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1. 发明授权

US08883473B2 Methods of treatment using allosteric processing inhibitors for matrix metalloproteinases 有权
标题翻译：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
申请人： 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
发明人： 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分类号： A61K31/4439 , A61K31/427 , A61P19/02 , A61K31/425
CPC分类号： A61K31/425 , A61K31/4439 , C07K2299/00 , G01N2333/96486
摘要： 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.
摘要翻译：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。

2. 发明授权

US08753857B2 Crystal structure of the pro form of a matrix metalloproteinase and an allosteric processing inhibitor 失效
标题翻译：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
申请人： 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
发明人： 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
IPC分类号： C12N9/00 , G01N31/00
CPC分类号： C12N9/6491 , C12Y304/24017 , C12Y304/24035
摘要： 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.
摘要翻译：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。

3. 发明授权

US08798939B2 Methods for designing, selecting and/or optimizing allosteric processing inhibitors for matrix metalloproteinases 有权
标题翻译：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
申请人： 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
发明人： 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
IPC分类号： G01N33/48 , G01N33/50 , G01N31/00
CPC分类号： G06F19/706 , C12N9/6491 , G06F19/16 , G06F19/18 , Y02A90/26
摘要： 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.
摘要翻译：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。

4. 发明申请

US20130166268A1 Crystal Structure of the Pro Form of a Matrix Metalloproteinase and an Allosteric Processing Inhibitor 有权
标题翻译：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
申请人： 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
发明人： 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分类号： G06F19/12
CPC分类号： G06F19/706 , C12N9/6491 , G06F19/16 , G06F19/18 , Y02A90/26
摘要： 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.
摘要翻译：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。

5. 发明申请

US20130040994A1 Methods of Treatment Using Allosteric Processing Inhibitors for Matrix Metalloproteinases 有权
标题翻译：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
申请人： 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
发明人： 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分类号： 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分类号： A61K31/425 , A61K31/4439 , C07K2299/00 , G01N2333/96486
摘要： 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.
摘要翻译：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。

6. 发明申请

US20130040360A1 Crystal Structure of the Pro Form of a Matrix Metalloproteinase and an Allosteric Processing Inhibitor 失效
公开(公告)号：US20130040360A1
公开(公告)日：2013-02-14
申请号：US13533108
申请日：2012-06-26
申请人： 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
发明人： 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分类号： C12N9/96
CPC分类号： C12N9/6491 , C12Y304/24017 , C12Y304/24035
摘要： 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.

7. 发明授权

US06242190B1 Method for high throughput thermodynamic screening of ligands 失效
标题翻译：配体高通量热力学筛选方法
公开(公告)号：US06242190B1
公开(公告)日：2001-06-05
申请号：US09451837
申请日：1999-12-01
申请人： Ernesto Freire , Matthew J. Todd
发明人： Ernesto Freire , Matthew J. Todd
IPC分类号： C12Q168
CPC分类号： G01N33/53
摘要： The present invention provides a method of rapidly screening ligands on the basis of their binding affinity and binding enthalpy by carrying out binding assays at a minimum of two temperatures. This technique permits the selection for further optimization of lead ligands that bind to the target molecules with favorable enthalpies. Those ligands will exhibit higher solubilities in aqueous solution than ligands selected by conventional means, and may exhibit lower susceptibilities to resistant mutations. The method may be utilized as a standalone technique, or may be adapted to, for example, known high throughput screening technologies. The present invention further comprises an apparatus for carrying out the described methods.
摘要翻译：本发明提供了一种通过在至少两个温度下进行结合测定来快速筛选基于其结合亲和力和结合焓的配体的方法。该技术允许选择进一步优化与合适的焓结合到靶分子的铅配体。那些配体在与通过常规方法选择的配体相比在水溶液中显示更高的溶解度，并且可能表现出较低的抗性突变敏感性。该方法可以用作独立技术，或者可以适用于例如已知的高通量筛选技术。本发明还包括用于执行所述方法的装置。

8. 发明申请

US20110124120A1 ASSAY FOR EVALUATING AFFINITY AND SPECIFICITY OF LIGAND-ALBUMIN BINDING 有权
标题翻译：用于评估配体结合物的亲和性和特异性的测定
公开(公告)号：US20110124120A1
公开(公告)日：2011-05-26
申请号：US12885865
申请日：2010-09-20
申请人： James K. Kranz , Gabrielle C. Todd , Matthew J. Todd
发明人： James K. Kranz , Gabrielle C. Todd , Matthew J. Todd
IPC分类号： G01N33/53
CPC分类号： G01N33/542 , G01N33/68 , G01N2333/76
摘要： A method for identifying a ligand or compound which binds to albumin comprises the steps of contacting a reaction mixture comprising a site-specific probe and albumin in the presence and the absence of the ligand or compound and measuring either dissociation constant KD, inhibitor concentration IC50 or fluorescence displacement; whereby a change in KD, IC50 and/or fluorescence in the presence of the ligand or compound is indicative of the ligand or compound binds to albumin.
摘要翻译：用于鉴定与白蛋白结合的配体或化合物的方法包括以下步骤：在存在和不存在配体或化合物的情况下使包含位点特异性探针和白蛋白的反应混合物接触并测量解离常数KD，抑制剂浓度IC50或荧光位移; 由此在配体或化合物存在下KD，IC 50和/或荧光的变化指示配体或化合物与白蛋白结合。

9. 发明授权

US08476081B2 Assay for evaluating affinity and specificity of ligand-albumin binding 有权
标题翻译：用于评估配体 - 白蛋白结合的亲和性和特异性的测定
公开(公告)号：US08476081B2
公开(公告)日：2013-07-02
申请号：US12885865
申请日：2010-09-20
申请人： James K. Kranz , Gabrielle C. Todd , Matthew J. Todd
发明人： James K. Kranz , Gabrielle C. Todd , Matthew J. Todd
IPC分类号： G01N33/566
CPC分类号： G01N33/542 , G01N33/68 , G01N2333/76
摘要： A method for identifying a ligand or compound which binds to albumin comprises the steps of contacting a reaction mixture comprising a site-specific probe and albumin in the presence and the absence of the ligand or compound and measuring either dissociation constant KD, inhibitor concentration IC50 or fluorescence displacement; whereby a change in KD, IC50 and/or fluorescence in the presence of the ligand or compound is indicative of the ligand or compound binds to albumin.
摘要翻译：用于鉴定与白蛋白结合的配体或化合物的方法包括以下步骤：在存在和不存在配体或化合物的情况下使包含位点特异性探针和白蛋白的反应混合物接触并测量解离常数KD，抑制剂浓度IC50或荧光位移; 由此在配体或化合物存在下KD，IC 50和/或荧光的变化指示配体或化合物与白蛋白结合。

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