IP Library Granted Patent US 12673935
Granted Patent B2
US 12673935 · App. 18/145,601 · Granted Jul 7, 2026

Pyrimidine derivative, and preparation method therefor and use thereof

Inventors: Qiang Yu (Suzhou, CN); Juping Ding (Suzhou, CN); Mulin Tang (Suzhou, CN); Yan Hao (Suzhou, CN); Qin Lu (Suzhou, CN); Shen Qian (Suzhou, CN); Xusheng Tian (Suzhou, CN)
Assignee: CGENETECH (SUZHOU, CHINA) CO., LTD.
C07D401/14
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Quick Facts
Patent No.
US 12673935
App. No.
18/145,601
Granted
Jul 7, 2026
Kind
B2
Abstract

Provided is a pyrimidine derivative, a preparation method and a use thereof, wherein the pyrimidine derivative is selected from a compound represented by Formula (I), or a tautomer, an enantiomer, a diastereomer, a mesomer, a racemate, or a mixture thereof, or a pharmaceutically acceptable salt or prodrug thereof. The pyrimidine derivative shows an excellent CDK-inhibiting effect and action.

Claims (13)

1 . A pyrimidine derivative, wherein the pyrimidine derivative is selected from a compound represented by Formula (I), or a tautomer, an enantiomer, a diastereomer, a mesomer, a racemate, or a mixture thereof, or a pharmaceutically acceptable salt or prodrug thereof:

wherein

R 1 and R 2 are fluorine;

R 3 is hydrogen;

A is a covalent bond;

Q is a carbon atom; X is —NR 4 R 6 , wherein R 4 is hydrogen;

R 6 is methyl.

2 . A method for preparing the pyrimidine derivative according to claim 1 , wherein the method comprises:

wherein, R 1 , R 2 , R 3 , A, Q, and X have the same meanings as the corresponding groups in the pyrimidine derivative according to claim 1 ; Y is chlorine; Boc is tert-butoxycarbonyl that is an amino protecting group; TFA is trifluoroacetic acid; DCM is dichloromethane; and TFA and DCM are reagents for removing the Boc protecting group.

3 . A method for treating abnormal cell proliferative diseases in a subject, comprising a step of administrating a therapeutically effective amount of the pyrimidine derivative according to claim 1 to the subject, wherein the abnormal cell proliferative disease is leukemia.

4 . The method according to claim 3 , wherein the leukemia is selected from acute myeloblastic leukemia, chronic myelocytic leukemia, acute lymphoblastic leukemia, or chronic lymphocytic leukemia.

5 . A pharmaceutical composition, comprising the pyrimidine derivative according to claim 1 as an active ingredient and one or more pharmaceutically acceptable carriers, diluents, or excipients.

6 . The pharmaceutical composition according to claim 5 , further comprising one or more other anticancer agents as active ingredients, wherein the other anticancer agents are paclitaxel.