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1.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
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。
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2.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
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。
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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
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.
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公开(公告)号：US5891661A
公开(公告)日：1999-04-06
申请号：US823932
申请日：1997-03-25
申请人： Paul L. Darke , Lawrence C. Kuo
发明人： Paul L. Darke , Lawrence C. Kuo
CPC分类号： C12N9/503 , C12Q1/37 , G01N2333/045
摘要： At low temperature, the protease of human cytomegalovirus (HCMV) is rendered highly active as a dimer of identical units. The protease is useful as a screening tool for HCMV antivirals as well as a diagnostic tool for diseases resulting from HCMV infection.
摘要翻译： 在低温下，人巨细胞病毒（HCMV）的蛋白酶作为相同单元的二聚体具有高活性。 该蛋白酶可用作HCMV抗病毒药物的筛选工具，以及用于HCMV感染引起的疾病的诊断工具。
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公开(公告)号：US5861501A
公开(公告)日：1999-01-19
申请号：US807104
申请日：1997-02-04
申请人： Fritz Benseler , James L. Cole , David B. Olsen , Lawrence C. Kuo
发明人： Fritz Benseler , James L. Cole , David B. Olsen , Lawrence C. Kuo
IPC分类号： C12N15/09 , A61K31/70 , A61K38/00 , A61K48/00 , A61P31/12 , A61P31/16 , C07H21/00 , C07H21/02 , C12N15/113 , C12N15/115 , C12Q1/68
CPC分类号： C12N15/115 , C07H21/00 , C12N15/1131 , A61K38/00 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/3513
摘要： A method is provided for making synthetic capped RNAs. These compounds serve as substrates for the virally encoded endonuclease associated with influenza virus. We are able to assay for this unique and specific viral activity of cleavage of a capped RNA in vitro. Therefore, screening of inhibitors of this activity is possible. In addition, short non-extendible (due to their length or because of the modification of the 3'-end of the oligo, i.e. 3'-dA) RNAs are potent inhibitors of the cleavage of capped RNAs by influenza endonuclease. Finally, these compounds may be used to investigate viral and cellular mechanisms of transcription/translation or mRNA maturation.
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公开(公告)号：US08822447B2
公开(公告)日：2014-09-02
申请号：US13091344
申请日：2011-04-21
申请人： Xuqing Zhang , Marta C. Abad , Alan C. Gibbs , Gee-Hong Kuo , Lawrence C. Kuo , Fengbin Song , Zhihua Sui
发明人： Xuqing Zhang , Marta C. Abad , Alan C. Gibbs , Gee-Hong Kuo , Lawrence C. Kuo , Fengbin Song , Zhihua Sui
IPC分类号： A61K31/416 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/519 , A61K31/551 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D471/04 , C07D487/04 , C07D487/08 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D491/08 , C07D231/56 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D471/04 , C07D487/04 , C07D487/10
摘要： The present invention is directed to substituted indazole compounds of formula (I) pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
摘要翻译： 本发明涉及式（I）的取代的吲唑化合物，这些化合物的药物组合物及其使用方法。 本发明的化合物是用于治疗或改善KHK介导的代谢紊乱和/或疾病如肥胖，II型糖尿病和代谢综合征X的酮基己糖激酶（KHK）抑制剂。
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7.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
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
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。
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公开(公告)号：US6111095A
公开(公告)日：2000-08-29
申请号：US480068
申请日：1995-06-07
申请人： Fritz Benseler , James L. Cole , David B. Olsen , Lawrence C. Kuo
发明人： Fritz Benseler , James L. Cole , David B. Olsen , Lawrence C. Kuo
IPC分类号： C12N15/09 , A61K31/70 , A61K38/00 , A61K48/00 , A61P31/12 , A61P31/16 , C07H21/00 , C07H21/02 , C12N15/113 , C12N15/115 , C12Q1/68 , C12N9/12
CPC分类号： C12N15/115 , C07H21/00 , C12N15/1131 , A61K38/00 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/3513
摘要： A method is provided for making synthetic capped RNAs. These compounds serve as substrates for the virally encoded endonuclease associated with influenza virus. We are able to assay for this unique and specific viral activity of cleavage of a capped RNA in vitro. Therefore, screening of inhibitors of this activity is possible. In addition, short non-extendible (due to their length or because of the modification of the 3'-end of the oligo, i.e. 3'-dA) RNAs are potent inhibitors of the cleavage of capped RNAs by influenza endonuclease. Finally, these compounds may be used to investigate viral and cellular mechanisms of transcription/translation or mRNA maturation.
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公开(公告)号：US5486470A
公开(公告)日：1996-01-23
申请号：US279754
申请日：1994-07-21
申请人： Paul L. Darke , Dawn L. Hall , Lawrence C. Kuo
发明人： Paul L. Darke , Dawn L. Hall , Lawrence C. Kuo
CPC分类号： C12N9/503 , Y10S435/815
摘要： A method of purifying proteases from the Herpes Simplex Virus 1 and 2 is taught. A precursor protease is cloned in a host cell and then separated from the cell culture using cation exchange chromatography. The resulting protease is subjected to autoprocessing conditions and an autolytic cleavage occurs, resulting in mature protease.
摘要翻译： 教导了从单纯疱疹病毒1和2单纯化蛋白酶的方法。 将前体蛋白酶克隆在宿主细胞中，然后使用阳离子交换层析从细胞培养物中分离。 所得到的蛋白酶经受自动加工条件并发生自溶解，导致成熟的蛋白酶。
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10.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
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
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。
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