Jeffrey A Edwards

US Patent:

20140051629, Feb 20, 2014

Filed:

Sep 21, 2011

Appl. No.:

13/825601

Inventors:

Robert M. Jones - San Diego CA, US
Juerg Lehmann - San Diego CA, US
Weichao Chen - San Diego CA, US
Jeffrey Edwards - San Diego CA, US
Glen Marquez - San Jose CA, US
Michael E. Morgan - San Diego CA, US
Abu J.M. Sadeque - San Diego CA, US
Sun Hee Kim - San Diego CA, US

Assignee:

ARENA PHARMACEUTICALS, INC. - San Diego CA

International Classification:

C07D 413/14
A61K 45/06
A61K 31/506

US Classification:

514 65, 544328, 514256

Abstract:

The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzamide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoro-propan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

US Patent:

20210340133, Nov 4, 2021

Filed:

Dec 15, 2020

Appl. No.:

17/122052

Inventors:

- San Diego CA, US
Juerg Lehmann - San Diego CA, US
Weichao Chen - San Diego CA, US
Jeffrey Edwards - San Diego CA, US
Glen Marquez - San Jose CA, US
Michael E. Morgan - San Diego CA, US
Abu J.M. Sadeque - San Diego CA, US
Sun Hee Kim - San Diego CA, US

International Classification:

C07D 413/14
A61K 31/506
A61K 45/06

Abstract:

The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzanide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoro-propan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.