Otsuka Pharmaceutical Company, Limited

Yoshimasa Nakano

Taketoshi Izawa

Wasei Miyazaki

Masanao Shinohara

Hirotsugu Kaise

Hitoshi Tone

Katsumi Tamura

Seiji Sato

Yasuo Oshiro

Hideaki Sato

Toshiki Miyazaki

Tomoyuki Kawaguchi

Kazumi Kondo

Masahiro Murakami

Satoshi Hayakawa

Shigeharu Tamada

Youichi Taniguchi

Yoshihiko Ito

Shinji Nishitani

Michiharu Sugawara

Yasumitsu Tamura

Setsuyoshi Uetsuki

Yasuyuki Kita

Shuji Akai

Hiromichi Fujioka

Katsuhide Matoba

Toshinori Kaneyasu

Masatoshi Morisue

Akira Wada

Piperazine derivatives and salts thereof

Novel pyrazine derivatives represented by the formula (1) and salts thereof which possess inhibitory effect against superoxide radicals (O.sub.2.sup.-) released from the macrophage cells of guinea pig by stimulation, and also possess anti-albuminuria activity in Masugi nephritis. ##STR1## The pyrazine derivatives (1) and salts thereof are useful agents for preventing and treating of various diseases caused by the superoxide radicals, for example, diseases of autoimmune such as rheumatoid arthritis, arteriosclerosis, ischemic heart disease, transient cerebral ischematic attack, hepatic insufficiency, renal insufficiency and the like, as well as they are useful agents for preventing and treating the nephritis in various clinical fields.

Pyrazinyl and piperazinyl substituted pyrazine compounds

The novel indole derivatives and salts thereof represented by the general formula (1) ##STR1## possess, for example, an inhibitory effect against superoxide (O.sub.2.sup.-) released from the macrophage cells of guinea pig by stimulation and an anti-albuminuria activity against Masugi nephritis, and are useful in various clinical fields as an agent for preventing and treating diseases and cases associated with the above superoxide radical, for example, autoimmune diseases (e.g. rheumatism), arteriosclerosis, ischemic disease, ischemic encephalopathia, hepatic insufficiency and renal insufficiency, and also as an agent for preventing and treating nephritis.

Indole derivatives

A novel pyrazinoxide compound of NF-1616-904 having the formula (1), ##STR1## prepared by hydrolyzing the intermediate compound of NF-1616-902 which is separated from a culture broth of a microorganism belonging to the genus Thielavia. The pyazinoxide compound of NF-1616-904 possess biological and pharmacological activities, and is useful agent for preventing and treating diseases caused by superoxide radicals (O.sub.2.sup.-), and nephritis.

Novel pyrazinoxide compound of NF-1616-904 and a pharmaceutical

A prophylactic or therapeutic composition for hepatitis is disclosed comprising a prophylactically or therapeutically effective amount of a sesquiterpene compound represented by the formula (I) or (II) ##STR1## or a pharmaceutically acceptable salt thereof as an active ingredient, and a pharmaceutically acceptable carrier.

Composition for prophylaxis and therapy of hepatitis

A pharmaceutical composition having an anticomplementary activity comprising a therapeutically effective amount of at least one soyasapogenol B compound represented by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a group represented by the formula: ##STR2## wherein R.sup.2 represents a hydrogen atom or a hydroxymethyl group, R.sup.3 represents a hydrogen atom or a rhamnopyranosyl group, and R.sup.4 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier.

Anticomplementary agents comprising soyasapogenol B compounds

A sesquiterpene derivative expressed by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or a lower alkanoyl group; R.sup.2 and R.sup.3, which may be the same or different, each represents a formyl group, a hydroxymethyl group, a hydroxyl group, a carboxyl group, a lower alkanoyloxymethyl group, or a group of the formula --CH.dbd.CR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom, a cyano group, a lower alkoxycarbonyl group or a carboxyl group, or R.sup.2 and R.sup.3 may combine to form a lactone ring of the formula ##STR2## in which R.sup.9 represents a hydrogen atom or a hydroxyl group; R.sup.4 and R.sup.6, which may be the same or different, each represents a hydroxyl group or a lower alkanoyloxy group; R.sup.5 represents a hydrogen atom; R.sup.4 and R.sup.5 may together form an oxo group (.dbd.O); and R.sup.4 and R.sup.6 may combine to form a lower alkylidenedioxy group, the pharmaceutically acceptable salts thereof, processes for the production of the compounds of the general formula (I) and the salts thereof, pharmaceutical composition containing the compounds of the general formula (I) and the salts thereof, and method of use of the compounds of the general formula (I) and the salts thereof.

Sesquiterpene derivatives having anti-complementary activity

3-0-(.beta.-D-Glucuronopyranosyl)-soyasapogenol B represented by the formula (I): ##STR1## and salts thereof and process for preparing the same are disclosed. The compound represented by the formula (I) and salts thereof have anticomplementary activity and are useful as therapeutic agents for autoimmune diseases, collagen diseases, and rheumatic diseases.

3-0-(.beta.-D-Glucuronopyranosyl)-soyasapogenol B

Growing community of inventors

Tokushima, Japan

Yoshimasa Nakano