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41.发明授权Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权六氢二氮杂酮作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病公开(公告)号：US07259160B2
公开(公告)日：2007-08-21
申请号：US10566235
申请日：2004-07-27
IPC分类号： C07D243/08 , A61K31/551 , A61P3/10
CPC分类号： C07D243/14 , C07D401/06 , C07D487/04
摘要： The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的六氢二氮杂酮化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如 糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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42.发明授权公开(公告)号：US07101871B2
公开(公告)日：2006-09-05
申请号：US10501059
申请日：2003-10-14
IPC分类号： C07D243/08 , A61K31/551 , A61P3/10
CPC分类号： C07D243/08 , C07D401/06 , C07D403/06 , C07K5/06191
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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43.发明授权Substituted sulfonamides as selective .beta..sub.3 agonists for the treatment of diabetes and obesity 失效取代磺酰胺作为治疗糖尿病和肥胖症的选择性β3激动剂
公开(公告)号：US5561142A
公开(公告)日：1996-10-01
申请号：US445630
申请日：1995-05-22
申请人： Michael H. Fisher , Elizabeth M. Naylor , Dong Ok , Ann E. Weber , Thomas Shih , Hyun Ok
发明人： Michael H. Fisher , Elizabeth M. Naylor , Dong Ok , Ann E. Weber , Thomas Shih , Hyun Ok
IPC分类号： C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/44 , A61K31/47 , C07D213/30
CPC分类号： C07D213/73 , C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
摘要翻译： 取代磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。
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44.发明申请NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 有权用作抗糖尿病药物的新型CYABAZABENZIMIDAZOLE衍生物公开(公告)号：US20110190308A1
公开(公告)日：2011-08-04
申请号：US13086563
申请日：2011-04-14
申请人： Scott D. Edmondson , Michael H. Fisher , Dooseop Kim , Malcolm Maccoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
发明人： Scott D. Edmondson , Michael H. Fisher , Dooseop Kim , Malcolm Maccoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
IPC分类号： A61K31/4985 , A61P3/10
CPC分类号： A61K31/4985 , A61K31/498 , A61K38/28 , A61K45/06 , C07D487/04 , Y10S514/866 , A61K2300/00
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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![Substituted 5,6,7,8-tetrahydropyrido[4,3-D]pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes](/abs-image/US/2011/04/19/US07928112B2/abs.jpg.150x150.jpg)
45.发明授权Substituted 5,6,7,8-tetrahydropyrido[4,3-D]pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权取代5,6,7,8-四氢吡啶并[4,3-D]嘧啶作为二肽基肽酶-IV抑制剂，用于治疗或预防糖尿病公开(公告)号：US07928112B2
公开(公告)日：2011-04-19
申请号：US12869869
申请日：2010-08-27
申请人： Tesfaye Biftu , Ping Chen , Danqing Feng , Ann E. Weber
发明人： Tesfaye Biftu , Ping Chen , Danqing Feng , Ann E. Weber
IPC分类号： A61K31/519
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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46.发明授权Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes 有权氨基环己烷作为二肽基肽酶-IV抑制剂治疗糖尿病公开(公告)号：US07906649B2
公开(公告)日：2011-03-15
申请号：US11920038
申请日：2006-05-19
申请人： Tesfaye Biftu , Danqing Feng , Xiaoxia Qian , Ann E. Weber , Jason Cox
发明人： Tesfaye Biftu , Danqing Feng , Xiaoxia Qian , Ann E. Weber , Jason Cox
IPC分类号： C07D513/02 , C07D513/00 , C07D498/00 , C07D403/02 , C07D487/02 , C07D209/44 , A61K31/425 , A61K31/42 , A61K31/415 , A61K31/40
CPC分类号： C07D487/04
摘要： The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的新型取代的氨基环己烷，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如 作为糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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47.发明授权Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权氨基哌啶作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病公开(公告)号：US07884104B2
公开(公告)日：2011-02-08
申请号：US11662064
申请日：2005-09-27
申请人： Jason M. Cox , Scott D. Edmondson , Bart Harper , Ann E. Weber
发明人： Jason M. Cox , Scott D. Edmondson , Bart Harper , Ann E. Weber
IPC分类号： A61K31/4545 , C07D487/04
CPC分类号： C07D401/04 , C07D471/04 , C07D487/04
摘要： The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的新的取代的氨基哌啶，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如 作为糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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48.发明申请公开(公告)号：US20100324054A1
公开(公告)日：2010-12-23
申请号：US12869869
申请日：2010-08-27
申请人： Tesfaye Biftu , Ping Chen , Danqing Feng , Ann E. Weber
发明人： Tesfaye Biftu , Ping Chen , Danqing Feng , Ann E. Weber
IPC分类号： A61K31/4985 , C07D487/04 , C07D471/04 , C07D498/04 , A61K31/519 , A61K31/437 , A61P3/10
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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![Substitued [1,2,4]triazolo[1,5-a]pyrazines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes](/abs-image/US/2010/10/12/US07812027B2/abs.jpg.150x150.jpg)
49.发明授权Substitued [1,2,4]triazolo[1,5-a]pyrazines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权取代的[1,2,4]三唑并[1,5-a]吡嗪作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病公开(公告)号：US07812027B2
公开(公告)日：2010-10-12
申请号：US12226584
申请日：2007-05-11
申请人： Tesfaye Biftu , Ping Chen , Danqing Feng , Ann E. Weber
发明人： Tesfaye Biftu , Ping Chen , Danqing Feng , Ann E. Weber
IPC分类号： A61K31/50
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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50.发明申请BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权用于治疗或预防糖尿病的β-氨基间苯二酚胰蛋白酶抑制剂公开(公告)号：US20100130504A1
公开(公告)日：2010-05-27
申请号：US12694758
申请日：2010-01-27
申请人： Scott D. Edmondson , Michael H. Fisher , Dooseop Kim , Malcolm Maccoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
发明人： Scott D. Edmondson , Michael H. Fisher , Dooseop Kim , Malcolm Maccoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
IPC分类号： A61K31/4985 , A61P3/10
CPC分类号： A61K31/4985 , A61K31/498 , A61K38/28 , A61K45/06 , C07D487/04 , Y10S514/866 , A61K2300/00
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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