INDAZOLE-3-CARBOXYLIC ACID HYDRAZIDES AND A PROCESS FOR THE PREPARATION THEREOF

摘要

New compounds of the general formula (I) (I) and salts thereof were prepared by reacting a compound of the general formula (II) (II) with a compound of the general formula (III) or (IV) (III) (IV) and optionally saturating the -C=N- bond. In the above formulae R1 and R2 are always the same and represent a C1-4 alkyl group, R3 stands for hydrogen, R4 and R5 each represent an unsubstituted or substituted phenyl, cyclohexyl or a straight-chained C1-16 alkyl or alkylidene group, the latter two groups being optionally substituted by a cyclohexyl, an unsubstituted or substituted phenyl, an unsubstituted or nitrosubstituted furyl or unsubstituted naphthyl group, wherein said substituted phenyl groups may contain up to three C1-3 alkoxy, hydroxy, benzyloxy, nitro, amino, di-C1-3 alkylamino, methylenedioxy, C1-3 alkylmercapto, C1-3 alkylsulfonyl or halogen substituents, and one of R4 and R5 may represent a hydrogen atom, or R4 and R5 may form together with the adjacent carbon atom a C6-12 cycloalkyl, C6-12 cycloalkylidene, piperidyl, C1-3 alkyl substituted piperidyl or phenyl-C1-3 alkyl substituted piperidyl group, or R4 and R5 may form a naphthylidene or an unsubstituted or nitro-substituted furfurylidene group, and R6 and R7 may stand for hydrogen, or R6 and R7 may form together a valence bond, and the R8 groups may each represent hydrogen, C1-3 alkyl or C2-4 alkanoyl, or the R8 groups may form together a C1-3 alkylene or C2-4 alkanoylene group. The compounds of the general formula (I) possess primarily gastric acid secretion inhibiting and central nervous activities, furthermore they exert favourable action on the development of certain microorganisms which can be utilized in therapy.