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US 10,501,466 B2Granted
WDR5 inhibitors and modulators
AssigneeVanderbilt University
InventorsStephen W. Fesik, Shaun R. Stauffer, James M. Salovich, William P. Tansey, Feng Wang, Jason Phan, Edward T. Olejniczak
Life of this patent
Estimating the term…
Abstract
Described are N-(6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl)benzamide and acetamide-containing compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.
Claims20
A compound of formula (I),
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is hydrogen or C1-4alkyl;
- R2 is hydrogen, C1-6alkyl, C3-8cycloalkyl, or C3-8cycloalkyl-C1-3alkylene-;
- X1 is a bond;
- R3 is G1 or -L1-G2;
- G1 and G2 are C3-8cycloalkyl, 4- to 8-membered heterocyclyl, aryl, or heteroaryl, wherein G1 and G2 are optionally substituted with 1-5 substituents independently selected from the group consisting of halogen, cyano, C1-4alkyl, C1-4haloalkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, OH, oxo, —C(O)C1-4alkyl, —C(O)C1-4haloalkyl, —NH2, —NH(C1-4alkyl), —N(C1-4alkyl)2, —NHC(O)C1-4alkyl, and —N(C1-4alkyl)C(O)C1-4alkyl;
- L1 is —C1-3alkylene-;
- R4a, at each occurrence, is independently hydrogen, halogen, cyano, C1-4alkyl, C1-4haloalkyl, —O—C1-4alkyl, or OH;
- R4b, at each occurrence, is independently hydrogen, halogen, or C1-4alkyl;
- or R4a and R4b together with the carbon to which they are attached form a C3-6cycloalkyl;
- n is 1 or 2;
- X2 is C(R4a)(R4b) or N(R5);
- R5 is hydrogen, C1-4alkyl, C1-4haloalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-3alkylene-, —C(O)C1-4alkyl, —C(O)C3-6cycloalkyl, or —C(O)OC1-4alkyl;
- R6a, R6b, R7a, R7b, R8a, and R8b are each hydrogen;
- and
- R9, R10, and R11 are each hydrogen.
13 more elements
Dependencies are inferred from the claim text.