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公开(公告)号：US08124633B2
公开(公告)日：2012-02-28
申请号：US12593168
申请日：2008-04-07
IPC分类号： A61K31/422 , C07D209/02
CPC分类号： C07D209/44 , C07D413/04
摘要： The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.
摘要翻译： 本发明涉及某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的羟甲基醚异二氢吲哚化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂 以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，LUTS，抑郁和焦虑）中的用途。
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公开(公告)号：US20100105747A1
公开(公告)日：2010-04-29
申请号：US12593168
申请日：2008-04-07
IPC分类号： A61K31/422 , C07D209/02 , C07D413/04 , A61K31/40
CPC分类号： C07D209/44 , C07D413/04
摘要： The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.
摘要翻译： 本发明涉及某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的羟甲基醚异二氢吲哚化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂 以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，LUTS，抑郁和焦虑）中的用途。
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公开(公告)号：US20220273770A1
公开(公告)日：2022-09-01
申请号：US17629501
申请日：2020-07-23
申请人： Danqing FENG , Erin N. GUIDRY , Pei HUO , Andrew J. KASSICK , Ahmet KEKEC , Songnian LIN , Christopher R MOYES , Dmitri A. PISSARNITSKI , Lin YAN , Yuping ZHU , Merck Sharp & Dohme Corp.
发明人： Danqing Feng , Erin N. Guidry , Pei Huo , Andrew J. Kassick , Ahmet Kekec , Songnian Lin , Christopher R. Moyes , Dmitri A. Pissarnitski , Lin Yan , Yuping Zhu
摘要： Glucose-responsive insulin conjugates that contain one or more trisaccharides are provided. Such insulin conjugates may 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.
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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：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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