摘要:
A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.
摘要:
A compound of the formula: ##STR1## or its pharmaceutically acceptable salt and pharmaceutical compositions containing these compounds as effective ingredients. These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic afflictions, congestive heart failure, hypertension, asthma, immediate-type allergy diseases and the like.
摘要:
A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.
摘要:
A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen, methyl, C.sub.3 -C.sub.6 alkenyl, C.sub.5 or C.sub.6 cycloalkyl, benzyl, phenyl, --(CH.sub.2).sub.m CO.sub.2 R.sub.3 (wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.5 alkyl, and m is an integer of from 1 to 4), --(CH.sub.2).sub.n A (wherein A is --OH or --N(R.sub.4).sub.2 wherein R.sub.4 is C.sub.1 -C.sub.3 alkyl, and n is an integer of from 2 to 6) or --CH.sub.2 CF.sub.3 ; R.sub.2 is chlorine or bromine; each of Y.sub.1 and Y.sub.2 which may be the same or different, is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --OR.sub.5 (wherein R.sub.5 is hydrogen, C.sub.1 -C.sub.8 alkyl or ##STR2## wherein q is an integer of from 1 to 4), --CO.sub.2 R.sub.6 (wherein R.sub.6 is hydrogen or C.sub.1 -C.sub.5 alkyl), --N(R.sub.7).sub.2 (wherein R.sub.7 is C.sub.1 -C.sub.4 alkyl) or --SR.sub.8 (wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl); and Y.sub.3 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --OR.sub.5 (wherein R.sub.5 is as defined above), --CO.sub.2 R.sub.6 (wherein R.sub.6 is as defined above), --N(R.sub.7).sub.2 (wherein R.sub.7 is as defined above) or --SR.sub.8 (wherein R.sub.8 is as defined above), or a pharmaceutically acceptable salt thereof.
摘要:
A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen, 2-propenyl or straight chained or branched C.sub.1 -C.sub.4 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; X is chlorine or bromine; Y is hydrogen, nitro, -NHR.sub.3 wherein R.sub.3 is hydrogen or straight chained or branched C.sub.1 -C.sub.4 alkyl, -AR.sub.4 wherein A is oxygen or sulfur and R.sub.4 is hydrogen, straight chained or branched C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl having one double bond, C.sub.3 -C.sub.6 alkynyl having one triple bond, phenyl or ##STR2## wherein R.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkyl, or halogen; Z.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, -OR.sub.6 wherein R.sub.6 is hydrogen, straight chained or branched C.sub.1 -C.sub.8 alkyl or ##STR3## wherein n is an integer of from 1 to 4, -N(R.sub.7).sub.2 wherein R.sub.7 is C.sub.1 -C.sub.4 alkyl, or halogen; Z.sub.2 is C.sub.1 -C.sub.4 alkyl, -OR.sub.6 wherein R.sub.6 is as defined above, -N(R.sub.7).sub.2 wherein R.sub.7 is as defined above, or halogen, provided that when R.sub.1 is straight chained or branched C.sub.2 -C.sub.4 alkyl, Y is not hydrogen and when R.sub.1 is hydrogen, methyl or 2-propenyl, Y and R.sub.2 are not simultaneously hydrogen, or a pharmaceutically acceptable salt thereof.
摘要:
A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is C.sub.2 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, chlorine or bromine; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --(CH.sub.2).sub.l A [wherein A is substituted amino of the formula --N(R.sub.4) (R.sub.5) (wherein each of R.sub.4 and R.sub.5 which may be the same or different, is C.sub.1 -C.sub.4 alkyl, or R.sub.4 and R.sub.5 together form C.sub.4 -C.sub.6 alkylene), morpholino, 4-R.sub.6 -piperazin-1-yl (wherein R.sub.6 is C.sub.1 -C.sub.3 alkyl) or --OR.sub.7 (wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.3 alkyl), and l is an integer of 0 to 3], --OR.sub.8 [wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.5 alkenyl, benzyl or --(CH.sub.2).sub.q --R.sub.9 [wherein R.sub.9 is CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CONHR.sub.3 (wherein R.sub.3 is as defined above) or --CH.sub.2 OR.sub.7 (wherein R.sub.7 is as defined above), and q is an integer of 1 to 5]], --CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CON(R.sub.10) (R.sub.11) [wherein each of R.sub.10 and R.sub.11 which may be the same or different, is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.5 alkenyl, or R.sub.10 and R.sub.11 together form C.sub.4 -C.sub.6 alkylene, --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 N(R.sub.6)(CH.sub.2).sub.2 -- (wherein R.sub.6 is as defined above)], --CONH(CH.sub.2).sub.m A (wherein A is as defined above, and m is an integer of 2 to 4), --CH.dbd.CHCOR.sub.12 (wherein R.sub.12 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --N(R.sub.13) (CH.sub.2).sub.n CO.sub.2 R.sub.3 (wherein R.sub.13 is hydrogen, C.sub.1 -C.sub.6 alkyl or cycloalkyl, R.sub.3 is as defined above, and n is an integer of 1 to 4)), --SR.sub.14 (wherein R.sub.14 is C.sub.1 -C.sub.4 alkyl), --CN or ##STR2## wherein R.sub.3 is as defined above), or two of Y.sub.1, Y.sub.2 and Y.sub.3 together form ##STR3## (wherein p is an integer of 1 or 2), and a pharmaceutically acceptable salt thereof.
摘要:
A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, chlorine or bromine; A is --NR.sub.3 -- or --O--; X is --(CH.sub.2).sub.n --, --CH(OR.sub.4)--, --CO-- or a single bond; when X is --(CH.sub.2).sub.n -- or a single bond, B is --O--, --S--, --NH--, --OSO.sub.2 --, or --OCO-- or a single bond, when X is --CH(OR.sub.4)--, B is --O--, --S--, --NH-- or --OSO.sub.2 --, and when X is --CO--, B is --O-- or --S--; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, ##STR2## or two of Y.sub.1, Y.sub.2 and Y.sub.3 together form ##STR3## and a pharmaceutically acceptable salt thereof.
摘要:
A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.2-6 cyclic alkylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: ##STR2## wherein R.sup.6 is a C.sub.1-4 alkyl group.
摘要:
A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.2-6 cyclic alkylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: ##STR2## wherein R.sup.6 is a C.sub.1-4 alkyl group.
摘要:
Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## �wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.