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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 9493505 B1

PDFFull Text
Date of Patent:
Nov. 15, 2016

Filed:

Oct. 31, 2014

Macrocyclic modulators of the ghrelin receptor

Applicant:

Ocera Therapeutics, Inc., Palo Alto, CA (US);

Inventors:

Eric Marsault, Sherbrooke, CA;

Carl St-Louis, Sherbrooke, CA;

Assignee:

OCERA THERAPEUTICS, INC., Palo Alto, CA (US);

Attorney:

Myers Bigel & Sibley, P.A.

Primary Examiner:

Jeanette Lieb

Int. Cl.
CPC ...
A61K 38/12 (2006.01); C07K 16/00 (2006.01); C07K 5/08 (2006.01); C07K 1/107 (2006.01); C07C 271/16 (2006.01); C07F 7/18 (2006.01); C07D 213/64 (2006.01); C07C 217/62 (2006.01); C07C 311/08 (2006.01); C07D 273/00 (2006.01); A61K 38/25 (2006.01); A61K 38/30 (2006.01); A61K 45/06 (2006.01); A61K 38/06 (2006.01); C07K 5/087 (2006.01);
U.S. Cl.
CPC ...
C07K 5/08 (2013.01); A61K 38/06 (2013.01); A61K 38/25 (2013.01); A61K 38/30 (2013.01); A61K 45/06 (2013.01); C07C 217/62 (2013.01); C07C 271/16 (2013.01); C07C 311/08 (2013.01); C07D 213/64 (2013.01); C07D 273/00 (2013.01); C07F 7/1852 (2013.01); C07K 1/1077 (2013.01); C07K 5/0827 (2013.01); C07K 5/0812 (2013.01);
Abstract

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

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