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公开(公告)号：US20070293578A1
公开(公告)日：2007-12-20
申请号：US11791250
申请日：2005-11-18
申请人： Jacques Gauthier , Chun Li , Christophe Mellon
发明人： Jacques Gauthier , Chun Li , Christophe Mellon
IPC分类号： A61K31/165 , A61P19/00 , C07C237/02
CPC分类号： C07C255/46 , C07C2601/02
摘要： This invention relates to a novel class of compounds, diagrammed below, wherein R1, R2, R3, R4, R5, R6, R7, D and n are defined therein, which are cysteine protein 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 reportion is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，如下所示，其中R 1，R 2，R 3，R 4， 其中定义为半胱氨酸蛋白抑制剂，包括但不限于，其中R 6，R 6，R 6，R 7， 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出骨抑制的疾病，例如骨质疏松症。
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公开(公告)号：US20060111440A1
公开(公告)日：2006-05-25
申请号：US11282536
申请日：2005-11-18
申请人： Jacques Gauthier , Chun Li , Christophe Mellon
发明人： Jacques Gauthier , Chun Li , Christophe Mellon
IPC分类号： A61K31/277 , A61K31/275 , C07C255/42
CPC分类号： C07C255/46 , C07C2601/02
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：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：US08518964B2
公开(公告)日：2013-08-27
申请号：US12085331
申请日：2006-11-17
申请人： Jean-Francois Truchon , Nicolas Lachance , Cheuk Lau , Yves Leblanc , Christophe Mellon , Patrick Roy , Elise Isabel , Ryan D Otte , Jonathan R Young
发明人： Jean-Francois Truchon , Nicolas Lachance , Cheuk Lau , Yves Leblanc , Christophe Mellon , Patrick Roy , Elise Isabel , Ryan D Otte , Jonathan R Young
IPC分类号： A61K31/437 , A61K31/444
CPC分类号： C07D491/10 , C07D471/04
摘要： The present invention provides inhibitors of kinases, specifically IκB kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-κB-mediated diseases.
摘要翻译： 本发明提供激酶抑制剂，特别是IkappaB激酶，JAK1，JAK2，JAK3和TYK2。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物施用于需要治疗骨髓增生性疾病，癌症或NF-κB介导的疾病的患者来抑制所述激酶活性的方法。
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公开(公告)号：US20110165632A1
公开(公告)日：2011-07-07
申请号：US12993341
申请日：2009-05-18
申请人： Louis-Charles Campeau , John Y. Chung , Danny Gauvreau , Melina Girardin-Rondeau , Gregory Hughes , Kevin M. Maloney , Christophe Mellon , Jeffrey C. Moore , Paul O'Shea , Stephane Quellet
发明人： Louis-Charles Campeau , John Y. Chung , Danny Gauvreau , Melina Girardin-Rondeau , Gregory Hughes , Kevin M. Maloney , Christophe Mellon , Jeffrey C. Moore , Paul O'Shea , Stephane Quellet
IPC分类号： C12P17/16 , C07D401/14
CPC分类号： C07D401/14 , C07D233/96 , C07D401/12
摘要： The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及制备食欲肽受体拮抗剂的吡啶基哌啶化合物的方法，其可用于治疗或预防涉及食欲肽受体的神经和精神疾病及疾病。
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6.发明申请Papain Family Cysteine Protease Inhibitors for the Treatment of Parasitic Diseases 审中-公开木瓜蛋白酶家族半胱氨酸蛋白酶抑制剂治疗寄生虫病公开(公告)号：US20090264479A1
公开(公告)日：2009-10-22
申请号：US11989437
申请日：2006-07-24
IPC分类号： A61K31/4402 , A61K31/165 , A61P33/00
CPC分类号： A61K31/275 , A61K45/06 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/423 , A61K2300/00
摘要： Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition of these proteases can be useful in the treatment of these parasitic diseases, including toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis or schistosomiasis.
摘要翻译： 负责哺乳动物疾病的几种寄生虫依赖于各种生命周期功能的半胱氨酸蛋白酶。 抑制这些蛋白酶可用于治疗这些寄生虫病，包括弓形体病，疟疾，非洲锥虫病，恰加斯病，利什曼病或血吸虫病。
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公开(公告)号：US08969394B2
公开(公告)日：2015-03-03
申请号：US12309941
申请日：2007-08-10
申请人： Marc Blouin , Jason Burch , Yongxin Han , Christophe Mellon
发明人： Marc Blouin , Jason Burch , Yongxin Han , Christophe Mellon
IPC分类号： A61K31/41 , A61K31/381 , A61P29/00 , C07D333/38 , C07D409/12
CPC分类号： C07D409/12 , C07D333/38
摘要： The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).
摘要翻译： 本发明涉及式I和II的噻吩甲酰胺衍生物作为EP4受体配体，拮抗剂或激动剂，其可用于治疗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，癌症和青光眼。 还包括药物组合物和使用方法。 （式I和II）。
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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：US20070099893A1
公开(公告)日：2007-05-03
申请号：US10581692
申请日：2004-12-09
申请人： Michael Boyd , Cheuk Lau , Christophe Mellon , Bruno Roy , John Scheigetz , Vouy Truong
发明人： Michael Boyd , Cheuk Lau , Christophe Mellon , Bruno Roy , John Scheigetz , Vouy Truong
IPC分类号： A61K31/44 , A61K31/426 , A61K31/397 , A61K31/277
CPC分类号： C07D213/56 , A61K31/277 , A61K31/397 , A61K31/426 , A61K31/44 , A61K31/663 , A61K45/06 , C07C255/46 , C07C2601/02 , A61K2300/00
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：US20070015234A1
公开(公告)日：2007-01-18
申请号：US10570925
申请日：2004-09-17
IPC分类号： C12Q1/37 , A61K31/655
CPC分类号： G01N33/5044 , C12Q1/37 , G01N33/60 , G01N33/6887 , G01N2500/00 , G01N2500/10
摘要： The present invention relates to a method of identifying and evaluating chemical inhibitors of cathepsin K activity in whole cells. The present invention also relates to probes that are capable of forming irreversible adducts with cathepsin K at the active site. The probes used in the instant invention comprise a radioactive functional group to allow the detection of the irreversible cathepsin K-probe adducts.
摘要翻译： 本发明涉及鉴定和评价全细胞中组织蛋白酶K活性的化学抑制剂的方法。 本发明还涉及能够在活性部位与组织蛋白酶K形成不可逆加合物的探针。 本发明中使用的探针包括放射性官能团，以允许检测不可逆的组织蛋白酶K-探针加合物。
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