Kissei Pharmaceutical Co., Ltd.

Kiyoshi Kasai

Junichi Sonehara

Toshihiro Nishimura

Yasunori Ueno

Hidetoshi Isawa

Masako Yoshida

Michio Toda

Tetsuji Ozawa

Ken Kikuchi

Minoru Kubota

Masahiro Kobayashi

Nobuhiko Fushimi

Eiji Tsuru

Tetsuro Tamai

Nobuyuki Tanaka

Hiromu Harada

Hideki Takeuchi

Takehiro Ishikawa

Satoshi Akahane

Hirotaka Teranishi

Yukihiko Hotei

Ritsu Suzuki

Koji Kamata

[Problem] To provide a novel compound that exhibits an agonistic effect on dopamine Dreceptors. [Solution] The present invention provides a compound represented by the general formula (I): in which Ris Calkyl or the like; Ris hydrogen or the like; Rand Rare each hydrogen, Calkyl, RRN&#x2014;Calkyl, aralkyl, or the like; Rand Rare hydrogen or the like; and Ris hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine Dreceptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.

[object Object]

The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein Ris cyano or the like; Rand Rare hydrogen or the like; Ris Calkyl or the like; Ris Calkyl, halo-Calkyl, cycloalkyl, cycloalkyl-Calkyl, aralkyl or the like; Rand Rare each hydrogen, Calkyl, halo-Calkyl, cycloalkyl, Calkoxy-Calkyl, RRN&#x2014;Calkyl or the like, which exhibit potent dopamine Dreceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof. 

Octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these

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 a novel crystal polymorph of ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.

Crystal polymorph of hydroxynorephedrin derivative hydrochloride

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 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

The present invention relates to a crystalline polymorph of 2-&lsqb;4-&lsqb;2-&lsqb;&lsqb;(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methylethyl&rsqb;amino&rsqb;ethyl&rsqb;phenoxy&rsqb;acetic acid having strong diffraction peaks (diffraction angle: 2&thgr;&plusmn;0.1&deg;) at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0&deg; in powder X-ray diffraction pattern, which has potent &bgr; - and &bgr; -adrenoceptor stimulating effects and is useful as an agent for relieving pain and promoting the removal of calculi in urolithiasis, and the like. For example, the crystalline polymorph can be prepared by hydrolyzing ethyl 2-&lsqb;4-&lsqb;2-&lsqb;&lsqb;(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl&rsqb;-amino&rsqb;ethyl&rsqb;phenoxy&rsqb;acetate phosphate by sodium hydroxide, adding an aqueous phosphoric acid solution at 40&deg; C. and over, adding a mixed solvent of water and methanol or methanol to the resulting compound, and stirring the suspension at 40&deg; C. to reflux temperature for 30 minutes to several hours.

Crystal polymorphism of aminoethylphenoxyacetic acid derivative

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Azumino, Japan

Kiyoshi Kasai