Pyrrole[2,3-b]pyridine derivatives as tyro3 inhibitors
AssigneeHalia Therapeutics, Inc.
InventorsDavid James BEARSS, John Sai Keong KAUWE, III, Alexis Henri Abel MOLLARD
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Abstract
Compounds having activity as inhibitors of Tyro3 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer, tautomer, or prodrug thereof, wherein X, Y, R1, R2a, R3a, R3b, and n are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds, and methods to modulate the activity of Tyro3 are also provided.
Claims64
A compound having the following Structure (I):
- or a pharmaceutically acceptable salt, stereoisomer, tautomer, or prodrug thereof, wherein:
- X is CH or N;
- Y is CR2b or N;
- R1 is hydrogen, halo, or C1-C6 alkyl;
- R2a is hydrogen, halo, or C1-C6 haloalkyl;
- R2b is hydrogen, C1-C6 haloalkyl, or C1-C4 alkoxy;
- R3a is C1-C6 alkyl, C3-C8 cycloalkyl, heterocyclyl, or heterocyclylalkyl;
- R3b is C1-C6 alkyl, halo, C1-C4 alkoxy, or heterocyclylalkyl;
- and
- n is 0, 1, or 2
- provided that:
- when R2b is methoxy, then X is N.
A method for inhibiting a Tyro3-mediated disease or disorder, the method comprising administering a therapeutically effective amount of a compound having the following Structure (II):
- or a pharmaceutically acceptable salt, stereoisomer, tautomer, or prodrug thereof, wherein:
- X is CH or N;
- Y is is CR2b or N;
- R1 is hydrogen, halo, or C1-C6 alkyl;
- R2a is hydrogen, halo, or C1-C6 haloalkyl;
- R2b is hydrogen, C1-C6 haloalkyl, or C1-C4 alkoxy;
- R3a is C1-C6 alkyl, C3-C8 cycloalkyl, heterocyclyl, or heterocyclylalkyl;
- R3b is C1-C6 alkyl, halo, C1-C4 alkoxy, or heterocyclylalkyl;
- and
- n is 0, 1, or 2.
Dependencies are inferred from the claim text.