Granted Patent B2

US 12,534,479 · App. 18/015,381 · Granted Jan 27, 2026

Inventors: Ning Xi (Beijing, CN); Shimin Xu (Beijing, CN); Tingjin Wang (Beijing, CN)

Assignee: Findcure Biosciences (Zhongshan) Co., Ltd.

C07D519/00A61K45/06

Abstract

Claims (25)

1 . A compound that has the structure of Formula (II) or (IIa):

or its stereoisomer, tautomer, nitrogen oxide, solvate, or pharmaceutically acceptable salt;

wherein:

U 1 is —CH—, and U 2 is —N—, or —CH—;

R 5 is —NH 2 ;

each of R 6 and R 7 is independently H, or D;

R 8 is F, Cl, or Br;

R 13 is —OH;

n is 0 or 1;

X 1 is —(CH 2 ) t1 — or —X 2 —(CH 2 ) t1 —, wherein t1 in —(CH 2 ) t1 — is 1 or 2, and t1 in —X 2 —(CH 2 ) t1 — is 1;

X 2 is O, or S;

m is 0, or 1;

R 1 is phenyl, pyridyl, pyridazinyl, pyrazinyl, pyrimidinyl, or pyrazolyl, wherein each of phenyl, pyridyl, pyridazinyl, pyrazinyl, pyrimidinyl, and pyrazolyl is optionally substituted with 0, or 1 substituents selected from R 11 ;

R 11 is F, C 1-6 alkyl, or C 1-6 alkoxy;

R 4 is

 wherein, Y 2 is —CH 2 —, or —N(R 11b )—;

R 11a is D, or —OH;

R 11b is H, —C(═O)C 1-4 alkyl, —C(═O)C 1-4 haloalkyl, —C(═O)C 1-4 hydroxyalkyl, —C(═O)C 3-6 cycloalkyl, or —C(═O)O—C 1-4 alkyl; and

n1 is 0, 1, or 2.

2 . The compound of claim 1 , wherein:

R 4 is

wherein, R 11b is H, Boc-, CH 3 CH 2 CH 2 C(═O)—, CH 3 (CH 3 )CHC(═O)—, t-Bu-C(═O)—, n-Bu-C(═O)—, i-Bu-C(═O)—, s-Bu-C(═O)—, CH 3 (CH 3 ) CFC(═O)—, CH 3 (CH 3 )C(OH)C(═O)—, cyclopropyl-C(═O)—, cyclobutyl-C(═O)—, or cyclopentyl-C(═O)—.

3 . The compound of claim 1 of one of the following structures:

or its stereoisomer, tautomer, nitrogen oxide, solvate, or pharmaceutically acceptable salt.

4 . A pharmaceutical composition comprising a compound of claim 1 or a stereoisomer, tautomer, nitrogen oxide, solvate, or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, diluent, carrier, or a combination thereof.

Assignments (2)

Priority Claims (1)

Continuity (1)

References Cited (21)