公开(公告)号：US09884125B2

公开(公告)日：2018-02-06

申请号：US15025912

申请日：2014-10-02

申请人： Merck Sharp & Dohme Corp.

发明人： Songnian Lin ,  Christopher R. Moyes

IPC分类号： A61K38/28 ,  C07K14/62 ,  A61K47/48 ,  A61P3/10

CPC分类号： A61K47/61 ,  A61K38/28 ,  A61K47/549 ,  A61K47/64 ,  C07K14/62

摘要： Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

公开(公告)号：US20180009796A1

公开(公告)日：2018-01-11

申请号：US15104537

申请日：2015-01-20

申请人： Merck Sharp & Dohme Corp.

发明人： Richard Berger ,  Timothy A. Blizzard ,  Brian T. Campbell ,  Helen Y. Chen ,  John S. Debenham ,  Sunita V. Dewnani ,  Byron Dubois ,  Candido Gude ,  Zack Zhiqiang Guo ,  Bart Harper ,  Zhiyong Hu ,  Songnian Lin ,  Ping Liu ,  Ming Wang ,  Feroze Ujjainwalla ,  Jiayi Xu ,  Libo Xu ,  Rui Zhang

IPC分类号： C07D413/14 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04

摘要： The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

公开(公告)号：US20170355743A1

公开(公告)日：2017-12-14

申请号：US15527363

申请日：2015-11-19

申请人： Merck Sharp & Dohme Corp.

发明人： Songnian Lin ,  Lin Yan ,  Pei Huo ,  Dmitri Pissarnitski ,  Danqing Feng ,  Ravi Nargund ,  Yuping Zhu ,  Ahmet Kekec ,  Christina B. Madsen-Duggan ,  Zhi-Cai Shi ,  Zhicai Wu ,  Yingjun Mu

IPC分类号： C07K14/62 ,  A61K38/28 ,  A61K47/55 ,  A61K47/60

CPC分类号： C07K14/62 ,  A61K38/00 ,  A61K38/28 ,  A61K47/55 ,  A61K47/60 ,  C07K2319/00

摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

公开(公告)号：US20170248580A1

公开(公告)日：2017-08-31

申请号：US15595115

申请日：2017-05-15

申请人： Merck Sharp & Dohme Corp.

发明人： Yingjun Mu ,  Ruojing Yang ,  Xinghai Li ,  Margaret Wu ,  Qing Dallas-yang ,  Yuli Chen ,  Ge Dai ,  Songnian Lin ,  David E. Kelley ,  Mark Erion

IPC分类号： G01N33/50 ,  G01N33/569

CPC分类号： G01N33/5055 ,  G01N33/74 ,  G01N2333/70596 ,  G01N2500/04

摘要： Methods for identifying drug-saccharide conjugates that bind the mannose receptor, C type 1, (MRC1) and may be taken up by cells expressing MRC1, and the use of such drug-saccharide conjugates for treatment of particular diseases are described. In particular, the methods for identifying insulin-saccharide conjugates that bind the MRC1 receptor and may be taken up by cells expressing the MRC1 and use of such conjugates for treatment of diabetes are described.

公开(公告)号：US20230285514A1

公开(公告)日：2023-09-14

申请号：US17785279

申请日：2020-12-18

申请人： Elisabetta BIANCHI ,  Paul E. CARRINGTON ,  Qiaolin DENG ,  Songnian LIN ,  Federica ORVIETO ,  Anandan PALANI ,  Antonello PESSI ,  Tomi K. SAWYER ,  Merck Sharp & Dohme LLC

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

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

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

摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：US20110306624A1

公开(公告)日：2011-12-15

申请号：US13148809

申请日：2010-02-03

申请人： Songnian Lin ,  Xibin Liao ,  Edward Metzger ,  Emma R. Parmee ,  Sheryl D. Debenham

发明人： Songnian Lin ,  Xibin Liao ,  Edward Metzger ,  Emma R. Parmee ,  Sheryl D. Debenham

IPC分类号： A61K31/4035 ,  C07D215/08 ,  A61K31/47 ,  C07D209/08 ,  A61K31/404 ,  C07D401/10 ,  A61K31/4439 ,  C07D403/12 ,  A61K31/4155 ,  C07D403/10 ,  A61K31/506 ,  C07D217/06 ,  A61K31/472 ,  A61P3/10 ,  C07D209/44

