公开(公告)号：US09556193B2

公开(公告)日：2017-01-31

申请号：US14420011

申请日：2013-08-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： James M. Apgar ,  Ashok Arasappan ,  Tesfaye Biftu ,  Ping Chen ,  Danqing Feng ,  Erin Guidry ,  Jacqueline Hicks ,  Ahmet Kekec ,  Kenneth J. Leavitt ,  Bing Li ,  Iyassu Sebhat ,  Xiaoxia Qian ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC: C07D493/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/4985 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/454 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D493/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/454 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

Abstract: The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract translation: 本发明的新型苯并咪唑六氢呋喃并[3,2-B]呋喃衍生物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

公开(公告)号：US09290517B2

公开(公告)日：2016-03-22

申请号：US14419774

申请日：2013-08-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： James M. Apgar ,  Ashok Arasappan ,  Tesfaye Biftu ,  Ping Chen ,  Danqing Feng ,  Erin Guidry ,  Jacqueline D. Hicks ,  Ahmet Kekec ,  Kenneth J. Leavitt ,  Bing Li ,  Troy McCracken ,  Iyassu Sebhat ,  Xiaoxia Qian ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC: C07D401/14 ,  A61K31/437 ,  C07D519/00 ,  A61K31/438 ,  A61K31/506 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

公开(公告)号：US20160251407A1

公开(公告)日：2016-09-01

申请号：US15025912

申请日：2014-10-02

Applicant: Songnian LIN ,  Lin YAN ,  Ahmet KEKEC ,  Yuping ZHU ,  David N. HUNTER ,  Pei HUO ,  Danqing FENG ,  Ravi P. NARGUND ,  Christopher R. MOYES ,  Zhiqiang ZHAO ,  Brenda PIPIK ,  Dimitri PISSARNITSKI ,  Joseph L. DUFFY ,  Erin N. GUIDRY ,  MERCK SHARP & DOHME CORP.

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

IPC: C07K14/62 ,  A61K38/28 ,  A61K47/48

CPC classification number: A61K47/61 ,  A61K38/28 ,  A61K47/549 ,  A61K47/64 ,  C07K14/62

Abstract: 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.

Abstract translation: 胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子，每个臂独立地连接到包含糖的配体，并且其中至少一个连接体的配体是岩藻糖。 胰岛素缀合物显示药代动力学（PK）和/或药效学（PD）谱，其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应，即使在不存在外源多价的情况下施用于有需要的受试者时 糖结合分子如Con A.

公开(公告)号：US20150284411A1

公开(公告)日：2015-10-08

申请号：US14419774

申请日：2013-08-19

Applicant: James M. APGAR ,  Ashok ARASAPPAN ,  Tesfaye BIFTU ,  Ping CHEN ,  Danqing FENG ,  Erin GUIDRY ,  Jacqueline HICKS ,  Ahmet KEKEC ,  Kenneth LEAVITT ,  Bing LI ,  Troy MCCRACKEN ,  Iyassu SEBHAT ,  Xiaoxia QIAN ,  Lan WEI ,  Robert WILKENING ,  Zhicai WU ,  Merck Sharp & Dohme Corp.

Inventor： James M. Apgar ,  Ashok Arasappan ,  Tesfaye Biftu ,  Ping Chen ,  Danqing Feng ,  Erin Guidry ,  Jacqueline D. Hicks ,  Ahmet Kekec ,  Kenneth J. Leavitt ,  Bing Li ,  Troy McCracken ,  Iyassu Sebhat ,  Xiaoxia Qian ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC: C07D519/00 ,  A61K31/438 ,  A61K45/06 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/437 ,  A61K31/506

CPC classification number: C07D519/00 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。