – D

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C07D 295/14 (2006.01) A61K 31/495 (2006.01) C07D 295/092 (2006.01) C07D 295/15 (2006.01) C07D 303/22 (2006.01) C07D 317/66 (2006.01) C07D 405/00 (2006.01)

Patent

CA 1256874

23550-FF ABSTRACT OF THE DISCLOSURE Novel compounds of the general formula Image (I) and the pharmaceutically acceptable esters and cold addition salts thereof, wherein: R1, R2, R3, R4 and R5 are each independently hydrogen, lower alkyl, lower alkoxy, cyano, trifluoro- methyl, 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 -OCH20-; R6, R7, R8, R9 and R10 are each independently hydrogen, lower acyl, aminocarbonyl- methyl, arylcyano, lower alkyl, lower alkoxy, trifluoro- methyl, 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 R9 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.

454628

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