CPC分类号： A61K31/40

摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

摘要翻译： 公开了胰高血糖素受体拮抗剂化合物。 该化合物可用于治疗2型糖尿病及相关病症。 还包括药物组合物和治疗方法。

公开(公告)号：US20110281795A1

公开(公告)日：2011-11-17

申请号：US13146220

申请日：2010-01-15

申请人： Songnian Lin ,  Fengqi Zhang ,  Emma R. Parmee ,  Sunita V. Dewnani

发明人： Songnian Lin ,  Fengqi Zhang ,  Emma R. Parmee ,  Sunita V. Dewnani

IPC分类号： A61K31/381 ,  C07D231/12 ,  A61K31/4155 ,  C07D257/06 ,  A61K31/41 ,  C07D257/04 ,  C07D261/06 ,  A61K31/422 ,  A61K31/397 ,  A61K31/40 ,  A61K31/485 ,  A61K31/5415 ,  A61K31/427 ,  A61K31/4439 ,  A61K38/28 ,  A61K38/31 ,  A61K31/445 ,  A61K31/715 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/454 ,  A61K31/44 ,  A61P3/10 ,  C07D333/56

CPC分类号： C07D413/12 ,  C07D333/24 ,  C07D333/60 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04

摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

公开(公告)号：US20070265332A1

公开(公告)日：2007-11-15

申请号：US11801841

申请日：2007-05-11

申请人： Min Ge ,  Jiafang He ,  Fiona Wai Yu Lau ,  Gui-Bai Liang ,  Songnian Lin ,  Weiguo Liu ,  Shawn P. Walsh ,  Lihu Yang

发明人： Min Ge ,  Jiafang He ,  Fiona Wai Yu Lau ,  Gui-Bai Liang ,  Songnian Lin ,  Weiguo Liu ,  Shawn P. Walsh ,  Lihu Yang

IPC分类号： A61K31/381 ,  A61K31/343 ,  A61K31/192 ,  A61K31/195

CPC分类号： C07D213/643 ,  C07C62/34 ,  C07C62/38 ,  C07C229/50 ,  C07C2603/08 ,  C07D307/93 ,  C07D311/94 ,  C07D333/78 ,  C07D405/04 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12

摘要： Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

摘要翻译： 与环双环稠合的环状羧酸或羧酸衍生物（如酰胺）的三环化合物（包括其药学上可接受的盐和前体药物）是G-蛋白偶联受体40（GPR40）的激动剂，可用作治疗性化合物，特别是在 2型糖尿病的治疗，以及经常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

公开(公告)号：US20110172256A1

公开(公告)日：2011-07-14

申请号：US13063820

申请日：2009-09-10

申请人： Songnian Lin ,  Christian P. Stevenson ,  Emma R. Parmee ,  Libo Xu ,  Xibin Liao ,  Edward metzger ,  Rui Liang ,  Fengqi Zhang ,  John E. Stelmach

发明人： Songnian Lin ,  Christian P. Stevenson ,  Emma R. Parmee ,  Libo Xu ,  Xibin Liao ,  Edward metzger ,  Rui Liang ,  Fengqi Zhang ,  John E. Stelmach

IPC分类号： A61K31/517 ,  C07D215/14 ,  A61K31/47 ,  A61P3/10 ,  C07D215/227 ,  C07D471/04 ,  A61K31/4375 ,  C07D239/74

CPC分类号： C07D215/18 ,  C07D215/227 ,  C07D217/22 ,  C07D217/24 ,  C07D239/70 ,  C07D403/04 ,  C07D413/04

摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

公开(公告)号：US07759493B2

公开(公告)日：2010-07-20

申请号：US11794705

申请日：2006-01-30

申请人： Min Ge ,  Lihu Yang ,  Changyou Zhou ,  Songnian Lin ,  Haifeng Tang ,  Eric Dean Cline ,  Sunita Malkani

发明人： Min Ge ,  Lihu Yang ,  Changyou Zhou ,  Songnian Lin ,  Haifeng Tang ,  Eric Dean Cline ,  Sunita Malkani

IPC分类号： A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4725 ,  A61K31/443 ,  A61K31/4439 ,  C07D417/12 ,  C07D413/12 ,  C07D233/72 ,  C07D277/34 ,  C07D271/06 ,  C07D263/44

CPC分类号： C07D263/44 ,  C07D233/74 ,  C07D271/07 ,  C07D277/34 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

摘要： Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

摘要翻译： 包含与环烷基或杂环稠合的苯基或吡啶环的双环化合物，其连接有5元杂环，包括其药学上可接受的盐和前药，是G蛋白偶联受体40（GPR40）的激动剂，并且是有用的 作为治疗性化合物，特别是治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。