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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：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：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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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：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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7.发明授权Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases 失效使用环氧合酶抑制剂治疗神经变性疾病
公开(公告)号：US5840746A
公开(公告)日：1998-11-24
申请号：US926291
申请日：1997-09-05
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/08 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C323/49 , C07D209/26 , C07D275/02 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04 , A61K31/38 , A61K31/27 , A61K31/34
CPC分类号： C07D275/02 , A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/08 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C323/49 , C07D209/26 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04 , C07C2101/08 , C07C2102/08
摘要： The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I: ##STR1##
摘要翻译： 本发明提供治疗神经变性疾病，特别是阿尔茨海默病的方法，其包括向有需要的人施用治疗有效量的非类固醇COX-II抑制剂。 尽管可以使用大范围的COX-II抑制剂，但优选使用式I的化合物：
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公开(公告)号：US5767291A
公开(公告)日：1998-06-16
申请号：US738144
申请日：1996-10-25
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
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.
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9.发明授权Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases 失效使用环氧合酶抑制剂治疗神经变性疾病公开(公告)号：US06486194B2
公开(公告)日：2002-11-26
申请号：US09796211
申请日：2001-02-28
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： A61K3138
CPC分类号： C07D275/02 , A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C2601/08 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04
摘要： The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I:
摘要翻译： 本发明提供治疗神经变性疾病，特别是阿尔茨海默病的方法，其包括向有需要的人施用治疗有效量的非类固醇COX-II抑制剂。 尽管可以使用大范围的COX-II抑制剂，但优选使用式I的化合物：
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公开(公告)号：US5710140A
公开(公告)日：1998-01-20
申请号：US699142
申请日：1996-08-16
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： C07D333/06 , A61K31/00 , A61K31/10 , A61K31/12 , A61K31/122 , A61K31/18 , A61K31/19 , A61K31/255 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/425 , A61K31/426 , A61K31/66 , A61P1/00 , A61P1/02 , A61P1/04 , A61P7/04 , A61P11/06 , A61P15/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P43/00 , C07C20060101 , C07C13/08 , C07C13/10 , C07C305/18 , C07C307/02 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C311/46 , C07C311/49 , C07C311/51 , C07C317/10 , C07C317/24 , C07C323/29 , C07D207/26 , C07D207/333 , C07D207/38 , C07D207/444 , C07D207/448 , C07D275/02 , C07D277/02 , C07D277/22 , C07D277/24 , C07D277/26 , C07D307/33 , C07D307/38 , C07D307/58 , C07D309/32 , C07D333/04 , C07D333/12 , C07D333/16 , C07D333/18 , C07D333/24 , C07D333/38 , C07D333/40 , C07D405/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D503/04 , C07F9/40 , C07F9/547 , C07F9/572 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/655 , A61K31/675 , C07F9/02
CPC分类号： C07D275/02 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04 , 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.
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