# US 8,772,482 B2 · 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use

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- Number: US 8,772,482 B2
- Document ID: US8772482B2
- Status: Granted
- Kind: B2
- Application number: 13/162,989
- Filed: 2011-06-17
- Published: 2012-02-16
- Granted: 2014-07-08
- Earliest claimed: 2006-12-12
- Assignees: Lexicon Pharmaceuticals, Inc.
- Applicants: Arokiasamy Devasagayaraj; Haihong Jin; Zhi-Cai Shi; Ashok Tunoori; Ying Wang; Chengmin Zhang
- Inventors: Arokiasamy Devasagayaraj; Haihong Jin; Zhi-Cai Shi; Ashok Tunoori; Ying Wang; Chengmin Zhang
- Web page: https://patentgrep.com/patent/US8772482B2

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/06: Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 1/10: Laxatives
- A61P 1/12: Antidiarrhoeals
- 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 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/02: Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/08: Bronchodilators
- A61P 17/00: Drugs for dermatological disorders
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 239/34: One oxygen atom
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- A61K 31/4152: having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:

## Claims

### Claim 1

A method of treating or managing irritable bowel syndrome, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein R4 is lower alkyl.

### Claim 2

A method of treating or managing Crohn's disease, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen or lower alkyl.

### Claim 3 (depends on 2)

The method of claim 2, wherein R4 is hydrogen.

### Claim 4 (depends on 2)

The method of claim 2, wherein R4 is lower alkyl.

### Claim 5 (depends on 4)

The method of claim 4, wherein R4 is ethyl.

### Claim 6

A method of treating or managing ulcerative colitis, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen or lower alkyl

### Claim 7 (depends on 6)

The method of claim 6, wherein R4 is hydrogen.

### Claim 8 (depends on 6)

The method of claim 6, wherein R4 is lower alkyl.

### Claim 9 (depends on 8)

The method of claim 8, wherein R4 is ethyl.