Kowa Company Limited

Minoru Koura

Kimiyuki Shibuya

Takayuki Matsuda

Sayaka Kurobuchi

Yukiyoshi Yamazaki

Ayumu Okuda

Yuki Yamaguchi

Yuichiro Watanabe

Takashi Enomoto

Takaaki Araki

Hisashi Sumida

Toru Miura

Koichi Yamazaki

Yuuichirou Watanabe

Sayaka (deceased) Kurobuchi

[Object] It is to provide a novel LXR&#x3b2; agonist 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: (wherein, each V and W independently show N or C&#x2014;R; each X and Y independently show CH, C&#x2550;O, SO, etc; Z shows CH or N; each R, Rand Rindependently show a hydrogen atom, Calkyl group, etc.; Rshows Calkyl group; Rshows an optionally substituted Caryl group or an optionally substituted 5- to 11-membered heterocyclic group; Rand Rshow a hydrogen atom, etc.; L shows a Calkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)

Carbinol derivatives having heterocyclic linker

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

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

A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided. A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.

Process for production of optically active PPAR-activating compound and intermediate of the same

A process for producing an optically active 2-hydroxybutyric ester represented by formula (1): by reacting an optically active 2,3-epoxypropionic ester represented by formula (2): with a methyl Grignard reagent CHMgX in the presence of a copper catalyst in an amount of 0.05 to 0.5 mol with respect to 1 mol of the 2,3-epoxypropionic ester.

Process for producing optically active 2-hydroxybutyric ester

The invention provides a process for producing an optically active butyric acid compound and a production intermediate therefore at high yield and high purity. The present invention provides a process for producing Compound (6), including reacting Compound (1) with optically active 2-trifluoromethanesulfonyloxybutyrolactone (2) in the presence of a base or reacting optically active 2-hydroxybutyrolactone (2) under Mitsunobu reaction conditions, to thereby form Compound (3); reacting Compound (3) with an alcohol and a halogenating agent, to thereby form Compound (4); dehalogenating Compound (4), to thereby form Compound (5); and de-esterifying Compound (5). 

Processes for production of optically active PPAR-activating compounds and intermediates for production thereof

The present invention provides a production intermediate for compound (A-1) and a method for producing the intermediate at high yield and high optical yield.

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Kawagoe, Japan

Minoru Koura