Benzopyran derivatives and processes for preparation thereof

Details Benzopyran derivatives and processes for preparation thereof Benzopyran derivatives and processes for preparation thereof

C - Chemistry, Metallurgy

07

D

167/233, 167/244

C07D 311/68 (2006.01) A61K 31/35 (2006.01) A61K 31/425 (2006.01) C07D 405/04 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2013163

ABSTRACT Benzopyran derivatives of the formula: Image wherein R1 and R2 are each lower alkyl, R3 is hydroxy or acyloxy and R4 is hydrogen, or R3 and R4 are linked together to from a bond, R5 is hydrogen or lower alkyl and R6 is hydrogen, lower alkyl or aryl, or R5 and R6 are linked together to form lower alkylene, R7 is cyano, acyl, halogen, nitro or lower alkyl, X is cyanoiminomethylene or sulfonyl, and Y is single bond, thio, imino which may have lower alkyl, provided that i) when R7 is cyano, X is cyanoiminomethylene and Y is thio or imino which may have lower alkyl, then R5 is hydrogen or lower alkyl and R6 is aryl; and ii) when R7 is cyano, R5 and R6 are linked together to form lower alkylene and X is sulfonyl, then Y is thio or imino which may have lower alkyl. These derivatives are useful as K+ channel activator, especially as vasodilating agent, for treating or preventing K+ channel mediated disease, for example vascular disorders such as hypertension, angina pectoris, cardiac insufficiency, peripheral and cerebral vascular diseases, atherosclerosis, arrhythmia, and the like in humans or animals. Processes for the preparation of these derivatives are also disclosed as well as pharmaceutical compositions containing these derivatives, methods of treatment using the derivatives and their uses as medicament, K+ channel activator and vasodilating agent.

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