Kissei Pharmaceutical Co., Ltd.

Hidetoshi Isawa

Yukihiko Hotei

Masayuki Isaji

Kiyoshi Kasai

Junichi Sonehara

Itaru Miyashita

Masaaki Takemura

Ken Kikuchi

Minoru Kubota

Masahiro Kobayashi

Nobuhiko Fushimi

Hiromu Harada

Satoshi Akahane

Den-ichi Momose

Yoshinori Nonaka

Tetsuji Ozawa

Michio Toda

Yasuo Takehana

Masaaki Satoh

Nobuko Yanagi

The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(&#x3b2;-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.

Pyrazole derivative and use thereof for medical purposes

The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R, R, R, Rand Rmay be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, Ris an alkyl group, for example Ris a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PGis a pivaloyl group or the like, as an example, Xis a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.

Process for production of glucopyranosyloxypyrazole derivative

The present invention provides ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride &#xbc; hydrate or a crystal thereof which can be determined by characteristic diffraction peaks of the powder X-ray diffraction, thermogravimetry-differential thermal analysis or the like, and obtained by manufacturing ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl-ethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.

Crystal of hydroxynorephedrin derivative hydrochloride &#xbc; hydrate

The present invention provides ethyl (&#x2212;)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent &#x3b2;-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

Crystals of hydroxynorephedrine derivative

1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds

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Joetsu, Japan

Hidetoshi Isawa