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公开(公告)号：US20120015920A1
公开(公告)日：2012-01-19
申请号：US13163457
申请日：2011-06-17
申请人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgürtel , Michael Essers , Joshua van Veldhuizen , Bert Nolte , Brian M. Gallagher, JR. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
发明人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgürtel , Michael Essers , Joshua van Veldhuizen , Bert Nolte , Brian M. Gallagher, JR. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
IPC分类号： A61K31/56 , A61K31/519 , A61K31/538 , A61P29/00 , A61P19/02 , A61P35/00 , A61P9/10 , A61P11/00 , A61P25/00 , A61P27/02 , A61P31/04 , A61P7/02 , A61P25/16 , A61P25/28 , A61P31/18 , C12N9/99 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译： 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。
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公开(公告)号：US20110112051A1
公开(公告)日：2011-05-12
申请号：US13006363
申请日：2011-01-13
申请人： Heiko KROTH , Tim Feuerstein , Frank Richter , Jürgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochguertel , Fritz-Frieder Frickel , Arthur Taveras , Christoph Steeneck
发明人： Heiko KROTH , Tim Feuerstein , Frank Richter , Jürgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochguertel , Fritz-Frieder Frickel , Arthur Taveras , Christoph Steeneck
IPC分类号： A61K31/41 , C07D403/12 , C07D413/14 , A61K31/5377 , C07D403/14 , C07D207/16 , A61K31/40 , C07F5/02 , A61K31/69 , C07D487/08 , A61K31/407 , C07D209/52 , A61K31/403 , A61K31/4196 , C07D413/12 , A61K31/4245 , A61K31/496 , C07D401/14 , A61K31/4545 , A61P3/10
CPC分类号： C07D207/16 , C07D209/02 , C07D209/52 , C07D401/12 , C07D403/12 , C07D413/12 , C07D487/08 , C07D495/04
摘要： The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
摘要翻译： 本发明一般涉及吡咯烷和噻唑烷DPP-IV抑制剂化合物。 本发明还提供了用于制备这种化合物的合成方法，使用这些化合物抑制DPP-IV的方法和含有它们的药物制剂用于治疗DPP-IV介导的疾病，特别是2型糖尿病。
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公开(公告)号：US20080161300A1
公开(公告)日：2008-07-03
申请号：US12001041
申请日：2007-12-07
申请人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgurtel , Michael Essers , Joshua Van Veldhuizen , Bert Nolte , Brian Gallagher , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Beisinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur Taveras
发明人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgurtel , Michael Essers , Joshua Van Veldhuizen , Bert Nolte , Brian Gallagher , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Beisinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur Taveras
IPC分类号： A61K31/536 , A61K31/519 , C07D265/36 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译： 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。
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公开(公告)号：US20060270701A1
公开(公告)日：2006-11-30
申请号：US11409481
申请日：2006-04-21
申请人： Heiko Kroth , Tim Feuerstein , Frank Richter , Jurgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochguertel , Fritz-Frieder Frickel , Arthur Taveras
发明人： Heiko Kroth , Tim Feuerstein , Frank Richter , Jurgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochguertel , Fritz-Frieder Frickel , Arthur Taveras
IPC分类号： A61K31/4745 , A61K31/407 , A61K31/41 , C07D471/02 , C07D403/02
CPC分类号： C07D207/16 , C07D209/02 , C07D209/52 , C07D401/12 , C07D403/12 , C07D413/12 , C07D487/08 , C07D495/04
摘要： The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
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公开(公告)号：US20090137547A1
公开(公告)日：2009-05-28
申请号：US12001043
申请日：2007-12-07
申请人： Christoph Steeneck , Christian Gege , Frank Riohter , Holko Kroth , Mouhlee Hochgueriel , Michael Essors , Joshua Van Veldhulzen , Bert Nolte , Brian M. Gallaghor, JR. , Tim Feuerstein , Matthias Schneider , Toralen Arndt , Hongbo Deng , Ralf Blesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholelld , Arthur G. Taverse
发明人： Christoph Steeneck , Christian Gege , Frank Riohter , Holko Kroth , Mouhlee Hochgueriel , Michael Essors , Joshua Van Veldhulzen , Bert Nolte , Brian M. Gallaghor, JR. , Tim Feuerstein , Matthias Schneider , Toralen Arndt , Hongbo Deng , Ralf Blesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholelld , Arthur G. Taverse
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译： 本发明一般涉及含酰胺基的药剂，特别涉及含有酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。
