| 摘要 |
The present application provides the compounds of formula (J),;;or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m′, A′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms. |
| 主权项 |
1. A compound having the structure of formula (I): wherein: X, Y and Z are independently selected from C(R′) or N, wherein at least one of X, Y, and Z is C(R′); n is 0, 1, 2, 3, or 4; m′ is 0 or 1; A is a single bond or C(O); each R′ is independently selected from hydrogen, halo, optionally substituted alkyl, optionally substituted haloalkyl, and optionally substituted cycloalkyl; each R1 is independently selected from halo, cyano, optionally substituted C1-6 alkyl, optionally substituted C1-6 alkoxy, hydroxy, optionally substituted C3-8 cycloalkyl, and optionally substituted sulfonyl; each R2 is independently selected from halo, optionally substituted C1-6 alkyl, optionally substituted C1-6 haloalkyl, and optionally substituted C3-8 cycloalkyl; R3 is hydrogen, optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, or optionally substituted C6-10 aryl; R4 is a six- to twelve-membered heteroaryl having at least two heteroatoms, wherein each heteroatom is independently selected from N, O, or S, wherein the heteroaryl is optionally substituted with one, two, or three members independently selected from halo, cyano, —NH2, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkynyl; and R5 is hydrogen or optionally substituted C1-6 alkyl; R5 and R3 together with the atoms to which they are attached optionally form a four- to eight-membered heterocyclic ring; or a pharmaceutically acceptable salt, isomer, or a mixture thereof. |
