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Multimeric VLA-4 antagonists comprising polymer moieties
专利权人:
Theodore Yednock;Andrei W. Konradi;Christopher M. Semko;Jenifer L. Smith;Michael A. Pleiss
发明人:
Andrei W. Konradi,Michael A. Pleiss,Christopher M. Semko,Theodore Yednock,Jenifer L. Smith
申请号:
US12877496
公开号:
US08263063B2
申请日:
2010.09.08
申请国别(地区):
US
年份:
2012
代理人:
摘要:
Disclosed are conjugates exhibiting VLA-4 antagonistic properties. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. The conjugates of this invention are characterized as containing more than one VLA-4 inhibiting compound covalently attached to a bio-compatible polymer, such as polyethylene glycol. Conjugates of the invention are defined by formula I,wherein A, B, and q are described in the specification. 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.
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