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1.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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2.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：EP2118080A1
公开(公告)日：2009-11-18
申请号：EP08799889.4
申请日：2008-02-08
发明人： HOVEYDA, Hamid , FRASER, Graeme , BEAUCHEMIN, Sophie , BRASSARD, Martin , DRUTZ, David , MARSAULT, Éric , OUELLET, Luc , PETERSON, Mark, L. , WANG, Zhigang , BENAKLI, Kamel
IPC分类号： C07D273/00 , C07K5/12 , A61K38/00 , A61P1/00
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.
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4.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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公开(公告)号：EP1633774B1
公开(公告)日：2010-02-17
申请号：EP04737852.6
申请日：2004-06-18
申请人： Tranzyme Pharma Inc.
发明人： FRASER, Graeme , MARSAULT, Eric , PETERSON, Mark , HOVEYDA, Hamid , BEAUBIEN, Sylvie , BENAKLI, Kamel , DEZIEL, Robert
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 present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
摘要翻译： 本发明涉及式（I）的新型大环化合物及其药学上可接受的盐，水合物或溶剂化物：其中R 1，R 2，R 3，R 4，R 5，R 6，n1，m，p Z1，Z2和Z3如 在说明书中描述。 本发明还涉及式（I）化合物，其是胃动素受体的拮抗剂并且可用于治疗与该受体相关的病症并伴有或伴随有运动功能障碍。
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公开(公告)号：EP1633774A1
公开(公告)日：2006-03-15
申请号：EP04737852.6
申请日：2004-06-18
申请人： Tranzyme Pharma Inc.
发明人： FRASER, Graeme , MARSAULT, Eric , PETERSON, Mark , HOVEYDA, Hamid , BEAUBIEN, Sylvie , BENAKLI, Kamel , DEZIEL, Robert
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 present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
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7.发明授权
公开(公告)号：EP2054429B1
公开(公告)日：2013-11-06
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
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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：EP1648922B3
公开(公告)日：2012-08-15
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：EP1648922A1
公开(公告)日：2006-04-26
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
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.
摘要翻译： 公开了含有特定构象控制元件的新型空间限定的大环化合物。 然后使用这些大环化合物的文库来选择与特定生物学目标呈现特异性相互作用的一种或多种大环化合物物种。 具体而言，公开了本发明的化合物作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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