4-substituted beta-carbolines as immunomodulators

Details 4-substituted beta-carbolines as immunomodulators 4-substituted beta-carbolines as immunomodulators

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/437 (2006.01) A61K 31/444 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) A61K 31/695 (2006.01) C07D 491/048 (2006.01) C07D 495/04 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2262796

This invention relates to 4-substituted .beta.-carbolines and .beta.-carboline analogs that inhibit Ca+2 influx and interleukin-2 (IL-2) production. The 4-substituted .beta.-carbolines and .beta.-carboline analogs of this invention are represented by formula (I) wherein Q, n, R, R', R" and R1-R4 are as defined herein. This invention also relates to methods for producing .beta.- carbolines. Because of their selective immunomodulating properties, the compounds and pharmaceutical compositions of this invention are particularly well suited for preventing and treating immune disorders, including autoimmune disease, inflammatory disease, organ transplant rejection and other disorders associated with IL-2 mediated immune response.

L'invention porte sur des beta -carbolines substituées en position 4 et des analogues de beta -carbolines inhibant l'influx de Ca<+2> et la production d'interleukine-2 (IL-2). Les beta -carbolines substituées en position 4 et les analogues de beta -carbolines objets de l'invention sont représentés par la formule (I) dans laquelle Q, n, R, R', R'' et R1-R4 sont tels que définis dans la description. L'invention porte également sur des procédés de production des beta -carbolines. En raison de leurs propriétés immunomodulatrices, les composés et préparations pharmaceutiques de l'invention sont particulièrement bien adaptés à la prévention et au traitement de troubles du système immunitaire, dont les maladies auto-immunes, les maladies inflammatoires, le rejet des organes transplantés, et autres troubles associés à la réponse immunitaire induite par l'IL-2.

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