Novel ligands of nuclear receptors ppar's

Details Novel ligands of nuclear receptors ppar's Novel ligands of nuclear receptors ppar's

C - Chemistry, Metallurgy

07

C

C07C 59/92 (2006.01) A61K 31/12 (2006.01) A61K 31/122 (2006.01) A61K 31/192 (2006.01) A61K 31/216 (2006.01) A61K 31/341 (2006.01) A61K 31/455 (2006.01) A61P 3/10 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) A61P 37/06 (2006.01) C07C 69/738 (2006.01) C07C 403/20 (2006.01) C07C 403/24 (2006.01) C07D 213/65 (2006.01) C07D 213/68 (2006.01) C07D 213/79 (2006.01) C07D 213/80 (2006.01) C07D 307/32 (2006.01) C07D 307/33 (2006.01) C07D 307/58 (2006.01) C07D 405/12 (2006

Patent

CA 2366281

Ligands of nuclear receptors PPAR's (peroxisome proliferator-activated receptors) which are compounds selected from the group consisting of ascofuranone; and ascofuranone homologs and ascochlorin homologs having at least an orcyl aldehyde moiety wherein the hydrogen atom(s) of the hydroxyl group(s) at the 2-position and/or the 4-position of the orcyl aldehyde moiety are substituted by C1-15 alkyl, C1-15 alkenyl, CH2COOH, CH2COO(C1-15 alkyl), C(C=O)(C1-15 alkyl), C(=O)(CH2)1-15COOH, nicotinoyl, isonicotinoyl, etc. These ligands are usable in preventing and/or treating diabetes; hypertension or cerebrovascular disorders; arteriosclerosis; complications of diabetes; chronic inflammation; cachexia; digestive cancers, etc.

L'invention concerne des ligands de récepteurs nucléaires PPAR (récepteurs activés par le proliférateur des péroxisomes), composés choisis dans le groupe constitué d'ascofuranone. Les homologues d'ascofuranone et les homologues d'ascochlorine ont au moins une fraction d'orcyle aldéhyde où l'(les) atome(s) d'hydrogène du(des) groupe(s) hydroxyle en position 2 et/ou en position 4 de la fraction d'orcyle aldéhyde sont substitués par C¿1-15? alkyle, C¿1-15? alcényle, CH¿2?COOH, CH¿2?COO(C¿1-15? alkyle), C(C=O) (C¿1-15? alkyle) C(=O) (CH¿2?)¿1-15?COOH, nicotinoyle, isonicotinoyle, etc. Ces ligands servent à prévenir et/ou à traiter le diabète, l'hypertension ou des troubles cérébrovasculaires, l'artériosclérose, des complications diabétiques, l'inflammation chronique, des cancers digestifs, etc.

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