ISOXAZOLE DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF

摘要

The invention relates to new isoxazole derivatives of the general formula (I) and acid addition salts thereof, (I) wherein R represents a C1-4 alkyl or a phenyl group, R2 denotes a halogen atom or a (C1-4 alkox )-carbonyl group, R1 represents a group of the formula -CH(NH2)-COOH, or a guanyl-thio, a bis(C1-4 alkoxycarbonyl-C1-4 alkanoylamido)methyl, an amino-oxy, a carbamoylamino-oxy, a guanidinooxy, a phthalimido-oxy group or a group of the general formula -NR3R4, wherein R3 stands for a hydrogen atom or a C1-4 alkyl, C3-6 cycloalkyl, .omega.-halogen-(C1-4 alkyl), di-(C1-4 alkyl)-amino-(C1-4 alkyl), 2,6-dihalogenbenzyl group or a p-amino-phenyl-sulfonyl group which latter may be N-substituted by a C1-4 alkanoyl group, and R4 stands for a hydrogen atom or a C1-4 alkyl group, or R3 and R4 together represent a 2,6-dihalogen-benzylidene group, or R3 and R4 form, together with the adjacent nitrogen atom a 6 membered heterocyclic ring which may optionally contain an oxygen as a further hetero atom, with the proviso that if R represents methyl and R1 stands for a guanyl-thio group, R2 may represent only chlorine. The new compounds of the general formula (I) can be prepared from the starting material of the general formula (II) (II) wherein R and R2 have the same meanings as above, The compounds of the general formula (I) possess valuable hypotensive, antiinflammatory and antipyretic effects and can be used to advantage in the therapy.