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1.发明授权Methods of treatment using allosteric processing inhibitors for matrix metalloproteinases 有权使用变构加工抑制剂治疗基质金属蛋白酶的方法公开(公告)号：US08883473B2
公开(公告)日：2014-11-11
申请号：US13533131
申请日：2012-06-26
Applicant: Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Carl Crysler , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Carl Manthey , Cynthia M. Milligan , Beverley Moore , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
Inventor： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Carl Crysler , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Carl Manthey , Cynthia M. Milligan , Beverley Moore , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
IPC: A61K31/4439 , A61K31/427 , A61P19/02 , A61K31/425
CPC classification number: A61K31/425 , A61K31/4439 , C07K2299/00 , G01N2333/96486
Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
Abstract translation: 本发明包括晶体，其包含基质金属蛋白酶（proMMP）的形式的复合物和抑制该proMMP活化的小分子变构加工抑制剂，用于鉴定抑制激活的小分子变构加工抑制剂的方法 proMMP和使用抑制proMMP激活的小分子变构加工抑制剂的治疗方法。 本发明涉及与抑制proMMP9激活的小分子变构加工抑制剂结合的proMMP9的复合物的晶体结构。 本发明还涉及用于设计，选择和/或优化抑制proMMP9和proMMP9同源物激活的小分子变构加工抑制剂的方法和结晶及相关结构信息的使用。 本发明还涉及小分子变构加工抑制剂用于治疗由不适当的基质金属蛋白酶（MMP）活性介导的疾病的用途。
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公开(公告)号：US20060110732A1
公开(公告)日：2006-05-25
申请号：US10519757
申请日：2003-07-23
Applicant: Roger Bone , Dionisios Rentzeperis , Hossein Askari , Barry Springer
Inventor： Roger Bone , Dionisios Rentzeperis , Hossein Askari , Barry Springer
CPC classification number: C40B30/04 , G01N33/6845
Abstract: The present invention relates generally to a method of identifying ligands that modulate protein-protein interactions. More particularly, the present invention relates to methods of determining agonists or antagonists of a co-regulator dependent target molecule based on the ability to modify the stability of the target molecule in a tissue-selective manner.
Abstract translation: 本发明一般涉及鉴定调节蛋白质 - 蛋白质相互作用的配体的方法。 更具体地，本发明涉及基于以组织选择性方式改变靶分子的稳定性的能力来确定共调节因子依赖性靶分子的激动剂或拮抗剂的方法。
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公开(公告)号：US20060024844A1
公开(公告)日：2006-02-02
申请号：US10522660
申请日：2002-09-20
Applicant: Dionisios Rentzeperis , Hossein Askari , Barry Springer , Roger Bone , Francis Salemme
Inventor： Dionisios Rentzeperis , Hossein Askari , Barry Springer , Roger Bone , Francis Salemme
IPC: G01N33/543 , G06F19/00 , G01N33/48 , G01N33/50
CPC classification number: C40B30/04 , G01N33/566 , G01N33/68 , G01N33/6803 , G01N33/6845 , G01N2333/4703 , G01N2333/70567 , G01N2333/723 , G01N2333/726 , G01N2333/9121 , G01N2500/00
Abstract: The present invention relates generally to a method of identifying ligands that modulate protein-protein interactions. More particularly, the present invention relates to methods of determining agonists or antagonists of a co-regulator dependent target molecule based on the ability to modify the stability of the target molecule.
