Suntory Limited

Daiichi Suntory Pharma Co., Ltd.

Masayuki Saitoh

Naoki Higuchi

Masaki Hashimoto

Takaharu Tanaka

Harukazu Fukami

Yasuhiro Hayashi

Shinjiro Niwata

Yoshinobu Kiso

Yoichi Nunokawa

Norio Iwasawa

Hiroshi Shibata

Kenji Suzuki

Takashi Nakatsuka

Motoo Sumida

Kenju Miura

Tohru Kodama

Junko Hashino

Tomohiko Ogawa

Keiichi Abe

Munetada Haruyama

Yasuo Kitajima

An NF-&#x3ba;B inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R, R, and Rare each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; Ris H, hydroxymethyl, alkyl, or carboxyl which is optionally esterified or amidated; Z is represented by the formula (A); and, n is an integer from 0 to 6, or its hydroquinone form or a pharmaceutically acceptable salt thereof.

NF-&#x3ba;B inhibitor comprising phenylmethyl benzoquinone as the active ingredient

An inhibitor of NF-&kgr;B comprising as an active ingredient an indan derivative represented by the general formula (I) or a salt thereof.

NF-&kgr;B inhibitor comprising an indan derivative as an active ingredient

Therapeutics for thrombocytopenia

Disaccharide derivative

A Novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or bridged cyclic alkyloxycarbonyl group having 4-15 carbon atoms; a benzyloxycarbonyl group which is unsubstituted or substituted with a halogen atom, nitro group or methoxy group; a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group; R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group; R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group; R.sub.4 is a butyl group, and R.sub.5 is a hydrogen atom; provided that R.sub.1 can be an unsubstituted benzyloxycarbonyl group only when R.sub.3 is a n-butyl group.

Proteinase inhibitor

A dipeptide derivative having the formula (I):

Dipeptide derivative and prophylactic or therapeutic agent for bone

A prophylactic or therapeutic agent for malignant hypercalcemia, bone Paget's disease and osteoporosis is disclosed, which contains as an active ingredient a dipeptide derivative represented by formula:

Dipeptide derivative and prophylactic and therapeutic agent for bone

A compound of the general formula: ##STR1## wherein m is an integer of 1 to 7,

Pyrrolidineamide derivatives of acylamino acid and pharmaceutical

A novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or partly branched cyclic alkyloxycarbonyl group having 4-15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutyryl group; R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group; R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group; R.sub.4 is a butyl group, a benzyl group or a methylthioethyl group; and R.sub.5 is a hydrogen atom or a chloromethyl group, which inhibits the activity of cysteine proteinases.

A novel depeptide derivative which exhibits inhibitory activity against prolyl endopeptidase and is effective for preventing and curing amnesia is disclosed. A process for chemical synthesis of such a derivative, as well as its use, is also disclosed.

Dipeptide derivative and synthesis and use thereof

A compound of the general formula: ##STR1## wherein m is an integer of 1 to 7, n is 0 or an integer of 1 to 5,

Pyrrolidineamide derivative of acylamino acid and pharmaceutical

A novel pyrrolidineamide derivative that exhibits inhibitory activity toward prolyl endopeptidase and its use as an inhibitor against said enzyme are provided. The pyrrolidineamide of the invention has the following general formula: ##STR1## wherein R.sup.1 is benzyloxycarbonyl or a group of the formula: ##STR2## (wherein m is an integer of from 1 to 5) and R.sup.2 is hydroxy, acyloxyy or a group of the formula: ##STR3## (wherein R.sup.3 and R.sup.4 independently are a hydrogen atom, a halogen atom, a lower alkyl or a lower alkoxy).

Pyrrolidineamide derivative having anti-prolyl endopeptidase

A novel compound that exhibits inhibitory activity against prolyl endopeptidase and a method for chemical synthesis of said compound, as well as its use as a prolyl endopeptidase inhibitor and an anti-amnesic agent that contains said compound as the active ingredient are provided.

Dipeptide derivative of fatty acid

A novel pyrrolidinylamide ester derivative that exhibits inhibitory activity against prolyl endopeptidase, methods for synthesis thereof and its use as an inhibitor against said enzyme are disclosed. The pyrrolidinylamide ester of the invention has the following general formula: ##STR1## wherein n is 0 or an integer of 1 to 7 and R is hydrogen atom or a straight or branched alkyl having 1 to 8 carbon atoms.

Growing community of inventors

Osaka, Japan

Masayuki Saitoh