摘要:
Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, OH, etc,; R.sup.2 is H, alkyl, halogen or alkoxy; R.sup.3 is phenyl-alkanoylamino, or ##STR2## R.sup.4 is H, --NR.sup.6 R.sup.7, alkenyloxy, HO-alkyl, --O--CO--A--NR.sup.8 R.sup.9, etc.; R.sup.5 is H, OH, etc., or a salt thereof, which have excellent vasopressin antagonistic activities and useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要:
An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist. The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.
摘要:
An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist.The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.
摘要:
Novel carbostyril derivatives of the formula: ##STR1## wherein X is 0 or S; Y is H or alkyl; R.sup.A is a group of the ##STR2## {wherein n is 1 or 2, A is alkylene, R.sup.1 is benzoyl having optionally 1-3 substituents, R.sup.2A is ##STR3## is (i) alkoxy, (ii) substituted or unsubstituted 5- or 6-membered heterocylic group, (iii) alkenylthio, (iv) pyrrolidinyl-alkyl--S--, (v) pyrrolidinyl-alkyl--SO--, (vi) pyrrolidinyl-alkyl--SO.sub.2 --, (vii) --O--B--NR.sup.4 R.sup.5 [B is alkylene having optionally OH, R.sup.4 is H, R.sup.5 is tricyclo[3.3.1.1]decanyl, tricyclo[3.3.1.1]decanylalkyl, etc., or R.sup.4 and R.sup.5 may together form a group of ##STR4## (R.sup.6 is substituted or unsubstituted amino)] or (viii) substituted alkoxy; m is 1 to 3]}, which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要:
Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.2 or a group: --N(R.sup.13)-- and further these groups having optionally 1 to 3 substituents of alkyl, alkoxycarbonyl, carboxy, OH, O, alkanoyloxy, etc., which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要:
Novel benzoheterocyclic compounds of the formula: ##STR1## which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要:
Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenyialkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substituted benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups being optionally replaced by O, S, SO, SO.sub.2 or a group: --N(R).sup.12 and further these groups having optionally 1 to 3 substituents of alkyl, alkoxycarbonyl, carboxy, OH, O, alkanoyloxy, etc., which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要:
The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity.Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.
摘要:
Peripheral vasodilating agents containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity, said piperidine derivative or pharmaceutically acceptable salt thereof being represented by the general formula (1) ##STR1## wherein R, R.sup.1 and R.sup.2 are as defined herein.
摘要:
The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity.Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.