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公开(公告)号:US08008481B2
公开(公告)日:2011-08-30
申请号:US11731950
申请日:2007-04-02
申请人: Anna M. Ericsson , Andrew Burchat , Kristine E. Frank , David J. Calderwood , Lily K. Abbott , Maria A. Argiriadi , David W. Borhani , Kevin P. Cusack , Richard W. Dixon , Thomas D. Gordon , Kelly D. Mullen , Robert V. Talanian , Xiaoyun Wu , Xiaolei Zhang , Lu Wang , Biqin Li , Claude E. Barberis , Neil Wishart
发明人: Anna M. Ericsson , Andrew Burchat , Kristine E. Frank , David J. Calderwood , Lily K. Abbott , Maria A. Argiriadi , David W. Borhani , Kevin P. Cusack , Richard W. Dixon , Thomas D. Gordon , Kelly D. Mullen , Robert V. Talanian , Xiaoyun Wu , Xiaolei Zhang , Lu Wang , Biqin Li , Claude E. Barberis , Neil Wishart
IPC分类号: C07D409/14 , C07D413/14
CPC分类号: C07D487/04 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/14
摘要: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.
摘要翻译: 式(I)的新型化合物或其药学上可接受的盐,前体药物和式(I)的生物活性代谢物,其中取代基如本文所定义,其可用作治疗剂。
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公开(公告)号:US20120053345A1
公开(公告)日:2012-03-01
申请号:US13198363
申请日:2011-08-04
申请人: Anna M. Ericson , Andrew Burchat , Kristine E. Frank , David J. Calderwood , Lily K. Abbott , Maria A. Argiriadi , David W. Borhani , Kevin P. Cusack , Richard W. Dixon , Thomas D. Gordon , Kelly D. Mullen , Robert V. Talanian , Xiaoyun Wu , Xiaolei Zhang , Lu Wang , Biqin Li , Claude E. Barberis , Neil Wishart
发明人: Anna M. Ericson , Andrew Burchat , Kristine E. Frank , David J. Calderwood , Lily K. Abbott , Maria A. Argiriadi , David W. Borhani , Kevin P. Cusack , Richard W. Dixon , Thomas D. Gordon , Kelly D. Mullen , Robert V. Talanian , Xiaoyun Wu , Xiaolei Zhang , Lu Wang , Biqin Li , Claude E. Barberis , Neil Wishart
IPC分类号: C07D495/04 , C07D401/14 , C07D403/14 , C07D231/54 , C07D487/04
CPC分类号: C07D487/04 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/14
摘要: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.
摘要翻译: 式(I)的新型化合物或其药学上可接受的盐,前体药物和式(I)的生物活性代谢物,其中取代基如本文所定义,其可用作治疗剂。
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公开(公告)号:US20080161341A1
公开(公告)日:2008-07-03
申请号:US11973147
申请日:2007-10-05
申请人: David J. Calderwood , Kristine E. Frank , David W. Borhani , Heather M. Davis , Nathan S. Josephsohn , Barbara S. Skinner
发明人: David J. Calderwood , Kristine E. Frank , David W. Borhani , Heather M. Davis , Nathan S. Josephsohn , Barbara S. Skinner
IPC分类号: A61K31/437 , C07D513/04 , C07D498/04 , A61K31/4439 , A61K31/424 , A61K31/429
CPC分类号: C07D498/04 , C07D513/04 , C07D519/00
摘要: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译: 本发明涉及新的式(I)化合物,其中变量如本文所定义。 式(I)化合物可用作激酶抑制剂,因此可用于治疗某些病症和疾病,特别是炎性病症和疾病以及增殖性病症和病症,例如癌症。
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公开(公告)号:US07790741B2
公开(公告)日:2010-09-07
申请号:US11973147
申请日:2007-10-05
申请人: David J. Calderwood , Kristine E. Frank , David W. Borhani , Heather M. Davis , Nathan S. Josephsohn , Barbara S. Skinner
发明人: David J. Calderwood , Kristine E. Frank , David W. Borhani , Heather M. Davis , Nathan S. Josephsohn , Barbara S. Skinner
IPC分类号: A61K31/437 , A61K31/4184 , A61K31/424 , A61K31/429 , C07D487/04 , C07D513/04 , C07D498/04
CPC分类号: C07D498/04 , C07D513/04 , C07D519/00
摘要: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译: 本发明涉及新的式(I)化合物,其中变量如本文所定义。 式(I)化合物可用作激酶抑制剂,因此可用于治疗某些病症和疾病,特别是炎性病症和疾病以及增殖性病症和病症,例如癌症。
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公开(公告)号:US20090202557A1
公开(公告)日:2009-08-13
申请号:US12322088
申请日:2009-01-29
申请人: Maria A. Argiriadi , David W. Borhani , Tao Xiang , Chengbin Wu , Tariq Ghayur
发明人: Maria A. Argiriadi , David W. Borhani , Tao Xiang , Chengbin Wu , Tariq Ghayur
IPC分类号: A61K39/395 , C07K1/00 , C07K14/54 , C07K16/24
CPC分类号: C30B29/58 , C07K1/306 , C07K16/244 , C07K2299/00 , C07K2317/21 , C07K2317/34 , C07K2317/55 , C07K2317/56 , C07K2317/76 , C07K2317/92 , C30B7/00
摘要: The invention provides methods of crystallizing antibodies and fragments thereof as well as crystals produced thereby. More particularly, the invention provides methods of crystallizing human and non-human Fab fragments of antibodies, either alone or as co-crystals with their target ligand. For example, a crystal comprising a murine Fab fragment of the antibody 125-2H or a human Fab fragment of the antibody ABT-325, which bind to IL-18, are provided as well as a co-crystal of a murine Fab fragment bound to IL-18. ABT-325 and 125-2H differ significantly in combining site character and architecture, thus explaining their ability to bind IL-18 simultaneously at distinct epitopes.
