1,5-benzoxathiepin derivatives

Details 1,5-benzoxathiepin derivatives 1,5-benzoxathiepin derivatives

1987-04-15

1988-06-14

Hollrah, Glennon H.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540544, 540545, 540553, 540554, 540575, 540596, 544145, 544372, 546197, 548454, C07D32702

Patent

active

047513160

ABSTRACT:
Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 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.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 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 S.sub.2 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 prophylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

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Cerioni, "Chemical Abstracts", vol. 98, 1983, col. 98:215576.
Sugihara, et al., "Chemical Abstracts", vol. 103, col. 103:196131f.
Sugihara, et al., "Chemical Abstracts", vol. 104, col. 104:68892p.

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