Abstract translation: 本发明一般涉及鉴定调节蛋白质 - 蛋白质相互作用的配体的方法。 更具体地，本发明涉及基于调节靶分子的稳定性的能力来确定共调节因子依赖性靶分子的激动剂或拮抗剂的方法。
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4.发明授权Crystal structure of the pro form of a matrix metalloproteinase and an allosteric processing inhibitor 失效基质金属蛋白酶和变构加工抑制剂的形式的晶体结构公开(公告)号：US08753857B2
公开(公告)日：2014-06-17
申请号：US13533108
申请日：2012-06-26
Applicant: Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
Inventor： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
CPC classification number: C12N9/6491 , C12Y304/24017 , C12Y304/24035
Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
Abstract translation: 本发明包括晶体，其包含基质金属蛋白酶（proMMP）的形式的复合物和抑制该proMMP活化的小分子变构加工抑制剂，用于鉴定抑制激活的小分子变构加工抑制剂的方法 proMMP和使用抑制proMMP激活的小分子变构加工抑制剂的治疗方法。 本发明涉及与抑制proMMP9激活的小分子变构加工抑制剂结合的proMMP9的复合物的晶体结构。 本发明还涉及用于设计，选择和/或优化抑制proMMP9和proMMP9同源物激活的小分子变构加工抑制剂的方法和结晶及相关结构信息的使用。 本发明还涉及小分子变构加工抑制剂用于治疗由不适当的基质金属蛋白酶（MMP）活性介导的疾病的用途。
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5.发明申请Crystal Structure of the Pro Form of a Matrix Metalloproteinase and an Allosteric Processing Inhibitor 有权基质金属蛋白酶和变构加工抑制剂的Pro形式的晶体结构公开(公告)号：US20130166268A1
公开(公告)日：2013-06-27
申请号：US13533201
申请日：2012-06-26
Applicant: Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett Andrew Tongue , Aihua Wang
Inventor： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett Andrew Tongue , Aihua Wang
IPC: G06F19/12
CPC classification number: G06F19/706 , C12N9/6491 , G06F19/16 , G06F19/18 , Y02A90/26
Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
Abstract translation: 本发明包括晶体，其包含基质金属蛋白酶（proMMP）的形式的复合物和抑制该proMMP的激活的小分子变构的加工抑制剂，用于鉴定抑制激活的小分子变构加工抑制剂的方法 proMMP和使用抑制proMMP激活的小分子变构加工抑制剂的治疗方法。 本发明涉及与抑制proMMP9激活的小分子变构加工抑制剂结合的proMMP9的复合物的晶体结构。 本发明还涉及用于设计，选择和/或优化抑制proMMP9和proMMP9同源物激活的小分子变构加工抑制剂的方法和结晶及相关结构信息的使用。 本发明还涉及小分子变构加工抑制剂用于治疗由不适当的基质金属蛋白酶（MMP）活性介导的疾病的用途。
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Patent Agency Ranking
6.发明申请Methods of Treatment Using Allosteric Processing Inhibitors for Matrix Metalloproteinases 有权使用变构加工抑制剂治疗基质金属蛋白酶的方法公开(公告)号：US20130040994A1
公开(公告)日：2013-02-14
申请号：US13533131
申请日：2012-06-26
Applicant: Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Carl Crysler , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Carl Manthey , Cynthia M. Milligan , Beverley Moore , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett Andrew Tongue , Aihua Wang
Inventor： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Carl Crysler , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Carl Manthey , Cynthia M. Milligan , Beverley Moore , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett Andrew Tongue , Aihua Wang
IPC: A61K31/427 , A61P35/00 , A61P19/02 , A61P9/00 , A61P1/04 , A61P9/12 , A61P11/00 , A61P1/02 , A61P17/02 , A61P1/16 , A61P9/10 , A61P25/00 , A61P11/06 , A61P13/12 , A61P25/06 , C12N9/99 , A61K31/4439
CPC classification number: A61K31/425 , A61K31/4439 , C07K2299/00 , G01N2333/96486
Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
Abstract translation: 本发明包括晶体，其包含基质金属蛋白酶（proMMP）的形式的复合物和抑制该proMMP活化的小分子变构加工抑制剂，用于鉴定抑制激活的小分子变构加工抑制剂的方法 proMMP和使用抑制proMMP激活的小分子变构加工抑制剂的治疗方法。 本发明涉及与抑制proMMP9激活的小分子变构加工抑制剂结合的proMMP9的复合物的晶体结构。 本发明还涉及用于设计，选择和/或优化抑制proMMP9和proMMP9同源物激活的小分子变构加工抑制剂的方法和结晶及相关结构信息的使用。 本发明还涉及小分子变构加工抑制剂用于治疗由不适当的基质金属蛋白酶（MMP）活性介导的疾病的用途。
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公开(公告)号：US20130040360A1
公开(公告)日：2013-02-14
申请号：US13533108
申请日：2012-06-26
Applicant: Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett Andrew Tongue , Aihua Wang
Inventor： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett Andrew Tongue , Aihua Wang
IPC: C12N9/96
CPC classification number: C12N9/6491 , C12Y304/24017 , C12Y304/24035
Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
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8.发明申请Crystal structure of the c-fms kinase domain: applications and use of heterologous substitutions of kinase insert domains for crystallization 审中-公开c-fms激酶结构域的晶体结构：应用和使用激酶插入结构域的异源取代进行结晶公开(公告)号：US20060094081A1
公开(公告)日：2006-05-04
申请号：US11255147
申请日：2005-10-20
Applicant: Carsten Schubert , Barry Springer , Ingrid Deckman , Raymond Patch , Geoffrey Struble , Hongchang Ma , Celine Schalk-Hihi , Benjamin Brandt , Ioanna Petrounia
Inventor： Carsten Schubert , Barry Springer , Ingrid Deckman , Raymond Patch , Geoffrey Struble , Hongchang Ma , Celine Schalk-Hihi , Benjamin Brandt , Ioanna Petrounia
CPC classification number: C07K14/7153 , C07K2299/00 , C07K2319/00 , C30B7/00 , G16B15/00 , G16B20/00 , G16B50/00
Abstract: The present invention includes a crystal structure of the kinase domain of c-fms and a methodology to produce diffraction quality crystals of the c-fms kinase domain by heterologous substitution of the kinase insert domain. Also included in the invention is the structure of the c-fms kinase domain in liganded form for use in the discovery of inhibitors of c-fms for the treatment of diseases caused by inappropriate activity of c-fms. The present invention includes descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of c-fms to be determined at atomic resolution so that ligand binding sites on can be identified and the interactions of ligands with amino acid residues can be modeled.
