Kissei Pharmaceutical Co., Ltd.

Hideki Takeuchi

Kenji Yokoyama

Yuichiro Kai

Yoshihiro Terao

Harunobu Mukaiyama

Kosuke Okazaki

Hiroaki Kobayashi

Masahiko Uchida

Kazumichi Jo

Norihiko Kikuchi

Hiroaki Shiohara

Yuji Hoyano

Eiji Tsuru

Ritsu Suzuki

Satoshi Akahane

Takehiro Ishikawa

Kiyoshi Kasai

Hiroyuki Oyachi

Tetsuji Ozawa

Koji Kamata

Sadamitsu Shiode

Satoru Mima

Kiyotaka Sugiura

The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.

Salt of fused heterocyclic derivative and crystal thereof

The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.

An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.

The present invention provides a novel form of 3-(3-{4-[3-(&#x3b2;-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since bis[3-(3-{4-[3-(&#x3b2;-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide]monosebacate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.

Monosebacate of pyrazole derivative

The present invention provides a novel form of 3-(3-{4-[3-(&#x3b2;-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(&#x3b2;-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.

Hemifumarate of a pyrazole derivative

The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: 

5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation

Crystals of a salt of 4'-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3&#x2032;,5&#x2032;-dimethylbiphenyl-4-carboxylic acid. The &#x3b1; type, &#x3b2; type and &#x3b3; type crystals produced by treating hydrochloride of 4&#x2032;-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3&#x2032;,5&#x2032;-dimethylbiphenyl-4-carboxylic acid with specified solvents, which can be discriminated by the characteristic diffraction peaks of powder X-ray diffractometry and the like.

Polymorphic crystal of 4'-{2-[ (1S, 2R)&#x2014;2-  hydroxy-2- (4-hydroxyphenyl)-1-methylethylamino]ethoxy} - 3 - isopropyl-3&#x2032;, 5&#x2032; -dimethylbiphenyl- 4 - carboxylic acid hydrochloride

The present invention provides a novel crystalline form of n-butyl[4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl) benzenesulfonylamino]ethyl]-2'-methanesulfonyl-3-yloxy] acetate hydrochloride, pharmaceutical compositions containing the same and their uses, which exhibits excellent inhibitory activities against activated blood coagulation factor X, and is useful for the treatment or prevention of a tromboembolic disease.

Crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative

The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein Ris a hydrogen atom or an optionally substituted lower alkyl group;

The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula:wherein Ris a hydrogen atom or a lower alkyl group;

5-amidino-n-(2-aminophenethyl)-n-hydroxy-benzenesulffonamide derivative, medical composition containing the same, pharmaceutical use thereof and intermediate therefor

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Joetsu, Japan

Hideki Takeuchi