Kaken Pharmaceutical Company, Ltd.

Kakenyaku Kako Kabushiki Kaisha

Shigeki Kurokawa

Motoyuki Yajima

Katsumi Nogimori

Michiko Nagahara

Yoshitaka Ohishi

Norio Kajikawa

Tsutomu Nakamura

Michio Ui

Taira Okamoto

Makoto Tamura

Koichi Hosoda

Akio Terashima

Chikanori Tomioka

Akira Itoh

Isamu Takahashi

Yoshinori Kanbayashi

Akira Ito

Yoshitaka Takehisa

A benzofuran derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a benzyl group, unsubstituted or substituted with a halogen atom or an alkyloxy group, or an alkyl group having 1 to 3 carbon atoms, R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R.sup.3 is acetyl group, ethyl group, carboxyl group or 4-methyl-2,5-dioxoimidazolidine-4-yl group, R.sup.4 is hydrogen atom, hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 9 carbon atoms, carboxymethoxy group, nitro group, acetoamino group, a benzylozy group unsubstituted or substituted with a halogen atom, nitro group or an alkyloxy group or a group having the formula: --OR.sup.6, wherein R.sup.6 is an alkenyl group having 2 to 4 carbon atoms or an alkyl group having 2 to 3 carbon atoms having a halogen atom, cyano group or oxo group, R.sup.5 is hydrogen atom or methylenedioxy group together with R.sup.4 group, n is 1 or 2, and the unsubstituted or substituted N-carboxymethylsulfamoyl group, R.sup.4 and R.sup.5 are attached at 3-position, 4-position, 5-position, 6-position or 7-position of the benzofuran ring, or a nontoxic salt thereof, process for preparing the same and a pharmaceutical composition containing the same. The compounds of the present invention have powerful aldose reductase inhibiting activity, platelet aggregation inhibiting activity and arachidonic acid metabolism inhibiting activity and are useful for a remedy for treatment of diabetic complications.

Benzofuran derivatives useful in treating diabetic complications

The present invention relates to biologically active substances obtained by reacting Islets-Activating Protein having an insulin secretion promoting action with a carbonyl compound in the presence of a reducing agent; to anti-diabetic composition in dosage unit form comprising the substance of the present invention; to pertussis vaccine in dosage unit form comprising the substance of the present invention; and to a process for the preparation of the same. The substances of the present invention are suppressed in leukocytosis-promoting effect.

Biologically active substance from Islets-Activating Protein

A rhodanine derivative having the following general formula (I): ##STR1## wherein R is an acyclic alkyl group having 2 to 10 carbon atoms which may be substituted by a halogen atom or an acyclic alkenyl group having 2 to 19 carbon atoms which may be substituted by a halogen atom; or a nontoxic salt thereof. The rhodanine derivative has potent platelet aggregation inhibiting activity and aldose reductase inhibiting activity and therefore is useful as a therapeutic agent for diabetic complications.

Rhodanines useful as a therapeutic agent for diabetic complications

A rhodanine derivative having the following general formula (I): ##STR1## wherein R is a mono- or di-alkylamino group having 1 to 6 carbon atoms which may be substituted by a hydroxyl group; an alkenylamino group having 3 to 6 carbon atoms; a phenylamino group, the benzene ring of which may be substituted by a lower alkyl group, a lower alkoxyl group, phenyl group or a halogen atom; or a cyclic amino group which may contain in the ring an oxygen atom or a nitrogen atom to which a lower alkyl group is attached; or a nontoxic salt thereof. The rhodanine derivative has potent platelet aggregation inhibiting activity and aldose reductase inhibiting activity and therefore is useful as a therapeutic agent for diabetic complications.

Novel biologically active substances prepared by dissociating the protein obtained from the cultivation of the microorganism Bordetella and having insulin secretion promoting action as well as glucose tolerance improving action for mammals.

Proteinic active substances

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Otsu, Japan

Shigeki Kurokawa