IP Library Granted Patent US 11,498,930
Granted Patent B2
US 11,498,930 · App. 16/969,392 · Granted Nov 15, 2022

Pyrimidine-fused cyclic compound, preparation method therefor and application thereof

Inventors: Bin Zou (Shanghai, CN); Xianlei Fu (Shanghai, CN); Rui Zhang (Shanghai, CN); Shichao Ma (Shanghai, CN); Shuaijie Xu (Shanghai, CN); Wencheng Fu (Shanghai, CN); Lanzhen Liu (Shanghai, CN)
Assignee: BLUERAY THERAPEUTICS (SHANGHAI) CO., LTD
C07D519/00C07D401/14C07D405/14C07D413/14C07D417/00
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Quick Facts
Patent No.
US 11,498,930
App. No.
16/969,392
Granted
Nov 15, 2022
Kind
B2
Abstract

Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.

Claims (18)

1. A compound selected from the group consisting of

and

or a pharmaceutically acceptable salt thereof.

2. The compound or pharmaceutically acceptable salt thereof as defined in claim 1 , wherein the compound is

3. The compound or pharmaceutically acceptable salt thereof as defined in claim 1 , wherein the compound is

4. The compound or pharmaceutically acceptable salt thereof as defined in claim 1 , wherein the compound is

5. A pharmaceutical composition, comprising the compound or pharmaceutically acceptable salt thereof as defined in claim 1 , and a pharmaceutically acceptable excipient.

6. A method for the treatment of a disease or condition associated with abnormal activity of SHP2 in a subject in need thereof, comprising administering the compound or the pharmaceutically acceptable salt thereof as defined in claim 1 to the subject, wherein the disease or condition is selected from Noonan syndrome, Leopard syndrome, juvenile myelomonocytic leukemia, neuroblastoma, melanoma, acute myeloid leukemia, breast cancer, esophageal cancer, lung cancer, colon cancer, head cancer, neuroblastoma, head and neck squamous cell carcinoma, gastric cancer, anaplastic large cell lymphoma and glioblastoma.

7. A pharmaceutical preparation, comprising the compound or pharmaceutically acceptable salt thereof as defined in claim 1 .

8. The pharmaceutical preparation as defined in claim 7 , wherein the pharmaceutical preparation is adapted for oral administration, sublingual administration, subcutaneous injection, intravenous injection, intramuscular injection, intrasternal injection, nasal administration, local topical administration or rectal administration;

and/or, the pharmaceutical preparation is adapted to be administered once or multiple times a day.

9. A combination product comprising

(i) the compound or pharmaceutically acceptable salt thereof as defined in claim 1 ; and

(ii) another medicament,

wherein the another medicament is selected from anticancer medicaments, tumor immune medicaments, antiallergic medicaments, antiemetic medicaments, analgesics, and cell protection medicaments.

10. A method for treatment of a disease or condition associated with abnormal activity of SHP2 in a subject in need thereof, comprising administering the pharmaceutical composition thereof as defined in claim 5 to the subject, wherein the disease or condition is selected from Noonan syndrome, Leopard syndrome, juvenile myelomonocytic leukemia, neuroblastoma, melanoma, acute myeloid leukemia, breast cancer, esophageal cancer, lung cancer, colon cancer, head cancer, neuroblastoma, head and neck squamous cell carcinoma, gastric cancer, anaplastic large cell lymphoma and glioblastoma.

11. A method for the treatment of a disease or condition associated with abnormal activity of SHP2 in a subject in need thereof, comprising administering the pharmaceutical composition thereof as defined in claim 7 to the subject, wherein the disease or condition is selected from Noonan syndrome, Leopard syndrome, juvenile myelomonocytic leukemia, neuroblastoma, melanoma, acute myeloid leukemia, breast cancer, esophageal cancer, lung cancer, colon cancer, head cancer, neuroblastoma, head and neck squamous cell carcinoma, gastric cancer, anaplastic large cell lymphoma and glioblastoma.

12. A method for the treatment of a disease or condition associated with abnormal activity of SHP2 in a subject in need thereof, comprising administering the pharmaceutical composition thereof as defined in claim 9 to the subject, wherein the disease or condition is selected from Noonan syndrome, Leopard syndrome, juvenile myelomonocytic leukemia, neuroblastoma, melanoma, acute myeloid leukemia, breast cancer, esophageal cancer, lung cancer, colon cancer, head cancer, neuroblastoma, head and neck squamous cell carcinoma, gastric cancer, anaplastic large cell lymphoma and glioblastoma.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 20, 2024
From: BLUERAY THERAPEUTICS (SHANGHAI) CO., LTD
To: SHANGHAI BLUERAY BIOPHARMA CO., LTD.
Reel/Frame 066838/0194 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 6, 2021
From: SHANGHAI BLUERAY BIOPHARMA CO., LTD.
To: BLUERAY THERAPEUTICS (SHANGHAI) CO., LTD.
Reel/Frame 056770/0109 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 12, 2020
From: ZOU, BIN; FU, XIANLEI; ZHANG, RUI; MA, SHICHAO; XU, SHUAIJIE; FU, WENCHENG; LIU, LANZHEN
To: SHANGHAI BLUERAY BIOPHARMA CO., LTD.
Reel/Frame 053475/0658 →
Priority Claims (2)
CN 201810144135.3 · Feb 13, 2018 · national
CN 201810692211.4 · Jun 29, 2018 · national
Continuity (1)
Related Publication 20210053989A1 · Feb 25, 2021