| abstract |
PCT No. PCT/JP80/00122 Sec. 371 Date Apr. 30, 1981 Sec. 102(e) Date Apr. 30, 1981 PCT Filed Jun. 4, 1980 PCT Pub. No. WO81/02421 PCT Pub. Date Sep. 3, 1981.Novel carbostyril derivative and its salt represented by the general formula (1), <IMAGE> (1) wherein R1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a phenyl-lower alkyl group; R2 is a hydrogen atom, a lower alkyl group or a group of the formula <IMAGE> wherein A is a lower alkylene group; R3 is a lower alkyl group, a hydroxy lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or a benzoyloxy-lower alkyl group; and R4 is a C3-10-cycloalkyl group which may have at least one hydroxyl group as the substituent(s) in the cycloalkyl ring, a C3-10-cycloalkyl-lower alkyl group, a phenyl group, a phenyl-lower alkyl group which may have at least one lower alkoxy group as the substituent(s) in the phenyl ring, a lower alkyl group which may have at least one hydroxyl group as the substituent(s), a heterocyclic ring residue or a lower alkyl group having one heterocyclic ring residue as the substituent; further, R3, R4 and the adjacent nitrogen atom, as well as with or without another nitrogen atom, may form a group of the formula <IMAGE> (wherein R5 is a phenyl group, a C3-10-cycloalkyl group or a phenyl-lower alkyl group; and B is a methine group or a nitrogen atom); the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single or double bond; the substituted position of the group of the formula <IMAGE> is any one of 5-, 6-, 7- or 8-position in the carbostyril skeleton; when the group of the formula <IMAGE> is substituted at 5-, 6-, 7- or 8-position in the carbostyril skeleton, then R2 is a hydrogen atom or a lower alkyl group; alternatively, when R2 is a group of the formula <IMAGE> then 5-, 6-, 7- and 8-positions in the carbostyril skeleton are hydrogen atoms and are not substituted with groups of the formula <IMAGE> and when R3 is a lower alkyl group, then R4 should be neither of a C3-10-cycloalkyl group, a C3-10-cycloalkyl-lower alkyl group nor a lower alkyl group, having effects for preventing and treating thrombosis and embolism. |