Pyridine derivatives

Details Pyridine derivatives Pyridine derivatives

C - Chemistry, Metallurgy

07

D

260/295, 260/280

C07D 409/06 (2006.01) C07D 213/18 (2006.01) C07D 213/30 (2006.01) C07D 213/48 (2006.01) C07D 213/55 (2006.01) C07D 213/57 (2006.01)

Patent

CA 1134828

ABSTRACT The pyridine derivatives of the general formula: Image I wherein A represents an alkylene group containing from 1 to 5 carbon atoms, 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 atom, E represents a grouping of the formula: Image or Image (in which R6 represents a hydrogen atom, or an akyl group con- taining from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: Image in which R2 represents a hydrogen atom, or an alkyl group con- taining from 1 to 4 carbon atoms, R3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbon atoms, the symbol Image represents a single or double bond, the carbon atom attached to R2 binds to B, and the carbon atom at- tached ro R3 binds to D, R1 represents a grouping of the formula: -COOR4a or -COSR4, in which R4 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, R5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with -1- 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 with the exclusion of compounds which are 3-[2-(2-pyrid- ylomethyl) phenyl] acrylic acid and 3-[2-(2-pyridylmethyl) phenyl] propionic acid and non-toxic acid addition salts thereof and, when R1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong in- hibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death. - 2 -

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