Preparation of pyrrolo[3,2-d]pyrimidine compounds and their use as PI3 kinase and mTOR kinase inhibitors for treating cancer and other diseases.

Abstract

Pyrrolo[3,2-d]pyrimidine compds., such as a compd. of the formula I (wherein R1 and R2 are independently (un)substituted C1-C6alkyl, C2-C6alkenyl, etc.; A is O, CH20, S, S(O), or S(O)2; m is 0-2; n is 1-5; R3-R5 are independently H, (un)substituted C1-C6alkyl, (un)substituted C2-C6alkenyl, etc.) or a pharmaceutically acceptable salt thereof, compns. comprising the compds., and methods for making and using the compds.as treatment for PI3K-related diseases and mTOR diseases are disclosed. A method for prepg. I is addnl. claimed. Example compd. II, prepd. by reacting the corresponding [[pyrrolo[3,2-d]pyrimidin-2-yl]phenyl]methanol intermediate with piperazine, had IC50 values of 4.3 μM, 30 nM, and 510 nM in assays measuring TOR kinase, PI3 kinase α, and PI3 kinase γ inhibition, resp. [on SciFinder(R)]