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公开(公告)号：US08076330B2
公开(公告)日：2011-12-13
申请号：US13006363
申请日：2011-01-13
申请人： Heiko Kroth , Tim Feuerstein , Frank Richter , Jürgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochgürtel , Fritz-Frieder Frickel , Arthur G. Taveras , Christoph Steeneck
发明人： Heiko Kroth , Tim Feuerstein , Frank Richter , Jürgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochgürtel , Fritz-Frieder Frickel , Arthur G. Taveras , Christoph Steeneck
IPC分类号： A61K31/5377 , A61K31/41 , A61K31/40 , C07D257/02 , C07D413/14
CPC分类号： C07D207/16 , C07D209/02 , C07D209/52 , C07D401/12 , C07D403/12 , C07D413/12 , C07D487/08 , C07D495/04
摘要： The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
摘要翻译： 本发明一般涉及吡咯烷和噻唑烷DPP-IV抑制剂化合物。 本发明还提供了用于制备这种化合物的合成方法，使用这些化合物抑制DPP-IV的方法和含有它们的药物制剂用于治疗DPP-IV介导的疾病，特别是2型糖尿病。
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公开(公告)号：US20080176870A1
公开(公告)日：2008-07-24
申请号：US11986622
申请日：2007-11-20
申请人： Bert Nolte , Irving Sucholeiki , Tim Feuerstein , Brian M. Gallagher , Xinyuan Wu , Christoph Steeneck , Christian Gege , Hongbo Deng , Joshua Van Veldhuizen , Arthur Taveras
发明人： Bert Nolte , Irving Sucholeiki , Tim Feuerstein , Brian M. Gallagher , Xinyuan Wu , Christoph Steeneck , Christian Gege , Hongbo Deng , Joshua Van Veldhuizen , Arthur Taveras
IPC分类号： A61K31/495 , C07D487/04 , A61P19/02 , A61P29/00 , A61P9/10
CPC分类号： C07D487/04
摘要： The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
摘要翻译： 本发明一般涉及含杂环的药物，特别是涉及杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环金属蛋白酶抑制化合物，其与当前已知的金属蛋白酶抑制剂相比表现出增加的效力。
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公开(公告)号：US07795245B2
公开(公告)日：2010-09-14
申请号：US12001043
申请日：2007-12-07
申请人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgurtel , Michael Essors , Joshua Van Veldhuizen , Bert Nolte , Brian M. Gallagher, Jr. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
发明人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgurtel , Michael Essors , Joshua Van Veldhuizen , Bert Nolte , Brian M. Gallagher, Jr. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
IPC分类号： A61K31/397 , A61K31/519 , A61K31/535 , A01N43/90 , C07D487/00 , C07D413/00
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds having the following formulas: wherein R1, R2, R3, and R4 are as defined in the specification. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds amide containing heterobicyclic compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译： 本发明一般涉及含酰胺基的药剂，特别涉及具有下式的含酰胺的杂双环金属蛋白酶抑制剂化合物：其中R1，R2，R3和R4如说明书中所定义。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其含有杂双环化合物的酰胺，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。
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公开(公告)号：US07553861B2
公开(公告)日：2009-06-30
申请号：US11409481
申请日：2006-04-21
申请人： Heiko Kroth , Tim Feuerstein , Arthur Taveras
发明人： Heiko Kroth , Tim Feuerstein , Arthur Taveras
IPC分类号： A61K31/41 , C07D257/04 , C07D257/10 , C07D403/00 , C07D487/00 , C07D295/00 , C07D207/00
CPC分类号： C07D207/16 , C07D209/02 , C07D209/52 , C07D401/12 , C07D403/12 , C07D413/12 , C07D487/08 , C07D495/04
摘要： The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
摘要翻译： 本发明一般涉及吡咯烷和噻唑烷DPP-IV抑制剂化合物。 本发明还提供了用于制备这种化合物的合成方法，使用这些化合物抑制DPP-IV的方法和含有它们的药物制剂用于治疗DPP-IV介导的疾病，特别是2型糖尿病。
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公开(公告)号：US08835441B2
公开(公告)日：2014-09-16
申请号：US13163457
申请日：2011-06-17
申请人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgürtel , Michael Essers , Joshua van Veldhuizen , Bert Nolte , Brian M. Gallagher, Jr. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
发明人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgürtel , Michael Essers , Joshua van Veldhuizen , Bert Nolte , Brian M. Gallagher, Jr. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide containing heterobicyclic compounds having the following formulas: wherein R1, R2, D, and Q are as defined in the specification. More particularly, the present invention provides a new class of amide containing heterobicyclic compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译： 本发明一般涉及具有下式的含酰胺的杂双环化合物：其中R1，R2，D和Q如说明书中所定义。 更具体地说，本发明提供了一类新的含有杂双环化合物的酰胺，其表现出与目前已知的MMP-13和MMP-3抑制剂有关的效力。
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