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

1985-12-10

1987-06-09

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514321, 514431, 544145, 544372, 546197, 548454, 549 10, 540544, 540545, 540553, 540554, 540575, 540596, A61K 31495, C07D41106

Patent

active

046720642

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 ##STR2## (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.

REFERENCES:
patent: 3306913 (1967-02-01), Monro et al.
patent: 3517031 (1970-06-01), Beereboo et al.
patent: 3584002 (1971-06-01), Williams et al.
patent: 3647479 (1972-03-01), Beereboom et al.
patent: 4188390 (1980-02-01), Campbell
Phosphorus and Sulfur 14, 151-156 (1983).
Federation Proceedings 42, 182-185 (1983).

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