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1.发明申请HIGH-THROUGHPUT ASSAY FOR EVALUATING DIPEPTIDYL PEPTIDASE I ACTIVITY 有权用于评估DIPEPTIDYL PEPTIDASE I活性的高通量测定公开(公告)号：US20100136594A1
公开(公告)日：2010-06-03
申请号：US12603372
申请日：2009-10-21
Applicant: Matthew Olson , Matthew Todd
Inventor： Matthew Olson , Matthew Todd
CPC classification number: C12Q1/37 , C07K5/06026 , C12N9/6483 , C12Y304/23004 , G01N2333/948 , G01N2500/02
Abstract: A method of screening a compound which modulates dipeptidyl peptidase I (DPPI) activities comprises the steps of adding a peptide substrate of DPPI to a reaction mixture which comprises DPPI and a compound, wherein the peptide substrate of DPPI has at least 3 amino acids and binds to a binding site of DPPI in addition to the S1-S2 site; and measuring the molecular weight of the substrate, wherein a change in the molecular weight of the substrate is indicative of the presence of DPPI activity.
Abstract translation: 筛选调节二肽基肽酶I（DPPI）活性的化合物的方法包括以下步骤：将DPPI的肽底物加入到包含DPPI和化合物的反应混合物中，其中DPPI的肽底物具有至少3个氨基酸并且结合 除了S1-S2位点之外，还与DPPI的结合位点; 并测量底物的分子量，其中底物分子量的变化表明存在DPPI活性。
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公开(公告)号：US08313920B2
公开(公告)日：2012-11-20
申请号：US12603372
申请日：2009-10-21
Applicant: Matthew Olson , Matthew Todd
Inventor： Matthew Olson , Matthew Todd
CPC classification number: C12Q1/37 , C07K5/06026 , C12N9/6483 , C12Y304/23004 , G01N2333/948 , G01N2500/02
Abstract: A method of screening a compound which modulates dipeptidyl peptidase I (DPPI) activities comprises the steps of adding a peptide substrate of DPPI to a reaction mixture which comprises DPPI and a compound, wherein the peptide substrate of DPPI has at least 3 amino acids and binds to a binding site of DPPI in addition to the S1-S2 site; and measuring the molecular weight of the substrate, wherein a change in the molecular weight of the substrate is indicative of the presence of DPPI activity.
Abstract translation: 筛选调节二肽基肽酶I（DPPI）活性的化合物的方法包括以下步骤：将DPPI的肽底物加入到包含DPPI和化合物的反应混合物中，其中DPPI的肽底物具有至少3个氨基酸并且结合 除了S1-S2位点之外，还与DPPI的结合位点; 并测量底物的分子量，其中底物分子量的变化表明存在DPPI活性。
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Patent Agency Ranking
3.发明申请HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS 有权异佛尔酮和维生素A亚胺基酰胺作为单糖胆碱酯酶抑制剂公开(公告)号：US20100324015A1
公开(公告)日：2010-12-23
申请号：US12765617
申请日：2010-04-22
Applicant: Kristen Chevalier , Jose Clemente , Scott Dax , Chris Flores , Li Liu , Mark Macielag , Mark McDonnell , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang , Bin Zhu
Inventor： Kristen Chevalier , Jose Clemente , Scott Dax , Chris Flores , Li Liu , Mark Macielag , Mark McDonnell , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang , Bin Zhu
IPC: A61K31/496 , C07D403/14 , A61K31/506 , C07D401/14 , C07D417/14 , C07D413/14 , A61P29/00 , A61P1/04 , A61P25/00
CPC classification number: C07D413/14 , C07D205/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.
Abstract translation: 公开了用于治疗受到抑制MGL（包括疼痛）的疾病，综合征，病症和障碍的化合物，组合物和方法。 这样的化合物由式（I）表示如下：其中Y，r，R 2和Z如本文所定义。
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4.发明授权Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors 有权杂芳基和芳香哌嗪基氮杂环丁烷酰胺作为单酰基甘油脂肪酶抑制剂公开(公告)号：US08435977B2
公开(公告)日：2013-05-07
申请号：US12765675
申请日：2010-04-22
Applicant: Chris Flores , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang
Inventor： Chris Flores , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang
IPC: A61K31/496
CPC classification number: C07D413/14 , C07D205/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and are defined herein.
