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公开(公告)号：WO2016126646A1
公开(公告)日：2016-08-11
申请号：PCT/US2016/016074
申请日：2016-02-02
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： MILLER, Michael Matthew , ALLEN, Martin Patrick , LI, Ling , MAPELLI, Claudio , POIRIER, Maude A. , SUN, Li-Qiang , ZHAO, Qian , MULL, Eric , GILLIS, Eric P. , SCOLA, Paul Michael
Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Abstract translation: 本公开提供了抑制PD-1 / PD-L1和PD-L1 / CD80蛋白质/蛋白质相互作用的新型大环肽，因此可用于改善各种疾病，包括癌症和 传染病。
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2.发明申请
公开(公告)号：WO2003033671A3
公开(公告)日：2003-04-24
申请号：PCT/US2002/033386
申请日：2002-10-18
Applicant: BRISTOL-MYERS SQUIBB COMPANY , NATARAJAN, Sesha, I. , BASTOS, Margarita, M. , BERNATOWICZ, Michael, S. , MAPELLI, Claudio , LEE, Ving , EWING, William, R.
Inventor： NATARAJAN, Sesha, I. , BASTOS, Margarita, M. , BERNATOWICZ, Michael, S. , MAPELLI, Claudio , LEE, Ving , EWING, William, R.
IPC: A61K38/00
Abstract: The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.
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公开(公告)号：WO1997016550A1
公开(公告)日：1997-05-09
申请号：PCT/US1996017365
申请日：1996-10-28
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： BRISTOL-MYERS SQUIBB COMPANY , MAPELLI, Claudio , MEYERS, Chester, A. , KRYSTEK, Stanley, R., Jr. , NOVOTNY, Jiri
IPC: C12N15/16
CPC classification number: C07K14/5759 , A61K38/00
Abstract: Novel C-terminal fragments of the obese gene product. The fragments retain anti-obesity and/or anti-diabetic activities. The fragments contain less than 68 amino acids, two of which are capable of forming cross-linkages, preferably cysteines.
Abstract translation: 肥胖基因产物的新C-末端片段。 片段保留抗肥胖和/或抗糖尿病活动。 片段含有少于68个氨基酸，其中两个能够形成交联，优选半胱氨酸。
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公开(公告)号：WO2023288213A1
公开(公告)日：2023-01-19
申请号：PCT/US2022/073630
申请日：2022-07-12
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： ALLEN, Martin Patrick , MAPELLI, Claudio , POSS, Michael A. , WANG, Tammy C. , QIAO, Jennifer X. , ZHANG, Yunhi
Abstract: In accordance with the present disclosure, macrocyclic compounds have been discovered that bind to PD-1 and are capable of inhibiting the interaction of PD-1 with PD-L1. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.
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公开(公告)号：WO2013163248A1
公开(公告)日：2013-10-31
申请号：PCT/US2013/037897
申请日：2013-04-24
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： KORNACKER, Michael G. , MAPELLI, Claudio , RIEXINGER, Douglas James
IPC: C07K7/06 , C07K14/705 , A61K38/00
CPC classification number: C07K7/06 , A61K38/00 , C07D487/04 , C07D513/04 , C07K14/705
Abstract: The present invention provides PAR4 agonist peptides. These peptides are useful for developing robust PAR4 receptor assays.
Abstract translation: 本发明提供PAR4激动剂肽。 这些肽可用于开发鲁棒的PAR4受体测定。
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Patent Agency Ranking6.发明申请
公开(公告)号：WO2004035606A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/032893
申请日：2003-10-15
Applicant: BRISTOL-MYERS SQUIBB COMPANY , KORNACKER, Michael, G. , COPELAND, Robert, A. , HENDRICK, Joseph , LAI, Zhihong , MAPELLI, Claudio , WITMER, MARK, Richard , MARCINKEVICIENE, Jovita , METZLER, William , LEE, Ving , RIEXINGER, Douglas
Inventor： KORNACKER, Michael, G. , COPELAND, Robert, A. , HENDRICK, Joseph , LAI, Zhihong , MAPELLI, Claudio , WITMER, MARK, Richard , MARCINKEVICIENE, Jovita , METZLER, William , LEE, Ving , RIEXINGER, Douglas
IPC: C07K
CPC classification number: C07K7/08 , C07K1/04 , C07K1/042 , C07K7/06 , C07K14/005 , C07K14/4702 , C07K14/4711 , C12N2740/16122
Abstract: The present invention provides peptides that specifically bind to BACE at a newly discovered exosite. The invention also provides methods for identifying peptides that bind to a BACE exosite. The invention further provides methods for identifying compounds that bind to a BACE exosite and modulate BACE activity. In another aspect, the invention provides methods for treating or preventing neurodegenerative disorders such as Alzheimer's disease by administering compounds that bind to a BACE exosite and modulate BACE activity.
