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US 12,435,030 B2Granted
PCNA inhibitors
AssigneeCity of Hope
InventorsLinda H. Malkas, David Horne, Robert J. Hickey, Long Gu
Life of this patent
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Abstract
Described herein, inter alia, are compositions of PCNA modulators and methods for treating or preventing cancer.
Claims20
A pharmaceutical composition comprising a compound, an anti-cancer agent, and a pharmaceutically acceptable excipient, wherein the anti-cancer agent is a platinum-based compound, topoisomerase inhibitor, EGFR inhibitor, ras inhibitor, MEK inhibitor, signal transduction inhibitor, or signal transduction modulator;
- and
- wherein the compound has the formula:
- or a pharmaceutically acceptable salt thereof;
- wherein
- Ring A is substituted or unsubstituted phenyl or substituted or unsubstituted 5 to 6 membered heteroaryl;
- Ring B is substituted or unsubstituted 1-naphthyl, or substituted or unsubstituted isoquinolinyl;
- R1 is independently a halogen, —CX13, —CHX12, —CH2X1, —CN, —SOn1R10, —SOv1NR7R8, —NHNH2, —ONR7R8, —NHC═(O)NHNH2, —NHC═(O)NR7R8, —N(O)m1, —NR7R8, —C(O)R9, —C(O)—OR9, —C(O)NR7R8, —OR10, —NR7SO2R10, —NR7C═(O)R9, —NR7C(O)—OR9, —NR7OR9, —OCX13, —OCHX12, —OCH2X1, 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;
- or two adjacent R1 substituents may optionally be joined to form a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R2 is independently hydrogen, halogen, —CX23, —CHX22, —CH2X2, —CN, —COOH, —CONH2, 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;
- R3 is independently hydrogen, halogen, —CX33, —CHX32, —CH2X3, —CN, —COOH, —CONH2, 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;
- R7, R8, R9, and R10 are independently hydrogen, halogen, —CXA3, —CHXA2, —CH2XA, —CN, —COOH, —CONH2, 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;
- or R7 and R8 substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- z1 is an integer from 0 to 4;
- m1 and v1 are independently 1 or 2;
- n1 is independently an integer from 0 to 4;
- and
- X1, X2, X3, and XA are independently —Cl, —Br, —I, or —F.
14 more elements
Dependencies are inferred from the claim text.