公开(公告)号：US20190338008A1

公开(公告)日：2019-11-07

申请号：US15759911

申请日：2016-10-21

申请人： Anandan PALANI ,  Ravi NARGUND ,  Paul E. CARRINGTON ,  Tomi SAWYER ,  Qiaolin DENG ,  Antonello PESSI ,  Elisabetta BIANCHI ,  Fe-derica ORYIETO ,  Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： C07K14/605 ,  A61P3/04 ,  A61K38/28

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

公开(公告)号：US10793615B2

公开(公告)日：2020-10-06

申请号：US15759911

申请日：2016-10-21

申请人： Merck Sharp & Dohme Corp. ,  Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

发明人： Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： A61K38/00 ,  A61K38/28 ,  A61P3/04 ,  A61P7/12 ,  A61P3/10 ,  C07K14/435 ,  C07K14/605

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

公开(公告)号：US20190175744A1

公开(公告)日：2019-06-13

申请号：US16083201

申请日：2017-03-13

申请人： Anandan PALANI ,  Chunhui HUANG ,  Zhiqiang YANG ,  Lin YAN ,  Songnian LIN ,  Pei HUO ,  Qiaolin DENG ,  Elisabetta BIANCHI ,  Federica ORVIETO ,  Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Chunhui Huang ,  Zhiqiang Yang ,  Lin Yan ,  Songnian Lin ,  Pei Huo ,  Qiaolin Deng ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： A61K47/64 ,  A61K38/28 ,  A61K38/26

摘要： Insulin-incretin conjugates comprising a peptide having agonist activity at the glucagon-like 1 (GLP-1) receptor, the glucagon (GCG) receptor, and/or the gastric inhibitory protein (GIP) receptor conjugated to an insulin molecule having agonist activity at the insulin receptor and use of the conjugates for treatment of metabolic diseases, for example, Type 2 diabetes, are described.

公开(公告)号：US11566057B2

公开(公告)日：2023-01-31

申请号：US16643881

申请日：2018-09-21

申请人： Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Qiaolin Deng ,  Chunhui Huang ,  Yuping Zhu ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： A61K38/28 ,  A61K38/26 ,  C07K14/605 ,  A61P3/10 ,  C07K14/62 ,  A61K38/00

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

公开(公告)号：US11492385B2

公开(公告)日：2022-11-08

申请号：US17003921

申请日：2020-08-26

申请人： Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： A61K38/00 ,  A61K38/28 ,  A61P3/04 ,  A61P7/12 ,  A61P3/10 ,  C07K14/435 ,  C07K14/605

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

公开(公告)号：US10413593B2

公开(公告)日：2019-09-17

申请号：US15519565

申请日：2015-10-22

申请人： MERCK SHARP & DOHME CORP.

发明人： Elisabetta Bianchi ,  Paul E. Carrington ,  Qiaolin Deng ,  Ravi Nargund ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Thomas Joseph Tucker ,  Chengwei Wu

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

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.

公开(公告)号：US20170360893A1

公开(公告)日：2017-12-21

申请号：US15519565

申请日：2015-10-22

申请人： MERCK SHARP & DOHME CORP.

发明人： Elisabetta Bianchi ,  Paul E. Carrington ,  Qiaolin Deng ,  Ravi Nargund ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Thomas Joseph Tucker ,  Chengwei Wu

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

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

公开(公告)号：US20160114000A1

公开(公告)日：2016-04-28

申请号：US14920012

申请日：2015-10-22

申请人： MERCK SHARP & DOHME CORP.

发明人： Elisabetta Bianchi ,  Paul E. Carrington ,  Qiaolin Deng ,  Ravi Nargund ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Thomas Joseph Tucker ,  Chengwei Wu

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

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，其已被修饰为对二肽基肽酶IV（DPP-IV）的切割和失活具有抗性，并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 胰高血糖素样肽1（GLP-1）受体和胰高血糖素（GCG）受体，以及使用这样的GLP-1受体/ GCG受体辅助激动剂来治疗代谢紊乱如糖尿病，非酒精性脂肪肝 疾病（NAFLD），非酒精性脂肪性肝炎（NASH）和肥胖症。

公开(公告)号：US10800826B2

公开(公告)日：2020-10-13

申请号：US15765505

申请日：2016-10-04

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

发明人： Paul Carrington ,  Grigori Ermakov ,  Robert M. Garbaccio ,  Wolfgang Seghezzi ,  Elisabetta Bianchi ,  Federica Orvieto ,  Dennis Gately ,  Nick Knudsen ,  Anthony Manibusan

IPC分类号： C07K14/605 ,  C07K16/26 ,  C07K16/28 ,  A61K47/68 ,  A61P3/10 ,  A61K39/00

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：US20200270325A1

公开(公告)日：2020-08-27

申请号：US16643881

申请日：2018-09-21

申请人： Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Qiaolin Deng ,  Chunhui Huang ,  Yuping Zhu ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： C07K14/605 ,  C07K14/62 ,  A61P3/10

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