5,8-DISUBSTITUTED QUINOLIC DERIVATIVES AND PROCESSES FOR PREPARING SAME

摘要

This invention discloses novel carbostyril derivatives represented by the general formula (I) (I) wherein R1 and R2, which may be the same or different, each represents a hydrogen atom, a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group; R4 represents a hydrogen atom or an alkyl group, R5 and R6, which may be the same or different, each represents a hydrogen atom, an alkyl group, a cycloalkyl group, or a phenylalkyl group, or R5 and R6 may, when taken together with the nitrogen atom to which they are attached, form a S- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen or oxygen atoms as hetero atoms; and the ring A has a partial structure: or wherein R3 represents a hydrogen atom, a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group, with the proviso that at least one of R1, R2 and R3 when R3 is present, or at least one of R1 and R2, represents a cycloalkylcarbonyl group, a cycloalkylalhanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group; and pharmaceutically acceptable bstract continued: acid addition salts of the carbostyril derivatives of the formula (I). Process for the preparation of these novel carbostyril compounds are also disclosed. These compounds exhibit excellent .beta.-adrenoreceptor stimulating activity and are useful as therapeutic agents such as bronchodilators, peripheral vasodilators, antihypertensive agents and the like.