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1.发明公开tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators 有权Intermediatenfürdie Synthese von Makrozyklische Ghrelin-Rezeptormodulatoren
公开(公告)号：EP2644618A1
公开(公告)日：2013-10-02
申请号：EP12195556.1
申请日：2008-02-08
发明人： Hoveyda, Hamid , Fraser, Graeme , Beauchemin, Sophie , Brassard, Martin , Drutz, David , Marsault, Eric , Quellet, Luc , Peterson, Mark L , Wang, Zhigang , Benkali, Kamel
IPC分类号： C07K5/12 , C07D213/65 , C07D307/80 , C07D491/04 , C07D311/02 , C07C271/12 , C07C211/27 , C07C403/18
CPC分类号： A61K31/395 , C07C215/42 , C07C215/54 , C07C271/16 , C07C2601/14 , C07D273/00 , C07D413/06 , C07D498/04 , C07D498/16
摘要： The present invention relates to intermediates of conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the ghrelin (growth hormone secretagogue) receptor including GHS-R1a and subtypes, isoforms and/or variants thereof and the use of these interemdaites to prepare said macrocyclic compounds.
摘要翻译： 本发明涉及构象定义的大环化合物的中间体，其与生长素释放肽（生长激素促分泌素）受体（包括GHS-R1a及其亚型，同种型和/或变体）结合和/或是功能性调节剂，以及这些结合蛋白的使用 制备大环化合物。
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2.发明公开
公开(公告)号：EP2054429A2
公开(公告)日：2009-05-06
申请号：EP07838009.4
申请日：2007-09-11
发明人： MARSAULT, Éric , FRASER, Graeme , BENAKLI, Kamel , ST-LOUIS, Carl , ROUILLARD, Alain , THOMAS, Helmut
IPC分类号： C07K5/08 , A61P1/00 , C07C271/16 , C07D213/64 , C07D213/65
CPC分类号： C07K5/0812 , A61K38/00 , C07C271/16 , C07D273/00 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： The present invention provides 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, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.
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公开(公告)号：EP2491004A4
公开(公告)日：2013-07-03
申请号：EP10825746
申请日：2010-10-22
申请人： TRANZYME PHARMA INC
发明人： MARSAULT ERIC , LEOGANE OLIVIER , MATHIEU AXEL , BEAUBIEN SYLVIE
IPC分类号： C07C225/00
CPC分类号： A61K31/395
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4.发明公开Macrocyclic antagonist of the motilin receptor for treatment of gastrointestinal dysmotility disorders 审中-公开胃动素受体的宏裁量拮抗剂用于胃肠运动障碍的治疗
公开(公告)号：EP2431380A3
公开(公告)日：2013-07-03
申请号：EP11075225.0
申请日：2007-09-11
发明人： Marsault, Eric , Fraser, Graeme , Benakli, Kamel , St-Louis, Carl , Rouillard, Alain , Thomas, Helmut
IPC分类号： C07K5/087 , A61P1/00 , C07C271/16 , C07D213/64 , C07D213/65
CPC分类号： C07K5/0812 , A61K38/00 , C07C271/16 , C07D273/00 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： The present invention provides 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, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.
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5.发明公开Spatially-defined macrocyclic compounds useful for drug discovery 有权on n n n n n n n n n n n n n n n n n n
公开(公告)号：EP2316846A2
公开(公告)日：2011-05-04
申请号：EP10011035.2
申请日：2004-08-02
申请人： Tranzyme Pharma Inc.
发明人： Deslongchamps, Pierre , Dory, Yves , Benakli, Kamel , Marsault, Eric , Ouellet, Luc , Vézina, Martin , Fortin, Daniel , Lan, Ruoxi , Li, Shigui , Villeneuve, Gérald , Beaubien, Sylvie , Peterson, Mark L. , Ramaseshan, Mahesh , Hoveyda, Hamid R.
摘要： 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.
摘要翻译： 公开了包含特定构象控制元件的新的空间定义的大环化合物。 然后使用这些大环的文库来选择一个或多个表现出与特定生物靶特异性相互作用的大环物种。 特别地，根据本发明的化合物公开为哺乳动物胃动素受体和哺乳动物生长素释放肽受体的激动剂或拮抗剂。
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6.发明授权SPATIALLY-DEFINED MACROCYCLIC COMPOUNDS USEFUL FOR DRUG DISCOVERY 有权国土DEFINED大环化合物WHICH药品DISCOVERY是合适
公开(公告)号：EP1648922B1
公开(公告)日：2010-12-01
申请号：EP04761605.7
申请日：2004-08-02
申请人： Tranzyme Pharma Inc.
