Preparation of tricyclic compounds for the treatment of immunological and oncological conditions.

Abstract

Title compds. I [T = N or CR3; U = N or CR4; V = N or CR5; R1 = H, (un)substituted alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl; R2 = H, (un)substituted cycloalkyl, heterocyclyl, aryl, heteroaryl, etc.; R3, R4 and R5 = independently H, Br, Cl, F, (un)substituted alkyl, etc.; R6 = H or NHRb; Rb = H, (un)substituted alkyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl; R7 = H, (CH2)nP(O)(OH)(OH), (CH2)nOP(O)(OH)(OH), (CH2)nP(O)(OH)(H) or CH=CHP(O)(OH)(OH); n = 0-2], and their pharmaceutically acceptable salts, pro-drugs or biol. active metabolites, are prepd. as kinase inhibitors. Thus, e.g., compd. II was prepd. by Suzuki coupling reaction of 3-bromo-7H-imidazo[1,2-c]pyrrolo[3,2-e]pyrimidine (prepn. given) with 2-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]propan-2-ol (prepn. given) under microwave condition. Compd. II exhibited inhibitory activity against Syk kinase with IC50 value in the range of 0.1 to 1.0 μM. The invention compds. are useful for the treatment of immunol. and oncol. conditions. [on SciFinder(R)]