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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：US07226921B2
公开(公告)日：2007-06-05
申请号：US11166829
申请日：2005-06-24
IPC分类号： A61K31/4245 , A61K31/5377 , C07D271/06 , C07D413/14 , C07D413/04
CPC分类号： C07D271/10 , A61K31/4245 , A61K31/4439 , A61K31/5377 , C07D271/06 , C07D401/04 , C07D409/04 , Y02A50/411
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译： 本发明涉及新的选择性组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。
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公开(公告)号：US07196099B2
公开(公告)日：2007-03-27
申请号：US10787367
申请日：2004-02-26
IPC分类号： A61K31/4468 , A61K31/45 , C07D401/12
CPC分类号： C07D295/215 , A61K38/00 , C07C317/48 , C07C317/50 , C07D205/085 , C07D207/24 , C07D207/48 , C07D223/12 , C07D307/32 , C07K5/0606 , C07K5/06078 , Y02A50/411 , Y02A50/423
摘要： The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译： 本发明涉及新型组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。
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4.发明申请公开(公告)号：US20060135781A1
公开(公告)日：2006-06-22
申请号：US11347630
申请日：2006-02-02
申请人： Jiayao Li , John Link , Colette Colladant
发明人： Jiayao Li , John Link , Colette Colladant
IPC分类号： C07F3/02
CPC分类号： C07D263/56 , C07D277/64 , C07F3/02
摘要： The present invention is directed to a novel process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents that are useful in the synthesis of a variety of pharmaceuticals, in particular certain cysteine protease inhibitors.
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公开(公告)号：US07064123B1
公开(公告)日：2006-06-20
申请号：US10035783
申请日：2001-12-24
申请人： Michael Graupe , John W. Patterson , Stephen D. Pickett , John O. Link , Jiayao Li , David Aldous , Sukanthini Thurairatnam , Andreas P. Timm , Frank Halley , Justine Lai Yeun Quai
发明人： Michael Graupe , John W. Patterson , Stephen D. Pickett , John O. Link , Jiayao Li , David Aldous , Sukanthini Thurairatnam , Andreas P. Timm , Frank Halley , Justine Lai Yeun Quai
IPC分类号： A61K31/535 , C07D295/00 , A61P29/00
CPC分类号： C07D207/273 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/40 , C07D223/10 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12 , Y02A50/411
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译： 本发明涉及新的选择性组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。
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公开(公告)号：US20050267044A1
公开(公告)日：2005-12-01
申请号：US11166829
申请日：2005-06-24
申请人： Jiayo Li , David Aldous , Sukanthini Thurairatnam
发明人： Jiayo Li , David Aldous , Sukanthini Thurairatnam
IPC分类号： A61K38/00 , A61P1/02 , A61P13/12 , A61P19/02 , A61P21/04 , A61P35/00 , A61P43/00 , C07D271/06 , C07D271/10 , C07D401/04 , C07D409/04 , C07K5/078 , A61K31/5377 , C07D413/14
CPC分类号： C07D271/10 , A61K31/4245 , A61K31/4439 , A61K31/5377 , C07D271/06 , C07D401/04 , C07D409/04 , Y02A50/411
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译： 本发明涉及新的选择性组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。
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公开(公告)号：US20050227976A1
公开(公告)日：2005-10-13
申请号：US11100781
申请日：2005-04-07
申请人： Eduardo Setti
发明人： Eduardo Setti
IPC分类号： A61K31/4025 , A61K31/4433 , A61K31/452 , A61K31/496 , A61K31/5377 , C07D307/81 , C07D405/06 , C07D45/02
CPC分类号： C07D405/06 , C07D307/81
摘要： The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
摘要翻译： 本发明涉及作为组蛋白脱乙酰酶抑制剂的某些异羟肟酸衍生物，因此可用于治疗与组蛋白脱乙酰酶活性相关的疾病。 还公开了制备这些化合物的药物组合物和方法。
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公开(公告)号：US20040142999A1
公开(公告)日：2004-07-22
申请号：US10719080
申请日：2003-11-21
发明人： Michael Graupe , Jiayao Li , John Link , Sheila Zipfel , Andreas Paul Timm , David John Aldous , Sukathini Thurairatnam
IPC分类号： A61K031/40
CPC分类号： C07D207/08 , C07C233/31 , C07C255/29 , C07C255/44 , C07C255/46 , C07C271/12 , C07C271/16 , C07C271/24 , C07C317/44 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D211/66 , C07D223/08 , C07D223/12 , C07D239/08 , C07D263/56 , C07D271/10 , C07D277/28 , C07D277/64 , C07D277/82 , C07D295/185 , C07D295/205 , C07D307/14 , C07D309/14 , C07D333/24 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
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公开(公告)号：US5925553A
公开(公告)日：1999-07-20
申请号：US925843
申请日：1997-09-08
CPC分类号： C12N9/6424 , C07K14/811
摘要： Serine protease inhibitors are provided comprising compounds having a P site binding moiety and a divalent cation(s) chelating moiety which are pre-prepared as divalent cation(s) complexes or combined with the serine protease in the presence of divalent cation(s). The compounds are shown to have high inhibitory activity when complexed to divalent cation(s) and find use in various processes associated with serine protease isolation and inhibition.
摘要翻译： 提供丝氨酸蛋白酶抑制剂，其包含具有P位结合部分和二价阳离子螯合部分的化合物，其在二价阳离子存在下预先制备为二价阳离子配合物或与丝氨酸蛋白酶组合。 当与二价阳离子络合时，这些化合物被证明具有高的抑制活性，可用于与丝氨酸蛋白酶分离和抑制相关的各种过程。
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公开(公告)号：US20070276019A1
公开(公告)日：2007-11-29
申请号：US10570885
申请日：2004-09-17
申请人： John Link
发明人： John Link
IPC分类号： C07D263/56 , A61K31/16 , A61K31/423 , A61P17/06 , A61P37/00 , C07C233/02
CPC分类号： C07D263/56
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
摘要翻译： 本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。 本发明涉及包含这些化合物的药物组合物及其制备方法。
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