Nippon Chemiphar Co., Ltd.

Velcura Therapeutics, Inc.

Atsushi Tendo

Toshihiro Takahashi

Tomio Yamakawa

Mitsuo Masaki

Haruhiko Shinozaki

Michiko Ishida

Norihisa Miyake

Kazuki Okai

Susumu Nihashi

Toshio Satoh

Shogo Sakuma

Shinichi Yoshida

Kunio Kobayashi

Hiromitsu Takeda

Mutsumi Muramatsu

Hiroyasu Sekine

Toshiyasu Imai

Yutaka Nomura

Kazuhide Inoue

Masatoshi Ushioda

Takashi Kanda

Yasunori Goto

Seiichiro Masui

Tsuyoshi Endo

Nobutaka Mochiduki

Yoriko Shinohara

Nobutaka Mochizuki

Yoshio Kikawa

Kaname Kondo

A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2Xreceptor antagonist: 

P 2&#xd7;4 receptor antagonist

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 compounds of the following formula (I) or their salts: in which Rrepresents ORor others, in which Ris an alkyl group having 1-8 carbon atoms which may have a substituent or the like; Ris halogen, nitro, cyano, carboxyl, or the like; Ris hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR, oxygen, or sulfur, in which Ris hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CRor nitrogen, in which Rhas the same meaning as Rabove, and a xanthine oxidase inhibitor containing the compound as an active ingredient.

Substituted thiazolopyrimidines as xanthine oxidase inhibitors

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

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

Disclosed are new alkylenediamine derivatives of the following formula which are effective for treatment of dysuria are disclosed: ##STR1## wherein R.sup.1 is hydrogen, alkyl, or a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.2 is a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic group; R.sup.3 and R.sup.4 represent hydrogen, alkyl, aralkyl or aryl; or R.sup.3 and R.sup.4 are combined to form one of substituted or unsubstituted 5- to 7-membered heterocyclic groups; X is oxygen, sulfur or imino; Y is oxygen or sulfur; Z is --CH.sub.2 --, --CO-- or --CS--; m is an integer of 0-4; n is an integer of 0-4; r is 0 or 1; and p and q represent an integer of 0-5 provided that p plus q is 1-5.

N-aminoalkyl-substituted nitrogen-containing six membered heterocyclic

Alkylenediamine derivatives

N-aminoalkyl-substituted nitrogen-containing five membered heterocyclic

A compound having the formula ##STR1## wherein R.sub.1 represents an indanyl, indolyl, quinolyl or chromonyl group, the group of the formula ##STR2## (in which R.sub.2 represents a halogen atom or a nitro group), or the group of the formula ##STR3## (in which R.sub.3 represents a halogen atom, or an alkyl, nitro, cyano, acetamino, aminosulfonyl, benzoyl, phenoxy or trifluoromethyl group, R.sub.4 represents a hydrogen or halogen atom, or an alkyl group, and R.sub.5 represents a hydrogen or halogen atom, or an alkyl group), or a pharmaceutically acceptable salt thereof. The compound is obtained by reacting 4-guanidinomethylcyclohexanecarboxylic acid or a reactive derivative thereof with a compound of the formula R.sub.1 --OH wherein R.sub.1 is the same as defined above, or a reactive derivative thereof.

Guanidinocyclohexanecarboxylic acid derivatives

A compound of the formula, ##STR1## wherein R represents a hydrogen atom, a naphthyl, indanyl, tetrahydronaphthyl or pyridyl group, or a phenyl group which may have 1 to 3 substituents selected from the group consisting of a halogen atom, and an alkyl, alkenyl, alkoxy, alkanoyl, cyano, formyl, trifluoromethyl, phenyl, phenylalkyl, alkanoyl-amino, aminosulfonyl, carboxyl, alkoxycarbonyl, benzyloxycarbonyl, benzoylvinyl, phenylvinylcarbonyl, carboxyvinyl, and diphenyl-methyloxycarobnylvinyl group, A represents an oxygen or sulfur atom, and n represents an integer of 0 to 3, with the proviso that when n is an integer of 0, R must not be a hydrogen atom, or a pharmaceutically acceptable salt thereof is effectively useful for inhibiting a complement reaction, inflammation caused by an allergic reaction, and platelet aggregation.

Amidinopiperidine derivatives

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Saitama, Japan

Atsushi Tendo