-
1.发明申请公开(公告)号：US20080194672A1
公开(公告)日：2008-08-14
申请号：US12028611
申请日：2008-02-08
申请人： Hamid Hoveyda , Graeme L. Fraser , Kamel Benakli , Sophie Beauchemin , Martin Brassard , David Drutz , Eric Marsault , Luc Ouellet , Mark L. Peterson , Zhigang Wang
发明人： Hamid Hoveyda , Graeme L. Fraser , Kamel Benakli , Sophie Beauchemin , Martin Brassard , David Drutz , Eric Marsault , Luc Ouellet , Mark L. Peterson , Zhigang Wang
IPC分类号： A61K31/395 , C07D267/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P35/04 , A61P19/00 , A61P29/00 , A61P1/00 , A61P5/00 , C07C43/205
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.
摘要翻译： 本发明提供新的构象定义的大环化合物，其可以作为生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂。 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。
-
2.发明授权公开(公告)号：US09371297B2
公开(公告)日：2016-06-21
申请号：US12028611
申请日：2008-02-08
申请人： Hamid Hoveyda , Graeme L. Fraser , Kamel Benakli , Sophie Beauchemin , Martin Brassard , Eric Marsault , Luc Oullet , Mark L. Peterson , Zhigang Wang
发明人： Hamid Hoveyda , Graeme L. Fraser , Kamel Benakli , Sophie Beauchemin , Martin Brassard , Eric Marsault , Luc Oullet , Mark L. Peterson , Zhigang Wang
IPC分类号： C07K5/12 , 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 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.
摘要翻译： 本发明提供新的构象定义的大环化合物，其可以作为生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂。 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。
-
3.发明授权Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists 有权构象控制的生物活性大环小分子作为胃动素拮抗剂或生长素释放肽激动剂公开(公告)号：US07452862B2
公开(公告)日：2008-11-18
申请号：US10911221
申请日：2004-08-02
申请人： Pierre Deslongchamps , Yves Dory , Mark Peterson , Kamel Benakli , Eric Marsault , Luc Ouellet , Mahesh Ramaseshan , Martin Vézina , Daniel Fortin , Ruoxi Lan , Shigui Li , Gérald Villeneuve , Hamid Hoveyda , Sylvie Beaubien , Graeme L Fraser
发明人： Pierre Deslongchamps , Yves Dory , Mark Peterson , Kamel Benakli , Eric Marsault , Luc Ouellet , Mahesh Ramaseshan , Martin Vézina , Daniel Fortin , Ruoxi Lan , Shigui Li , Gérald Villeneuve , Hamid Hoveyda , Sylvie Beaubien , Graeme L Fraser
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种或多种与特定生物目标具有特异性相互作用的大环类物质。 特别地，根据本发明的化合物被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。
-
公开(公告)号：US20090240027A1
公开(公告)日：2009-09-24
申请号：US12273638
申请日：2008-11-19
申请人： Eric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
发明人： Eric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07K5/12 , C07D239/52
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R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 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：US09181298B2
公开(公告)日：2015-11-10
申请号：US12273638
申请日：2008-11-19
申请人： Eric Marsault , Kamel Benakli , Hamid Hoveyda , Mark Peterson , Sylvie Beaubien , Luc Oullet , Carl St-Louis , Sophie Beauchemin
发明人： Eric Marsault , Kamel Benakli , Hamid Hoveyda , Mark Peterson , Sylvie Beaubien , Luc Oullet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07C49/84 , C07C45/46 , A61K31/122 , C07K5/08 , A61K38/12 , A61K38/22 , C07D273/00 , C07D413/06 , C07D498/04 , C07K5/087 , C07K5/097
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R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 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：US20050137127A1
公开(公告)日：2005-06-23
申请号：US10911221
申请日：2004-08-02
申请人： Pierre Deslongchamps , Yves Dory , Mark Peterson , Kamel Benakli , Eric Marsault , Luc Ouellet , Mahesh Ramaseshan , Martin Vezina , Daniel Fortin , Ruoxi Lan , Shigui Li , Gerald Villeneuve , Hamid Hoveyda , Sylvie Beaubien
发明人： Pierre Deslongchamps , Yves Dory , Mark Peterson , Kamel Benakli , Eric Marsault , Luc Ouellet , Mahesh Ramaseshan , Martin Vezina , Daniel Fortin , Ruoxi Lan , Shigui Li , Gerald Villeneuve , Hamid Hoveyda , Sylvie Beaubien
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种或多种与特定生物目标具有特异性相互作用的大环类物质。 特别地，根据本发明的化合物被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。
-
公开(公告)号：US08440851B2
公开(公告)日：2013-05-14
申请号：US13036204
申请日：2011-02-28
申请人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
发明人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07C69/96 , C07C217/10
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种或多种与特定生物目标具有特异性相互作用的大环类物质。 特别地，根据本发明的化合物被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。
-
公开(公告)号：US20110237785A1
公开(公告)日：2011-09-29
申请号：US13036204
申请日：2011-02-28
申请人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
发明人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07H7/02 , C07C271/16 , C07D263/34 , C07D277/30 , C07D493/04 , C07C69/96 , C07D307/28
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种或多种与特定生物目标具有特异性相互作用的大环类物质。 特别地，根据本发明的化合物被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。
-
公开(公告)号：US08497242B2
公开(公告)日：2013-07-30
申请号：US13036484
申请日：2011-02-28
申请人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
发明人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： A61K38/25
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R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 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：US20110245459A1
公开(公告)日：2011-10-06
申请号：US13036484
申请日：2011-02-28
申请人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
发明人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07K5/12
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R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 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。
-
-
-
-
-
-
-
-
-
搜索结果
17 条记录 (耗时 0.038 秒)
