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US 12,195,490 B2Granted
STRAD-binding agents and uses thereof
AssigneesThe Regents of the University of California, ShangPharma Innovation Inc.
InventorsJohn Gordan, Dominique Mitchell, Richard Beresis, Marc Adler
Life of this patent
Estimating the term…
Abstract
Disclosed herein, inter alia, are compounds for binding STRAD pseudokinase and uses thereof.
Claims14
A compound having the formula:
- wherein,
- W1 is N, CH, or CR1;
- W2 is N, CH, or CR1;
- R1 is independently halogen, —CX13, —CHX12, —CH2X1, —OCX13, —OCH2X1, —OCHX12, —CN, —SOn1R1D, —SOv1NR1AR1B, —NR1CNR1AR1B, —ONR1AR1B, —NHC(O)NR1CNR1AR1B, —NHC(O)NR1AR1B, —N(O)m1, —NR1AR1B, —C(O)R1C, —C(O)—OR1C, —C(O)NR1AR1B, —OR1D, —NR1ASO2R1D, —NR1AC(O)R1C, —NR1AC(O)OR1C, —NR1AOR1C, —N3, 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;
- 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;
- z1 is an integer from 0 to 4;
- Ring B is aryl or heteroaryl;
- R2 is independently oxo, halogen, —CX23, —CHX22, —CH2X2, —OCX23, —OCH2X2, —OCHX22, —CN, —SOn2R2D, —SOv2NR2AR2B, —NR2CNR2AR2B, —ONR2AR2B, —NHC(O)NR2CNR2AR2B, —NHC(O)NR2AR2B, —N(O)m2, —NR2AR2B, —C(O)R2C, —C(O)—OR2C, —C(O)NR2AR2B, —OR2D, —NR2ASO2R2D, —NR2AC(O)R2C, —NR2AC(O)OR2C, —NR2AOR2C, —N3, 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;
- two adjacent R2 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;
- z2 is an integer from 0 to 6;
- L3 is a bond, —NH—, —O—, —C(O)—, —C(O)NH—, —NHC(O)—, —NHC(O)NH—, —C(O)O—, —OC(O)—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- R3 is —P(O)(OR3C)(OR3D), —P(O)(OR3D)(NR3AR3B), —P(O)(R3C)(OR3D), —P(O)(R3C)(R3D), —P(S)(OR3C)(OR3D), —P(S)(OR3D)(NR3AR3B), —P(S)(R3C)(OR3D), —P(S)(R3C)(R3D), —NR3ASO2R3D, —NR3CSO2NR3AR3B, —NR3AC(O)R3C, —NR3AC(O)OR3C, —SO2R3C, —SO2-L3A-R3C, —SO2NR3AR3B, —SO2NR3ASO2R3C, —SO2NR3AP(O)(OR3C)(OR3D), —SO2P(O)(OR3C)(OR3D), —SO2CH2P(O)(OR3C)(OR3D), —SO2P(O)(OR3D)(NR3AR3B), —SO2P(O)(R3C)(OR3D), —SO2P(O)(R3C)(R3D), —SO2-L3A-P(O)(OR3C)(OR3D), —SO2-L3A-P(O)(OR3D)(NR3AR3B), —SO2-L3A-P(O)(R3C)(OR3D), —SO2-L3A-P(O)(R3C)(R3D), —S(O)(NR3A)R3C, —C(O)OR3C, —C(O)NR3AR3B, —NR3AC(O)OR3C substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- L3A is —CH2—, —CH(CH3)—, —C(CH3)2—, —CH(X3A)—, or —C(X3A)2—;
- L4 is —C(O)NH— or —NHC(O)—;
- R4 and R5 are independently hydrogen, —CCl3, —CBr3, —CF3, —CI3, CHCl2, —CHBr2, —CHF2, —CHI2, —CH2Cl, —CH2Br, —CH2F, —CH2I, —CN, —OH, —NH2, —COOH, —CONH2, —OCCl3, —OCF3, —OCBr3, —OCI3, —OCHCl2, —OCHBr2, —OCHI2, —OCHF2, —OCH2Cl, —OCH2Br, —OCH2I, —OCH2F, 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;
- R4 and R5 substituents bonded to the same nitrogen may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R1A, R1B, R1C, R1D, R2A, R2B, R2C, and R2D are independently hydrogen, —CCl3, —CBr3, —CF3, —CI3, CHCl2, —CHBr2, —CHF2, —CHI2, —CH2Cl, —CH2Br, —CH2F, —CH2I, —CN, —OH, —NH2, —COOH, —CONH2, —OCCl3, —OCF3, —OCBr3, —OCI3, —OCHCl2, —OCHBr2, —OCHI2, —OCHF2, —OCH2Cl, —OCH2Br, —OCH2I, —OCH2F, 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;
- R1A and R1B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R2A and R2B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R3A, R3B, R3C, and R3D are independently hydrogen, oxo, halogen, —CCl3, —CBr3, —CF3, —CI3, —CHCl2, —CHBr2, —CHF2, —CHI2, —CH2Cl, —CH2Br, —CH2F, —CH2I, —CN, —OH, —NH2, —COOH, —CONH2, —NO2, —SH, —SO3H, —SO4H, —SO2NH2, —NHNH2, —ONH2, —NHC(O)NHNH2, —NHC(O)NH2, —NHSO2H, —NHC(O)H, —NHC(O)OH, —NHOH, —OCCl3, —OCF3, —OCBr3, —OCI3, —OCHCl2, —OCHBr2, —OCHI2, —OCHF2, —OCH2Cl, —OCH2Br, —OCH2I, —OCH2F, —N3, —SO2CH3, —NHC(O)CH3, —C(O)CH3, 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;
- R3A and R3B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R3A and R3D substituents may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- X1, X2, and X3A are independently —F, —Cl, —Br, or —I;
- n1 and n2 are independently an integer from 0 to 4;
- and
- m1, m2, v1, and v2 are independently 1 or 2;
- wherein Ring B is not pyridyl.
24 more elements
Dependencies are inferred from the claim text.