-
公开(公告)号：US09493505B2
公开(公告)日：2016-11-15
申请号：US14530311
申请日：2014-10-31
发明人： Eric Marsault , Carl St-Louis
IPC分类号： A61K38/12 , C07K16/00 , C07K5/08 , C07K1/107 , C07C271/16 , C07F7/18 , C07D213/64 , C07C217/62 , C07C311/08 , C07D273/00 , A61K38/25 , A61K38/30 , A61K45/06 , A61K38/06 , C07K5/087
CPC分类号： C07K5/08 , A61K38/06 , A61K38/25 , A61K38/30 , A61K45/06 , C07C217/62 , C07C271/16 , C07C311/08 , C07D213/64 , C07D273/00 , C07F7/1804 , C07K1/1077 , C07K5/0812 , C07K5/0827 , A61K2300/00
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：US20150148290A1
公开(公告)日：2015-05-28
申请号：US14530311
申请日：2014-10-31
发明人： Eric Marsault , Carl St-Louis
IPC分类号： C07K5/08
CPC分类号： C07K5/08 , A61K38/06 , A61K38/25 , A61K38/30 , A61K45/06 , C07C217/62 , C07C271/16 , C07C311/08 , C07D213/64 , C07D273/00 , C07F7/1804 , C07K1/1077 , C07K5/0812 , C07K5/0827 , A61K2300/00
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：US10258602B2
公开(公告)日：2019-04-16
申请号：US15938038
申请日：2018-03-28
发明人： Hamid Hoveyda , Graeme Fraser , Kamel Benakli , Eric Marsault , Mark L. Peterson
IPC分类号： A61K38/00 , A61K31/395 , C07D273/00 , C07C271/16 , C07C215/42 , C07C215/54 , C07D413/06 , C07D498/04 , C07D498/16
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that can function as 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, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
-
公开(公告)号：US09949949B2
公开(公告)日：2018-04-24
申请号：US15178303
申请日：2016-06-09
发明人： Hamid Hoveyda , Graeme Fraser , Kamel Benakli , Eric Marsault , Mark L. Peterson
IPC分类号： C07K5/12 , A61K31/395 , C07D273/00 , C07C271/16 , C07C215/42 , C07C215/54 , C07D413/06 , C07D498/04 , C07D498/16
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 provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone sceretagogue 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, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
-
公开(公告)号：US20160221927A1
公开(公告)日：2016-08-04
申请号：US14873056
申请日：2015-10-01
发明人： Eric Marsault , Kamel Benakli , Hamid Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Oullet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07C213/08 , C07C41/18 , C07C67/343
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 described 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R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在说明书中描述。 本发明还涉及作为胃动素受体的拮抗剂的式（I）化合物，并且可用于治疗与该受体相关并伴有或具有运动功能障碍的病症。
-
公开(公告)号：US20180228768A1
公开(公告)日：2018-08-16
申请号：US15938038
申请日：2018-03-28
发明人： Hamid Hoveyda , Graeme Fraser , Kamel Benakli , Eric Marsault , Mark L. Peterson
IPC分类号： A61K31/395 , C07C271/16 , C07C215/42 , C07C215/54 , C07D273/00 , C07D498/04 , C07D498/16 , C07D413/06
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 provides novel conformationally-defined macrocyclic compounds that can function as 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, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
-
公开(公告)号：US10040751B2
公开(公告)日：2018-08-07
申请号：US14873056
申请日：2015-10-01
发明人： Eric Marsault , Kamel Benakli , Hamid Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： A01N29/12 , A61K31/03 , C07C213/08 , A61K38/12 , A61K38/22 , C07D273/00 , C07D413/06 , C07D498/04 , C07K5/087 , C07K5/097 , C07K5/08 , C07C41/18 , C07C67/343
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 described 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.
-
8.发明申请公开(公告)号：US20170042858A1
公开(公告)日：2017-02-16
申请号：US15178303
申请日：2016-06-09
发明人： Hamid Hoveyda , Graeme Fraser , Kamel Benakli , Eric Marsault , Mark L. Peterson
IPC分类号： A61K31/395
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 provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone sceretagogue 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, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
摘要翻译： 本发明提供可用作生长素释放肽受体（生长激素神经递质受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病， 中枢神经系统疾病，骨骼疾病，遗传疾病，过度增殖性疾病和炎症性疾病。
-
-
-
-
-
-
-
搜索结果
8 条记录 (耗时 0.023 秒)