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1. 发明授权

US07400979B2 Method of identifying inhibitors of Lck 有权
标题翻译：鉴定Lck抑制剂的方法
公开(公告)号：US07400979B2
公开(公告)日：2008-07-15
申请号：US10212346
申请日：2002-08-05
申请人： David W. Borhani , David Calderwood , Richard W. Dixon , Gavin C. Hirst , Peter Hrnciar , Andreas Loew , Adelaine Leung , Kurt Ritter
发明人： David W. Borhani , David Calderwood , Richard W. Dixon , Gavin C. Hirst , Peter Hrnciar , Andreas Loew , Adelaine Leung , Kurt Ritter
IPC分类号： G06F17/11 , G06F17/50 , G06F19/00
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention relates to polypeptides which comprise the ligand binding domain of Lck, crystalline forms of these polypeptides, and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Lck. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential selective inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain selectively.
摘要翻译：本发明涉及包含Lck的配体结合结构域，这些多肽的结晶形式的多肽，以及这些结晶形式用于确定Lck催化结构域的三维结构的多肽。本发明还涉及在设计和/或鉴定Lck活性的潜在抑制剂的方法中单独或与抑制剂复合的Lck催化结构域的三维结构的用途，例如抑制结合的化合物天然底物到Lck催化结构域。本发明还涉及在设计和/或鉴定Lck活性的潜在选择性抑制剂的方法中单独或与抑制剂复合的Lck催化结构域的三维结构的用途，例如抑制Lck活性结合的化合物选择性地对Lck催化结构域的天然底物。

2. 发明授权

US07737160B2 Thienopyridine and furopyridine kinase inhibitors 有权
标题翻译：噻吩并吡啶和呋喃啶激酶抑制剂
公开(公告)号：US07737160B2
公开(公告)日：2010-06-15
申请号：US11675183
申请日：2007-02-15
申请人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
发明人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
IPC分类号： A61K31/4745 , A61K31/4743 , A61K31/4741
CPC分类号： A61K31/4743 , A61K31/4741 , A61K31/4745 , C07D491/04 , C07D495/04 , Y02A50/401
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有该式的化合物可用于抑制蛋白酪氨酸激酶。本发明还公开了制备化合物的方法，含有该化合物的组合物和使用该化合物的处理方法。

3. 发明授权

US08273736B2 Thienopyridine and furopyridine kinase inhibitors 有权
标题翻译：噻吩并吡啶和呋喃啶激酶抑制剂
公开(公告)号：US08273736B2
公开(公告)日：2012-09-25
申请号：US12623026
申请日：2009-11-20
申请人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
发明人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
IPC分类号： A61K31/4365 , A61K31/55 , A61K31/5377 , A61K31/496 , C07D495/04
CPC分类号： A61K31/4743 , A61K31/4741 , A61K31/4745 , C07D491/04 , C07D495/04 , Y02A50/401
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有该式的化合物可用于抑制蛋白酪氨酸激酶。本发明还公开了制备化合物的方法，含有该化合物的组合物和使用该化合物的处理方法。

4. 发明授权

US07202363B2 Thienopyridine and furopyridine kinase inhibitors 有权
标题翻译：噻吩并吡啶和呋喃啶激酶抑制剂
公开(公告)号：US07202363B2
公开(公告)日：2007-04-10
申请号：US10899168
申请日：2004-07-26
申请人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
发明人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
IPC分类号： C07D491/04 , C07D421/04
CPC分类号： A61K31/4743 , A61K31/4741 , A61K31/4745 , C07D491/04 , C07D495/04 , Y02A50/401
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有式的化合物

