Tyrosine kinase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 417/12 (2006.01) A61K 31/44 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 27/02 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2450562

The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals. A compound of Formula (I) wherein n is 0 or 1; X is C-H or N, provided X is C-H if n=1 and R1 is SO2-(C1- C6 alkyl) and provided that X is C-H if R1 is NH(C=O)NR3H; R1 is SO2-(C1-C6 alkyl), (C=O)NR3H, or NH(C=O)NR3H; R2 is OH OC1-C6 alkyl, C1-C6 alkyl, or halo; and R3 is C1-C6 alkyl.

L'invention concerne des composés inhibant, régulant et/ou modulant une transduction de signal de tyrosine kinase, des compositions contenant ces composés, et des méthodes utilisant ces composés afin de traiter des troubles et des maladies associés à la tyrosine kinase, tels que l'angiogénèse, le cancer, la croissance tumorale, l'athérosclérose, la dégénération maculaire liée à l'âge, la rétinopathie diabétique, les maladies inflammatoires, et analogues chez les mammifères. Un composé est représenté par la formule (I) dans laquelle n est égal à 0 ou 1; X représente C-H ou N, à condition que X représente C-H lorsque n=1 et que R?1¿ représente SO¿2?-(C¿1?-C¿6? alkyl), et à condition que X représente C-H lorsque R?1¿ représente NH(C=O)NR?3¿H; R?1¿ représente SO¿2?-(C¿1?-C¿6? alkyl), (C=O)NR?3¿H, ou NH(C=O)NR?3¿H; R?2¿ représente H, OH, OC¿1?-C¿6? alkyle, C¿1?-C¿6? alkyle, ou halo; et R?3¿ représente C¿1?-C¿6? alkyle.

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