Back to results
US 2023/0147285 A1Published application
Allosteric chromenone inhibitors of phosphoinositide 3-kinase (pi3k) for the treatment of disease
AssigneePetra Pharma Corporation
InventorsEdward A. KESICKI, Eugene R HICKEY
Life of this patent
Estimating the term…
Abstract
The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I): or pharmaceutically acceptable salts thereof wherein R, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein. The disclosure also relates to methods of making and using compounds of Formula (I) or pharmaceutically acceptable salts thereof.
Claims35
A compound of the Formula:
- or pharmaceutically acceptable salt thereof, wherein:
- R is —H or C1-C3 alkyl;
- is a group of the formula:
- R2 is a cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl, each optionally substituted with one to three R10 substituents, or R2 is a group of the formula:
- R3 is —H, halogen, —CN, C1-C6 alkyl C1-C6 haloalkyl, C3-C5 cycloalkyl, a heterocycle of 3 to 5 ring atoms containing 1, 2, or 3 ring heteroatoms independently selected from N, O, or S, or a heteroaryl of 5 ring atoms containing 1, 2, or 3 ring heteroatoms independently selected from N, O, or S;
- each of R4, R5 and R6 is independently —H, halogen, C1-C6 alkyl or C1-C6 haloalkyl;
- R7 is —CN, C1-C6 alkyl or C1-C6 haloalkyl;
- R8 is —H or C1-C6 alkyl;
- each R9 is independently —H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, or C3-C5 cycloalkyl;
- each R10 is independently —H, —CN, halogen, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, —SO2R11, —CONR11R11, —NR11R11, —NR11—CO2R11, —OH, an optionally substituted C1-C6 alkyl, an optionally substituted C2-C6 alkenyl, an optionally substituted C2-C6 alkynyl, an optionally substituted C3-C5 cycloalkyl, an optionally substituted heterocycle selected from pyrrolidine, pyrrolidinone, piperidine or morpholine, an optionally substituted phenyl, an optionally substituted 1,3-benzodioxole, an optionally substituted 2,3-dihydro-1,4-benzodioxine or an optionally substituted heteroaryl selected from pyrazole, isoxazole, isothiazole, imidazole, oxazole, or thiazole;
- wherein the optionally substituted C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl is each optionally substituted with a —CN, —OH, oxetanyl, or C1-C3 alkoxy;
- the optionally substituted C3-C5 cycloalkyl, phenyl, 1,3-benzodioxole, 2,3-dihydro-1,4-benzodioxine, heterocycle or heteroaryl is each optionally substituted with one to three substituents each independently selected from halogen, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, —SO2R11, —NR11R11, —OH or —CN;
- and
- each R11 is independently —H or C1-C3 alkyl.
11 more elements
(canceled)
(canceled)
-13. (canceled)
(canceled)
(canceled)
(canceled)
-46. (canceled)
Dependencies are inferred from the claim text.