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公开(公告)号：US20150045325A1
公开(公告)日：2015-02-12
申请号：US14525396
申请日：2014-10-28
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译： 本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。 本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。
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公开(公告)号：US08013159B2
公开(公告)日：2011-09-06
申请号：US11920275
申请日：2006-05-15
申请人： Michel Belley , Jason Burch , John Colucci , Julie Farand , Mario Girard , Yongxin Han
发明人： Michel Belley , Jason Burch , John Colucci , Julie Farand , Mario Girard , Yongxin Han
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.
摘要翻译： 本发明涉及可用于治疗EP4介导的疾病或病症（例如急性和慢性疼痛，骨关节炎，类风湿性关节炎和癌症）的前列腺素E型受体拮抗剂的喹啉衍生物。 衍生物具有式（I）的以下结构：其中A和B表示氮原子或CH基团，条件是它们不能同时为CH，Q可以表示氮或碳原子，Y和Z 是氮原子，N（O）基或C（R5）基团。 还包括包含式（I）的衍生物的药物组合物。
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公开(公告)号：US20100298347A1
公开(公告)日：2010-11-25
申请号：US12743610
申请日：2008-12-01
申请人： Michel Belley , Denis Deschenes , Rejean Fortin , Jean-Francois Fournier , Sebastien Gagne , Yves Gareau , Jacques Yves Gauthier , Lianhai Li , Joel Robichaud , Michel Therien , Geoffrey K. Tranmer , Zhaoyin Wang
发明人： Michel Belley , Denis Deschenes , Rejean Fortin , Jean-Francois Fournier , Sebastien Gagne , Yves Gareau , Jacques Yves Gauthier , Lianhai Li , Joel Robichaud , Michel Therien , Geoffrey K. Tranmer , Zhaoyin Wang
IPC分类号： A61K31/519 , C07C63/72 , C07D333/34 , C07D333/22 , C07C63/42 , C07D317/54 , C07D409/12 , C07D487/04 , C07D249/08 , C07D211/94 , C07D211/32 , A61K31/192 , A61K31/381 , A61K31/194 , A61K31/36 , A61K31/4436 , A61K31/4196 , A61K31/451 , A61P3/10 , A61P5/50 , A61P3/04 , A61P3/00
CPC分类号： C07D211/34 , C07C65/24 , C07C65/30 , C07C65/40 , C07C69/76 , C07C69/94 , C07C317/44 , C07C317/46 , C07C323/62 , C07D211/52 , C07D249/08 , C07D317/60 , C07D333/16 , C07D333/24 , C07D333/34 , C07D487/04
摘要： Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.
摘要翻译： 结构式的取代的2-萘甲酸作为GPR105蛋白的生物活性的拮抗剂是有效的。 它们可用于治疗，控制或预防对该受体的拮抗作用有响应的病症，例如糖尿病，特别是2型糖尿病，胰岛素抵抗，高血糖症，脂质障碍，肥胖症，动脉粥样硬化和与代谢综合征有关的病症。
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4.发明申请公开(公告)号：US20100179173A1
公开(公告)日：2010-07-15
申请号：US12663556
申请日：2008-06-26
申请人： Daniel Guay , Christian Beaulieu , Michel Belley , Sheldon N. Crane , Jeancarlo De Luca , Rejean Fortin , Yves Gareau , Lianhai Li , Michel Therien , Geoffrey K. Tranmer , Vouy Linh Truong , Zhaoyin Wang
发明人： Daniel Guay , Christian Beaulieu , Michel Belley , Sheldon N. Crane , Jeancarlo De Luca , Rejean Fortin , Yves Gareau , Lianhai Li , Michel Therien , Geoffrey K. Tranmer , Vouy Linh Truong , Zhaoyin Wang
IPC分类号： A61K31/519 , C07D471/04 , A61P3/10
CPC分类号： C07D471/04
摘要： Fused pyrimidine compounds of structural formula (I) are effective as antagonists of the biological activity of the GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and Metabolic Syndrome.