Abstract translation: 本发明包括c-fms的激酶结构域的晶体结构和通过激酶插入结构域的异源取代产生c-fms激酶结构域的衍射质量晶体的方法。 本发明还包括配体形式的c-fms激酶结构域用于发现c-fms抑制剂用于治疗由c-fms的不适当活性引起的疾病的结构。 本发明包括晶体的X射线衍射图案的描述。 衍射图允许以原子分辨率确定c-fms的三维结构，从而可以鉴定配体结合位点，并且可以建模与配体与氨基酸残基的相互作用。
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9.发明授权Methods for designing, selecting and/or optimizing allosteric processing inhibitors for matrix metalloproteinases 有权用于设计，选择和/或优化基质金属蛋白酶变构加工抑制剂的方法公开(公告)号：US08798939B2
公开(公告)日：2014-08-05
申请号：US13533201
申请日：2012-06-26
Applicant: Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
Inventor： Kristi A. Leonard , Richard Scott Alexander , Joseph Kent Barbay , Roger F. Bone , Ingrid Christa Deckman , Paul F. Jackson , Lawrence C. Kuo , Frank A. Lewandowski , Diane M. Maguire , Cynthia M. Milligan , Kenneth J. Rhodes , Robert H. Scannevin , Celine Schalk-Hihi , Barry Springer , John C. Spurlino , Matthew J. Todd , Brett A. Tounge , Aihua Wang
CPC classification number: G06F19/706 , C12N9/6491 , G06F19/16 , G06F19/18 , Y02A90/26
Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.
Abstract translation: 本发明包括晶体，其包含基质金属蛋白酶（proMMP）的形式的复合物和抑制该proMMP活化的小分子变构加工抑制剂，用于鉴定抑制激活的小分子变构加工抑制剂的方法 proMMP和使用抑制proMMP激活的小分子变构加工抑制剂的治疗方法。 本发明涉及与抑制proMMP9激活的小分子变构加工抑制剂结合的proMMP9的复合物的晶体结构。 本发明还涉及用于设计，选择和/或优化抑制proMMP9和proMMP9同源物激活的小分子变构加工抑制剂的方法和结晶及相关结构信息的使用。 本发明还涉及小分子变构加工抑制剂用于治疗由不适当的基质金属蛋白酶（MMP）活性介导的疾病的用途。
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10.发明申请Analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, asparate 101 or leucine 137 有权在一种或多种位置谷氨酸盐89，天冬氨酸101或亮氨酸137突变的人碱性成纤维细胞生长因子的类似物公开(公告)号：US20050159350A1
公开(公告)日：2005-07-21
申请号：US10785436
申请日：2004-02-23
Applicant: Barry Springer , Michael Pantoliano , Celia Sharp
Inventor： Barry Springer , Michael Pantoliano , Celia Sharp
CPC classification number: C07K14/503 , A61K38/00
Abstract: The present invention relates to novel muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the production of said muteins. Also disclosed are methods for stimulating cell division, treating a wound, treating ischemia, treating heart disease, treating neural injury, treating peripheral vascular disease, treating a gastric ulcer and treating a duodenal ulcer.
Abstract translation: 本发明涉及具有超强调性质的人碱性成纤维细胞生长因子的新颖突变蛋白。 公开了蛋白质和各自编码的核酸物质。 本发明还体现了用于扩增所述核酸序列和产生所述突变蛋白的载体和宿主细胞。 还公开了刺激细胞分裂，治疗伤口，治疗缺血，治疗心脏病，治疗神经损伤，治疗外周血管疾病，治疗胃溃疡和治疗十二指肠溃疡的方法。
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