Patent application number | Description | Published |
20090048291 | Novel Piperidine-4-Acetic Acid Derivatives and Their Use - The present invention is directed to compounds of formula I | 02-19-2009 |
20090054451 | Use of Piperidine Derivatives as Agonists of Chemokine Receptor Activity - The present invention is directed to novel piperidine derivatives and to the use of piperidine derivatives of formula I | 02-26-2009 |
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 |
20090275648 | 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 (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, cardiovascular disorders, obesity and obesity-associated disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders. | 11-05-2009 |
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 |
20110237785 | 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. | 09-29-2011 |
20110245159 | Salts, Solvates and Pharmaceutical Compositions of Macrocyclic Ghrelin Receptor Agonists and Methods of Using the Same - The present invention provides novel salts and solvates of macrocyclic compounds that bind to and/or are functional agonists of the ghrelin (growth hormone secretagogue) receptor. The invention also relates to polymorphs of these salts and solvates, pharmaceutical compositions containing these salts or solvates, and methods of using the pharmaceutical compositions. These pharmaceutical compositions are useful as therapeutics for a range of disease indications, in particular, for treatment and prevention of gastrointestinal disorders including, but not limited to, postoperative ileus, gastroparesis, including diabetic and postsurgical gastroparesis, opioid bowel dysfunction, chronic intestinal pseudo-obstruction, short bowel syndrome, functional gastrointestinal disorders and gastrointestinal dysmotility, such as that occurring in conjunction with other disease states, in critical care situations or as a result of treatment with pharmaceutical agents. Additionally, the pharmaceutical compositions have application to the treatment and prevention of metabolic and/or endocrine disorders, cardiovascular disorders, central nervous system disorders, bone disorders, inflammatory disorders, hyperproliferative disorders, disorders characterized by apoptosis and genetic disorders. | 10-06-2011 |
20120165566 | 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: | 06-28-2012 |
20120226066 | 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: | 09-06-2012 |
20120226067 | 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: | 09-06-2012 |
20120226072 | 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: | 09-06-2012 |
20130023530 | NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS - The present invention is directed to novel compounds of formula I | 01-24-2013 |
20130023539 | PYRROLIDINE OR THIAZOLIDINE CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS AS AGONISTS OF G-PROTEIN COUPLED RECEPTOR 43 (GPR43) - The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases. | 01-24-2013 |
20140275097 | NOVEL CHIRAL N-ACYL-5,6,7(8-SUBSTITUTED)-TETRAHYDRO-[1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR MEDIATED DISORDERS AND CHIRAL SYNTHESIS THEREOF - The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I. | 09-18-2014 |
20140371218 | NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS - The present invention is directed to novel compounds of formula I | 12-18-2014 |