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公开(公告)号：EP2398483A1
公开(公告)日：2011-12-28
申请号：EP09840594.7
申请日：2009-12-18
申请人： Merck Sharp & Dohme Corp. , Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. , Indiana University Research&Technology Corporation
发明人： CARRINGTON, Paul, E. , EIERMANN, George, J. , MARSH, Donald, J. , METZGER, Joseph. M. , POCAI, Alessandro , SINHA ROY, Ranabir , BIANCHI, Elisabetta , INGALLINELLA, Paolo , PESSI, Antonello , SANTOPRETE, Alessia , CAPITO, Elena , DIMARCHI, Richard , WARD, Brian
IPC分类号： A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , C07K14/575
摘要： Peptide analogs of oxyntomodulin (OXM, glucagon-37), which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to act as a dual GLP-1/glucagon receptor (GCGR) agonist, are described. The peptide analogs are useful for treatment of metabolic disorders such as diabetes and obesity.
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公开(公告)号：EP2398483B1
公开(公告)日：2014-09-24
申请号：EP09840594.7
申请日：2009-12-18
申请人： Merck Sharp & Dohme Corp. , Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L. , Indiana University Research&Technology Corporation
发明人： CARRINGTON, Paul, E. , EIERMANN, George, J. , MARSH, Donald, J. , METZGER, Joseph. M. , POCAI, Alessandro , SINHA ROY, Ranabir , BIANCHI, Elisabetta , INGALLINELLA, Paolo , PESSI, Antonello , SANTOPRETE, Alessia , CAPITO, Elena , DIMARCHI, Richard , WARD, Brian
IPC分类号： A61K38/00 , C07K14/605 , C07K14/575
CPC分类号： C07K14/605 , A61K38/00 , C07K14/575
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公开(公告)号：EP1755667B1
公开(公告)日：2013-07-17
申请号：EP05804850.5
申请日：2005-05-27
IPC分类号： A61K39/12 , G01N33/68 , C07K14/005
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , A61K39/12 , C12N2740/15022 , C12N2740/16122 , C12N2740/16134 , G01N2333/16 , G01N2500/02
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公开(公告)号：EP2170947A2
公开(公告)日：2010-04-07
申请号：EP08779751.0
申请日：2008-06-18
发明人： BIANCHI, Elisabetta , PESSI, Antonello , INGENITO, Raffaele , WANG, Jun , CARBALLO-JANE, Ester , CHANG, Ching, H.
IPC分类号： C07K14/775
CPC分类号： C07K14/775 , A61K38/00
摘要： The invention relates to peptide mimetics for treating disorders associated with hypercholesterolemia and cardiovascular disease. In particular, the invention relates to peptides that mimic the activity of apolipoprotein A-I (Apo AI).
摘要翻译： 本发明涉及用于治疗与高胆固醇血症和心血管疾病相关的病症的肽模拟物。 特别地，本发明涉及模拟载脂蛋白A-1（Apo AI）活性的肽。
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公开(公告)号：EP1999143B1
公开(公告)日：2011-07-13
申请号：EP07753276.0
申请日：2007-03-16
发明人： MARSH, Donald J. , PESSI, Antonello , BEDNAREK, Maria A. , BIANCHI, Elisabetta , INGALLINELLA, Paolo , PEIER, Andrea M.
CPC分类号： C07K14/575 , A61K38/00 , A61K47/543 , A61K47/554 , A61K47/60
摘要： Neuromedin U receptor agonists for use in the treatment of metabolic disorders such as obesity and diabetes are disclosed.
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公开(公告)号：EP1704167B1
公开(公告)日：2011-01-12
申请号：EP04820430.9
申请日：2004-12-10
CPC分类号： C07K14/005 , C12N2740/16122 , C12N2760/16122
摘要： The present invention provides a method for making a peptide-carrier conjugate. The method comprises modifying a first peptide to produce a second peptide so that the pI of the second peptide is in a favorable range or closer to the range than the pI of the first peptide, and conjugating a plurality of the second peptide to OMPC to obtain a peptide-carrier conjugate. The peptide load, or the solubility of the conjugate, or both of them are increased by the modification.
