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公开(公告)号：US20060287402A1
公开(公告)日：2006-12-21
申请号：US10569351
申请日：2004-08-23
申请人： Christopher Bayly , Cameron Black , Daniel McKay
发明人： Christopher Bayly , Cameron Black , Daniel McKay
IPC分类号： A61K31/13 , C07C211/01
CPC分类号： C07D295/108 , C07C255/24 , C07C255/29 , C07C255/46 , C07C323/41 , C07C2601/02 , C07D223/08 , C07D295/135 , C07D307/33 , C07D333/20 , C07D333/24 , C07D401/12 , C07K5/06191
摘要： This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3 and R4 are indicated therein, 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, osteoarthritis and rheumatoid arthritis.
摘要翻译： 本发明涉及由下式（I）表示的新一类化合物，其中R 1，R 2，R 3，R 3， SUB>和R 4，其中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抑制 骨吸收表现为骨质疏松症，骨关节炎和类风湿性关节炎。
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公开(公告)号：US20070167635A1
公开(公告)日：2007-07-19
申请号：US10560672
申请日：2004-06-28
申请人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel McKay , Renata Oballa , Joel Robichaud
发明人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel McKay , Renata Oballa , Joel Robichaud
IPC分类号： G01N33/48 , C07D233/14 , C07D233/22
CPC分类号： C07D213/83 , C07C255/29 , C07C311/06 , C07C323/25 , C07C323/49 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D211/20 , C07D213/32 , C07D231/12 , C07D233/64 , C07D235/06 , C07D257/04
摘要： This invention relates to a class of compounds having the general formula (I) 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： 本发明涉及一类具有通式（I）的化合物，它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抑制骨的疾病 表示吸收，如骨质疏松症。
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公开(公告)号：US07405229B2
公开(公告)日：2008-07-29
申请号：US10560672
申请日：2004-06-28
申请人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel J. McKay , Renata Oballa , Joel Robichaud
发明人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel J. McKay , Renata Oballa , Joel Robichaud
IPC分类号： A61K31/44 , A61K31/445 , A61K31/417 , A61K31/4184 , C07D211/80 , C07D233/54 , C07D235/04
CPC分类号： C07D213/83 , C07C255/29 , C07C311/06 , C07C323/25 , C07C323/49 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D211/20 , C07D213/32 , C07D231/12 , C07D233/64 , C07D235/06 , C07D257/04
摘要： This invention relates to a class of compounds having the general formula (I) 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： 本发明涉及一类具有通式（I）的化合物，它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抑制骨的疾病 表示吸收，如骨质疏松症。
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公开(公告)号：US20090176859A1
公开(公告)日：2009-07-09
申请号：US10585147
申请日：2005-01-06
申请人： Christopher Bayly , Cameron Black , Michel Therien
发明人： Christopher Bayly , Cameron Black , Michel Therien
IPC分类号： A61K31/4015 , C07D307/32 , A61K31/341 , C07D207/24 , A61P3/06
CPC分类号： C07D401/04 , C07D207/24 , C07D211/74 , C07D213/56 , C07D223/08 , C07D307/32 , C07D309/30 , C07D401/06 , C07D401/12 , C07D413/06
摘要： The present invention relates to a novel class of compounds mainly, leucinamide-amino-carboxylate derivatives of formula (I) wherein Y is CR1R2, O, S, —SO2, C=0 or NR9; Z is CR1R2, O, S, —SO2, C═O or NR9 and each G is independently a CR1CR2. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B and to pharmaceutical compositions thereof. These compounds are useful for treating and preventing cathepsin dependent conditions 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，主要是其中Y为CR 1 R 2，O，S，-SO 2，C = O或NR 9的式（I）的亮氨酰胺 - 氨基 - 羧酸酯衍生物; Z是CR 1 R 2，O，S，-SO 2，C-O或NR 9，每个G独立地是CR 1 CR 2。 所述化合物是组织蛋白酶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的抑制剂及其药物组合物。 这些化合物可用于治疗和预防指示骨吸收抑制的组织蛋白酶依赖性条件，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：US06225288B1
公开(公告)日：2001-05-01
申请号：US09526840
申请日：2000-03-16
申请人： Yongxin Han , Andre Giroux , Erich Grimm , Renee Aspiotis , Sebastien Francoeur , Robert Zamboni , Petpiboon Prasit , Christopher Bayly , Dan McKay , Cameron Black
发明人： Yongxin Han , Andre Giroux , Erich Grimm , Renee Aspiotis , Sebastien Francoeur , Robert Zamboni , Petpiboon Prasit , Christopher Bayly , Dan McKay , Cameron Black
IPC分类号： C07K506
CPC分类号： C07D239/34 , C07C323/59
摘要： Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.
摘要翻译： 由式I表示的化合物及其药学上可接受的盐，酯和水合物与药物组合物和治疗方法一起公开。 该化合物可用作半胱天冬酶-3的抑制剂，其涉及调节凋亡。
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公开(公告)号：US20090148850A1
公开(公告)日：2009-06-11
申请号：US12286566
申请日：2008-10-01
IPC分类号： C12Q1/68
CPC分类号： G01N33/566 , G01N2333/726 , G01N2500/02
摘要： Methods for identifying modulators of P2RY14 are described. The methods are particularly useful for identifying agents that are useful for treating metabolic syndrome.
摘要翻译： 描述了用于鉴定P2RY14的调节剂的方法。 该方法对于鉴定可用于治疗代谢综合征的药剂特别有用。
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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：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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