Multivalent vla-4 antagonists comprising polyethylene glycol...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2573245

Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates 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 conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

L'invention concerne des conjugués qui se lient à l'antigène VLA-4. Certains de ces conjugués inhibent également l'adhérence des leucocytes, en particulier l'adhérence des leucocytes dont la médiation est assurée par VLA-4. Les conjugués selon l'invention peuvent servir à traiter des maladies inflammatoires chez un patient mammalien, par exemple un patient humain, ces maladies inflammatoires comprenant l'asthme, la maladie d'Alzheimer, l'athérosclérose, le syndrome démentiel lié au SIDA, le diabète, les maladies intestinales inflammables, l'arthrite rhumatoïde, la greffe de tissus, la métastase tumorale, et l'ischémie myocardique. Ces conjugués peuvent aussi être administrés pour traiter des maladies cérébrales inflammatoires telles que la sclérose en plaques.

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