公开(公告)号：US08143289B2

公开(公告)日：2012-03-27

申请号：US12616831

申请日：2009-11-12

申请人： Tesfaye Biftu ,  Ping Chen ,  Jason M. Cox ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Ping Chen ,  Jason M. Cox ,  Ann E. Weber

IPC分类号： A61K31/4439 ,  A61K31/4162 ,  A61P3/10 ,  C07D401/14 ,  C07D487/04

CPC分类号： C07D309/30 ,  A61K9/2054 ,  A61K31/4162 ,  A61K38/1709 ,  A61K38/26 ,  A61K45/06 ,  C07D487/04

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。

公开(公告)号：US07956061B2

公开(公告)日：2011-06-07

申请号：US11793093

申请日：2006-01-18

申请人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hong Dong ,  Ying-Duo Gao ,  Giovanna Scapin ,  Ann E. Weber

发明人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hong Dong ,  Ying-Duo Gao ,  Giovanna Scapin ,  Ann E. Weber

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P3/10

CPC分类号： C07D487/04 ,  C07D495/14

摘要： The present invention is directed to novel substituted bicyclic pyrimidines 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双环嘧啶，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 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。

公开(公告)号：US07678905B2

公开(公告)日：2010-03-16

申请号：US11728673

申请日：2007-03-27

申请人： Tesfaye Biftu ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Ann E. Weber

IPC分类号： C07D251/00

CPC分类号： C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

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。

公开(公告)号：US07671073B2

公开(公告)日：2010-03-02

申请号：US11579265

申请日：2005-05-13

申请人： Joseph L. Duffy ,  David E. Kaelin, Jr. ,  Ann E. Weber ,  Brian A Kirk

发明人： Joseph L. Duffy ,  David E. Kaelin, Jr. ,  Ann E. Weber ,  Brian A Kirk

IPC分类号： A61K31/44 ,  A61K31/41 ,  A61K31/42 ,  A61K31/415 ,  A61K31/40 ,  C07D401/10 ,  C07D271/06 ,  C07D263/24 ,  C07D249/16

CPC分类号： C07D207/27 ,  C07D207/10 ,  C07D211/38 ,  C07D401/08 ,  C07D401/12 ,  C07D413/08 ,  C07D471/04

摘要： The present invention is directed to novel cyclohexylalanine derivatives 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”）的抑制剂的新型环己基丙氨酸衍生物，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。

公开(公告)号：US07482336B2

公开(公告)日：2009-01-27

申请号：US11628686

申请日：2005-06-17

申请人： Tesfaye Biftu ,  Danqing Feng ,  Ying-Duo Gao ,  Suresh Singh ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Danqing Feng ,  Ying-Duo Gao ,  Suresh Singh ,  Ann E. Weber

IPC分类号： A01N43/00 ,  A01N43/58 ,  A01N43/60 ,  A01N43/90 ,  A01N43/38 ,  A61K31/00 ,  A61K31/50 ,  A61K31/495 ,  A61K31/519 ,  A61K31/40 ,  C07D243/00 ,  C07D471/00

CPC分类号： C07D487/04 ,  C07D209/44 ,  C07D243/08 ,  C07D471/04

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。

公开(公告)号：US5541197A

公开(公告)日：1996-07-30

申请号：US404566

申请日：1995-03-21

申请人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Ann E. Weber

发明人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Ann E. Weber

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 ,  C07D215/04 ,  A61K31/47

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.

公开(公告)号：US5194605A

公开(公告)日：1993-03-16

申请号：US714115

申请日：1991-06-11

申请人： William J. Greenlee ,  Ralph A. Rivero ,  Ann E. Weber ,  Lihu Yang

发明人： William J. Greenlee ,  Ralph A. Rivero ,  Ann E. Weber ,  Lihu Yang

IPC分类号： A61K31/335 ,  A61K31/357 ,  A61K31/395 ,  A61K31/40 ,  A61K31/41 ,  A61K31/435 ,  A61K31/445 ,  A61K31/535 ,  A61K38/00 ,  A61P5/38 ,  A61P9/00 ,  A61P9/12 ,  A61P27/02 ,  A61P31/12 ,  A61P43/00 ,  C07D243/00 ,  C07D245/02 ,  C07D267/00 ,  C07D281/00 ,  C07D321/00 ,  C07D327/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D487/04 ,  C07F9/655 ,  C07F9/6558 ,  C07F9/6561 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K14/81

CPC分类号： C07D403/12 ,  C07D243/00 ,  C07D245/02 ,  C07D267/00 ,  C07D281/00 ,  C07D321/00 ,  C07D327/02 ,  C07D401/12 ,  C07D405/12 ,  C07D413/10 ,  C07D417/12 ,  C07D453/02 ,  C07D487/04 ,  C07F9/65525 ,  C07F9/65586 ,  C07F9/6561 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06139 ,  A61K38/00

摘要： Compounds of the formula ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.

摘要翻译： 公开了式（I）的化合物。 这些化合物抑制天然蛋白水解酶肾素的血管紧张素原切割作用可用于治疗，预防或控制肾素相关性高血压，醛固酮增多症，充血性心力衰竭和青光眼。

公开(公告)号：US08716482B2

公开(公告)日：2014-05-06

申请号：US13390708

申请日：2010-09-15

申请人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

发明人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

IPC分类号： C07D211/32 ,  A61K31/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The present invention is directed to novel substituted aminopiperidines 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-ÏV 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的新型取代氨基哌啶，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-κV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。

公开(公告)号：US08653059B2

公开(公告)日：2014-02-18

申请号：US12672100

申请日：2008-08-18

申请人： Tesfaye Biftu ,  Danqing Feng ,  Ann E. Weber ,  Jason M. Cox ,  Xiaoxia Qian ,  Jinyou Xu

发明人： Tesfaye Biftu ,  Danqing Feng ,  Ann E. Weber ,  Jason M. Cox ,  Xiaoxia Qian ,  Jinyou Xu

IPC分类号： A61K31/33

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D487/14 ,  C07D498/04 ,  C07D513/04

摘要： The present invention is directed to substituted six-membered heterocyclic compounds 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 obesity and diabetes, 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酶的抑制剂的结构式（I）的取代的六元杂环化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 如肥胖和糖尿病，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。

公开(公告)号：US08415297B2

公开(公告)日：2013-04-09

申请号：US13398887

申请日：2012-02-17

申请人： Tesfaye Biftu ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Ann E. Weber

IPC分类号： A61K31/4162 ,  A61K38/28 ,  C07D487/04 ,  A61P3/10

CPC分类号： C07D309/30 ,  A61K9/2054 ,  A61K31/4162 ,  A61K38/1709 ,  A61K38/26 ,  A61K45/06 ,  C07D487/04

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.