Title:
PPARを調節する二芳香族化合物
Document Type and Number:
Japanese Patent JP5355089
Kind Code:
B2
Abstract:
Biaromatic compounds (I) and their salts, solvates and/or hydrates, are new. Biaromatic compounds of formula (I) and their salts, solvates and/or hydrates, are new. R1 : -OR6, -NR6-OR6 or -NR6R6; R2 : halo, 1-12C alkyl, -OR7, -NHR7 or aralkyl; R3 : 1-12C alkyl, 3-12C cycloalkyl or -(CH 2) mR8; X : -(CH 2) z-NR9-C(Y1)-(NR10) w-; m : 0-4; Y1 : S or O; z, w : 0-1; Ar1, Ar2 : aromatic radical (optionally substituted by R4 or R5) such as Ar1 is 1,3-diphenyl, pyridin-2,6-diyl, pyridin-2,4-diyl, pyridin-3,5-diyl, pyrimidin-2,4-diyl, pyrazin-2,6-diyl or pyrimidin-4,6-diyl and Ar2 may also be 1,4-diphenyl, pyridin-2,5-diyl, pyrimidin-2,5-diyl or pyrazin-2,5-diyl; R4, R5 : H, halo, 1-12C alkyl, OH, alkoxy, polyether, aralkyl, aryl or amino (optionally substituted by 1-2 radicals of 1-12C alkyl or aralkyl); R6 : H, 1-7C alkyl, aryl or aralkyl; R7 : H, 1-7C alkyl, aryl or aralkyl; R8 : 1-7C alkyl, cycloalkyl, aryl, aralkyl, heteroaryl or heterocycloalkyl, -OR11 or optionally substituted amino; R9, R10 : H or1-4C alkyl; and R11 : H, 1-7C alkyl, aryl or aralkyl. Independent claims are included for (1) a composition comprising (I) and an excipient; (2) a cosmetic composition comprising (I) in a support; and (3) the preparation of (I). [Image] ACTIVITY : Antiinflammatory; Dermatological; Antiseborrheic; Antipsoriatic; Antirheumatic; Antiallergic; Respiratory-Gen; Cytostatic; Virucide; Immunosuppressive; Nootropic; Anorectic; Metabolic; Cardiovascular-Gen.; Antiarthritic; Endocrine-Gen; Antiasthmatic; Immunostimulant; Immunomodulator; Antidiabetic; Neuroprotective; Antiarteriosclerotic; Hypotensive. MECHANISM OF ACTION : Peroxisome proliferator-activated receptor (PPAR) modulator. The potency of (I) in modulating PPAR receptor was tested in HeLN cells and was determined using the luminescence produced. The result showed that (Z)-2-ethoxy-3-{3'-[(methyl-octanoyl-amino)-methyl] -biphenyl-4-yl}-acrylic acid exhibited an apparent binding constant of 2000 nM.
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Inventors:
Jean-Gee Boito
Laurence Clary
Laurent Chantara
Michelle rivier
Laurence Clary
Laurent Chantara
Michelle rivier
Application Number:
JP2008537238A
Publication Date:
November 27, 2013
Filing Date:
October 19, 2006
Export Citation:
Assignee:
Galderma Research and Development
International Classes:
C07C233/47; A61K8/42; A61K8/49; A61K31/17; A61K31/195; A61K31/404; A61K31/433; A61K31/44; A61K31/505; A61P1/00; A61P3/04; A61P3/06; A61P3/10; A61P9/00; A61P9/10; A61P9/12; A61P11/00; A61P11/06; A61P17/00; A61P17/02; A61P17/06; A61P17/08; A61P17/10; A61P17/12; A61P17/14; A61P17/16; A61P19/02; A61P25/00; A61P29/00; A61P35/00; A61P35/02; A61P37/02; A61P37/08; A61Q5/00; A61Q19/00; C07C231/12; C07C233/87; C07C235/52; C07C273/18; C07C275/42; C07D209/18; C07D213/55; C07D213/75; C07D239/42; C07D285/14
Domestic Patent References:
| JP4638423B2 |
Foreign References:
| WO2002012210A1 |
Other References:
Chemical Abstracts,2002年,136:167181
Attorney, Agent or Firm:
Masatake Shiga
Takashi Watanabe
Yasuhiko Murayama
Shinya Mitsuhiro
Takashi Watanabe
Yasuhiko Murayama
Shinya Mitsuhiro