1,5-benzoxathiepin derivatives, their production and use

Details 1,5-benzoxathiepin derivatives, their production and use 1,5-benzoxathiepin derivatives, their production and use

C - Chemistry, Metallurgy

07

D

167/207, 260/279

C07D 327/02 (2006.01) A61K 31/33 (2006.01) C07D 411/06 (2006.01) C07D 411/12 (2006.01)

Patent

CA 1247613

Abstract Novel 1,5-benzoxathiepin derivatives of the formula: (I) Image [wherein R1 and R2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R3 and R4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ?C=O or ?CH-OR5 (wherein R5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S2 receptor blocking activity, calcium antagonism, actions to relieve cerebral vasospasm and to improve renal circulation and diuretic and antithrombotic activities, and are of value as a pro- phylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

469996

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