摘要翻译: 本发明提供了结晶抗体及其片段以及由此制备的晶体的方法。 更具体地说,本发明提供了将人抗体和非人Fab片段单独结晶或与其靶配体共结晶的方法。 例如,提供了包含结合IL-18的抗体125-2H的鼠Fab片段或抗体ABT-325的人Fab片段的结晶以及结合于鼠Fab片段的共晶体 到IL-18。 ABT-325和125-2H在组合位点特征和结构上有显着差异,从而说明了它们在不同表位同时结合IL-18的能力。
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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
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。
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公开(公告)号:US08753839B2
公开(公告)日:2014-06-17
申请号:US12228038
申请日:2008-08-08
IPC分类号: C12P21/06 , A61K39/395 , A01N61/00 , C07K16/24 , A61K39/00
CPC分类号: C07K16/241 , A61K2039/505 , C07K1/306 , C07K2299/00 , C07K2317/14 , C07K2317/54 , C07K2317/76 , C30B29/58 , Y02A50/388
摘要: The present invention relates to a batch crystallization method for crystallizing anti-human TNFalpha (hTNFalpha) antibody and antibody fragments which allows the production of said antibody on an industrial scale; a method of controlling the size of antibody crystals, for example, crystals of anti-hTNFalpha antibody fragments, compositions containing said crystals as well as methods of use of said crystals and compositions.
摘要翻译: 本发明涉及用于结晶抗人TNFα(hTNFα)抗体的分批结晶方法和允许以工业规模生产所述抗体的抗体片段; 控制抗体晶体大小的方法,例如抗hTNFα抗体片段的晶体,含有所述晶体的组合物以及使用所述晶体和组合物的方法。
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公开(公告)号:US08034906B2
公开(公告)日:2011-10-11
申请号:US11977677
申请日:2007-10-25
申请人: David W. Borhani , Wolfgang Fraunhofer , Hans-Juergen Krause , Anette Koenigsdorfer , Gerhard Winter , Stefan Gottschalk
发明人: David W. Borhani , Wolfgang Fraunhofer , Hans-Juergen Krause , Anette Koenigsdorfer , Gerhard Winter , Stefan Gottschalk
CPC分类号: C07K16/241 , A61K9/50 , A61K39/3955 , C07K2299/00 , C07K2317/565 , C07K2317/76 , C07K2317/92
摘要: The present invention relates to a batch crystallization method for crystallizing an anti-hTNFalpha antibody which allows the production of said antibody on an industrial scale; antibody crystals as obtained according to said method; compositions containing said crystals as well as methods of use of said crystals and compositions.
摘要翻译: 本发明涉及一种用于使抗hTNFα抗体结晶的分批结晶方法,其允许以工业规模生产所述抗体; 根据所述方法获得的抗体晶体; 含有所述晶体的组合物以及所述晶体和组合物的使用方法。
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公开(公告)号:US20080292642A1
公开(公告)日:2008-11-27
申请号:US12079434
申请日:2008-03-27
申请人: David W. Borhani , Wolfgang Fraunhofer , Hans-Juergen Krause , Anette Koenigsdorfer , Gerhard Winter , Stefan Gottschalk
发明人: David W. Borhani , Wolfgang Fraunhofer , Hans-Juergen Krause , Anette Koenigsdorfer , Gerhard Winter , Stefan Gottschalk
CPC分类号: C07K16/244 , A61K39/39591 , C07K2299/00 , C30B7/00 , Y02A50/401
摘要: The invention relates to batch crystallization methods for crystallizing an anti-hIL-12 antibody that allows the production of the antibody on an industrial scale, antibody crystals obtained according to the methods, compositions containing the crystals, and methods of using the crystals and the compositions.
摘要翻译: 本发明涉及用于结晶能够以工业规模生产抗体的抗-hIL-12抗体的分批结晶方法,根据该方法获得的抗体晶体,含有晶体的组合物,以及使用晶体和组合物的方法 。
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公开(公告)号:US20120288494A1
公开(公告)日:2012-11-15
申请号:US13374693
申请日:2012-01-06
IPC分类号: C07K16/24 , C12N15/13 , A61P25/00 , A61P17/06 , A61P29/00 , A61P19/02 , A61P1/04 , A61P37/06 , A61P37/00 , A61P35/00 , C12N15/63 , C12N5/10 , C12N1/00 , G01N33/566 , C07K1/00 , A61K39/395
CPC分类号: C07K16/244 , A61K2039/505 , C07K2299/00 , C07K2317/21 , C07K2317/565 , C07K2317/73
摘要: The present invention provides antibodies, and antigen-binding portions thereof, that bind to epitopes comprising at least one amino acid residues from residues 1-197 of the p40 subunit of IL-12 and/or IL-23. The invention further provides nucleic acids encoding the antibodies, compositions, vectors and host cells comprising the antibodies, and methods of making and using the same.
摘要翻译: 本发明提供了与包含IL-12和/或IL-23的p40亚基的残基1-197的至少一个氨基酸残基的表位结合的抗体及其抗原结合部分。 本发明还提供编码抗体,组合物,载体和包含抗体的宿主细胞的核酸,以及制备和使用该抗体的方法。
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