Heteroaryl compounds which inhibit leukocyte adhesion...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/69 (2006.01) A61K 31/505 (2006.01) C07D 239/50 (2006.01)

Patent

CA 2480756

Disclosed are compounds which bind 4 integrins, where the 4integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by 4integrins, where the 4 integrin is preferably 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 multiple sclerosis.

L'invention concerne des composés se liant aux intégrines alpha-4 étant, de préférence, VLA-4. Certains de ces composés inhibent également l'adhésion leucocytaire et, notamment, l'adhésion leucocytaire induite par des intégrines alpha-4 étant, de préférence VLA-4. De tels composés sont utiles dans le traitement de maladies inflammatoires chez un patient mammifère, par exemple un être humain. On peut citer parmi de telles maladies inflammatoires : l'asthme, la maladie d'Alzheimer, l'athérosclérose, la démence du SIDA, les diabètes, une maladie intestinale inflammatoire, la polyarthrite rhumatoïde, une greffe tissulaire, des métastases tumorales et l'ischémie myocardique. Les composés peuvent également être administrés pour le traitement de maladies inflammatoires cérébrales, telles que la sclérose en plaques.

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