Kowa Company Limited

Tadaaki Ohgiya

Kimiyuki Shibuya

Toru Miura

Koichi Yamazaki

Yukihiro Sato

Seiichi Sato

Takahiro Kitamura

Takayuki Matsuda

Katsumi Kawamine

Katsutoshi Miyosawa

Yoshinori Kyotani

Kazuhiro Onogi

Hiromichi Shigyo

Ayumu Okuda

Mitsuteru Hirata

Taro Aoki

Toshiyuki Edano

Chiyoka Ozaki

Toshiharu Arai

Haruki Shibata

Taichi Kusakabe

Junya Tagashira

Noriaki Gomi

Ryohei Sekimoto

Rie Ishida

Hitomi Aoki

Takashi Yamaguchi

Hajime Yamada

Masao Ohkuchi

Yasumi Uchida

Tsutomu Toma

Tomoyuki Koshi

Tomio Ohta

Takaaki Araki

Kazutoyo Abe

Takahisa Ogamino

Gen Watanabe

Natsuyo Kumai

Kyoko Kotaki

Kennosuke Matsuda

Hisashi Nakashima

Toshiaki Watanabe

Takahiro Mori

Takeshi Murakami

Noriyuki Inoue

Toshiaki Oda

Yukiyoshi Yamazaki

Hideo Yoshizaki

Yoshio Takahashi

Noboru Shimizu

Toshiharu Morimoto

Yukihiro Okuno

Yuriko Habata

Tomoaki Koshizawa

Nao Yamasaki

Yuji Kurihara

Mitsuo Kawada

Yasushi Kaneko

Mikio Fujii

Ryoko Mori, Legal Representative

It is an object of the present invention to provide a novel form of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (S)-trans-{4-[({2-[({1-[3,5-bis(Trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid hydrochloride.

Form of pyrimidine compound having dibenzylamine structure

The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.

Production method for isoquinoline derivatives and salts thereof

The present invention provides: a compound represented by general formula (I) below, that has both angiotensin II receptor antagonism and a PPAR&#x3b3; activation effect and that is useful as a preventative and/or therapeutic agent for high blood pressure, cardiac disease, arteriosclerosis, type-2 diabetes, and the like; and a drug composition containing the compound. General formula (I) (in the formula: ring A represents a pyridine ring; ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C&#x2014;Ror a nitrogen atom; Rrepresents an alkyl group; Rrepresents an alkyl group or a cycloalkyl group; and R, R, and Reach independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar. 

Phenylpyridine derivative and drug containing same

A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R)(R)(R) (in the formula, R, R, and Rindependently represent a Caryl group, a Caryloxy group, a Calkyl group, a Calkoxyl group, a Ccycloalkyl group, or a Ccycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.

Method for preparing optically active 1-bromo-1[3,5-bis(trifluoromethyl)phenyl]ethane

Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.

Optically active dibenzylamine derivative, and method for preparing thereof

A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (Rrepresents hydrogen atom or a Calkyl group, and Rrepresents a Calkyl group, a Ccycloalkyl group, a (Ccycloalkyl)(Calkyl) group, a Caryl group, or a Caralkyl group). 

Method for preparing trans-{4-[(alkylamino) methyl]- cyclohexyl}acetic acid ester

Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPAR&#x3b3;-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound. Specifically disclosed are: a compound represented by general formula (I) (wherein the ring A represents a pyridine ring; the ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C&#x2014;Ror a nitrogen atom; Rrepresents a Calkyl group; Rrepresents a Calkyl group or a Ccycloalkyl group; and R, R, Rindependently represent a hydrogen atom, a halogen atom, a Calkyl group, a halo-Calkyl group, or a Calkoxy group which may have a substituent), a salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical composition containing the compound, the salt or the solvate.

Phenylpyridine derivative and medicinal agent comprising same

The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic &#x3b2; cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and the compound represented by the following formula (1): 

Condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same

Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPAR&#x3b3; activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; Rand Rindependently represent a Calkyl group; and each of Rto Ris absent or represents H, a halogen atom, OH, NO, a halo-Calkyl group, a (substituted) Calkoxy group, a (substituted) Ccycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]

Compound having 3-heteroarylpyrimidin-4-(3H)-one structure and pharmaceutical preparation containing same

Monohydrochloride acid addition salts of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. These monohydrochlorides can be produced by reacting a polyacidic basic compound with an acid salt of pyridine.

Method for preparing acid addition salts of polyacidic basic compounds

[Object] It is to provide a novel compound useful for preventing and/or treating diseases that involves 11&#x3b2;-hydroxysteroid dehydrogenase 1 (in particular diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome). [Means to Solve the Object] A 1,2-diazetidin-3-one derivative represented by the following general formula (1) or salt thereof, or their solvate. 

1,2-diazetidin-3-one derivatives and drugs containing same

It is to provide a novel compound useful for preventing and/or treating diseases that involves 11&#x3b2;-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate. [wherein A ring represents Caryl group, 5- to 14-membered heteroaryl group, Ris a hydrogen atom, halogen atom, Calkoxycarbonyl group, hydroxyl group, carboxyl group or carbamoyl group; Rand Rare the same or different and are a Calkyl group; R, R, and Rare same or different, and are a hydrogen atom, halogen atom, Calkyl group, Calkoxy group, Caryl group, or Rand R, or Rand Rmay together form a Calkylenedioxy group, Rand Rare the same of different and represent a hydrogen atom or Calkyl group, or may together form a Ccyclic hydrocarbon group, n represents an integer of 0 or 1].

1-adamantyl azetidin-2-one derivatives and drugs containing same

A compound represented by the following general formula (I), wherein R, R, R, Rand Rrepresent hydrogen atom, a halogen atom, a lower alkyl group and the like, Rrepresents an alkyl group, a cycloalkyl group and the like, Rand Rrepresent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, Rrepresents hydrogen atom, a halogen atom, a lower alkoxy group and the like, Rand Rrepresent hydrogen atom, a lower alkyl group, a lower alkoxy group, a halo(lower alkyl) group and the like, and A represents a heterocyclic ring constituted by 6 to 10 atoms, which has potent inhibitory activity on cholesterol ester transfer protein (CETP). 

Substituted pyrimidine compounds and their utility as CETP inhibitors

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Saitama, Japan

Tadaaki Ohgiya