The disclosure is directed to new derivatives of thiophene-2-carboxylic acid and the pharmaceutically acceptable acid or base addition salts thereof as well as to the process for the preparation thereof. The compounds of the invention have the structural formula ##STR1## in which R in position 3 or 4 of the thiophene nucleus is hydrogen, methyl, chlorine or bromine and R.sub.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl. The compounds have a remarkably strong inhibitory effect on the thromboxane synthetase and are useful for the treatment of conditions such as inflammation, hypertension, thrombus, apoplexy, asthma, angina pectoris, ischemic heart diseases, ischemic conditions, migraine and vascular complications in connection with diabetes.

Laevosan-Gesellschaft m.b.H. &amp; Co. KG

Derivatives of thiophene-2-carboxylic acid and their pharmaceutically acceptable acid or base addition salts and use in treatment of conditions caused by thromboxane A.sub.2

The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, R represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbom atoms; the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.1 represents a hydroxy group, or a grouping of the formula: --COOR.sup.4 or --COSR.sup.4, in which R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R.sup.5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R.sup.1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents in the prevention or treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death.

Ono Pharmaceutical Co., Ltd.,

Kissei Pharmaceutical Co., Ltd.

Pyridine derivatives

The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, E represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbon atoms, the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.1 represents a hydroxy group, or a grouping of the formula: --COOR.sup.4 or --COSR.sup.4, in which R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl group unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R.sup.5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R.sup.1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents in the prevention and treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death.

Ono Pharmaceutical Co., Ltd.

The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, E represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atoms, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbon atoms, the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.1 represents a hydroxy group, or a grouping of the formula: --COOR.sup.4 or --COSR.sup.4, in which R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl group unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R.sup.5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R.sup.1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for the treatment or prevention of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, and cerebral infarction.

bromine/moždani udar

Derivatives of thiophene-2-carboxylic acid and their pharmaceutically acceptable acid or base addition salts and use in treatment of conditions caused by thromboxane A.sub.2

Pyridine derivatives

Pyridine derivatives

Pyridine alkyl benzoic and thenoic acid compounds and their pharmaceutical compositions

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