C40-, C28-, and C-32-linked rapamycin analogs as mTOR inhibitors
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
1. A method of treating a cancer selected from the group consisting of head and neck cancers, lung cancer, liver cancer, ovarian cancer, prostate cancer, pancreatic cancers, endometrial cancer, vulva cancer, intestinal or rectal cancer, bile duct cancer, and thyroid cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of either a compound or a composition selected from the group consisting of
(1) a compound having the formula
or a stereoisomer thereof;
(2) a compound having the formula
or a tautomer thereof;
(3) a compound having the formula
or an oxepane isomer thereof;
(4) a compound having the formula
or a stereoisomer thereof;
(5) a compound having the formula
or a tautomer thereof;
(6) a compound having the formula
(7) a compound having the formula
(8) a composition comprising a mixture of
or a stereoisomer or tautomer thereof
and
or a stereoisomer or tautomer thereof; and
(9) a composition comprising a mixture of
and
2. The method of claim 1 , wherein the compound is
or a stereoisomer thereof.
3. The method of claim 1 , wherein the compound is
or a tautomer thereof.
4. The method of claim 1 , wherein the compound is
or an oxepane isomer thereof.
5. The method of claim 1 , wherein the compound is
or a stereoisomer thereof.
6. The method of claim 1 , wherein the compound is
or a tautomer thereof.
7. The method of claim 1 , wherein the compound is
8. The method of claim 1 , wherein the compound is
9. The method of claim 1 , wherein the composition comprises a mixture of
or a stereoisomer or tautomer thereof
and
or a stereoisomer or tautomer thereof.
10. The method of claim 1 , wherein the composition comprises a mixture of
and