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7.发明授权METHOD FOR ASSAYING IN VITRO THE PROTEOLYTIC ACTIVITY OF POLYPEPTIDES HAVING HCV NS3 PROTEASE ACTIVITY AND PEPTIDE SUBSTRATES TO BE USED IN THIS METHOD. 无效丙型肝炎病毒NS3蛋白酶多肽具有活性和肽底体外测试蛋白水解活性的方法此过程中使用
公开(公告)号：EP0846164B1
公开(公告)日：2005-03-02
申请号：EP96926574.3
申请日：1996-08-20
发明人： STEINKÜHLER, Christian , PESSI, Antonello , BIANCHI, Elisabetta , TALIANI, Marina , TOMEI, Licia , URBANI, Andrea , DE FRANCESCO, Raffaele , NARJES, Frank
CPC分类号： C07K14/005 , C12N9/506 , C12N2770/24222
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8.发明公开METHODOLOGY TO PRODUCE, PURIFY AND ASSAY POLYPEPTIDES WITH THE PROTEOLYTIC ACTIVITY OF THE HCV NS3 PROTEASE 无效丙型肝炎病毒NS3蛋白酶多肽具有活性和肽底体外测试蛋白水解活性的方法此过程中使用
公开(公告)号：EP0846164A2
公开(公告)日：1998-06-10
申请号：EP96926574.0
申请日：1996-08-20
发明人： STEINKÜHLER, Christian , PESSI, Antonello , BIANCHI, Elisabetta , TALIANI, Marina , TOMEI, Licia , URBANI, Andrea , DE FRANCESCO, Raffaele , NARJES, Frank
CPC分类号： C07K14/005 , C12N9/506 , C12N2770/24222
摘要： The process according to the present invention allows expression and isolation of polypeptides with the proteolytic activity of HCV NS3 protease in a pure, catalytically active form, and in amounts that are sufficient for discovery of NS3 protease inhibitors and for determination of the three-dimensional structure of the NS3 protease. A further subject of the present invention is a procedure that defines the chemical and physical conditions necessary for completion of the proteolytic activity of the above polypeptides. The invention further comprises new compositions of matter (expression vectors) containing nucleotide sequences capable of expressing the above mentioned polypeptides in culture cells. Finally, new compounds of matter are defined, suitable to measure the above proteolytic activity, and useful to develop NS3 protease inhibitors and therefore therapeutic agents for use against HCV. The figure shows the kinetic parameters of HCV NS3 protease using the S3 depsipeptide substrate (SEQ ID NO:45).
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公开(公告)号：EP1755667A2
公开(公告)日：2007-02-28
申请号：EP05804850.5
申请日：2005-05-27
IPC分类号： A61K39/21
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , A61K39/12 , C12N2740/15022 , C12N2740/16122 , C12N2740/16134 , G01N2333/16 , G01N2500/02
摘要： Methods of covalently-stabilizing alpha-helical, chimeric peptides constrained within a homotrimeric or heterotrimeric coiled-coil structure are disclosed. The coiled-coil structures made by the methods disclosed within this specification mimic all or a portion of the internal, trimeric coiled-coil motif contained within the fusogenic conformation of an enveloped virus membrane-fusion protein, particularly the internal coiled-coil domain of the HIV gp41 ectodomain. The HIV-derived, chimeric peptides disclosed comprise a non-HIV, soluble, trimeric form of a coiled-coil fused in helical phase to all or a portion of the N-helix of HIV gp41 and are covalently-stabilized in a homotrimeric or heterotrimeric coiled-coil structure through the formation of disulfide or chemoselective bonds between said peptides. The covalently-stabilized, HIV-derived, homotrimeric or heterotrimeric coiled-coil structures made by the methods disclosed herein represent a close mimetic of a HIV gp41 fusion intermediate and are potent inhibitors of HIV infectivity. These HIV-derived chimeric peptides may provide for therapeutic treatment against HIV infection by inhibiting the virus-host cell membrane fusion process.
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公开(公告)号：EP1615610A2
公开(公告)日：2006-01-18
申请号：EP04750008.7
申请日：2004-04-12
申请人： Merck & Co., Inc. (a New Jersey corp.) , ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.
发明人： KIM, Peter, S. , ECKERT, Debra , GARSKY, Victor, M. , FREIDINGER, Roger, M. , GELEZIUNAS, Romas , PESSI, Antonello
IPC分类号： A61K6/00
CPC分类号： C07K14/005 , A61K39/00 , C12N2740/16043 , C12N2770/20022 , C12N2810/609
摘要： The present invention relates to inhibitors of coronaviruses including severe acute respiratory syndrome (SARS); methods of identifying inhibitors of coronaviruses; methods and compositions useful for therapy (treatment, or prevention) of coronavirus infections. The coronavirus inhibitors target different regions of the coronavirus Spike protein to inhibit coronavirus replication. In particular embodiments, the inhibitors include Five-Helix proteins, HR2 peptides, HR1 peptides, HR1 chimeric peptides. The present invention also features retro-inverso analogue of the coronavirus inhibitors, coronavirus inhibitors containing one or more tryptophan analogs, and / or one or more lactam bridges.
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