Inhibitors of human phosphatidyl-inositol 3-kinase delta

Details Inhibitors of human phosphatidyl-inositol 3-kinase delta Inhibitors of human phosphatidyl-inositol 3-kinase delta

C - Chemistry, Metallurgy

07

D

C07D 473/34 (2006.01) A61K 31/52 (2006.01) C07D 473/16 (2006.01)

Patent

CA 2463294

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K.delta.) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K.delta. plays a role in leukocyte function with compounds of formula (1) are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K.delta., while not significantly inhibiting activity of other PI3K isoforms. Compounds of formula (1) are provided that inhibit PI3K.delta. activity, including compounds that selectively inhibit PI3K.delta. activity. Methods of using PI3K.delta. inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K.delta. inhibitory compounds to inhibit PI3K.delta.-mediated processes in vitro and in vivo. Wherein R1-R3, X, Y and A are defined herein.

L'invention concerne des procédés d'inhibition de l'activité d'isoformes phosphatidyl-inositol 3-kinase delta (PI3K.delta.) et des méthodes de traitement de maladies, telles que des troubles immunitaires et inflammatoires, dans lesquelles PI3K.delta. joue un rôle dans une fonction de leucocyte, au moyen de composés de formule (1). Les méthodes mettent en oeuvre, de préférence, des principes actifs inhibant de manière sélective PI3K.delta. sans inhiber de façon importante l'activité d'autres isoformes PI3K. L'invention concerne également des composés de formule (1) inhibant l'activité de PI3K.delta., notamment des composés inhibant de manière sélective l'activité de PI3K.delta.. L'invention concerne en outre des procédés d'utilisation des composés inhibant PI3K.delta., aux fins d'inhibition de croissance ou prolifération cellulaire cancéreuse. L'invention concerne, par conséquent, des procédés d'utilisation des composés PI3K.delta., aux fins d'inhibition de processus induits par PI3K.delta. <i>in vitro</i> et <i>in vivo<. Dans la formule 1, R1-R3, X, Y et A sont tels que définis dans la description.

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