Abstract: A compound (Ia): wherein the variables are defined in the specification, its prodrug or a pharmaceutically acceptable salt thereof useful in the treatment of angina, hypertension etc.

Abstract: Novel anthranilic acid derivatives having an inhibiting activity of cGMP-PDE are represented by the formula I where A is a lower alkylene group: 1

Abstract: A compound of formula (I): wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH2; and B is benzazapinyl, which may be optionally substituted, or a salt thereof, that possesses vasopressin antagonistic activity and is useful as a vasopressin antagonist.

Abstract: Compounds of formula (I) where R1 is hydrogen; R2 is nitro, cyano or halo(lower)alkyl; R3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R4 is a group CR6R7R8 wherein R6 and R7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R8 is hydrogen; its prodrug and a salt thereof.

Abstract: This invention relates to a compound of the formula: wherein A1 is lower alkylene, R1 is substituted quinolyl, etc., R2 is hydrogen, halogen or lower alkyl, R3 is halogen or lower alkyl, and R4 is a group of the formula: —Q—A2—R5, etc.,  in which R5 is amino, acylamino, etc., A2 is lower alkylene or a single bond, and Q is a group of the formula:  and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: This invention relates to a heterocyclic compound of the formula wherein a group of the formula: is a group of the formula X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: The invention relates to a pharmaceutical composition for ophthalmic administration comprising a compound of the formula: wherein X1, X2, X3, R1, R2, R3, R4, R5, Q and A are as defined in the disclosure. This invention also relates to methods of using the pharmaceutical composition in the prevention and/or treatment of bradykinin or its analogues mediated diseases in the eye, such as allergy, inflammation and pain of the eye.

Abstract: This invention relates to compounds of formula: ##STR1## wherein R.sup.6, R.sup.7, R.sup.2, R.sup.2, R.sup.3 and A.sup.1 are as defined in the disclosure; and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of hypertension or the like.

Abstract: This invention relates to a compound of the formula: ##STR1## wherein A.sup.1 is lower alkylene,R.sup.1 is substituted quinolyl, etc.,R.sup.2 is hydrogen, halogen or lower alkyl,R.sup.3 is halogen or lower alkyl, andR.sup.4 is a group of the formula:--Q--A.sup.2 --R.sup.5, etc.,in whichR.sup.5 is amino, acylamino, etc.,A.sup.2 is lower alkylene or a single bond, andQ is a group of the formula: ##STR2## etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.2 is hydrogen, lower alkyl or a heterocyclic group,R.sup.3 is hydrogen, lower alkyl or halogen,R.sup.4 is lower alkyl or halogen,R.sup.5 is nitro or amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, andA is lower alkylene.

Abstract: This invention relates to a compound of formula (1) wherein R.sup.1 is halogen, etc., R.sup.2 is halogen, etc., R.sup.3 is amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, etc., R.sup.4 is heterocyclic (lower)alkyl, R.sup.5 is lower alkyl, and A.sup.1 is lower alkylene, and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of hypertension or the like.

Abstract: This invention relates to a compound of formula (I) wherein A.sup.1 is lower alkylene, R.sup.1 is substituted quinolyl, etc., R.sup.2 is hydrogen, halogen or lower alkyl, R.sup.3 is halogen or lower alkyl, and R.sup.4 is a group of the formula: -Q-A.sup.2 -R.sup.5, etc., in which R.sup.5 is amino, acylamino, etc., A.sup.2 is lower alkylene or a single bond, and Q is a group of formula (a), and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: This invention relates to a compound of the formula: ##STR1## wherein Z is a group of the formula: ##STR2## in which X.sup.1 is N or C--R.sup.1,X.sup.2 is N or C--R.sup.9,X.sup.3 is N or C--R.sup.2,R.sup.1 is lower alkyl,R.sup.2 is hydrogen, lower alkyl, etc.,R.sup.9 is hydrogen or lower alkyl,R.sup.3 is halogen, etc.,R.sup.4 is halogen, etc.,R.sup.5 is a group of the formula: ##STR3## A is lower alkylene, and Y is O, etc.,and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods to using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: A compound of the formula: ##STR1## wherein --X.sup.3 .dbd.X.sup.2 --X.sup.1 .dbd.N-- is a group of the formula: ##STR2## R.sup.1 is hydrogen or halogen, R.sup.2 is halogen,R.sup.3 is hydrogen, nitro, amino optionally having at least one substituent or a heterocyclic group optionally having at least one substituent,R.sup.4 and R.sup.5 are each hydrogen, or halogen,R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,R.sup.7 is hydrogen or lower alkyl,A is lower alkylene, andQ is O or N--R.sup.9 is hydrogen or acyl,provided that R.sup.3 is not hydrogen when X.sup.1 is C--R.sup.6, in which R.sup.6 is hydrogen, andpharmaceutically acceptable salts thereof.

Abstract: The invention relates to bradykinin antagonists of the formula: ##STR1## wherein R.sup.1 is halogen,R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, halo(lower)alkyl or acyl,R.sup.4 is aryl having suitable substituent(s), or a heterocyclic group optionally having suitable substituent(s),Q is O or N--R.sup.11, in which R.sup.11 is hydrogen or acyl, andA is lower alkylene,and pharmaceutically acceptable salts thereof.

Abstract: A compound of the formula: ##STR1## or its salt is prepared by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## Wherein the variables are all defined in claim 1.

Abstract: The invention relates to novel bradykinin antagonists of the formula: ##STR1## wherein R.sup.1 is halogen,R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, halo(lower)alkyl or acyl,R.sup.4 is aryl having suitable substituent(s), or a heterocyclic group optionally having suitable substituent(s),Q is O or N--R.sup.11, in which R.sup.11 is hydrogen or acyl, andA is lower alkylene,and pharmaceutically acceptable salts thereof.