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1. 发明授权

US08497242B2 Processes for intermediates for macrocyclic compounds 有权
标题翻译：大环化合物中间体的方法
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。

2. 发明授权

US08440851B2 Spatially-defined macrocyclic compounds useful for drug discovery 有权
标题翻译：用于药物发现的空间定义的大环化合物
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。

3. 发明申请

US20110237785A1 SPATIALLY-DEFINED MACROCYCLIC COMPOUNDS USEFUL FOR DRUG DISCOVERY 有权
标题翻译：用于药物发现的空间定义的大环化合物
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。

4. 发明申请

US20110245459A1 Processes for Intermediates for Macrocyclic Compounds 有权
标题翻译：大环化合物中间体的制备方法
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。

5. 发明申请

US20090240027A1 INTERMEDIATES FOR MACROCYCLIC COMPOUNDS 有权
标题翻译：大环化合物的中间体
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。

6. 发明申请

US20090198050A1 Macrocyclic Modulators of the Ghrelin Receptor 审中-公开
标题翻译：生长素释放肽受体的大环调节剂
公开(公告)号：US20090198050A1
公开(公告)日：2009-08-06
申请号：US12263179
申请日：2008-10-31
申请人： Eric Marsault , Luc Ouellet , Carl St-Louis , Sylvie Beaubien , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Shridhar Bhat
发明人： Eric Marsault , Luc Ouellet , Carl St-Louis , Sylvie Beaubien , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Shridhar Bhat
IPC分类号： C07D225/04 , C07D487/04 , C07C229/34 , C07D311/04
CPC分类号： C07K5/0808 , A61K38/00 , 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.
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。

7. 发明授权

US09181298B2 Intermediates for macrocyclic compounds 有权
标题翻译：大环化合物的中间体
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。

8. 发明申请

US20100093720A1 MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS 有权
标题翻译：用于治疗胃肠疾病的动物感受因子的大分子拮抗剂
公开(公告)号：US20100093720A1
公开(公告)日：2010-04-15
申请号：US12440802
申请日：2007-09-11
申请人： Eric Marsault , Graeme L. Fraser , Kamel Benakli , Carl St-Louis , Alain Rouillard , Helmut Thomas
发明人： Eric Marsault , Graeme L. Fraser , Kamel Benakli , Carl St-Louis , Alain Rouillard , Helmut Thomas
IPC分类号： A61K31/5377 , C07D487/00 , A61K31/33 , A61P1/00
CPC分类号： C07K5/0812 , A61K38/00 , C07C271/16 , C07D273/00 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.
摘要翻译：本发明提供了构象定义的大环化合物，其与胃动素受体结合和/或是功能性调节剂，包括亚型，同种型和/或其变体。这些大环化合物至少具有足够的药理学性质，可用作一系列疾病适应症的治疗剂。特别地，这些化合物可用于治疗和预防以高肌钙蛋白血症和/或胃肠动力学特征为特征的疾病，包括但不限于腹泻，癌症治疗相关性腹泻，癌症引起的腹泻，化学疗法诱发的腹泻，放射性肠炎，辐射诱发的腹泻，应激性腹泻，慢性腹泻，艾滋病相关性腹泻，艰难梭菌相关性腹泻，旅行者腹泻，图形与宿主病引起的腹泻，其他类型的腹泻，消化不良，肠易激综合征，化疗诱发的恶心和呕吐（呕吐）和术后恶心呕吐和功能性胃肠道疾病。此外，这些化合物具有治疗以肠胃吸收不良为特征的疾病和病症的用途，例如短肠综合症，乳糜泻和恶病质。所述化合物还可用于治疗炎性疾病和胃肠道疾病，例如炎性肠病，溃疡性结肠炎，克罗恩病和胰腺炎。因此，还提供了治疗这些病症的方法和包括本发明化合物的药物组合物。

9. 发明授权

US09133235B2 Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders 有权
标题翻译：胃动素障碍的胃动素受体大环拮抗剂
公开(公告)号：US09133235B2
公开(公告)日：2015-09-15
申请号：US12440802
申请日：2007-09-11
申请人： Eric Marsault , Graeme L. Fraser , Kamel Benakli , Carl St-Louis , Alain Rouillard , Helmut Thomas
发明人： Eric Marsault , Graeme L. Fraser , Kamel Benakli , Carl St-Louis , Alain Rouillard , Helmut Thomas
IPC分类号： C07K5/087 , C07C271/16 , C07D273/00 , C07D413/06 , C07D417/12 , A61K38/00
CPC分类号： C07K5/0812 , A61K38/00 , C07C271/16 , C07D273/00 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.
摘要翻译：本发明提供了构象定义的大环化合物，其与胃动素受体结合和/或是功能性调节剂，包括亚型，同种型和/或其变体。这些大环化合物至少具有足够的药理学性质，可用作一系列疾病适应症的治疗剂。特别地，这些化合物可用于治疗和预防以高肌钙蛋白血症和/或胃肠动力学特征为特征的疾病，包括但不限于腹泻，癌症治疗相关性腹泻，癌症引起的腹泻，化学疗法诱发的腹泻，放射性肠炎，辐射诱发的腹泻，应激性腹泻，慢性腹泻，艾滋病相关性腹泻，艰难梭菌相关性腹泻，旅行者腹泻，图形与宿主病引起的腹泻，其他类型的腹泻，消化不良，肠易激综合征，化疗诱发的恶心和呕吐（呕吐）和术后恶心呕吐和功能性胃肠道疾病。此外，这些化合物具有治疗以肠胃吸收不良为特征的疾病和病症的用途，例如短肠综合症，乳糜泻和恶病质。所述化合物还可用于治疗炎性疾病和胃肠道疾病，例如炎性肠病，溃疡性结肠炎，克罗恩病和胰腺炎。因此，还提供了治疗这些病症的方法和包括本发明化合物的药物组合物。

10. 发明授权

US08334256B2 Pharmaceutical salts of macrocyclic modulators of the ghrelin receptor 有权
标题翻译：生长素释放肽受体的大环调节剂的药物盐
公开(公告)号：US08334256B2
公开(公告)日：2012-12-18
申请号：US12351395
申请日：2009-01-09
申请人： Eric Marsault , Carl St-Louis
发明人： Eric Marsault , Carl St-Louis
IPC分类号： A61K38/25 , C09F1/04
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.
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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