C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) A61K 31/435 (2006.01) A61P 3/10 (2006.01) A61P 25/18 (2006.01) A61P 25/28 (2006.01) A61P 35/00 (2006.01) C07D 401/14 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2422354
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula (V) wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substitutents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2', R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
L'invention concerne des nouvelles compositions pyrazoliques renfermant un support pharmaceutiquement acceptable ainsi qu'un composé de formule (V), dans laquelle Z?1¿ est N, CR?a¿ ou CH et Z?2¿ est N ou CH, à condition que Z?1¿ ou Z?2¿ soit azote; G est le noyau C ou le noyau D; le noyau C est choisi parmi un noyau phényle, pyridinyle, pyrimidinyle, pyridazinyle, pyrazinyle ou 1,2,4-triazinyle, ledit noyau C comportant un ou deux substituants ortho choisis indépendamment parmi les groupes -R?1¿; le noyau D est un noyau monocyclique de 5 à 7 éléments ou un noyau bicyclique de 8 à 10 éléments choisi parmi aryle, hétéroaryle, hétérocyclyle ou carbocyclyle; R?x¿ et R?y¿ sont indépendamment choisis parmi les groupes T-R?3¿, ou R?x¿ et R?y¿ sont pris ensemble avec leurs atomes intermédiaires de manière à former un cycle accolé; et R?1¿, R?2¿, R?2'¿, R?3¿ et T sont tels que définis dans la description. Ces composés sont utiles comme inhibiteurs de la protéine kinase, et notamment comme inhibiteurs d'aurora-2 et de GSK-3, dans le traitement de maladies telles que le cancer, le diabète et la maladie d'Alzheimer.
Bebbington David
Binch Hayley
Charrier Jean-Damien
Davies Robert
Forster Cornelia
Smart & Biggar
Vertex Pharmaceuticals Incorporated
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