C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 43/23 (2006.01) A61K 31/085 (2006.01) A61K 31/12 (2006.01) A61P 3/00 (2006.01) C07C 49/84 (2006.01)
Patent
CA 2637375
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1 ; t is 0 or 1 ; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R3 and R4 is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are =O; R5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon. Alternatively, the. agent can be a pharmaceutically acceptable salt of the compound of Formula I.
L'invention concerne des agents convenant pour le traitement de divers troubles du métabolisme tels que: syndrome de résistance à l'insuline, diabète, syndrome de Stein-Leventhal, hyperlipidémie, stéatose hépatique, cachexie, obésité, athérosclérose ou artériosclérose.(...). Dans cette formule, n vaut 1 ou 2; m vaut 0, 1,2, 3 ou 4; q vaut 0 ou 1; t vaut 0 ou 1; R1est un alkyle comptant de 1 à 3 atomes de carbone; R2 est hydrogène, halo, alkyle à 1-3 atomes de carbone, ou alkoxy à 1-3 atomes de carbone; L'un de R3 et de R4est hydrogène ou hydroxy, l'autre est hydrogène; oui bien R3 et R4 ensemble = O; R5 est un hydrogène ou un alkyle comptant un, deux, trois, quatre ou cinq atomes de carbone; A est un phényle non substitué ou substitué par 1 ou 2 groupes pris parmi: halo, hydroxy, alkyle à 1-2 atomes de carbone, perfluorométhyle, alkoxy à 1-2 atomes de carbone, et perfluorométhoxy, ou un cycloalkyle comptant de trois à 6 atomes de carbone cycliques, le cycloalkyle est non substitué ou bien un ou deux atomes de carbone cycliques sont indépendamment mono-substitués par méthyle ou éthyle; ou un noyau aromatique à 5 ou 6 éléments comptant 1 ou 2 hétéroatomes cycliques pris dans N, S et O est lié par covalence au restant du composé de formule (I) par un carbone cyclique. En variante, l'agent peut être constitué par un sel pharmacompatible du composé de formule (I).
Sharma Shalini
von Borstel Reid W.
Gowling Lafleur Henderson Llp
Wellstat Therapeutics Corporation
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