发明人： DESLONGCHAMPS, Pierre , DORY, Yves , PETERSON, Mark , BENAKLI, Kamel , MARSAULT, Eric , OUELLET, Luc , RAMASESHAN, Mahesh , VEZINA, Martin , FORTIN, Daniel , LAN, Ruoxi , LI, Shigui , VILLENEUVE, Gérald , HOVEYDA, Hamid , BEAUBIEN, Sylvie , FRASER, Graeme
CPC分类号： C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要： 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.
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公开(公告)号：EP2210612A3
公开(公告)日：2010-11-24
申请号：EP10001568.4
申请日：2004-06-18
申请人： Tranzyme Pharma Inc.
发明人： Marsault, Eric , Benakli, Kamel , Peterson, Mark , Beaubien, Sylvie , St-Louis, Carl , Ouellet, Luc , Beauchemin, Sophie , Hoveyda, Hamid
IPC分类号： A61K38/22 , C07K5/08 , C07C13/00 , C07C15/00 , C07D213/00
CPC分类号： C07C213/08 , A61K38/12 , A61K38/2214 , C07C41/18 , C07C67/343 , C07D273/00 , C07D413/06 , C07D498/04 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要： The invention provides a first group of intermediates useful in the manufacture of conformationally-defined macrocyclic compounds, a method for making some of these and a second group of intermediate compounds prepared in this method, use of the first group of intermediates in the manufacture of conformationally-defined macrocyclic compounds and a method of so manufacturing, and conformationally-defined macrocyclic compounds made from the first group of intermediates.
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8.发明授权SPATIALLY-DEFINED MACROCYCLIC COMPOUNDS USEFUL FOR DRUG DISCOVERY 有权国土DEFINED大环化合物WHICH药品DISCOVERY是合适
公开(公告)号：EP1648922B9
公开(公告)日：2013-04-03
申请号：EP04761605.7
申请日：2004-08-02
申请人： Tranzyme Pharma Inc.
发明人： DESLONGCHAMPS, Pierre , DORY, Yves , PETERSON, Mark , BENAKLI, Kamel , MARSAULT, Eric , OUELLET, Luc , RAMASESHAN, Mahesh , VEZINA, Martin , FORTIN, Daniel , LAN, Ruoxi , LI, Shigui , VILLENEUVE, Gérald , HOVEYDA, Hamid , BEAUBIEN, Sylvie , FRASER, Graeme
CPC分类号： C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
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9.发明公开MACROCYCLIC GHRELIN RECEPTOR ANTAGONISTS AND INVERSE AGONISTS AND METHODS OF USING THE SAME 审中-公开万家乐CYCLICAL生长素受体拮抗剂和反对激动剂和其使用方法
公开(公告)号：EP2493910A1
公开(公告)日：2012-09-05
申请号：EP10774101.9
申请日：2010-10-29
发明人： HOVEYDA, Hamid , MARSAULT, Éric , THOMAS, Helmut , FRASER, Graeme , BEAUBIEN, Sylvie , MATHIEU, Axel , BEIGNET, Julien , BONIN, Marc-André , PHOENIX, Serge , DRUTZ, David , PETERSON, Mark , BEAUCHEMIN, Sophie , BRASSARD, Martin , VÉZINA, Martin
IPC分类号： C07K5/12 , A61K38/12 , A61P25/00 , A61P35/00 , A61P5/00 , A61P3/00 , A61P1/00 , A61P29/00 , A61P9/00
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0804 , C07K5/0812
摘要： The present invention provides novel conformationalIy- defined macrocyclic compounds of formula (I) 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.
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公开(公告)号：EP1773869B1
公开(公告)日：2012-08-22
申请号：EP05785185.9
申请日：2005-06-13
IPC分类号： C07K5/08
CPC分类号： C07K5/0827 , A61K38/00 , C07D273/00 , C07D498/08 , C07K5/0808 , C07K5/0812
摘要： 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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