Shionogi Company Limited

Nobuo Chomei

Susumu Takada

Makoto Adachi

Akira Matsushita

Takashi Sasatani

Masaaki Uenaka

Tomoyuki Ogawa

Koji Masuda

Masami Eigyo

Satoru Tanaka

Kazuo Kawasaki

Tsuyoshi Kihara

Disclosed is a compound useful as an inhibitor of 11&#x3b2;-hydroxysteroid dehydrogenase type 1. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof,

Isoxazole derivative and isothiazole derivative having inhibitory activity on 11&#x3b2;-hydroxysteroid dehydrogenase type 1

Cyanoiminoquinoxaline derivatives

A process for the preparation of 3-isoxazolecarboxlic acid which is an intermediate for prepearing useful compounds is provided, said process being characterized in that a compound of formula (I) is reacted with hydroxylamine to obtain a compound of formula (II), and the compound thus obtained is treated with an alkali: ##STR1## wherein R.sup.1 is a lower alkyl, R.sup.2 is a carboxy protecting group, X is a halogen atom, and Y is a hydrogen atom, or X and Y together may form a single bond.

Process for the preparation of 3-isoxazolecarboxylic acid

An oxopyridinylquinoxaline derivative represented by the following Formula I or pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1 is hydrogen, halogen, nitro, or trihalomethyl; R.sup.2 is hydrogen, halogen, nitro, cyano, trihalomethyl, carbamoyl, carbamoyl substituted with lower alkyl, sulfamoyl, or sulfamoyl substituted with lower alkyl; R.sup.3 is hydrogen, nitro, or halogen; R.sup.4 is hydrogen, lower alkyl, substituted lower alkyl, lower cycloalkyl, or substituted lower cycloalkyl; R.sup.5 's are substituents independently selected from the group consisting of halogen, nitro, cyano, lower alkyl, carbamoyl, and carbamoyl substituted with lower alkyl; and n is an integer of 0 to 4. The derivative works as an antagonistic agent against both the NMDA receptors and the AMPA receptors, so that it is effective as a therapeutic agent for neurological disorders caused by excitatory amino acids binding to the receptors.

Oxopyridinylquinoxaline derivative

A compound of the formula: ##STR1## wherein R is an optionally substituted phenyl group, 5-membered; the A ring is a 5 to 7 membered alicyclic group in which said A ring may have an alkyl group as a substituent, or a pharmaceutically acceptable salt thereof, and is useful as a psychotropic agent.

Condensed imidazopyridine derivatives

A compound of the formula: ##STR1## wherein R is an optionally substituted aryl group or an optionally substituted aromatic heterocycle group; A ring is a 5 to 9 membered alicyclic group, in which one or more of carbon atoms constituting said A ring may be replaced by O, or S and said A ring may have alkyl as a substituent, or a pharmaceutically acceptable salt thereof.

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Sakai, Japan

Nobuo Chomei