The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.本申請案提供新穎經取代之喹唑啉及吡啶并-嘧啶化合物及其醫藥學上可接受之鹽、前藥及溶劑合物。亦提供製備此等化合物之方法。此等化合物適用於藉由向患者投與治療有效量之一或多種化合物來共調控PI3K及/或mTOR活性。藉由此舉,此等化合物有效治療與PI3K/AKT/mTOR路徑之調控異常相關之病狀。有利的是,此等化合物充當雙重PI3K/mTOR抑制劑。多種病狀可使用此等化合物加以治療且包括特徵在於發炎或異常細胞增殖之疾病。在一個實施例中,疾病為癌症。