Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use

Patent metadata

Field	Value
Publication number	US-2016250184-A1
Application number	US-201415030779-A
Country	US
Kind code	A1
Filing date	Oct 30, 2014
Priority date	Nov 4, 2013
Publication date	Sep 1, 2016
Grant date	—

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.

First claim

1 . A compound which is:

or a pharmaceutically acceptable salt thereof.

2 . The compound of claim 1 which is:

or a pharmaceutically acceptable salt thereof.

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

4 . 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.

5 . 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.

6 . 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.

7 . 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.

8 . 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.

9 . 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.

10 . 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.

11 . The method of claim 9 wherein the cholesterol absorption inhibitor compound is:

or a pharmaceutically acceptable salt thereof.

12 - 14 . (canceled)

Assignees

• Lin Songnian
• Xu Libo
• Parmee Emma R
• Liao Xibin
• Merck Sharp & Dohme

Inventors

• Lin Songnian
• Xu Libo
• Parmee Emma R
• Liao Xibin

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• C07D209/20

  substituted additionally by nitrogen atoms, e.g. tryptophane · CPC title

• A61K31/4035

  Isoindoles, e.g. phthalimide · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• C07D209/18

  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 · CPC title