IP Library › Granted Patent US 10,221,191
Granted Patent B2
US 10,221,191 · App. 15/387,349 · Granted Mar 5, 2019

Compounds for the treatment of cancer and inflammatory disease

Inventors: Yaron R. Hadari (Harrison, NY); Luca Carta (New York, NY); Michael Schmertzler (New Canaan, CT); Theresa M. Williams (Harleysville, PA); Charles H. Reynolds (Lansdale, PA)
C07D495/04C07D221/04C07D239/94C07D265/30C07D271/06C07D401/04C07D401/12C07D401/14C07D407/14C07D409/14C07D413/14C07D417/14C07D471/04C07D473/30C07D487/04C07D495/14
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Quick Facts
Patent No.
US 10,221,191
App. No.
15/387,349
Granted
Mar 5, 2019
Kind
B2
Abstract

Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

Claims (12)

1. A compound of Formula VIb1:

or a pharmaceutically acceptable salt thereof,

wherein R 1b1 is 2-pyridyl;

R 8b1 is H;

R 9b1 is substituted phenyl, heteroaryl, heterocyclyl, C(O)NR 6 R 7 , wherein the heteroaryl group is not a substituted pyrazole;

R 6 and R 7 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, or R 6 and R 7 are combined to form a heteroaryl or heterocyclyl structure including the nitrogen atom to which they are both attached;

wherein heteroaryl is a monocyclic or multicyclic aromatic ring system of 5 to 15 members where one to three of the atoms in the ring system is nitrogen, oxygen or sulfur; and

wherein heterocyclyl is a monocyclic or multicyclic non-aromatic ring system of 3 to 10 members where one to three of the atoms in the ring system is nitrogen, oxygen or sulfur.

2. A method of treating cancer, comprising administering to a subject a compound or a pharmaceutically acceptable salt thereof of claim 1 , wherein the cancer is a solid tumor, and wherein the solid tumor is hepatocellular carcinoma, prostate cancer, pancreatic cancer, ovarian cancer, or glioblastoma.

3. The method of claim 2 , wherein the solid tumor is pancreatic cancer.

4. A method of treating an inflammatory disease, comprising administering to a subject a compound or a pharmaceutically acceptable salt thereof of claim 1 , wherein the inflammatory disease is inflammatory bowel disease, Barrett's esophagus, asbestosis, gingivitis, pancreatitis, or bronchitis.

5. A pharmaceutical composition, comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 19, 2019
From: HADARI, YARON R.; CARTA, LUCA; SCHMERTZLER, MICHAEL; WILLIAMS, THERESA M.; REYNOLDS, CHARLES H.
To: SHY THERAPEUTICS LLC
Reel/Frame 048376/0054 →
Continuity (2)
Provisional Application 62271185 · Dec 22, 2015
Related Publication 20170174699A1 · Jun 22, 2017
Cited By (4)
US 12,391,705 US 12,435,046 US 12,653,810 US 12,714,713