IP Library Granted Patent US 10,301,297
Granted Patent B2
US 10,301,297 · App. 15/942,772 · Granted May 28, 2019

Substituted nicotinimide inhibitors of BTK and their preparation and use in the treatment of cancer, inflammation and autoimmune disease

Inventors: Xiangyang Chen (Beijing, CN); Yingxiang Gao (Beijing, CN); Chong Liu (Beijing, CN); Haihong Ni (Beijing, CN); Mark Mulvihill (Sudbury, MA)
Assignee: Guangzhou Innocare Pharma Tech Co., Ltd.
C07D417/04C07D211/34C07D213/82C07D231/14C07D277/56C07D295/185C07D401/04C07D401/12C07D401/14C07D403/04C07D413/04
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Quick Facts
Patent No.
US 10,301,297
App. No.
15/942,772
Granted
May 28, 2019
Kind
B2
Abstract

Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).

Claims (15)

1. A compound having a Formula IId′, or a pharmaceutically acceptable salt or solvate thereof:

wherein X is

Z is CH or N;

G 1 , G 2 , and G 3 are H, or optionally substituted with one or more substituents independently selected from the group consisting of D (deuterium), C 1-12 alkyl, halogen, CN, and CF 3 ;

R 2 and R 3 are each independently selected from the group consisting of H, D, C 1-12 alkyl, halogen, CN, and CF 3 , wherein C 1-12 alkyl is optionally substituted with NR 11 R 12 ;

R 4 is selected from the group consisting of H, D, C 1-12 alkyl, halogen, CN, and CF 3 ; and

R 11 and R 12 are independently H or C 1-6 alkyl.

2. The compound according to claim 1 , wherein

wherein X is

3. The compound according to claim 1 , wherein G 1 , G 2 , and G 3 are H, or optionally substituted with one or more halogen.

4. The compound according to claim 1 , wherein R 2 and R 3 are H or C 1-12 alkyl, wherein C 1-12 alkyl is optionally substituted with NR 11 R 12 , and R 11 and R 12 are H or CH 3 .

5. The compound according to claim 1 , which is

6. The compound according to claim 1 , which is

7. The compound according to claim 1 , which is

8. The compound according to claim 1 , which is

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2018
From: BEIJING INNOCARE PHARMA TECH CO., LTD.
To: GUANGZHOU INNOCARE PHARMA TECH CO., LTD.
Reel/Frame 046931/0129 →
Priority Claims (1)
CN 2013 1 0485048 · Oct 16, 2013 · national
Continuity (3)
Continuation 15025654
Provisional Application 61884958 · Sep 30, 2013
Related Publication 20180222897A1 · Aug 9, 2018