公开(公告)号：US20200087375A1

公开(公告)日：2020-03-19

申请号：US16495703

申请日：2018-03-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： Danqing Feng ,  David N. Hunter ,  Pei Huo ,  Ahmet Kekec ,  Songnian Lin ,  Christopher R. Moyes ,  Ravi Nargund ,  Brenda Pipik ,  Dmitri A. Pissarnitski ,  Lin Yan ,  Zhiqiang Zhao ,  Yuping Zhu

IPC: C07K14/62 ,  A61K47/61 ,  A61K47/54

Abstract: An insulin conjugate comprising or consisting of a tri-valent sugar cluster is described. In particular aspects, the insulin conjugate displays 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：US10183981B2

公开(公告)日：2019-01-22

申请号：US16007046

申请日：2018-06-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07K14/62 ,  A61K38/28 ,  A61K47/55 ,  A61K47/60 ,  A61K38/00

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

公开(公告)号：US20180291078A1

公开(公告)日：2018-10-11

申请号：US16007046

申请日：2018-06-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07K14/62 ,  A61K47/60 ,  A61K38/28 ,  A61K47/55 ,  A61K38/00

CPC classification number: C07K14/62 ,  A61K38/00 ,  A61K38/28 ,  A61K47/55 ,  A61K47/60 ,  C07K2319/00

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

公开(公告)号：US20170355743A1

公开(公告)日：2017-12-14

申请号：US15527363

申请日：2015-11-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07K14/62 ,  A61K38/28 ,  A61K47/55 ,  A61K47/60

CPC classification number: C07K14/62 ,  A61K38/00 ,  A61K38/28 ,  A61K47/55 ,  A61K47/60 ,  C07K2319/00

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

公开(公告)号：US09018224B2

公开(公告)日：2015-04-28

申请号：US14358241

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Edmondson ,  Zhiyong Hu ,  Ping Liu ,  Gregori J. Morriello ,  Jason W. Szewczyk ,  Bowei Wang ,  Liping Wang ,  Harold B. Wood ,  Cheng Zhu ,  Yuping Zhu ,  Zhiqiang Guo

IPC: A01N43/54 ,  A61K31/505 ,  C07D513/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D239/42 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

CPC classification number: C07D513/04 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 披露式（I）的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。