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US 10,023,588 B2Granted
Compositions and methods for treating cancer
AssigneeThe Regents of the University of California
InventorsJonathan Ostrem, Ulf Peters, Kevan M. Shokat
Life of this patent
Estimating the term…
Abstract
K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
Claims17
A compound of Formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- e5 is an integer from 0 to 5;
- X′ is —O—, —NH—, or —S—;
- R2A and R2B are independently hydrogen or unsubstituted alkyl;
- R3 is independently oxo, halogen, —CX3, —CN, SO2Cl, —SOnR10, —SOvNR7R8, —NHNH2, —ONR7R8, —NHC═(O)NHNH2, —NHC═(O)NR7R8, —N(O)m, —NR7R8, —C(O)R9, —C(O)—OR9, —C(O)NR7R8, —OR10, —NR7SO2R10, —NR7C═(O)R9, —NR7C(O)—OR9, —NR7OR9, —OCX3, —OCHX2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- L2 is unsubstituted piperazino or unsubstituted piperidino;
- L3 is a bond;
- E is an unsubstituted vinyl sulfone moiety, substituted or unsubstituted vinyl sulfonamide moiety, substituted or unsubstituted peroxide moiety, substituted or unsubstituted fluoro(C1-C4)alkylketone moiety, substituted or unsubstituted chloro(C1-C4)alkylketone moiety, substituted or unsubstituted acrylamide moiety, substituted or unsubstituted disulfide moiety, substituted or unsubstituted thiol moiety, substituted or unsubstituted phosphonate moiety, unsubstituted aldehyde moiety, substituted or unsubstituted enone moiety, substituted or unsubstituted diazomethylketone moiety, substituted or unsubstituted diazomethylamide moiety, substituted or unsubstituted cyanocyclopropyl carboxamide moiety, substituted or unsubstituted epoxide moiety, substituted or unsubstituted epoxyketone moiety, substituted or unsubstituted epoxyamide moiety, substituted or unsubstituted aryl aldehyde moiety, substituted or unsubstituted aryl dialdehyde moiety, substituted or unsubstituted dialdehyde moiety, substituted or unsubstituted nitrogen mustard moiety, substituted or unsubstituted propargyl moiety, substituted or unsubstituted propargylamide moiety,
- R7, R8, R9, and R10 are independently hydrogen, halogen, —CF3, —CN, —OH, —NH2, —COOH, —CONH2, —NO2, —SH, —SO2Cl, —SO3H, —SO4H, —SO2NH2, ——NHNH2, —ONH2, —NHC═(O)NHNH2, —NHC═(O) NH2, —NHSO2H, —NHC═(O)H, —NHC(O)—OH, —NHOH, —OCF3, —OCHF2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 independently hydrogen, methyl, ethyl, —CN, or —NO2;
- m is 1 or 2;
- v is 1 or 2;
- n is an integer from 0 to 4;
- and
- X is —Cl, —Br, —I, or —F.
12 more elements
Dependencies are inferred from the claim text.