| Patent application number | Description | Published |
|---|
| 20080287371 | MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR MODULATION OF THE MIGRATING MOTOR COMPLEX - The present invention relates to novel conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds are useful as therapeutics for a range of gastrointestinal disorders, in particular those in which suppression or inhibition of the migrating motor complex (MMC) is effective or malfunction of gastric motility or increased motilin secretion is observed, such as hypermotilinemia, imitable bowel syndrome, dyspepsia, including gallbladder dyspepsia, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, | 11-20-2008 |
| 20090137817 | SPATIALLY-DEFINED MACROCYCLIC COMPOUNDS USEFUL FOR DRUG DISCOVERY - Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor. | 05-28-2009 |
| 20090137835 | PROCESSES FOR INTERMEDIATES FOR MACROCYCLIC COMPOUNDS - The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: | 05-28-2009 |
| 20090198050 | Macrocyclic Modulators of the Ghrelin Receptor - 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. | 08-06-2009 |
| 20090240027 | INTERMEDIATES FOR MACROCYCLIC COMPOUNDS - The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: | 09-24-2009 |
| 20090312540 | SPATIALLY-DEFINED MACROCYCLES INCORPORATING PEPTIDE BOND SURROGATES - Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target, in particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor. | 12-17-2009 |
| 20110105389 | Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same - The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse 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, obesity and obesity-associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders. | 05-05-2011 |
