IP Library Granted Patent US 9,440,981
Granted Patent B2
US 9,440,981 · App. 14/404,217 · Granted Sep 13, 2016

Pyrrolo[2, 1-F] [1,2,4]triazine derivative and use thereof for treating tumors

Inventors: Xihan Wu (Jiangsu, CN); Minmin Yang (Jiangsu, CN); Qingning Shu (Jiangsu, CN); Chunrui Zhu (Jiangsu, CN)
Assignee: PHARMABLOCK (NANJING) R&D CO. LTD
C07D487/04A61K31/5377C07D519/00
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Quick Facts
Patent No.
US 9,440,981
App. No.
14/404,217
Granted
Sep 13, 2016
Kind
B2
Abstract

Disclosed are a pyrrolo[2,1-f][1,2,4]triazine derivative of Formula (I) and use thereof for treating tumors. The compound has remarkable antiproliferative activity for a variety of human tumor cell lines, and is useful for treating cancers, especially solid tumors such as gastric cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostatic cancer, and oral cancer.

Claims (12)

1. A compound of structural Formula (I), or a pharmaceutically acceptable salt thereof:

wherein R 1 represents indolyl, indazolyl, azaindolyl, or aminopyrimidinyl;

R 2 represents

R 3 represents C 1 -C 6 alkyl, R 4 represents C 1 -C 6 alkyl, and R 5 represents C 1 -C 6 alkyl.

2. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 1 represents:

3. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 3 represents methyl or ethyl.

4. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 4 represents methyl or cyclopropyl.

5. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 5 represents methyl.

6. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein the pharmaceutically acceptable salt is a salt of the compound of claim 1 with arginine, hydrochloric acid, sulfuric acid, phosphoric acid, maleic acid, fumaric acid, citric acid, methansulfonic acid, p-toluene sulfonic acid, or tartaric acid.

7. A pharmaceutical composition, comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

8. A method of treating a tumor comprising administering a compound according to claim 1 to a subject in need thereof, wherein the tumor is selected from the group consisting of gastric cancer, lung cancer, liver cancer, breast cancer, colon cancer, and prostatic cancer.

9. A method of treating a tumor comprising administering a composition according to claim 7 to a subject in need thereof, wherein the tumor is selected from the group consisting of gastric cancer, lung cancer, liver cancer, breast cancer, colon cancer, and prostatic cancer.

Assignments (2)
CHANGE OF NAME Recorded Nov 23, 2016
From: PHARMABLOCK (NANJING) R&D CO., LTD.
To: PHARMABLOCK SCIENCES (NANJING), INC.
Reel/Frame 040410/0871 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 14, 2015
From: WU, XIHAN; YANG, MINMIN; SHU, QINGNING; ZHU, CHUNRUI
To: PHARMABLOCK (NANJING) R&D CO. LTD.
Reel/Frame 035635/0923 →
Priority Claims (1)
CN 2012 1 0178854 · Jun 1, 2012 · national
Continuity (1)
Related Publication 20160115166A1 · Apr 28, 2016