Fused pyrazole derivatives and methods of treatment of...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 231/54 (2006.01) A61K 31/4155 (2006.01) A61K 31/416 (2006.01) A61P 9/10 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2589648

The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of .alpha.-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG- CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.

L'invention concerne certains dérivés de pyrazole condensés de formule (Ia), et des sels pharmaceutiquement acceptables de ces dérivés, lesdits dérivés et sels présentant des propriétés pharmacologiques utiles, par exemple, en tant qu'agonistes du récepteur RUP25. Cette invention concerne également des compositions pharmaceutiques contenant les composés de l'invention, et des procédés d'utilisation des composés et compositions selon l'invention pour traiter des troubles liés au métabolisme, y compris la dyslipidemie, l'athérosclérose, les maladies coronariennes, la résistance à l'insuline, le diabète de type 2, le syndrome X, et analogue. De plus, la présente invention concerne l'utilisation desdits composés en association avec d'autres agents actifs tels que ceux appartenant à la classe des inhibiteurs de l'.alpha.-glucosidase, des inhibiteurs de l'aldose réductase, des biguanides, des inhibiteurs de la HMG-CoA réductase, des inhibiteurs de la synthèse de squalène, des fibrates, des renforçateurs du catabolisme des LDL, des inhibiteurs de l'enzyme de conversion de l'angiotensine (ACE), des renforçateurs de la sécrétion d'insuline, des antagonistes du récepteur DP, et analogue.

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