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.

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

公开(公告)号：EP3359191A1

公开(公告)日：2018-08-15

申请号：EP16854155.5

申请日：2016-10-04

申请人： Merck Sharp & Dohme Corp. ,  Ambrx, Inc.

发明人： GARBACCIO, Robert, M. ,  CARRINGTON, Paul, E. ,  SEGHEZZI, Wolfgang ,  ERMAKOV, Grigori ,  BIANCHI, Elisabetta ,  ORVIETO, Federica ,  KNUDSEN, Nick ,  MANIBUSAN, Anthony ,  GATELY, Dennis

IPC分类号： A61K39/395 ,  C07K16/08 ,  C07K16/10 ,  C07K19/00 ,  C07K14/605 ,  C07K14/575 ,  A61P3/10 ,  A61P3/08

CPC分类号： C07K14/605 ,  A61K47/6811 ,  A61K47/6843 ,  A61K2039/505 ,  C07K16/26 ,  C07K16/2869 ,  C07K2317/75 ,  C07K2319/00

摘要： Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, 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 have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：EP3209682A1

公开(公告)日：2017-08-30

申请号：EP15790398.0

申请日：2015-10-22

申请人： Merck Sharp & Dohme Corp.

发明人： CARRINGTON, Paul, E. ,  DENG, Qiaolin ,  NARGUND, Ravi ,  PALANI, Anandan ,  TUCKER, Thomas Joseph ,  WU, Chengwei ,  BIANCHI, Elisabetta ,  ORVIETO, Federica ,  PESSI, Antonello

IPC分类号： C07K14/605 ,  A61K38/26 ,  A61K38/28

CPC分类号： A61K38/28 ,  A61K38/26 ,  C07K14/605 ,  A61K2300/00

摘要： Described are peptide analogs of glucagon, 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 have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity

摘要翻译： 描述了胰高血糖素的肽类似物，其已经被修饰以抵抗二肽基肽酶IV（DPP-IV）的切割和失活并且增加肽类似物的体内半衰期，同时使肽类似物具有相对平衡的激动剂活性 对胰高血糖素样肽1（GLP-1）受体和胰高血糖素（GCG）受体的应用，以及此类GLP-1受体/ GCG受体共激动剂用于治疗代谢病症例如糖尿病，非酒精性脂肪肝 疾病（NAFLD），非酒精性脂肪性肝炎（NASH）和肥胖。

公开(公告)号：EP3394091A2

公开(公告)日：2018-10-31

申请号：EP16873641.1

申请日：2016-12-05

申请人： Merck Sharp & Dohme Corp.

发明人： PALANI, Anandan ,  CARRINGTON, Paul, E. ,  PESSI, Antonello ,  LAHM, Armin ,  BIANCHI, Elisabetta ,  DEMARTIS, Anna

IPC分类号： C07K14/605 ,  C07K14/575 ,  C07K14/435

CPC分类号： A61K38/16 ,  A61K38/00 ,  A61P1/16 ,  A61P3/10 ,  C07K14/575

摘要： Co-agonists of the glucagon and GLP-1 receptors are described.

公开(公告)号：EP3377521A2

公开(公告)日：2018-09-26

申请号：EP16860542.6

申请日：2016-10-21

申请人： Merck Sharp & Dohme Corp.

发明人： PALANI, Anandan ,  NARGUND, Ravi ,  CARRINGTON, Paul, E. ,  SAWYER, Tomi ,  DENG, Qiaolin ,  PESSI, Antonello ,  BIANCHI, Elisabetta ,  ORVIETO, Federica

IPC分类号： C07K14/605 ,  C07K14/705 ,  A61K38/00 ,  A61K38/26 ,  A61K38/28 ,  A61P3/04 ,  A61P3/10 ,  A61P7/12 ,  C12N15/10

CPC分类号： C07K14/435 ,  A61K38/00 ,  A61K38/28 ,  C07K14/605 ,  A61K2300/00

摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.