Kowa Company Limited

Ayumu Okuda

Kimiyuki Shibuya

Toru Miura

Koichi Yamazaki

Yukiyoshi Yamazaki

Takayuki Matsuda

Yuki Yamaguchi

Sayaka Kurobuchi

Hidefumi Ozawa

Tadaaki Ohgiya

Masahiro Nishikawa

Taro Aoki

Tsutomu Toma

Minoru Koura

Katsutoshi Miyosawa

Yuichiro Watanabe

Kazutoyo Abe

Toshiharu Arai

Haruki Shibata

Soichi Oda

Takashi Enomoto

Takaaki Araki

Hisashi Sumida

Hajime Yamada

Hiroyuki Ishiwata

Shinsuke Itoh

Takahisa Ogamino

Yoshiharu Miyake

Shin Tanikawa

Ayako Tosaka

Yuuichirou Watanabe

Okihisa Tokuda

Tomoaki Fukuda

The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic &#x3b2;-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group;Rand R, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo Calkyl group, a Caryl group, a cyano group, a Calkyl group optionally having a substituent, a Calkenyl group optionally having a substituent, etc.; Rrepresents a hydrogen atom, a Calkyl group optionally having a substituent, etc.; and Rrepresents a hydrogen atom, a halogen atom, a Calkyl group optionally having a substituent, etc.]

Spiroindoline compound, and medicinal agent comprising same

There is provided a novel LXR&#x3b2; agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.

Substituted carbinol compound

[Object] To provide a novel LXR&#x3b2; agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate. 

Carbinol derivatives having cyclic linker

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

To provide a novel LXR&#x3b2; agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. A quinoline compound represented by the following general formula (1) or salt thereof, or their solvate. 

Quinoline compounds

The object is to provide a novel LXR&#x3b2; agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate. 

1,3-dihydroisobenzofuran derivatives

To provide a novel LXR&#x3b2; agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate. 

2-oxochromene derivatives

A compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: (wherein R, R, R, Rand Rare the same or different, and represent hydrogen atom, a halogen atom, a lower alkyl group etc., R, Rand Rare the same or different, and represent hydrogen atom, a halogen atom, a lower alkyl group etc., Rand Rare the same or different, and represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group etc., and Rrepresents hydrogen atom, a halogen atom, a lower alkoxy group, a (lower alkyl)thio(lower alkoxy) group, a (lower alkyl)sulfinyl(lower alkoxy) group, a (lower alkyl)sulfonyl(lower alkoxy) group etc.), which has potent inhibitory activity on CETP.

Pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same

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

Pyrimidine compound having dibenzylamine structure and medicament comprising the same

The present invention provides a compound selectively activating PPAR&#x3b1;, which is useful as a medicament. The present invention is specifically directed to a benzoic acid derivative represented by the following general formula (1): wherein A represents an oxygen atom, a nitrogen atom, or a sulfur atom; R represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkyl-alkyl group, an aryl group, an aryl-alkyl group an aryl-oxy-alkyl group, a pyridyl-alkyl group, an alkoxycarbonyl-alkyl group, or a carboxy-alkyl group; X represents an oxygen atom, an NH group, or an S(O)group (wherein n represents an integer of 0, 1, or 2); and m represents an integer from 2 to 8; or a salt thereof. The present invention also provides a medicament comprising the benzoic acid derivative or the salt thereof as an active ingredient.

PPAR-activating compound

A compound represented by the following formula (1): (wherein each of Rand R, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R, R, R, and R, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a Calkyl group, a trifluoromethyl group, a Calkoxy group, a Calkylcarbonyloxy group, a di-Calkylamino group, a Calkylsulfonyloxy group, a Calkylsulfonyl group, a Calkylsulfinyl group, or a Calkylthio group, or Rand R, or Rand Rmay be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N&#x2014;R(Rrepresents a hydrogen atom, a Calkyl group, a Calkylsulfonyl group, or a Calkyloxycarbonyl group); Y represents an oxygen atom, S(O)(l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosulfonyl group; Z represents CH or N; n is a number of 1 to 6; and m is a number of 2 to 6) or a salt thereof; and therapeutic drugs containing any of such a compound or salt.

PPAR-activating compound and pharmaceutical composition comprising the compound

A compound represented by the following formula (1): Or a salt thereof; and therapeutic durgs containing the compound. The compound selectively activates PPAR&#x3b1;.

Growing community of inventors

Tokyo, Japan

Ayumu Okuda