Depsipeptide and congeners thereof for use as...

C - Chemistry – Metallurgy – 07 – K

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C07K 11/00 (2006.01) A61K 38/15 (2006.01) C07K 5/10 (2006.01) C07K 5/103 (2006.01) C07K 7/56 (2006.01) C07K 11/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2393682

\ Depsipeptides and congeners thereof are disclosed hav- ing structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for ex- ample, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoim- mune or immune system-related diseases including graft-versus-host dis- ease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.

L'invention concerne des depsipeptides et leurs congénères ayant la structure (I) dans laquelle <i>m</i>, <i>n</i>, <i>p</i>, <i>q</i>, X, R1, R2 et R3 ont la notation ci-définie. Ces composés, notamment FR901228, présentent une activité, par exemple, en tant qu'immunodépresseurs, et également dans la prévention ou le traitement de patients souffrant ou présentant un risque de souffrir de maladies inflammatoires, auto-immunes ou liées au système immun notamment une maladie du greffon contre l'hôte et l'amélioration de la survie du greffon/des tissus après transplantation. L'invention concerne également des méthodes d'inhibition de l'activation, la prolifération des lymphocytes, et/ou de suppression des sécrétions d'IL-2.

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