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US 2023/0052528 A1Published application
Taspase1 inhibitors and uses thereof
AssigneesThe Regents of the University of California, Washington University in St. Louis, Vanderbilt University, SRI International, The United States of America, as represented by the Secretary, Department of Health and Human Servic
InventorsMichelle R. Arkin, R. Jeffrey Neitz, Adam R. Renslo, James Hsieh, Shubhankar Dutta, Clifford Bryant, William J. Moore, Alex G. Waterson, Lidia Sambucetti, Somnath Jana, lan M. Romaine, Alexander P. Lamers, Yassir Younis Adam, Claire Repellin
Life of this patent
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Abstract
Disclosed herein, inter alia, are compounds and methods for inhibiting Taspase1 and the treatment of cancer.
Claims34
A compound having the formula:
- R1 is independently halogen, —CX13, —CHX12, —CH2X1, —OCX13, —OCH2X1, —OCHX12, —CN, —SOn1R1D, —SOv1NR1AR1B, —NR1CNR1AR1B, —ONR1AR1B, —NHC(O)NR1CNR1B, —NHC(O)NR1AR1BN(O)m1, —NR1AR1B, —C(O)R1C, —C(O)—OR1C, —C(O) NR1AR1B, —OR1D, —NR1ASO2R1D, —NR1AC(O)R1C, —NR1AC(O)OR1C, —NR1AOR1C, —SF5, —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;
- L2 is substituted or unsubstituted alkylene;
- 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, —SF5, —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 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;
- R3 is independently —CN,
- wherein R16 is independently hydrogen, halogen, —CX163, —CHX162, —CH2X16, —CN, —SOn16R16A—SOv16NR16AR16B, —NHNR16AR16B, —ONR16AR16B, —NHC(O)NHNR16AR16B, —NHC(O)NR16AR16B, —N(O)m16, —NR16AR16B, —C(O)R16A, —C(O)—OR16A, —C(O)NR16AR16B, —OR16A, —NR16ASO2R16B, —NR16AC(O)R16B, —NR16AC(O)OR16B, —NR16AOR16B, —OCX163, —OCHX162, —OCH2X16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl;
- R17 is independently hydrogen,
- halogen, —CX173, —CHX172, —CH2X17, —CN, —SOn17R17A, —SOv17NR17AR17B, —NHNR17AR17B, —ONR17AR17B, —NHC(O)NHNR17AR17B,
- —NHC(O)NR17AR17B, —N(O)m17, —NR17AR17B, —C(O)R17A, —C(O)—OR17A, —C(O)NR17AR17B, —OR17A, —NR17ASO2R17B, —NR17AC(O)R17B, —NR17AC(O)OR17B, —NR17AOR17B, —OCX173, —OCHX172, —OCH2X17, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl;
- R18 is independently hydrogen,
- halogen, —CX183, —CHX182, —CH2X18, —CN, —SOn18R18A, —SOv18NR18AR18B, —NHNR18AR18B, —ONR18AR18B, —NHC(O)NHNR18AR18B,
- —NHC(O)NR18AR18B, —N(O)m18, —NR18AR18B, —C(O)R18A, —C(O)—OR18A, —C(O)NR18AR18B, —OR18A, —NR18ASO2R18B, —NR18AC(O)R18B, —NR18AC(O)OR18B—NR18AOR18B, —OCX183, —OCHX182, —OCH2X18, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl;
- R19 is independently hydrogen,
- halogen, —CX193, —CHX192, —CH2X19, —CN, —SOn19R19A, —SOv19NR19AR19B, —NHNR19AR19B, —ONR19AR19B, —NHC(O)NHNR19AR19B,
- —NHC(O)NR19AR19B, —N(O)m19, —NR19AR19B, —C(O)R19A, —C(O)—OR19A, —C(O)NR19AR19B, —OR19A, —NR19ASO2R19B, —NR19AC(O)R19B, —NR19AC(O)OR19B, —NR19AOR19B, —OCX193, —OCHX192, —OCH2X19, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl;
- R1A, R1B, R1C, R1D, R2A, R2B, R2C, R2D, R16A, R16B, R17A, R17B, R18A, R18B, R19A, and R19B are independently hydrogen, —CX3, —CHX2, —CH2X, —CN, —OH, —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;
- 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;
- R16A and R16B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R17A and R17B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R18A and R18B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- R19A and R19B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- X, X1, X2, X16, X17, X18, and X19 are independently —F, —Cl, —Br, or —I;
- n1, n2, n16, n17, n18, and n19 are independently an integer from 0 to 4;
- m1, m2, m16, m17, m18, m19, v1, v2, v16, v17, v18, and v19 are independently 1 or 2;
- z1 is an integer from 0 to 5;
- and
- z2 is an integer from 0 to 8.
26 more elements
Dependencies are inferred from the claim text.