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US 11,999,731 B2Granted
EGFR dimer disruptors and use of the same
AssigneeThe Regents of the University of Michigan
InventorsMukesh K. Nyati, Theodore S. Lawrence, Christopher Whitehead, Jason Christopher Rech, Brennan Taylor Watch
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Abstract
Provided herein are compounds that modulate EGFR and methods of using the same, for example to treat cancer.
Claims20
A compound, or pharmaceutically acceptable salt thereof, having the structure of Formula I:
- wherein
- X is S—C0-6alkylene, and said alkylene is optionally substituted with 1-3 groups independently selected from halo, N(R3)2, and OR3;
- Y is null;
- A is C6-10 aryl optionally substituted with 1 to 3 R4;
- B is 5-10 membered heteroaryl having 1-4 heteroatoms selected from N, O, and S, and said heteroaryl is optionally substituted with 1 to 3 R5;
- R1 and R2 together with the carbon atom to which they are attached form a 6 membered heterocycloalkyl ring, wherein the heterocycloalkyl ring has 1 or 2 ring heteroatoms selected from O, S, and N, and wherein said cycloalkyl ring or heterocycloalkyl ring is optionally substituted with 1-2 R6;
- each R3 is independently H or C1-6 alkyl;
- each R4 and R5 is independently C1-6 alkyl, C1-6 haloalkyl, halo, or C1-6 alkoxy;
- and
- R6 is C1-6 alkyl, C1-6 haloalkyl, (C═O)R3, (C═O)OR3, CON(R3)2, C0-3alkylene-C3-8cycloalkyl, C0-3alkylene-C6-10aryl, or C0-3alkylene-(5-10 membered heteroaryl having 1-4 heteroatoms selected from N, O, and S), wherein the aryl or heteroaryl is optionally substituted with 1 to 3 R5.
7 more elements
A compound which is compound 8C:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.