C-22 ring stabilized rapamycin derivatives

Details C-22 ring stabilized rapamycin derivatives C-22 ring stabilized rapamycin derivatives

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2169277

This invention provides C-22 substituted rapamycin derivatives of formulas (Ia) or (Ib) or a pharmaceutically acceptable salt thereof or a proline analogue thereof or a pharmaceutically acceptable salt of a proline analogue thereof which are useful for inducing immunosuppression and treating transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphomas and hyperproliferative vascular disorders.

L'invention porte sur des dérivés substitués en position C-22 de la rapamycine, de formule (Ia) ou (Ib), ou un de leurs sels pharmacocompatibles, ou une proline analogue, ou un sel pharmacocompatible de ladite proline. Ces produits se sont avérés utiles comme inducteurs d'immunosuppression et dans le traitement du rejet des transplants, des rejets de greffons, des affections autoimmumes, des maladies inflammatoires, des tumeurs nodulaires, des mycoses, des leucémies/lymphomes à cellules T de l'adulte, et de l'hyperprolifération vasculaire.

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