CONDENSED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS, THEIR PRODUCTION AND USE

    公开(公告)号:CA1300143C

    公开(公告)日:1992-05-05

    申请号:CA510045

    申请日:1986-05-27

    Abstract: Novel condensed seven-membered heterocyclic compounds of the formula: wherein R1 and R2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy, R3 and R4 are independently hydrogen, optionally substituted lower alkyl, 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 or in which R5 is hydrogen, acyl or optioinally substituted carbamoyl, A is oxygen atom or sulfur atom, E is oxygen atom or methylene, and G is lower alkylene, provided that when A is sulfur atom, E is methylene, and salts thereof exhibit serotonin S2 receptor blocking activity, actions to relieve cerebral vasospasm and antithrombotic activity, and are of value as a prophylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

    PROCESS FOR PRODUCING 1,5-BENZOXATHIEPIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME

    公开(公告)号:HU201922B

    公开(公告)日:1991-01-28

    申请号:HU465784

    申请日:1984-12-13

    Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: [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 &rdurule& C=O or &rdurule& 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 prophylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

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