公开(公告)号：US08853212B2

公开(公告)日：2014-10-07

申请号：US13520653

申请日：2011-02-17

申请人： Robert R. Wilkening ,  James M. Apgar ,  Tesfaye Biftu ,  Danqing Feng ,  Xiaoxia Qian ,  Lan Wei

发明人： Robert R. Wilkening ,  James M. Apgar ,  Tesfaye Biftu ,  Danqing Feng ,  Xiaoxia Qian ,  Lan Wei

IPC分类号： C07D487/04 ,  C07D498/04 ,  A61K31/519 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4188 ,  A61K31/424 ,  A61K31/4985 ,  A61P29/00 ,  A61P37/00 ,  A61P9/00 ,  A61P3/10 ,  C07D335/02

CPC分类号： C07D487/04 ,  C07D335/02 ,  C07D498/04 ,  C07B2200/07

摘要： The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof 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： 本发明涉及作为二肽基肽酶-IV酶的抑制剂的结构式（I）的新型取代的氨基四氢硫代吡喃及其衍生物，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：US20060258646A1

公开(公告)日：2006-11-16

申请号：US10556805

申请日：2004-05-10

申请人： Tesfaye Biftu ,  Danqing Feng ,  Gui Liang ,  Xiaoxia Qian

发明人： Tesfaye Biftu ,  Danqing Feng ,  Gui Liang ,  Xiaoxia Qian

IPC分类号： A61K31/551 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The pre-sent invention is directed to 3-amino-4-phenylbutanoic acid 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.

公开(公告)号：US20150284411A1

公开(公告)日：2015-10-08

申请号：US14419774

申请日：2013-08-19

申请人： 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.

发明人： 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分类号： C07D519/00 ,  A61K31/438 ,  A61K45/06 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/437 ,  A61K31/506

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

摘要： 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.

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。

公开(公告)号：US20120277240A1

公开(公告)日：2012-11-01

申请号：US13520653

申请日：2011-02-17

申请人： Robert R. Wilkening ,  James M. Apgar ,  Tesfaye Biftu ,  Danqing Feng ,  Xiaoxia Qian ,  Lan Wei

发明人： Robert R. Wilkening ,  James M. Apgar ,  Tesfaye Biftu ,  Danqing Feng ,  Xiaoxia Qian ,  Lan Wei

IPC分类号： A61K31/519 ,  C07D498/04 ,  C07D409/04 ,  A61K31/4162 ,  A61K31/424 ,  A61K31/404 ,  A61K31/4985 ,  A61K31/4188 ,  A61P3/10 ,  A61P3/06 ,  A61P3/04 ,  A61P9/10 ,  A61P1/02 ,  A61P29/00 ,  A61P1/18 ,  A61P25/28 ,  A61P9/00 ,  A61P37/06 ,  A61P31/18 ,  A61P35/04 ,  A61P15/16 ,  A61P19/10 ,  A61P25/22 ,  A61P5/28 ,  A61P13/12 ,  A61P7/00 ,  A61P5/00 ,  A61P27/02 ,  A61P37/00 ,  A61P9/08 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D335/02 ,  C07D498/04 ,  C07B2200/07

摘要： The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof 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： 本发明涉及作为二肽基肽酶-IV酶的抑制剂的结构式（I）的新型取代的氨基四氢硫代吡喃及其衍生物，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：US20150011590A1

公开(公告)日：2015-01-08

申请号：US14376787

申请日：2013-02-12

申请人： Ann E. WEBER ,  Tesfaye BIFTU ,  Merck Sharp & Dohme Corporation

发明人： Ann E. Weber ,  Tesfaye Biftu

IPC分类号： C07D487/04 ,  A61K31/155 ,  A61K31/4439 ,  A61K31/4162

CPC分类号： C07D487/04 ,  A61K31/155 ,  A61K31/4162 ,  A61K31/4439 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention is directed to novel substituted dihydropyrrolopyrazoles 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的新型取代二氢吡咯并吡唑，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：US08980929B2

公开(公告)日：2015-03-17

申请号：US13643121

申请日：2011-05-16

申请人： Jacqueline D. Hicks ,  Tesfaye Biftu ,  Ping Chen ,  Xiaoxia Qian ,  Robert R. Wilkening

发明人： Jacqueline D. Hicks ,  Tesfaye Biftu ,  Ping Chen ,  Xiaoxia Qian ,  Robert R. Wilkening

IPC分类号： A01N43/78 ,  A61K31/425 ,  C07D413/00 ,  C07D498/00 ,  C07D417/00 ,  C07D513/00 ,  C07D271/12 ,  C07D285/14 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04

摘要： The present invention is directed to novel amino-substituted seven-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 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）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，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：US08796258B2

公开(公告)日：2014-08-05

申请号：US13812536

申请日：2012-02-23

申请人： Rajan Anand ,  James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Lin Chu ,  Vincent J. Colandrea ,  Guizhen Dong ,  James F. Dropinski ,  Danqing Feng ,  Jacqueline D. Hicks ,  Jinlong Jiang ,  Alexander J. Kim ,  Kenneth J. Leavitt ,  Bing Li ,  Xiaoxia Qian ,  Iyassu Sebhat ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

发明人： Rajan Anand ,  James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Lin Chu ,  Vincent J. Colandrea ,  Guizhen Dong ,  James F. Dropinski ,  Danqing Feng ,  Jacqueline D. Hicks ,  Jinlong Jiang ,  Alexander J. Kim ,  Kenneth J. Leavitt ,  Bing Li ,  Xiaoxia Qian ,  Iyassu Sebhat ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC分类号： A61K31/00 ,  C07D513/02

CPC分类号： A61K31/5377 ,  A61K31/351 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： Novel compounds of 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，预防和抑制由AMPK激活的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：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：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：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。