Nippon Chemiphar Co., Ltd.

Shizuoka Prefectural University Corporation

Velcura Therapeutics, Inc.

Tomio Yamakawa

Shogo Sakuma

Yutaka Nomura

Seiichiro Masui

Mitsuo Masaki

Atsushi Tendo

Takashi Kanda

Susumu Okabe

Hitoshi Matsukura

Toshihiro Takahashi

Masaru Satoh

Shinichi Yoshida

Kunio Kobayashi

Kazuki Okai

Susumu Nihashi

Nobutaka Mochiduki

Masatoshi Hayashi

Hiromitsu Takeda

Yasushi Yoshino

Masuharu Hirano

Yoriko Shinohara

Tadashi Kobayashi

Masatoshi Ushioda

Tsuyoshi Endo

Rie Takahashi

Yasunori Iwao

Shigeru Itai

Takashi Ohta

Nobutaka Mochizuki

Shuji Noguchi

Toshihisa Ishikawa

Hikaru Saito

The present invention relates to a solid dispersion containing a compound represented by General Formula (I): 

Solid dispersion

A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR&#x3b4;. 

Activating agent for peroxisome proliferator activated receptor &#x3b4;

An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.

Agent for overcoming resistance to anti-cancer agent

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

A compound represented by the following general formula (I):  (wherein Rrepresents phenyl, etc. which can have substituents selected from the group consisting of Calkyl, Calkyl having halogen, halogen, hydroxyl, etc.; Rrepresents Calkyl, etc.; A represents oxygen, sulfur, etc.; X represents Calkylene chain, etc.; Y represents C(&#x2550;O), CH&#x2550;CH, etc.; R, R, and Reach represents hydrogen, Calkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; Rand Reach represents hydrogen, Calkyl, etc.; and Rrepresents hydrogen or Calkyl; provided that at least one of R, R, and Ris not hydrogen) or a salt of the compound; and a PPAR-&#x3b4; activator which contains the compound or salt as the active ingredient.

Activator of peroxisome proliferator-activated receptor &#x3b4;

Activator for peroxisome proliferator-activated receptor &#x3b4;

The invention relates to compounds of the following formula (I) or their salts: in which Ris a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, carboxyl, halogen, hydroxyl, nitro, or cyano; Ris cyano, nitro, or the like; Ris hydroxyl or the like; X is oxygen, sulfur, or the like; and Y is oxygen or sulfur, and a xanthine oxidase inhibitor containing the compound.

Substituted 1,3-thiazolo[5,4-d]pyrimidines as xanthine oxidase inhibitors

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

A compound represented by the formula (I) or a salt of the compound, and a PPAR-&#x3b4; activator which contains the compound or salt as the active ingredient:  (wherein A represents O or S; Brepresents N, etc.; Brepresents O, etc.; each of Xand Xrepresents O, S, a bond, etc.; Y represents Calkylene chain; z represents O or S; Rrepresents aryl, etc. which can have substituents; Rrepresents Calkyl, etc.; Rrepresents Calkyl, Calkenyl, etc.; each of Rand Rrepresents hydrogen, Calkyl, etc.; and Rrepresents hydrogen, etc.; provided that each of Z and Ris attached to the benzene ring, and Xis not attached to the benzene ring).

A compound represented by the following general formula (I): 

Activator of peroxisome proliferator-activated re-ceptor &#x3b4;

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

A compound represented by the formula (I) or a salt of the compound, and a PPAR-&#x3b4; activator which contains the compound or salt as the active ingredient: 

Activator of peroxisome proliferator-activated receptor delta

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.

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Chiba, Japan

Tomio Yamakawa