Substituted bis-acridines and related compounds as ccr5...

C - Chemistry – Metallurgy – 07 – D

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C07D 219/12 (2006.01) A61K 31/015 (2006.01) A61K 31/47 (2006.01) A61K 31/473 (2006.01) A61K 31/496 (2006.01) C07C 15/28 (2006.01) C07D 219/00 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2276525

This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.

Cette invention se rapporte à des bis-acridines substituées et à des composés associés qui sont des ligands, et notamment des antagonistes, du récepteur CCR5. Cette invention se rapporte en outre au traitement et à la prévention d'états pathologiques liés à la présence du CCR5, et notamment, mais pas exclusivement, au traitement et à la prévention de l'asthme et des troubles atopiques (dermatoses et allergies atopiques entre autres), de la polyarthrite rhumatoïde, de l'athérosclérose, du psoriasis, des maladies auto-immunes telles que la sclérose en plaques, et des maladies intestinales inflammatoires, toutes ces maladies pouvant affecter des mammifères, au moyen de ces bis-acridines substituées et des composés associés qui sont des antagonistes du récepteur CCR5. En outre, le fait que CCR5 soit un co-récepteur pour le point d'entrée du VIH dans les cellules, les ligands sélectifs vis à vis de ce récepteur peuvent s'avérer utiles au traitement de l'infection par le VIH.

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