Nisshin Flour Milling Co., Ltd.

Nippon Chemiphar Co., Ltd.

Hitachi, Ltd.

Nisshin Pharma Inc.

The Kitasato Institute

Kyorin Pharmaceutical Co., Ltd.

Velcura Therapeutics, Inc.

Ihitachi Taga Technology, Ltd.

Toshihiro Takahashi

Yoshiyuki Tahara

Makoto Yanai

Masao Nagase

Yoshikazu Watanabe

Daisuke Saito

Tomio Yamakawa

Hiroyasu Koyama

Reiko Kubota

Yasuhiro Komatsu

Yoshikuni Suzuki

Koichi Nakamaru

Teruhito Yamaguchi

Masashi Suzuki

Yutaka Nomura

Atsushi Tendo

Hitoshi Inoue

Koji Kawamura

Masahiro Ueno

Tatsuo Horaguchi

Shogo Sakuma

Norio Oshida

Hideyuki Tobita

Masanori Sugita

Masato Horigome

Kohei Inomata

Koichi Itoh

Yasushi Yoshino

Koichiro Nishioka

Kenichi Momose

Kazuki Okai

Chikako Suzuki

Shinji Nagai

Kouichi Katsuyama

Susumu Nihashi

Mitsuo Masaki

Koichi Ito

Toshiyasu Imai

Hideaki Fujii

Hiroshi Nagase

Masatoshi Ushioda

Noriyoshi Sueda

Koichiro Hagihara

Masahiro Tsuji

Toshiji Sugai

Eriko Nakata

Hiroyuki Yamazaki

Koichi Katsuyama

Takao Kishiye

Tsutomu Takasawa

Kouji Kawamura

Hiroyuki Ikemoto

Shinichi Yoshida

Yukio Saito

Haruo Seto

Kozo Tamura

Kazuhide Inoue

Kunio Kobayashi

Shigeru Hiramoto

Takashi Kanda

Nobuhiro Kinoshita

Seiichiro Masui

Isao Hiyama

Hiromitsu Takeda

Shoichi Ito

Kazuo Shin-Ya

Naoya Moritoh

Shinichi Kaji

Tsuyoshi Endo

Shigeharu Nakano

Shigeo Hatanaka

Tamiko Hamada

Masato Ariga

Yoshitaka Shibata

Kazuyuki Yano

Kaoru Hara

Toshiharu Kodato

Kazuhike Inoue

Nobutaka Mochizuki

Kiyomi Takamaru

Tomotaka Honda

Masaki Kaji

Nobutoshi Kubota

Naohito Iwata

Masatoshi Yasuda

Satoko Fuchizawa

The present invention relates to a morphinan derivative represented by the following general formula (I), wherein Rrepresents hydrogen, Calkyl, Caryl, etc., Rand R, which are the same or different, represent hydrogen, hydroxy, etc., Rand Rrepresent hydrogen, Calkyl, etc., Rrepresents hydrogen, hydroxy, Calkyl, etc., X represents O or CH, Y represents C&#x2550;O, C(&#x2550;O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient. 

Morphinan derivative

A morphinan derivative represented by the following general formula (I): 

A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2Xreceptor antagonist: wherein Rrepresents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, Rand Rrepresent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, Rand Rrepresent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.

Diazepinedione derivative

The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics:

Salt of (2S, 3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid

Salt of (2S, 3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl] carbamoyl] oxirane-2-carboxylic acid

The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175&#xb0; C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm.

Salt of (2S, 3S) -3- [[(1S) -1- isobutoxymethyl-3-methylbutyl] carbamoly] oxirane-2-carboxylic acid

The invention relates to (1S)-1-isobutoxymethyl-3-methylbutylamine useful as an intermediate in the synthesis of sodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate and a process for production thereof. The process comprises reacting L-leucinol with a compound represented by the following formula in the presence of a base and reducing the obtained (1S)-1-(2-methyl-2-propenoxymethyl)-3-methylbutyl-amine: [in which X is a leaving group].

Amine derivative

This invention relates to a medicament containing as an active ingredient, a novel propanolamine having a 1,4-benzodioxane ring or a pharmaceutically acceptable salt thereof: The present compound is represented by the above formula wherein Rmay be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxy group, a (C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group, a (C&#x2013;C)alkylsulfonamido group, or a phenyl group; Reach represents a hydrogen atom or a (C&#x2013;C)alkyl group; and A represents any of a benzene ring, a pyridine ring and a pyrimidine ring. This compound is useful as a prophylactic or therapeutic agent for diabetes, obesity, hyperlipemia, depression, a respiratory disease, or a gastrointestinal disease.

Propanolamine derivative having 1, 4-benzodioxane ring

Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R and R each are hydrogen, C alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X and X are each a free valency, oxygen, S(O) (wherein p is an integer of 0 to 2), C(&boxH;O), C(&boxH;O)NH, NHC(&boxH;O), CH&boxH;CH, or the like; Y is optionally substituted C alkylene; Z is oxygen or sulfur; R and R are each optionally substituted C alkyl; and R is hydrogen or C alkyl, with the proviso that when X is a free valency, X is not O or S(O) , while when X is C(&boxH;O)NH, X is not a free valency.

PPAR delta activators

Quinazoline derivatives

Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R and R are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; R is alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a hetericyclic-alkyl group; X is &mdash;O&mdash; or &mdash;NR &mdash; (wherein R is hydrogen, alkyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; Y is OR , SR , or NR R (wherein each of R , R and R is hydrogen, alkyl, aryl, aralkyl, acyl, a heterocyclic group, or a heterocyclic-alkyl group, and R is the same as defined for R ); and Y is hydrogen or alkyl, or alternatively Y and Y can be combined to form &boxH;O, &boxH;S, &boxH;N&mdash;R , or &boxH;N&mdash;OR (wherein each of R and R is the same as defined for R ), provided that each of the alkyl, aryl and heterocyclic groups defined for R to R can have one or more specific substituents and that each of the group defined for R to R and Y is specificed in the number of carbon atoms.

Epoxysuccinamide derivatives

Optically active 1,4-benzodioxin-2-carboxylic acid derivatives and process for producing the same

Disclosed are optically active alcohols having formula (1) and (2)

Growing community of inventors

Saitama, Japan

Toshihiro Takahashi