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US 2026/0217735 A1Published application
Heterocycles and uses thereof
AssigneeKumquat Biosciences Inc.
InventorsPingda Ren, Xiaohui He, Xiaoming Li, Siling Zhao, Baogen Wu
Life of this patent
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Abstract
The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic protein.
Claims20
A compound of Formula (II):
- or a pharmaceutically acceptable salt or solvate thereof, wherein:
- X1 is selected from CR6 and N;
- R4a is selected from C1-6 alkyl and C2-6 alkenyl;
- L2 is saturated, monocyclic 4- to 7-membered heterocycle, wherein the heterocycle is optionally substituted with C1-6 alkyl, and wherein —C(O)R19 is bound to L2 via a nitrogen atom, thereby forming a urea;
- R19 is selected from pyrrol-1-yl, pyrazol-1-yl, imidazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, and 1,2,4-triazol-4-yl, each of which is optionally substituted with one or two substituents independently selected from halogen, —CN, C1-6 alkyl, —O(C1-6 alkyl), and C3-6 cycloalkyl, wherein each of C1-6 alkyl, —O(C1-6 alkyl), and C3-6 cycloalkyl is optionally substituted with one, two, or three substituents independently selected from halogen, —CN, C1-6 alkyl, —O(C1-6 alkyl), and —O(C1-6 haloalkyl);
- R2 is —O(C1-3 alkyl)(4- to 10-membered heterocycle) optionally substituted with one, two, or three substituents independently selected from halogen, C1-3 alkyl, C1-3 haloalkyl, and ═C(R21)2, wherein R21 is independently selected at each occurrence from hydrogen, halogen, and C1-3 alkyl;
- R5 is hydrogen;
- R6 is selected from hydrogen, halogen, and C1-3 haloalkyl;
- R7 is selected from C6-12 aryl and 5- to 12-membered heteroaryl, each of which is substituted with one, two, three, or four substituents independently selected from halogen, —CN, —CH3, —CH2CH3, —CH═CH2, —CF3, —C═CH, —OH, —NH2, and -cyclopropyl;
- and
- R8 is fluorine.
8 more elements
A compound of the formula
- or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.