Acyl derivatives which treat vla-4 related disorders

Details Acyl derivatives which treat vla-4 related disorders Acyl derivatives which treat vla-4 related disorders

C - Chemistry, Metallurgy

07

D

C07D 239/42 (2006.01) A61K 31/38 (2006.01) A61K 31/381 (2006.01) A61K 31/41 (2006.01) A61K 31/415 (2006.01) A61K 31/433 (2006.01) A61K 31/44 (2006.01) A61K 31/4468 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/505 (2006.01) A61K 31/506 (2006.01) A61K 31/53 (2006.01) A61P 1/00 (2006.01) A61P 3/10 (2006.01) A61P 7/00 (2006.01) A61P 7/02 (2006.01) A61P 9/00 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P

Patent

CA 2359115

Disclosed are compounds such as IIa which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiples sclerosis.

L'invention concerne des composés représentés par les formules Ia et Ib, qui se lient à VLA-4. Certains de ces composés inhibent également l'adhérence leucocytaire et, en particulier, l'adhérence leucocytaire dépendant de VLA-4. Ces composés sont utiles pour traiter des maladies inflammatoires chez un patient mammifère, p. ex. l'être humain, telles que l'asthme, la maladie d'Alzheimer, l'athérosclérose, le syndrome démentiel lié au SIDA, le diabète, l'affection intestinale inflammatoire, la polyarthrite rhumatoïde, la greffe de tissus, les métastases de tumeur et l'ischémie myocardique. Les composés peuvent également être administrés pour traiter des affections cérébrales inflammatoires telles que la sclérose en plaques.

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