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公开(公告)号：US5945521A
公开(公告)日：1999-08-31
申请号：US948152
申请日：1997-10-09
申请人： George Just , Zhili Xin , Eric Marsault , Yi Jin
发明人： George Just , Zhili Xin , Eric Marsault , Yi Jin
IPC分类号： C07H21/04 , B01J31/02 , C07F9/141 , C07F9/6584 , C07H9/04 , C07H9/06 , C07H19/10 , C07H21/00 , C12N15/09 , C12Q1/68 , C07H1/02
CPC分类号： C07H9/04 , C07F9/1411 , C07F9/65846 , C07H19/10 , C07H21/00 , C07H9/06
摘要： Methods and intermediates for the preparation of oligomers containing diastereomerically enriched phosphorothioate linkages are disclosed.
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公开(公告)号：US20120226067A1
公开(公告)日：2012-09-06
申请号：US13412148
申请日：2012-03-05
申请人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
发明人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
IPC分类号： C07C271/16 , C07C213/08 , C07C269/06 , C07C217/62 , C07C213/02
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 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）的化合物，并且可用于治疗与该受体相关并与运动功能障碍相关的病症。
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公开(公告)号：US20120165566A1
公开(公告)日：2012-06-28
申请号：US13411979
申请日：2012-03-05
申请人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
发明人： Eric Marsault , Luc Ouellet , Hamid R. Hoveyda
IPC分类号： C07C69/734 , C07C209/08 , C07C59/64 , C07C69/736
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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24.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：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：US06596857B1
公开(公告)日：2003-07-22
申请号：US09452604
申请日：1999-12-01
申请人： George Just , Zhili Xin , Eric Marsault , Yi Jin
发明人： George Just , Zhili Xin , Eric Marsault , Yi Jin
IPC分类号： C07H2100
CPC分类号： C07H9/04 , C07F9/1411 , C07F9/65846 , C07H9/06 , C07H19/10 , C07H21/00
摘要： Methods and intermediates for the preparation of oligomers containing diastereomerically enriched phosphorothioate linkages are disclosed.
摘要翻译： 公开了制备含有非对映体富集的硫代磷酸酯键的低聚物的方法和中间体。
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27.发明授权Matriptase inhibitors and uses thereof against orthomyxoviridae infections 有权Matriptase抑制剂及其针对正粘病毒科感染的用途公开(公告)号：US09365853B2
公开(公告)日：2016-06-14
申请号：US14118768
申请日：2012-05-28
申请人： Martin Richter , Richard Leduc , Eloic Colombo , Eric Marsault
发明人： Martin Richter , Richard Leduc , Eloic Colombo , Eric Marsault
IPC分类号： C07D277/04 , C07D277/60 , C07D277/00 , C07D263/60 , C07D263/00 , C07D249/08 , C07D249/10 , A61K31/425 , A61K31/42 , A61K31/41 , C12N15/113 , A61K45/06 , A61K31/713 , C12N9/64 , A61K31/427 , C07K16/40 , A61K38/07 , C07K5/11 , C07K5/062 , C07K5/093 , C07K5/09 , C07K5/072 , A61K31/428 , A61K38/06 , A61K9/00 , A61K39/00 , A61K38/00
CPC分类号： C12N15/1131 , A61K9/0075 , A61K9/0078 , A61K31/427 , A61K31/428 , A61K31/713 , A61K38/00 , A61K38/06 , A61K38/07 , A61K45/06 , A61K2039/505 , C07K5/06026 , C07K5/06095 , C07K5/06104 , C07K5/0817 , C07K5/0819 , C07K5/1019 , C07K16/40 , C07K2317/565 , C07K2317/76 , C12N9/6424 , C12N2310/14 , A61K2300/00 , A61L2300/00
摘要： The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.
摘要翻译： 本发明提供了用于治疗和预防正义粘病毒感染如流感感染的基质酶抑制剂和组合物。 本发明还提供新颖的化合物，组合物，使用方法，用途和用于抑制matriptase的试剂盒。 这样的化合物可用于治疗和预防正义粘病毒感染，例如流感感染，以及用于抑制肿瘤生长，进展和/或转移。
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28.发明申请公开(公告)号：US20140086936A1
公开(公告)日：2014-03-27
申请号：US14118768
申请日：2012-05-28
申请人： Martin Richter , Richard Leduc , Eloic Colombo , Eric Marsault
发明人： Martin Richter , Richard Leduc , Eloic Colombo , Eric Marsault
CPC分类号： C12N15/1131 , A61K9/0075 , A61K9/0078 , A61K31/427 , A61K31/428 , A61K31/713 , A61K38/00 , A61K38/06 , A61K38/07 , A61K45/06 , A61K2039/505 , C07K5/06026 , C07K5/06095 , C07K5/06104 , C07K5/0817 , C07K5/0819 , C07K5/1019 , C07K16/40 , C07K2317/565 , C07K2317/76 , C12N9/6424 , C12N2310/14 , A61K2300/00 , A61L2300/00
摘要： The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.
摘要翻译： 本发明提供了用于治疗和预防正义粘病毒感染如流感感染的基质酶抑制剂和组合物。 本发明还提供新颖的化合物，组合物，使用方法，用途和用于抑制matriptase的试剂盒。 这样的化合物可用于治疗和预防正义粘病毒感染，例如流感感染，以及用于抑制肿瘤生长，进展和/或转移。
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29.发明申请Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same 审中-公开大环素Ghrelin受体拮抗剂和反激动剂及其使用方法公开(公告)号：US20110105389A1
公开(公告)日：2011-05-05
申请号：US12916205
申请日：2010-10-29
申请人： Hamid R. Hoveyda , Eric Marsault , Helmut Thomas , Graeme Fraser , Sylvie Beaubien , Axel Mathieu , Julien Beignet , Marc-André Bonin , Serge Phoenix , David Drutz , Mark Peterson , Sophie Beauchemin , Martin Brassard , Martin Vezina
发明人： Hamid R. Hoveyda , Eric Marsault , Helmut Thomas , Graeme Fraser , Sylvie Beaubien , Axel Mathieu , Julien Beignet , Marc-André Bonin , Serge Phoenix , David Drutz , Mark Peterson , Sophie Beauchemin , Martin Brassard , Martin Vezina
IPC分类号： A61K38/12 , C07K5/08 , C07K5/087 , A61K38/26 , A61P3/04 , A61P3/10 , A61P25/00 , A61P25/32 , A61P9/00 , A61P1/00 , A61P3/00 , A61P1/16 , A61P5/00 , A61P25/30
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0804 , 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 (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse 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, obesity and obesity-associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system 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（GRLN，生长激素促分泌素受体，GHS-R1a和亚型，同种型和/或其变体）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拮抗剂或反向激动剂，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/或内分泌紊乱，肥胖症和肥胖相关疾病，食欲或饮食 疾病，成瘾性疾病，心血管疾病，胃肠道疾病，遗传疾病，过度增殖性疾病，中枢神经系统疾病和炎症性疾病。
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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。
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