Abstract: The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a method for producing an optically active 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.

Abstract: The present invention provides a method for producing an optically active 4-[.alpha.-hydro-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) ##STR1## wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.

Abstract: Thienylazole compounds (I) and thienotriazolodiazepine compounds (II) of the formulas ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, halogen, C.sub.1 -C.sub.5 alkyl and the like; --A.dbd.B-- is --N.dbd.N-- and the like; R.sup.3 and R.sup.19 are hydrogen, C.sub.1 -C.sub.5 alkyl and the like; Y is --NHCO--, --NHCONH--, --NHCOO-- and the like; Z.sup.1 and Z.sup.2 are aryl, heteroaryl and the like; Ar is halogen-substituted phenyl and the like; and m is 0 or an integer of 1-5.The compounds of the present invention have CCK antagonistic action and gastrin antagonistic action, particularly potent antagonistic action against CCK-A receptor, and are useful as agents for the prophylaxis and treatment of central and peripheral nervous system diseases (e.g., anxiety, schizophrenia, and the like) and digestive diseases (e.g., pancreatitis, gastric ulcer, enterelcosis, irritable bowel syndrome, constipation, and the like).

Abstract: N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno ?3,2-f!?1,2,4!triazolo?4,3-a!?1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.