US 12,410,136 B2
Pyridinyl morpholine compound, preparation method therefor, and application thereof
Jianqi Li, Shanghai (CN); Yangli Qi, Shanghai (CN); Xiaowen Chen, Shanghai (CN); Junwei Xu, Shanghai (CN); Ruixiang Yuan, Shanghai (CN); and Qiang Pu, Shanghai (CN)
Assigned to SHANGHAI ZHONGZE THERAPEUTICS, CO. LTD., Shanghai (CN); and SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, Shanghai (CN)
Appl. No. 18/007,840
Filed by SHANGHAI ZHONGZE THERAPEUTICS, CO. LTD., Shanghai (CN); and SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, Shanghai (CN)
PCT Filed May 28, 2021, PCT No. PCT/CN2021/096683
§ 371(c)(1), (2) Date Dec. 2, 2022,
PCT Pub. No. WO2021/244416, PCT Pub. Date Dec. 9, 2021.
Claims priority of application No. 202010506972.3 (CN), filed on Jun. 5, 2020.
Prior Publication US 2023/0242486 A1, Aug. 3, 2023
Int. Cl. C07D 213/74 (2006.01); C07D 213/87 (2006.01); C07D 401/04 (2006.01); C07D 405/04 (2006.01); C07D 405/12 (2006.01); C07D 405/14 (2006.01); C07D 409/04 (2006.01); C07D 409/14 (2006.01)
CPC C07D 213/74 (2013.01) [C07D 213/87 (2013.01); C07D 401/04 (2013.01); C07D 405/04 (2013.01); C07D 405/12 (2013.01); C07D 405/14 (2013.01); C07D 409/04 (2013.01); C07D 409/14 (2013.01)] 18 Claims
 
1. A pyridinyl morpholine compound represented by formula I, a pharmaceutically acceptable salt thereof, or a hydrate of the pharmaceutically acceptable salt thereof:

OG Complex Work Unit Chemistry
wherein, R1 is

OG Complex Work Unit Chemistry
R3 is C1-C3 alkyl, “C1-C3 alkyl substituted by one C1-C3 alkoxy”, C3-C6 cycloalkyl, phenyl, “5- to 6-membered heteroaryl with 1 to 2 heteroatoms selected from one or more of N, O and S”, “5- to 6-membered heterocycloalkyl with one heteroatom of N, and 0 or 1 heteroatom selected from N, O and S”, or, “5- to 6-membered heterocycloalkyl with one heteroatom of N, and 0 or 1 heteroatom selected from N, O and S” substituted by one C1-C3 alkyl; the heterocycloalkyl is connected to the carbonyl in R1 by N atom;
R4 and R5 are independently hydrogen or C1-C3 alkyl;
R2 is phenyl, “5- to 6-membered heteroaryl with 1 to 2 heteroatoms selected from one or more of N, O and S”, or, phenyl substituted by one or more R2-1;
R2-1 is independently C1-C3 alkoxy or halogen.