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公开(公告)号：US20150105317A1
公开(公告)日：2015-04-16
申请号：US14504476
申请日：2014-10-02
发明人： 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 N. Guidry
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 the saccharide for 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.
摘要翻译： 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，并且其中所述连接体的至少一个配体的糖是岩藻糖。 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.
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公开(公告)号：US08394969B2
公开(公告)日：2013-03-12
申请号：US12563782
申请日：2009-09-21
申请人： Brett C. Bookser , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
发明人： Brett C. Bookser , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
IPC分类号： A61K31/4184 , C07D235/26 , C07D235/28 , C07D235/30
CPC分类号： C07D235/26 , C07D235/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
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33.发明申请公开(公告)号：US20110263533A1
公开(公告)日：2011-10-27
申请号：US13124898
申请日：2009-10-12
申请人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
发明人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
IPC分类号： A61K31/675 , C07F9/40 , C07F9/6574 , A61P35/00 , A61P3/04 , A61P3/06 , A61P9/12 , C07F9/6506 , A61P3/10
CPC分类号： C07F9/65068 , C07F9/65583 , C07F9/657181
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 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，高胆固醇血症和高血压。
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34.发明申请公开(公告)号：US20100081643A1
公开(公告)日：2010-04-01
申请号：US12563782
申请日：2009-09-21
申请人： BRETT C. BOOKSER , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
发明人： BRETT C. BOOKSER , Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka
IPC分类号： A61K31/4184 , C07D235/26 , C07D403/12 , C07D401/12 , C07D413/10 , A61K31/397 , A61K31/44 , A61K31/5025 , A61K31/4439 , A61P3/00 , A61P9/00
CPC分类号： C07D235/26 , C07D235/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 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。
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公开(公告)号：US08895596B2
公开(公告)日：2014-11-25
申请号：US13578302
申请日：2011-02-21
IPC分类号： C07D235/06 , C07D235/26 , C07D235/28 , C07D235/30 , A61K45/06 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4985 , C07D401/12 , A61K31/4412 , C07D403/12 , C07D405/12
CPC分类号： C07D405/12 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4412 , A61K31/4985 , A61K45/06 , C07D235/26 , C07D401/12 , C07D403/12 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 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。
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公开(公告)号：US08410284B2
公开(公告)日：2013-04-02
申请号：US13124898
申请日：2009-10-12
申请人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
发明人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
IPC分类号： A61K31/675 , C07F9/00 , C07F9/6506
CPC分类号： C07F9/65068 , C07F9/65583 , C07F9/657181
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 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，高胆固醇血症和高血压。
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公开(公告)号：US20120309736A1
公开(公告)日：2012-12-06
申请号：US13578302
申请日：2011-02-21
IPC分类号： A61K31/4184 , C07D405/12 , C07D413/10 , A61K31/5377 , C07D403/10 , C07D401/10 , A61K31/454 , A61K31/397 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/12 , A61P35/00 , A61K31/4439 , A61K31/44 , A61K31/4985 , C07D235/26
CPC分类号： C07D405/12 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4412 , A61K31/4985 , A61K45/06 , C07D235/26 , C07D401/12 , C07D403/12 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 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。
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