Chemokine receptor modulators, production and use

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/435 (2006.01) A61K 38/16 (2006.01) A61K 38/17 (2006.01) A61K 38/19 (2006.01) A61K 47/48 (2006.01) C07K 14/47 (2006.01) C07K 14/52 (2006.01) C07K 14/715 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2412162

Chemokine receptor modulators comprising a chemically modified carboxyl- terminus (C-terminus) and/or amino-terminus (N-terminus) for modulating potency and pharmacokinetic properties, and methods of production and use are disclosed. The compounds and methods of the invention are exemplified by novel N-terminal, C-terminal and N/C-terminal analogs of CC and CXC chemokines. The chemokine receptor modulator analogs of the invention are useful for the treatment of disorders involving the naturally occurring chemokine that the analogs of the invention antagonize, such as for the treatment of HIV and AIDS related disorders and for the treatment of asthma, allergic rhinitis, atopic dermatitis, atheroma/atherosclerosis, organ transplant rejection, and rheumatoid arthritis.

L'invention concerne des modulateurs du récepteur de la chimiokine comprenant un terminus C modifié chimiquement et/ou un terminus N permettant de moduler les propriétés actives et pharmacocinétiques. L'invention concerne également des méthodes de production et d'utilisation desdits modulateurs. Les composés et méthodes selon l'invention sont exemplifiés par de nouveaux analogues N-terminaux, C-terminaux et N/C-terminaux de chimiokines CC et CXC. Les analogues des modulateurs du récepteur de la chimiokine selon l'invention sont utiles pour le traitement de troubles dans lesquels interviennent des chimiokines naturelles qui ont pour antagonistes les analogues selon l'invention, notamment pour le traitement des troubles associés au VIH et au SIDA et pour le traitement de l'asthme, de la rhinite allergique, de la dermite atopique, de l'athérome/athérosclérose, du rejet de greffe et de la polyarthrite rhumatoïde.

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