US 11,053,260 B2
Tri-cycle compound and applications thereof
Haiying He, Shanghai (CN); Jing Wang, Shanghai (CN); Zhigan Jiang, Shanghai (CN); Yaxun Yang, Shanghai (CN); Peng Shao, Shanghai (CN); Chen Zhang, Shanghai (CN); Jian Li, Shanghai (CN); and Shuhui Chen, Shanghai (CN)
Assigned to FUJIAN COSUNTER PHARMACEUTICAL CO., LTD., Ningde (CN)
Appl. No. 16/488,244
Filed by FUJIAN COSUNTER PHARMACEUTICAL CO., LTD., Fujian (CN)
PCT Filed Feb. 9, 2018, PCT No. PCT/CN2018/075995
§ 371(c)(1), (2) Date Aug. 23, 2019,
PCT Pub. No. WO2018/153285, PCT Pub. Date Aug. 30, 2018.
Claims priority of application No. 201710100309.1 (CN), filed on Feb. 23, 2017; application No. 201710648155.X (CN), filed on Aug. 1, 2017; and application No. 201810008592.X (CN), filed on Jan. 4, 2018.
Prior Publication US 2020/0247819 A1, Aug. 6, 2020
Int. Cl. C07D 513/04 (2006.01); A61P 31/12 (2006.01); C07D 519/00 (2006.01)
CPC C07D 513/04 (2013.01) [A61P 31/12 (2018.01); C07D 519/00 (2013.01)] 18 Claims
 
1. A compound of formula (I), a tautomer or stereoisomer thereof or a pharmaceutically acceptable salt thereof,

OG Complex Work Unit Chemistry
L1 is a single bond or —C1-6 alkyl-;
R1 is H, Cl, F, Br I or C1-3 alkyl which is optionally substituted by 1, 2 or 3 R;
R2 is selected from the group consisting of C1-3 heteroalkyl, 4-8 membered heterocycloalkyl, 5-10 membered heteroaryl, 4-8 membered partially unsaturated heterocycloalkyl, phenyl, C1-3 alkyl, C3-8 cycloalkyl, 4-8 membered heterocycloalkyl-O— and 5-10 membered heteroaryl-O—, each of which is optionally substituted by 1, 2 or 3 R;
R3 is H or C1-3 alkyl;
each of R is independently H, Cl, F, Br, I, NH2, OH or CN, or selected from the group consisting of C1-6 alkyl, C1-6 heteroalkyl, phenyl, phenyl-O—C(═O)— and 5-6 membered heteroaryl, each of which is optionally substituted by 1, 2 or 3 R′;
each of R′ is independently selected from the group consisting of Cl, F, Br, I, NH2, CH3, CN and N(CH3)2;
each of the “hetero” in the C1-3 heteroalkyl, 4-8 membered heterocycloalkyl, 5-10 membered heteroaryl, C1-6 heteroalkyl, 5-6 membered heteroaryl and 4-8 membered partially unsaturated heterocycloalkyl is independently selected from the group consisting of —S—, —O—, —NH—, N, —C(═O)—, —O—C(═O)—, —S(═O)2—, —S(═O)—, —NH—C(═O)— and —NH—C(═O)—O—;
in any of the above cases, the number of the heteroatom or the heteroatomic group is independently 1, 2, 3 or 4.