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1.发明授权Methods of treating cachexia with macrocyclic modulators of the ghrelin receptor 有权用生长素释放肽受体的大环调节剂治疗恶病质的方法公开(公告)号：US08349887B2
公开(公告)日：2013-01-08
申请号：US13173929
申请日：2011-06-30
IPC分类号： A01N43/02
CPC分类号： C07K5/0827 , A61K31/395 , A61K31/4545 , A61K31/55 , A61K38/06 , A61K38/12 , C07K5/0808 , C07K5/0812 , Y02A50/395
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.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（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，遗传疾病，过度增殖性疾病和炎症性疾病。
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公开(公告)号：US07521420B2
公开(公告)日：2009-04-21
申请号：US10872142
申请日：2004-06-18
申请人： Graeme L. Fraser , Éric Marsault , Mark Peterson , Hamid Hoveyda , Sylvie Beaubien , Kamel Benakli , Robert Dèziel
发明人： Graeme L. Fraser , Éric Marsault , Mark Peterson , Hamid Hoveyda , Sylvie Beaubien , Kamel Benakli , Robert Dèziel
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。
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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。
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公开(公告)号：US20060025566A1
公开(公告)日：2006-02-02
申请号：US11149731
申请日：2005-06-10
申请人： Hamid Hoveyda , Mark Peterson , Graeme Fraser , Mahesh Ramaseshan
发明人： Hamid Hoveyda , Mark Peterson , Graeme Fraser , Mahesh Ramaseshan
IPC分类号： C07K5/12
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.
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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。
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公开(公告)号：US20130211045A1
公开(公告)日：2013-08-15
申请号：US13716748
申请日：2012-12-17
申请人： TRANZYME PHARMA INC.
发明人： Eric Marsault , Carl St-Louis
IPC分类号： C07K1/107 , C07C311/08 , C07D213/64 , C07C217/62 , C07C271/16 , C07F7/18
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.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（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，遗传疾病，过度增殖性疾病和炎症性疾病。
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公开(公告)号：US08129561B2
公开(公告)日：2012-03-06
申请号：US12273648
申请日：2008-11-19
申请人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
发明人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
IPC分类号： C07C69/76
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。
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8.发明授权Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders 有权使用生长素释放肽受体的大环激动剂治疗胃肠动力障碍的方法公开(公告)号：US08088733B2
公开(公告)日：2012-01-03
申请号：US11774185
申请日：2007-07-06
CPC分类号： A61K31/33
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective agonists of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Such compounds are useful as medicaments for treatment and prevention of a range of medical conditions characterized by disturbed gastrointestinal motility including, but not limited to, post-surgical gastroparesis and post-operative ileus in combination with opioid-induced bowel dysfunction. These agents are effective for multiple disorders at dose levels equivalent to those required to treat a single disorder.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性激动剂的新的构象定义的大环化合物。 这些化合物可用作治疗和预防特征为紊乱的胃肠蠕动的一系列医学病症的药物，包括但不限于手术后胃轻瘫和与阿片样物质诱导的肠功能障碍联合的术后肠梗阻。 这些药剂对于与治疗单一病症所需的剂量水平相当的剂量水平对多种疾病有效。
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公开(公告)号：US20090137835A1
公开(公告)日：2009-05-28
申请号：US12273648
申请日：2008-11-19
申请人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
发明人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
IPC分类号： C07C69/76 , C07C211/27 , C07C59/48
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。
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公开(公告)号：US07491695B2
公开(公告)日：2009-02-17
申请号：US11149512
申请日：2005-06-10
CPC分类号： C07K5/0827 , A61K31/395 , A61K31/4545 , A61K31/55 , A61K38/06 , A61K38/12 , C07K5/0808 , C07K5/0812 , Y02A50/395
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.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（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，遗传疾病，过度增殖性疾病和炎症性疾病。
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