# US 10,870,657 B2 · Compounds for the treatment of cancer and inflammatory disease

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- Number: US 10,870,657 B2
- Document ID: US10870657B2
- Status: Granted
- Kind: B2
- Application number: 16/246,027
- Filed: 2019-01-11
- Published: 2019-07-18
- Granted: 2020-12-22
- Earliest claimed: 2015-12-22
- Assignees: SHY Therapeutics LLC
- Applicants: SHY Therapeutics LLC
- Inventors: Yaron R. Hadari; Luca Carta; Michael Schmertzler; Theresa M. Williams; Charles H. Reynolds
- Web page: https://patentgrep.com/patent/US10870657B2

## CPC

- C07D 495/04: Ortho-condensed systems
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/08: of the prostate
- A61P 13/10: of the bladder
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 33/12: Schistosomicides
- A61P 35/00: Antineoplastic agents
- C07D 221/04: Ortho- or peri-condensed ring systems
- C07D 239/94: Nitrogen atoms
- C07D 265/30: not condensed with other rings
- C07D 271/06: 1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 401/14: containing three or more hetero rings
- C07D 407/14: containing three or more hetero rings
- C07D 409/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 473/30: attached in position 6, e.g. hypoxanthine
- C07D 487/04: Ortho-condensed systems
- C07D 495/14: Ortho-condensed systems
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## 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

### Claim 1

A compound of Formula VIIIb1:
or a pharmaceutically acceptable salt thereof,
wherein R1b1 is 2-pyridyl;
R8b1 is H;
R9b1 is halo;
R6b1 and R7b1 are combined to form a cyclic structure including the nitrogen atom to which they are both attached.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 2)

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

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 1)

A pharmaceutical composition, comprising a therapeutically effective amount of the compound of Formula VIIIb1 of claim 1 and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 1)

The compound of claim 1, wherein the compound is:

### Claim 7 (depends on 6)

A pharmaceutical composition, comprising a therapeutically effective amount of the compound of claim 6 and a pharmaceutically acceptable carrier.
