| 摘要 |
The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I),;
or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ. |
| 主权项 |
1. A compound having the structure of formula (II):or a pharmaceutically acceptable salt thereof, wherein:
R1 is unsubstituted C6-12 aryl; C6-12 aryl substituted with 1 or 2 substituents independently selected from the group consisting of halo, —OR1b, —C(O)R1b and C1-6 alkyl substituted with OH, wherein R1b is C1-6 alkyl or C1-6 haloalky; unsubstituted C3-12 heteroaryl with 1 or 2 heteroatoms independently selected from the group consisting of nitrogen, oxygen, and sulfur; C3-12 heteroaryl with 1 or 2 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur, and substituted with 1 or 2 substituents independently selected from the group consisting of halo, —OR1c, —C(O)OR1c, —C(O)R1c, NH2, C1-6 haloalkyl, C1-6 alkyl, and C1-6 alkyl substituted with OH or NH2, wherein R1c is H, C1-6 alkyl, C1-6 haloalkyl, NH2, or —O(C1-6 alkyl); unsubstituted C3-12 cycloalkyl; unsubstituted C1-6 alkyl; or C1-6 alkyl substituted with OH; n is 0, 1, 2, or 3; each R2 is independently selected from the group, consisting of OH CN, C1-6 alkyl, C1-6 haloalkyl, and SO2R2a, wherein R2a is C1-6 alkyl; R3 is unsubstituted C6-12 aryl; C6-12 aryl substituted with 1 or 2 substituents independently selected from the group consisting of halo, alkyl, haloalkyl, aryl, cyano, —OR3a, —C(O)NR3aR3b, —SO2R3a, —SO2NR3aR3b, alkyl substituted with NR3aR3b, wherein R3a and R3b are independently hydrogen, C1-6 alkyl, or —SO2R3c, wherein R3c is C1-6 alkyl; unsubstituted C3-12 heteroaryl 1 or 2 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur; unsubstituted C3-12 heterocycloalkyl with 1 or 2 heteroatom independently selected from the group consisting of nitrogen, oxygen and sulfur; or C3-12 heterocycloalkyl with 1 or 2 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur, and substituted with 1 or 2 C1-6 alkyl substituents; R4 is hydrogen, C1-6 alkyl, or NH2; R5 is C1-6 alkyl substituted with OH or OR5a, wherein R5a is C1-6 alkyl; and R6 is hydrogen, or R5 together with the carbon to which it is attached and R6 together with the nitrogen to which it is attached are taken together to form a, four-, five- or six-membered heterocycle. |