Abstract translation: 本发明提供了在新发现的外部位点特异性结合BACE的肽。 本发明还提供了鉴定与BACE外部位点结合的肽的方法。 本发明还提供用于鉴定结合BACE外部位点并调节BACE活性的化合物的方法。 另一方面，本发明提供了通过施用与BACE外部位点结合并调节BACE活性的化合物来治疗或预防神经变性疾病如阿尔茨海默病的方法。
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7.发明申请HUMAN GLUCAGON-LIKE-PEPTIDE-1 MIMICS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS 审中-公开人类GLUCAGON-PEPTIDE-1 MIMICS及其在治疗糖尿病及相关病症中的应用
公开(公告)号：WO2003033671A2
公开(公告)日：2003-04-24
申请号：PCT/US2002/033386
申请日：2002-10-18
Applicant: BRISTOL-MYERS SQUIBB COMPANY , NATARAJAN, Sesha, I. , BASTOS, Margarita, M. , BERNATOWICZ, Michael, S. , MAPELLI, Claudio , LEE, Ving , EWING, William, R.
Inventor： NATARAJAN, Sesha, I. , BASTOS, Margarita, M. , BERNATOWICZ, Michael, S. , MAPELLI, Claudio , LEE, Ving , EWING, William, R.
IPC: C12N
CPC classification number: A61K45/06 , A61K38/00 , C07K14/605
Abstract: The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.
Abstract translation: 本发明提供了模拟天然GLP-1肽的生物学活性的新型人胰高血糖素样肽-1（GLP-1）肽模拟物，因此可用于治疗或预防与GLP活性相关的疾病或病症。 此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。 这些合成肽GLP-1模拟物表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。
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8.发明申请MACROCYCLIC INHIBITORS OF THE PD-1/PD-L1 AND CD80 (B7-1)/PD-LI PROTEIN/PROTEIN INTERACTIONS 审中-公开PD-1 / PD-L1和CD80（B7-1）/ PD-L1蛋白/蛋白质相互作用的大环内酰胺酶抑制剂
公开(公告)号：WO2016039749A1
公开(公告)日：2016-03-17
申请号：PCT/US2014/055093
申请日：2014-09-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： MILLER, Michael Matthew , MAPELLI, Claudio , ALLEN, Martin Patrick , BOWSHER, Michael S. , GILLIS, Eric P. , LANGLEY, David R. , MULL, Eric , POIRIER, Maude A. , SANGHVI, Nishith , SUN, Li-Qiang , TENNEY, Daniel J. , YEUNG, Kap-Sun , ZHU, Juliang , GILLMAN, Kevin W. , ZHAO, Qian , GRANT-YOUNG, Katharine A. , SCOLA, Paul Michael
IPC: A61K38/10 , C07K7/08 , G01N33/574
Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Abstract translation: 本公开提供了抑制PD-1 / PD-L1和PD-L1 / CD80蛋白/蛋白相互作用的新型大环肽，因此可用于改善各种疾病，包括癌症和感染性疾病。
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9.发明申请IMMUNOASSAY STANDARDS AND MEASUREMENT OF CLINICAL BIOMARKERS USING INTRA-ASSAY CALIBRATION STANDARDS 审中-公开临床生物标志物的免疫标准和测量使用内标测定标准
公开(公告)号：WO2011100292A1
公开(公告)日：2011-08-18
申请号：PCT/US2011/024151
申请日：2011-02-09
Applicant: BRISTOL-MYERS SQUIBB COMPANY , RHYNE, Paul , MAPELLI, Claudio , WONG, Oitak , BERISHA, Flora , NEELY, Robert, John
Inventor： RHYNE, Paul , MAPELLI, Claudio , WONG, Oitak , BERISHA, Flora , NEELY, Robert, John
IPC: G01N33/68 , G01N33/531 , C07K19/00
CPC classification number: G01N33/6896 , C07K14/4711 , C07K16/28 , G01N33/531 , G01N33/54393 , G01N2333/4709 , G01N2496/00
Abstract: The present invention provides novel compositions and methods for creating quantitative standards to calibrate analytes. These compositions and methods enable the creation of standards and calibrators for analyzing analytes and measuring clinical biomarkers. Also provided are kits comprising the novel compositions for use in assays, for example sandwich immunoassays.
Abstract translation: 本发明提供用于产生校准分析物的定量标准的新型组合物和方法。 这些组合物和方法可以创建用于分析分析物和测量临床生物标志物的标准品和校准品。 还提供了包含用于测定的新型组合物的试剂盒，例如夹心免疫测定。
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10.发明申请HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS 审中-公开人类GLUCAGON-PEPTIDE-1调节剂及其在治疗糖尿病及相关病症中的应用
公开(公告)号：WO2007082264A2
公开(公告)日：2007-07-19
申请号：PCT/US2007/060383
申请日：2007-01-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY , HAQUE, Tasir Shamsul , EWING, William R. , MAPELLI, Claudio , LEE, Ving G. , SULSKY, Richard B. , RIEXINGER, Douglas James , MARTINEZ, Rogelio L. , ZHU, Yeheng , RUAN, Zheming
Inventor： HAQUE, Tasir Shamsul , EWING, William R. , MAPELLI, Claudio , LEE, Ving G. , SULSKY, Richard B. , RIEXINGER, Douglas James , MARTINEZ, Rogelio L. , ZHU, Yeheng , RUAN, Zheming
IPC: C07K14/43
CPC classification number: C07K14/605 , A61K38/26 , A61K38/28 , C07C271/16 , C07C2603/18 , A61K2300/00
Abstract: The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified compounds that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The compounds of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
Abstract translation: 本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症 。 此外，本发明提供新颖的化学修饰的化合物，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。 这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。 本发明的化合物在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。
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