This led to the discovery of substituted 6-aminoheterocyclic 2, 4-bis morpholino pyrimidines (89), of which the highest soluble and the most potent compound was compound 90 (NVP-BKM120, PI3Kα IC50 ~ 30nM, mTOR IC50 ~ 4600nM) that has entered into Phase II clinical trials for the treatment of cancer. The gene discussed is MTOR; the disease is cancer.