5. 发明申请

US20100069371A1 THIENOPYRIDINE AND FUROPYRIDINE KINASE INHIBITORS 有权
标题翻译：三烯吡啶和呋咱激酶抑制剂
公开(公告)号：US20100069371A1
公开(公告)日：2010-03-18
申请号：US12623026
申请日：2009-11-20
申请人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
发明人： Patrick Betschmann , Andrew F. Burchat , David J. Calderwood , Michael L. Curtin , Steven K. Davidsen , Heather M. Davis , Robin R. Frey , Howard R. Heyman , Gavin C. Hirst , Peter Hrnciar , Michael R. Michaelides , Melanie A. Muckey , Kelly D. Mullen , Paul Rafferty , Carol K. Wada
IPC分类号： A61K31/4365 , C07D495/04 , A61K31/55 , A61K31/5377 , A61K31/496
CPC分类号： A61K31/4743 , A61K31/4741 , A61K31/4745 , C07D491/04 , C07D495/04 , Y02A50/401
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有该式的化合物可用于抑制蛋白酪氨酸激酶。本发明还公开了制备化合物的方法，含有该化合物的组合物和使用该化合物的处理方法。

6. 发明申请

US20070155776A1 THIENOPYRIDINE AND FUROPYRIDINE KINASE INHIBITORS 有权
标题翻译：三烯吡啶和呋喃亚胺激酶抑制剂
公开(公告)号：US20070155776A1
公开(公告)日：2007-07-05
申请号：US11675183
申请日：2007-02-15
申请人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Melanie Muckey , Kelly Mullen , Paul Rafferty , Carol Wada
发明人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Melanie Muckey , Kelly Mullen , Paul Rafferty , Carol Wada
IPC分类号： A61K31/4745 , A61K31/4743 , A61K31/4741 , C07D491/02 , C07D498/02
CPC分类号： A61K31/4743 , A61K31/4741 , A61K31/4745 , C07D491/04 , C07D495/04 , Y02A50/401
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有该式的化合物可用于抑制蛋白酪氨酸激酶。本发明还公开了制备化合物的方法，含有该化合物的组合物和使用该化合物的处理方法。

7. 发明申请

US20050043347A1 Thienopyridine and furopyridine kinase inhibitors 有权
标题翻译：噻吩并吡啶和呋喃啶激酶抑制剂
公开(公告)号：US20050043347A1
公开(公告)日：2005-02-24
申请号：US10899168
申请日：2004-07-26
申请人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Melanie Muckey , Paul Rafferty , Carol Wada
发明人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Melanie Muckey , Paul Rafferty , Carol Wada
IPC分类号： A61K31/4741 , A61K31/4743 , A61K31/4745 , C07D491/04 , C07D491/048 , C07D495/04 , C07D491/02 , C07D498/02
CPC分类号： A61K31/4743 , A61K31/4741 , A61K31/4745 , C07D491/04 , C07D495/04 , Y02A50/401
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有该式的化合物可用于抑制蛋白酪氨酸激酶。本发明还公开了制备化合物的方法，含有该化合物的组合物和使用该化合物的处理方法。

8. 发明申请

US20050026944A1 Thienopyridine and furopyridine kinase inhibitors 审中-公开
公开(公告)号：US20050026944A1
公开(公告)日：2005-02-03
申请号：US10838132
申请日：2004-05-03
申请人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Melanie Muckey , Paul Rafferty , Carol Wada
发明人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Melanie Muckey , Paul Rafferty , Carol Wada
IPC分类号： A61P35/00 , C07D491/04 , C07D495/04 , C07D498/04 , C07D491/02 , A61K31/4741 , A61K31/4743 , C07D498/02
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

9. 发明申请

US20050020619A1 Thienopyridine kinase inhibitors 审中-公开
标题翻译：噻吩并吡啶激酶抑制剂
公开(公告)号：US20050020619A1
公开(公告)日：2005-01-27
申请号：US10626092
申请日：2003-07-24
申请人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Paul Rafferty
发明人： Patrick Betschmann , Andrew Burchat , David Calderwood , Michael Curtin , Steven Davidsen , Heather Davis , Robin Frey , Howard Heyman , Gavin Hirst , Peter Hrnciar , Michael Michaelides , Paul Rafferty
IPC分类号： C07D491/04 , C07D495/04 , C07D498/02 , A61K31/4743
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：具有该式的化合物可用于抑制蛋白酪氨酸激酶。本发明还公开了制备化合物的方法，含有该化合物的组合物和使用该化合物的处理方法。

10. 发明授权

US08633193B2 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
标题翻译：吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物
公开(公告)号：US08633193B2
公开(公告)日：2014-01-21
申请号：US13014066
申请日：2011-01-26
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

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