-
1.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.
-
公开(公告)号：EP1773869B9
公开(公告)日：2013-01-23
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
-
公开(公告)号：EP1773869A1
公开(公告)日：2007-04-18
申请号：EP05785185.9
申请日：2005-06-13
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.
-
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
-
5.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.
-
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.
-
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。
-
公开(公告)号：EP1648923A1
公开(公告)日：2006-04-26
申请号：EP04761607.3
申请日：2004-08-02
申请人： Tranzyme Pharma Inc.
发明人： DESLONGCHAMPS, Pierre , DORY, Yves , OUELLET, Luc , VILLENEUVE, Gérald , RAMASESHAN, Mahesh , FORTIN, Daniel , PETERSON, Mark , HOVEYDA, Hamid , BEAUBIEN, Sylvie , MARSAULT, Eric
CPC分类号： C07K1/047 , C07K5/0802
摘要： 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.
摘要翻译： 公开了结合肽键替代物的新型空间定义的大环化合物。 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。
-
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.
-
10.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.
-
-
-
-
-
-
-
-
-
搜索结果
12 条记录 (耗时 0.032 秒)
