IP Library › Granted Patent US 12661357
Granted Patent B2
US 12661357 · App. 18/261,832 · Granted Jun 23, 2026

Use of pyrido[1,2-a]pyrimidone analogue

Inventors: Yongguo Li (Shanghai, CN); Wei Wei (Shanghai, CN); Wei Ye (Shanghai, CN)
Assignees: GUANGZHOU JOYO PHARMATECH CO., LTD; SHANGHAI JIA TAN PHARMATECH CO., LTD.
A61K31/519A61K9/0053A61P35/00C12Q1/6886C12Q2600/156
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Quick Facts
Patent No.
US 12661357
App. No.
18/261,832
Granted
Jun 23, 2026
Kind
B2
Abstract

Use of a pyrido[1,2-a]pyrimidone analogue. Specifically disclosed is use of a compound I or a pharmaceutically acceptable salt thereof in the preparation of a medicament for treating and/or preventing cancers in the digestive tract system. The compound I or the pharmaceutically acceptable salt thereof has good antitumor activity against one or more of head and neck cancer, hepatocellular cancer, colorectal cancer, esophageal cancer, gastric cancer and nasopharyngeal cancer.

Claims (15)

1 . A method for treating or preventing cancers in digestive tract system, comprising administering to a patient a therapeutically effective amount of compound I or a pharmaceutically acceptable salt thereof, wherein the structure formula of the compound I is as follows:

wherein the cancer in the digestive tract system is head and neck cancer or colorectal cancer.

2 . The method according to claim 1 , wherein the cancer in the digestive tract system is wild-type or PIK3CA-mutated cancer in the digestive tract system.

3 . The method according to claim 1 , wherein the cancer in the digestive tract system is head and neck cancer.

4 . The method according to claim 3 , wherein the head and neck cancer is PIK3CA wild-type head and neck cancer or PIK3CA-mutated head and neck cancer.

5 . The method according to claim 3 , wherein the head and neck cancer is pleomorphic adenoma.

6 . The method according to claim 3 , wherein the head and neck cancer is maxillary sinus carcinoma or adenoid cystic carcinoma.

7 . The method according to claim 1 , wherein the cancer in the digestive tract system is colorectal cancer.

8 . The method according to claim 1 , wherein, the method further includes a step of detecting whether the patient carries PIK3CA gene mutation.

9 . The method according to claim 5 , wherein the head and neck cancer is malignant pleomorphic adenoma.

10 . The method according to claim 1 , wherein the administration dosage of the compound I or the pharmaceutically acceptable salt thereof is 0.1 mg per dose, 0.2 mg per dose, 0.3 mg per dose, 0.4 mg per dose, 0.5 mg per dose, 0.6 mg per dose, 0.7 mg per dose, 0.8 mg per dose, 0.9 mg per dose, 1.0 mg per dose, 1.1 mg per dose, 1.2 mg per dose, 1.3 mg per dose, 1.4 mg per dose, 1.5 mg per dose, 1.6 mg per dose, 1.7 mg per dose, 1.8 mg per dose, 1.9 mg per dose or 2.0 mg per dose.

11 . The method according to claim 1 , wherein the compound I or the pharmaceutically acceptable salt thereof is presented in an oral dosage form.

12 . The method according to claim 1 , wherein the compound I or the pharmaceutically acceptable salt thereof is presented in a tablet form.

13 . The method according to claim 1 , wherein the administration dosage of the compound I or the pharmaceutically acceptable salt thereof is 0.1-2.0 mg per dose.

14 . The method according to claim 1 , wherein the administration frequency of the compound I or the pharmaceutically acceptable salt thereof is once a day or twice a day.