# US 2016/0250184 A1 · Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use

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- Number: US 2016/0250184 A1
- Document ID: US20160250184A1
- Status: Published application
- Kind: A1
- Application number: 15/030,779
- Filed: 2014-10-30
- Published: 2016-09-01
- Earliest claimed: 2013-11-04
- Assignees: Merck Sharp & Dohme Corp.
- Applicants: Merck Sharp & Dohme Corp.
- Inventors: SONGNIAN LIN; Libo Xu; Emma R. Parmee; Xibin Liao
- Web page: https://patentgrep.com/patent/US20160250184A1

## CPC

- A61K 31/404: Indoles, e.g. pindolol
- A61K 31/397: having four-membered rings, e.g. azetidine
- A61K 31/4035: Isoindoles, e.g. phthalimide
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- C07D 209/18: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D 209/20: substituted additionally by nitrogen atoms, e.g. tryptophane
- 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

Glucagon receptor antagonist compounds are disclosed which are of long duration of action. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

## Claims

### Claim 1

A compound which is:
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The compound of claim 1 which is:
or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier.

### Claim 4 (depends on 1)

A method of treating type 2 diabetes mellitus in a mammalian patient in need of such treatment comprising administering to said patient the compound of claim 1 or a pharmaceutically acceptable salt thereof in an amount that is effective to treat said type 2 diabetes mellitus.

### Claim 5 (depends on 1)

A method of treating hyperglycemia, diabetes or insulin resistance in a mammalian patient in need of such treatment which comprises administering to said patient an effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 1)

A method of treating a condition selected from the group consisting of: (1) hyperglycemia, (2) low glucose tolerance, (3) insulin resistance, (4) retinopathy, (5) nephropathy, (6) neuropathy, (7) Syndrome X, and other conditions and disorders where insulin resistance is a component, in a mammalian patient in need of such treatment, comprising administering to the patient the compound of claim 1 or a pharmaceutically acceptable salt thereof in an amount that is effective to treat said condition.

### Claim 7 (depends on 4)

A method of claim 4 where the compound or a pharmaceutically acceptable salt thereof is used in combination with one or more other active ingredients.

### Claim 8 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof in combination with one or more other active ingredients and a pharmaceutically acceptable carrier.

### Claim 9 (depends on 1)

A method of treating a condition selected from the group consisting of hypercholesterolemia, atherosclerosis, low HDL levels, high LDL levels, hyperlipidemia, hypertriglyceridemia and dyslipidemia, in a mammalian patient in need of such treatment, comprising administering to the patient the compound of claim 1 or a pharmaceutically acceptable salt thereof in combination with an HMG-CoA reductase inhibitor.

### Claim 10 (depends on 1)

A method of treating a condition selected from the group consisting of hypercholesterolemia, atherosclerosis, low HDL levels, high LDL levels, hyperlipidemia, hypertriglyceridemia and dyslipidemia, in a mammalian patient in need of such treatment, comprising administering to the patient the compound of claim 1 or a pharmaceutically acceptable salt thereof in combination with an cholesterol absorption inhibitor.

### Claim 11 (depends on 9)

The method of claim 9 wherein the cholesterol absorption inhibitor compound is:
or a pharmaceutically acceptable salt thereof.

### Claim at position 12

12-14. (canceled)