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1.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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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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3.发明授权Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors 失效具有含硫取代基的芳基二氟甲基膦酸作为PTP-1B抑制剂公开(公告)号：US06498151B2
公开(公告)日：2002-12-24
申请号：US09813489
申请日：2001-03-21
申请人： Chun Sing Li , Christopher Bayly , Jacques Yves Gauthier , Yves Leblanc , Cheuk Kun Lau , Patrick Roy , Michel Therien , Zhaoyin Wang , Claude Dufresne , Rejean Fortin
发明人： Chun Sing Li , Christopher Bayly , Jacques Yves Gauthier , Yves Leblanc , Cheuk Kun Lau , Patrick Roy , Michel Therien , Zhaoyin Wang , Claude Dufresne , Rejean Fortin
IPC分类号： C07D23995
CPC分类号： C07F9/65583 , A61K31/66 , A61K45/06 , C07F9/3882 , C07F9/4056 , C07F9/5537 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/6506 , C07F9/65068 , C07F9/6512 , C07F9/65128 , C07F9/6518 , C07F9/6524 , C07F9/65312 , C07F9/65318 , C07F9/6539 , C07F9/65395 , C07F9/6552 , C07F9/65522 , A61K2300/00
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 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型化合物，其是PTP-1B酶的抑制剂。本发明还包括治疗或预防PTP-1B介导的疾病包括糖尿病的药物组合物和方法。
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公开(公告)号：US08318748B2
公开(公告)日：2012-11-27
申请号：US13115462
申请日：2011-05-25
申请人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
发明人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
IPC分类号： A61K31/4965 , A61K31/66 , A61K31/44 , A61K31/445 , A61K31/425 , A61K31/415
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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公开(公告)号：US20110230446A1
公开(公告)日：2011-09-22
申请号：US13115462
申请日：2011-05-25
申请人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Chirstophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
发明人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Chirstophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
IPC分类号： A61K31/277 , A61K31/495 , A61K31/4418 , A61K31/426 , A61K31/4174 , A61K31/663 , A61P19/08 , A61P19/10 , A61P1/02 , A61P19/02 , A61P35/00 , A61P19/00
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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公开(公告)号：US06329421B1
公开(公告)日：2001-12-11
申请号：US08793931
申请日：1997-02-25
申请人： Petpiboon Prasit , Daniel Guay , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Petpiboon Prasit , Daniel Guay , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： A61K3134
CPC分类号： C07D307/79 , C07D209/10 , C07D333/18 , C07D495/04
摘要： The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
摘要翻译： 本发明包括式I的新化合物以及治疗环加氧酶-2介导的疾病的方法，包括向需要这种治疗无需治疗有效量的式I化合物的患者施用本发明还包括 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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公开(公告)号：US20080188529A1
公开(公告)日：2008-08-07
申请号：US12082104
申请日：2008-04-08
申请人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
发明人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
IPC分类号： A61K31/4418 , C07C233/40 , A61K31/165 , C07D213/57
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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公开(公告)号：US20050240023A1
公开(公告)日：2005-10-27
申请号：US10505796
申请日：2003-02-28
申请人： Christopher Bayly , Cameron Black , Serge Leger , Chun Ku , Dan McKay , Christophe Mellon , Jacques Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien
发明人： Christopher Bayly , Cameron Black , Serge Leger , Chun Ku , Dan McKay , Christophe Mellon , Jacques Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien
IPC分类号： C07D295/12 , A61K31/275 , A61K31/381 , A61K31/404 , A61K31/417 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K45/00 , A61P1/02 , A61P3/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C255/60 , C07C259/10 , C07C311/37 , C07C317/32 , C07C317/36 , C07D209/08 , C07D211/26 , C07D211/38 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/06 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D295/135 , C07D295/22 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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公开(公告)号：US07973037B2
公开(公告)日：2011-07-05
申请号：US12082104
申请日：2008-04-08
申请人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
发明人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
IPC分类号： A61K31/535 , A61K31/497 , A61K31/435 , A61K31/385 , C07D265/30 , C07D241/04 , C07D211/08 , C07D333/02 , C07D255/03
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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公开(公告)号：US07375134B2
公开(公告)日：2008-05-20
申请号：US10505796
申请日：2003-02-28
申请人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien
发明人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Christophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien
IPC分类号： A01N37/34
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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