US 12,459,939 B2
Acylaminopyrrolo-pyridone compound, preparation method therefor and use thereof
Huixin Wan, Nantong (CN); Jianfeng Pan, Nantong (CN); and Jingui Ma, Nantong (CN)
Assigned to SHANGHAI RINGENE BIOPHARMA CO., LTD., Shanghai (CN)
Appl. No. 17/440,040
Filed by SHANGHAI RINGENE BIOPHARMA CO., LTD., Shanghai (CN)
PCT Filed Mar. 12, 2020, PCT No. PCT/CN2020/078963
§ 371(c)(1), (2) Date Sep. 16, 2021,
PCT Pub. No. WO2020/187123, PCT Pub. Date Sep. 24, 2020.
Claims priority of application No. 201910200772.2 (CN), filed on Mar. 17, 2019; and application No. 201911073573.6 (CN), filed on Nov. 6, 2019.
Prior Publication US 2022/0185808 A1, Jun. 16, 2022
Int. Cl. C07D 471/04 (2006.01); A61P 35/00 (2006.01); A61P 35/02 (2006.01)
CPC C07D 471/04 (2013.01) [A61P 35/00 (2018.01); A61P 35/02 (2018.01)] 14 Claims
 
1. An acylaminopyrrolo-pyridone compound represented by general formula I, or a pharmaceutically acceptable salt thereof, or an enantiomer, a diastereomer, or a tautomer thereof,

OG Complex Work Unit Chemistry
wherein:
R1 is C1-C8 alkyl, 3-8 membered cycloalkyl, C1-C8 alkyl substituted by 3-8 membered cycloalkyl, or

OG Complex Work Unit Chemistry
the C1-C8 alkyl, 3-8 membered cycloalkyl, C1-C8 alkyl substituted by 3-8 membered cycloalkyl, and

OG Complex Work Unit Chemistry
are optionally substituted by one or more substituents, the substituents are independently selected from halogen, cyano, hydroxyl, ═O, C1-C6 alkyl, C1-C6 alkyl-O—, and C1-C6 alkyl-(SO2)—; when there are multiple substituents, they are the same or different;
L1 is —(C1-C8 alkyl)-, —(C2-C6 alkynyl)-, or —(C1-C6 alkyl)-(CH2OCH2)m1—(C1-C6 alkyl)-;
m1 is 1, 2, 3 or 4;
L2 is a connecting bond,

OG Complex Work Unit Chemistry
W is —CH2— or —C(O)—;
R2 is hydrogen;
X1 is CH; X2 is NH;
R3 and R5 are hydrogen;
R4 is

OG Complex Work Unit Chemistry
R6 and R7 are independently selected from hydrogen or -L-R10;
L is —O—;
R10 is independently selected from C1-C6 alkyl, 6-10 membered aryl, or 6-10 membered aryl substituted by one or more substituents; the substituents in the 6-10 membered aryl substituted by one or more substituents are independently halogen or C1-C6 alkyl; when there are multiple substituents, they are the same or different;
or, R4 is C1-C6 alkylsulfone or C1-C6 alkylsulfoxide, R6 and R7 form a 6-membered heterocycloalkyl or a 6-membered heterocycloalkyl substituted by one or more substituents, the heteroatoms in the 6-membered heterocycloalkyl are selected from N and O, and the number of the heteroatoms is 2; the substituent is independently C1-C6 alkyl or ═O; when the substituents are multiple, they are the same or different.