摘要翻译： 结构式（I）的稠合嘧啶化合物作为GPR105蛋白质的生物活性的拮抗剂是有效的。 它们可用于治疗，控制或预防对该受体的拮抗作用有响应的病症，例如糖尿病，特别是2型糖尿病，胰岛素抵抗，高血糖症，脂质障碍，肥胖，动脉粥样硬化和代谢综合征。
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5.发明授权公开(公告)号：US06169188A
公开(公告)日：2001-01-02
申请号：US09422151
申请日：1999-10-21
申请人： Michel Belley , Jacques Yves Gauthier , Erich Grimm , Yves LeBlanc , Chun-Sing Li , Michel Therien , Cameron Black , Petpiboon Prasit , Cheuk-Kun Lau , Patrick Roy
发明人： Michel Belley , Jacques Yves Gauthier , Erich Grimm , Yves LeBlanc , Chun-Sing Li , Michel Therien , Cameron Black , Petpiboon Prasit , Cheuk-Kun Lau , Patrick Roy
IPC分类号： C07D31744
CPC分类号： C07D405/12 , C07C317/24 , C07C2601/08 , C07D307/58 , C07D307/60 , C07D307/62 , C07D307/64 , C07D307/66 , C07D307/68 , C07D307/83 , C07D307/94 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
摘要翻译： 本发明包括可用于治疗环加氧酶-2介导的疾病的新颖的式I化合物。本发明还包括用于治疗包含式I化合物的环氧合酶-2介导的疾病的某些药物组合物。
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6.发明授权
公开(公告)号：US6020343A
公开(公告)日：2000-02-01
申请号：US97543
申请日：1998-06-15
申请人： Michel Belley , Jacques Yves Gauthier , Erich Grimm , Yves LeBlanc , Chun-Sing Li , Michel Therien , Cameron Black , Petpiboon Prasit , Cheuk-Kun Lau , Patrick Roy
发明人： Michel Belley , Jacques Yves Gauthier , Erich Grimm , Yves LeBlanc , Chun-Sing Li , Michel Therien , Cameron Black , Petpiboon Prasit , Cheuk-Kun Lau , Patrick Roy
IPC分类号： C07C317/24 , C07D307/58 , C07D307/60 , C07D307/62 , C07D307/64 , C07D307/66 , C07D307/68 , C07D307/83 , C07D307/94 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/665
CPC分类号： C07D405/12 , C07C317/24 , C07D307/58 , C07D307/60 , C07D307/62 , C07D307/64 , C07D307/66 , C07D307/68 , C07D307/83 , C07D307/94 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07C2101/08
摘要： The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
摘要翻译： 本发明包括可用于治疗环氧合酶-2介导的疾病的新颖的式I化合物。 本发明还包括用于治疗包含式I化合物的环氧合酶-2介导的疾病的某些药物组合物。
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7.发明授权Heteroaryl and haloaryl quinoline derivatives of cyclopropaneacetic acid as leukotriene antagonists 失效环丙烷乙酸的杂芳基和卤代芳基喹啉衍生物作为白三烯拮抗剂
公开(公告)号：US5438141A
公开(公告)日：1995-08-01
申请号：US65734
申请日：1993-05-21
申请人： Marc LaBell , Yves LeBlanc , Michel Belley , Erich L. Grimm , Daniel Guay , Yi B. Xiang
发明人： Marc LaBell , Yves LeBlanc , Michel Belley , Erich L. Grimm , Daniel Guay , Yi B. Xiang
IPC分类号： C07D215/12 , A61K31/47 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/18 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/48 , C07D401/10 , C07D401/12 , C07D405/10 , C07D417/10 , C07D401/06 , A61K31/41 , C07D215/16
CPC分类号： C07D215/18
摘要： Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
摘要翻译： 具有式I的化合物：I是白三烯的作用的拮抗剂。 这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。 它们也可用于治疗心绞痛，脑痉挛，肾小球肾炎，肝炎，内毒素血症，葡萄膜炎和同种异体移植排斥。
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公开(公告)号：US08168815B2
公开(公告)日：2012-05-01
申请号：US12518899
申请日：2008-01-24
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
IPC分类号： C07D215/38
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译： 本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。 本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。
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公开(公告)号：US20100022477A1
公开(公告)日：2010-01-28
申请号：US12518899
申请日：2008-01-24
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译： 本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。 本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。
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10.发明授权Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment 失效羧酸和酰基磺酰胺，含有这些化合物的组合物和处理方法公开(公告)号：US06242493B1
公开(公告)日：2001-06-05
申请号：US09266047
申请日：1999-03-10
申请人： Yves Gareau , Marc LaBelle , Helene Juteau , Michel Gallant , Nicolas LaChance , Michel Belley
发明人： Yves Gareau , Marc LaBelle , Helene Juteau , Michel Gallant , Nicolas LaChance , Michel Belley
IPC分类号： C07C31151
CPC分类号： C07D213/70 , C07C311/29 , C07D209/08 , C07D209/18 , C07D215/18 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/32 , C07D307/64 , C07D333/34 , C07D333/60 , C07D409/12 , C07D417/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.
摘要翻译： 公开了式I化合物及其药学上可接受的盐，水合物和酯。该化合物可用于治疗或预防前列腺素介导的疾病。 还包括含有这些化合物和治疗方法的药物组合物。
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