# US 9,040,517 B2 · Compounds as diacylglycerol acyltransferase inhibitors

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- Number: US 9,040,517 B2
- Document ID: US9040517B2
- Status: Granted
- Kind: B2
- Application number: 14/478,309
- Filed: 2014-09-05
- Published: 2014-12-25
- Granted: 2015-05-26
- Earliest claimed: 2011-05-20
- Assignees: GlaxoSmithKline Intellectual Property (No. 2) Limited
- Applicants: GlaxoSmithKline Intellectual Property (No.2) Limited
- Inventors: Mui Cheung; Raghuram Tangirala
- Web page: https://patentgrep.com/patent/US9040517B2

## CPC

- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 498/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.

## Claims

### Claim 1

A compound which is 4-amino-6-[1-(2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-5H,6H,7H,8H-pyrimido[5,4-f][1,4]oxazepin-5-one, represented by the formula:
or a pharmaceutically acceptable salt thereof.

### Claim 2

A compound which is 4-amino-6-[1-(2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-5H,6H,7H,8H-pyrimido[5,4-f][1,4]oxazepin-5-one, represented by the formula:

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the compound or salt according to claim 1, and a pharmaceutically acceptable carrier.

### Claim 4 (depends on 2)

A pharmaceutical composition comprising the compound according to claim 2, and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 1)

A method of treating obesity comprising administering to a human in need thereof an effective amount of the compound or salt according to claim 1.

### Claim 6 (depends on 2)

A method of treating obesity comprising administering to a human in need thereof an effective amount of the compound according to claim 2.

### Claim 7 (depends on 3)

A method of treating obesity comprising administering to a human in need thereof an effective amount of the pharmaceutical composition according to claim 3.

### Claim 8 (depends on 4)

A method of treating obesity comprising administering to a human in need thereof an effective amount of the pharmaceutical composition according to claim 4.