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

IPC分类号： C07K5/08 ,  C07K5/12

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

申请人： Tranzyme Pharma, Inc.

发明人： HOVEYDA, Hamid ,  PETERSON, Mark ,  FRASER, Graeme ,  RAMASESHAN, Mahesh

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

申请人： Tranzyme Pharma, Inc.

发明人： HOVEYDA, Hamid ,  PETERSON, Mark ,  FRASER, Graeme ,  RAMASESHAN, Mahesh

IPC分类号： C07K5/12 ,  A61K38/12 ,  A61P1/14

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：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

IPC分类号： C07K5/08 ,  C07K5/12

CPC分类号： C07K5/0808 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/0827

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

申请人： Tranzyme Pharma, Inc.

发明人： HOVEYDA, Hamid ,  PETERSON, Mark ,  FRASER, Graeme ,  RAMASESHAN, Mahesh

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：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

IPC分类号： C07K5/00 ,  C07K5/08 ,  C07K1/04

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：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

IPC分类号： C07K5/08 ,  C07K5/12

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：EP1648923B1

公开(公告)日：2008-12-31

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

IPC分类号： C07K5/00 ,  C07K5/08 ,  C07K1/04

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.

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

IPC分类号： C07K5/00 ,  C07K5/08 ,  C07K1/04

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。