摘要:
The invention relates to 1-heteroaryl-4-aryl-pyrazolin-5-ones, a preparation process and the use in combating diseases, in particular for use as lipoxygenase inhibitors.
摘要:
For the control of coronary diseases and thromboses there are provided the novel compounds ##STR1## in which R.sup.1 is an optionally substituted phenyl or heterocyclic radical,R.sup.2 is a cyano, keto, carboxy, ester or amide group, andX is from 0 to 6,and physiologically acceptable salts thereof.
摘要:
1,4-Dihydropyridines of the formula ##STR1## in which R.sup.1 is hydrogen, or alkyl optionally substituted by halogen, nitro, cyano, alkoxy, carboxyl, alkoxycarbonyl or carboxamide,R.sup.2 is hydrogen or alkyl,R.sup.3 is hydrogen, alkyl, carboxyl, alkoxycarbonyl or aryl optionally substituted by hydroxyalkyl, carboxyl, sulphoxy, acloxyalkyl, or ##STR2## R.sup.4 is alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, ##STR3## X is oxygen, sulphur or NH, and n is 1 to 6,or physiologically acceptable salts thereof, which are active in combating thromboembolic and ischaemic disorders.
摘要:
A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm, inflammations of the skin and the eye, and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, shock lung, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of a compound of the formula ##STR1## wherein R represents an aryl or heteroaryl radical which has 6 to 12 C atoms and optionally contains 1 to 3 identical or different substituents from the group comprising halogen, trifluoromethyl, alkyl, alkenyl, alkoxy, alkylamino, cyano, trifluoromethoxy, nitro, hydroxyl, SO.sub.n -alkyl (n=0 to 2) or SO.sub.n -trifluoromethyl (n=0 to 2), alkyl, alkenyl and alkoxy in each case being understood as meaning radicals with 1 to 4 C atoms,R.sup.1 represents hydrogen or a hydrocarbon radical which has 1 to 18 C atoms and optionally contains a hydroxyl, ether, ester or carboxyl group and optionally 1 to 3 halogen atoms,R.sup.2 has the meaning of R.sup.1 or represents radical ##STR2## R.sup.3 represents hydrogen or an acyl or sulphonyl radical with in each case 1 to 15 C atoms andX represents one of the groups --O--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.sub.2 or ##STR3## the oxygen or sulphur atom being bonded to the radical R, and with the provisio that X does not represent --O--CH.sub.2 --CH.sub.2 -- if R=.beta.-naphthyl, R.sup.1 =CH.sub.3 and R.sup.2 =R.sup.3 =H.
摘要:
New phenylsulphonamide of the formula in which ##STR1## R.sup.1 represents a pyridyl, quinolyl or isoquinolyl radical which is unsubstituted or substituted by halogen, alkyl, cycloalkyl, alkoxy, cyano, nitro, halogenoalkyl, halogenoalkoxy, alkoxycarbonyl or alkylsulphonyl,R.sup.2 represents hydrogen, cyano, nitro, halogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkoxycarbonyl,R.sup.3 represents an aryl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted by halogen, halogenoalkyl, halogenoalkoxy, alkyl, alkoxy, alkylthio, alkylsulphonyl, cyano, nitro or alkoxycarbonyl, the substituents being identical or different, or represents pentafluorophenyl or represents a straight-chain, branched or cyclic alkyl which is unsubstituted or substituted by halogen, aryl, aryloxy, cyano, alkoxycarbonyl, alkoxy, alkylthio or trifluoromethyl, andX represents an --O--, --A--B-- or --B--A-- groupwhereA denotes --O--, ##STR2## and B denotes --CH.sub.2 -- or ##STR3## where R.sup.1 does not represent a pyridyl radical when x represents an --O-- group, and salts thereof are prepared by reacting appropriate amines with sulphonyl halides. The substituted phenylsulphonamides can be employed as active compounds for inhibiting enzymatic reactions and for inhibiting thrombocyte aggregations.
摘要:
Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antoganize thromboxane A.sub.2.
摘要:
Certain intermediate aminomethyl-5,6,7,8-tetrahydronaphthyl-oxyacetic acid derivatives of the formula ##STR1## in which R.sup.2 is hydroxyl, alkoxy, phenoxy, benzoxy or NR.sup.4 R.sup.5, andR.sup.4 and R.sup.5 each independently is hydrogen or alkyl, or one of the radicals R.sup.4 or R.sup.5 is benzyl,which are useful in preparing the corresponding aryl-sulfonamides which in-turn have antithrombotic, antiatherosclerotic and antiischaemic properties.
摘要:
For the treatment of circulation disorders, the novel 5-nitro-1,4-dihydropyridines of the formula ##STR1## in which R represents C.sub.6 -C.sub.14 -aryl which can be mono- to pentasubstituted by identical or different substituents from the series comprising halogen, nitro, cyano, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, trifluoromethyl, trifluoromethoxy, difluoromethoxy, trifluoromethylthio and benzyl, benzyloxy or benzylthio optionally substituted by nitro, cyano, trifluoromethyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, orrepresents a heterocycle from the series pyrryl, thienyl, furyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, quinolyl, benzoxadiazolyl, chromenyl or thiochromenyl optionally mono- to tetrasubstituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkyl orrepresents straight-chain, branched or cyclic alkyl with up to 14 carbon atoms,and their physiologically acceptable salts.
摘要:
1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.
摘要:
A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of nafazatrom.