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US 11,597,727 B2Granted
Inhibitors of integrin alpha 2 beta 1 and methods of use
AssigneeThe Regents of the University of California
InventorsDean Sheppard, Aparna Sundaram, William F. DeGrado, Hyunil Jo
Life of this patent
Estimating the term…
Abstract
Disclosed herein, inter alia, are inhibitors of integrin alpha 2 beta 1 and methods of using the same.
Claims27
A compound having the formula:
- wherein,
- R1 is substituted or unsubstituted alkyl, unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- L1 is a bond or —C(O)—;
- R2 is hydrogen or substituted or unsubstituted alkyl;
- R3 is hydrogen, halogen, —CX33, —CHX32, —CH2X3, —OCX33, —OCH2X3, —OCHX32, —CN, —SOn3R3D, —SOv3NR3AR3B, —NHC(O)NR3AR3B, —N(O)m3, —NR3AR3B, —C(O)R3C, —C(O)—OR3C, —C(O)NR3AR3B, —OR3D, —NR3ASO2R3D, —NR3AC(O)R3C, —NR3AC(O)OR3C, —NR3AOR3C, 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 —OR3 is a prodrug moiety;
- R4 is hydrogen or substituted or unsubstituted alkyl;
- W1 is O, S, NR8;
- W2 is O, S, NR5;
- R5 is hydrogen;
- L2 is a bond or —C(R6)2—;
- R6 is independently hydrogen, ═NH, substituted or unsubstituted alkyl, or substituted or unsubstituted heteroalkyl;
- W1 and R6 may optionally be joined to form a substituted or unsubstituted 5 to 6 membered heterocycloalkyl, or substituted or unsubstituted 5 to 6 membered heteroaryl;
- R7 is hydrogen, halogen, —CX73, —CHX72, —CH2X7, —OCX73, —OCH2X7, —OCHX72, —CN, —SOn7R7D, SOv7NR7AR7B, —NHC(O)NR7AR7B, —N(O)m7, —NR7AR7B, —C(O)R7C, —C(O)—OR7C, —C(O)NR7AR7B, —OR7D, NR7AC(O)OR7C, —NR7AOR7C, substituted or unsubstituted 2,3-dihydro-1H-indenyl, substituted or unsubstituted bridged monocyclic cycloalkyl, substituted or unsubstituted bridged bicyclic cycloalkyl, substituted or unsubstituted spirocyclic bicyclic cycloalkyl, or substituted or unsubstituted heteroaryl;
- R8 is hydrogen or substituted or unsubstituted alkyl;
- R3A, R3B, R3C, R3D, R7A, R7B, R7C, and R7D are independently hydrogen, —CX3, —CN, —COOH, —CONH2, —CHX2, —CH2X, 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;
- R7A and R7B substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
- each X, X3, and X7 are independently —F, —Cl, —Br, or —I;
- n3 and n7 are independently an integer from 0 to 3;
- and
- m3, m7, v3 and v7 are independently 1 or 2.
19 more elements
Dependencies are inferred from the claim text.