Tanabe Seiyaku Company, Limited

Tanabe Seiysku Co., Ltd.

Ikuo Iijima

Yutaka Saiga

Masakatsu Ozeki

Mamoru Matsumoto

Yuzo Matsuoka

Masanori Inamasu

Toshikazu Miyagishima

Kunihito Okumura

Kunio Nosaka

Tohru Ishizuka

Koichi Homma

Shigeru Nishimoto

Mitsunori Gaino

Tokuo Fujii

Kuichiro Ikeda

Novel benzoxazole derivatives of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a substituted or unsubstituted cycloalkyl group or a substituted or unsubstituted heterocyclic group; Alk is single bond, a substituted or unsubstituted lower alkylene group, a lower alkenylene group or a lower alkynylene group; the group is a group of the formula: --CH.sub.2 -- or --CH.dbd., and a pharmaceutically acceptable salt thereof are disclosed. Said derivative (I) and a salt thereof are useful as therapeutic agents for diabetes.

Benzoxazole derivatives

Novel benzoxazole derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a substituted or unsubstituted cycloalkyl group or a substituted or unsubstituted heterocyclic group; Alk is single bond, a substituted or unsubstituted lower alkylene group, a lower alkenylene group or a lower alkynylene group; the group ##STR2## is a group of the formula: --CH.sub.2 -- or --CH.dbd., and a pharmaceutically aceptable salt thereof are disclosed. Said derivative (I) and a salt thereof are useful as therapeutic agents for diabetes.

A novel benzofuran derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkoxy group or a halogen atom, one of R.sup.2 and R.sup.3 is a lower alkyl group and the other is a lower alkyl group or a phenyl-lower alkyl group, or R.sup.2 and R.sup.3 combine together with adjacent nitrogen atom to form a heteromonocyclic group, Ring A is a substituted or unsubstituted phenyl group, Y is oxygen atom or sulfur atom and n is an integer of 2 or 3, or a pharmaceutically acceptable salt thereof is disclosed. The compound (I) or a pharmaceutically acceptable salt thereof has a potent inhibitory activity against reflective contractions of urinary bladder.

Benzofuran derivative and processes for preparing the same

Novel benzo-furan(or -thiophene) derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl-lower alkyl group or a substituted or unsubstituted phenyl group, R.sup.2 is hydrogen atom, a lower alkyl group, an acyl group or phenyl group, R.sup.3 is hydrogen atom, a halogen atom, nitro group, a lower alkoxy group, amino group or an acylamino group, R.sup.4 is a group of the formula: ##STR2## A is a lower alkylene group optionally substituted with hydroxy group, B is single bond or a lower alkylene group, one of R.sup.5 and R.sup.6 is hydrogen atom or a lower alkyl group and the other is a lower alkyl group or a phenyl-lower alkyl group, or R.sup.5 and R.sup.6 combine together with adjacent nitrogen atom to form a heteromonocyclic group, R.sup.7 is a lower alkyl group, X is oxygen atom or sulfur atom, Y is oxygen atom, imino group, a lower alkylimino group or a phenyl-lower alkylimino group and a salt thereof are disclosed. Said compound (I) and a salt thereof have a potent inhibitory activity against reflective contraction of urinary bladder.

Benzo-furan derivative

Novel benzoxazine derivative of the formula: ##STR1## wherein R.sup.1 is phenyl group or a substituted thiazolyl group; R.sup.2 is hydrogen atom or a lower alkyl group; Q is single bond or a lower alkylene group, or a salt thereof are disclosed. Said derivative (I) and a salt thereof are useful as therapeutic agents for diabetes.

Benzoxazine derivatives

Novel thioketene derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group, a lower alkenyl group, a phenyl group or a group of the formula: --B--Y;

3-(1,3-dithiol-2-ylidene)-2,4-dioxopyrrolidines, -piperidines, and

Novel tetrahydro-.beta.-carboline derivatives of the formula: ##STR1## wherein R.sup.1 is carboxyl, a lower alkoxycarbonyl, carbamoyl, an N,N-di-lower alkylcarbamoyl, an N-(phenyl-substituted lower alkylidenamino)carbamoyl, a [N,N-di(lower alkyl)amino]-lower alkyl, or a nitrogen-containing monocyclic heterocyclic group;

Tetrahydro-.beta.-carboline derivatives and treatment of liver diseases

Tetrahydro-.beta.-carboline derivative of the formula: ##STR1## wherein R.sup.2 is lower alkyl, and either (A)

Tetrahydro-.beta.-carboline derivatives

Tetrahydro-.beta.-carboline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group, a cycloalkyl group, phenyl group or a hydroxy-substituted lower alkyl group, R.sup.2 is hydrogen atom, an alkyl group, or a group of the formula: --(CH.sub.2).sub.m Y, Y is thienyl or a substituted or unsubstituted phenyl group, and m and n are an integer of 1 or 2, which have excellent alleviating, curing and preventing hepatic damages and are useful as a therapeutic or prophylactic agent for hepatic diseases, and a process for the preparation of said compounds.

Tetrahydro-.beta.-carboline dithioic acid derivatives and treatment of

A benzothiazepine derivative of the formula: ##STR1## wherein R is hydrogen or acetyl, is prepared by condensing a compound of the formula: ##STR2## wherein R is the same as defined above, with 2-(diamethylamino)ethyl halide (i) in the presence of potassium hydroxide in acetone; or (ii) in the presence of potassium carbonate in acetone, lower alkyl acetate, a mixture of acetone and water or a mixture of lower alkyl acetate and water.

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Urawa, Japan

Ikuo Iijima