Abstract translation: 公开了用于治疗受到抑制MGL（包括疼痛）的疾病，综合征，病症和障碍的化合物，组合物和方法。 这样的化合物由式（I）表示如下：其中R1，W和本文定义。
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5.发明授权Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors 有权杂芳基和芳香哌嗪基氮杂环丁烷酰胺作为单酰基甘油脂肪酶抑制剂公开(公告)号：US08415341B2
公开(公告)日：2013-04-09
申请号：US12765617
申请日：2010-04-22
Applicant: Kristen Chevalier , Jose Clemente , Scott Dax , Chris Flores , Li Liu , Mark Macielag , Mark McDonnell , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang , Bin Zhu
Inventor： Kristen Chevalier , Jose Clemente , Scott Dax , Chris Flores , Li Liu , Mark Macielag , Mark McDonnell , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang , Bin Zhu
IPC: A61K31/496 , A61K31/551 , C07D401/06 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12
CPC classification number: C07D413/14 , C07D205/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.
Abstract translation: 公开了用于治疗受到抑制MGL（包括疼痛）的疾病，综合征，病症和障碍的化合物，组合物和方法。 这样的化合物由式（I）表示如下：其中Y，r，R 2和Z如本文所定义。
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公开(公告)号：US20120302573A1
公开(公告)日：2012-11-29
申请号：US13479421
申请日：2012-05-24
Applicant: Paul Francis JACKSON , Carl Manthey , Kenneth Rhodes , Robert Scannevin , Kristi Anne Leonard , Joseph Kent Barbay , Matthew Todd , Barry A. Springer
Inventor： Paul Francis JACKSON , Carl Manthey , Kenneth Rhodes , Robert Scannevin , Kristi Anne Leonard , Joseph Kent Barbay , Matthew Todd , Barry A. Springer
IPC: C12N9/99 , A61K31/4439 , A61K31/497 , A61K31/437 , A61K31/519 , A61K31/444 , A61K31/4985 , A61P35/00 , A61P19/02 , A61P9/00 , A61P1/04 , A61P9/12 , A61P11/00 , A61P1/00 , A61P1/02 , A61P17/02 , A61P25/06 , A61K31/427
CPC classification number: A61K31/519 , A61K31/427 , A61K31/454 , A61K31/4985
Abstract: This invention relates to methods for preventing, treating or ameliorating an MMP9 and/or MMP13 mediated syndrome, disorder or disease comprising administering to a subject in need thereof an effective amount of a compound listed in the examples section of this specification, or a form, composition or medicament thereof. Disorders treated and/or prevented include rheumatoid arthritis.
Abstract translation: 本发明涉及用于预防，治疗或改善MMP9和/或MMP13介导的综合征，障碍或疾病的方法，包括向有需要的受试者施用有效量的本说明书实施例部分列出的化合物或形式， 组合物或药物。 治疗和/或预防的疾病包括类风湿性关节炎。
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7.发明申请HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS 有权异佛尔酮和维生素A亚胺基酰胺作为单糖胆碱酯酶抑制剂公开(公告)号：US20100324016A1
公开(公告)日：2010-12-23
申请号：US12765675
申请日：2010-04-22
Applicant: Chris FLORES , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang
Inventor： Chris FLORES , Marina Nelen , Erica Nulton , Stephen Prouty , Matthew Todd , Sui-Po Zhang
IPC: A61K31/496 , C07D401/14 , C07D403/12 , C07D413/14 , A61P29/00 , A61P1/04 , A61P25/00
CPC classification number: C07D413/14 , C07D205/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12
Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and are defined herein.
Abstract translation: 公开了用于治疗受到抑制MGL（包括疼痛）的疾病，综合征，病症和障碍的化合物，组合物和方法。 这样的化合物由式（I）表示如下：其中R1，W和本文定义。
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