公开(公告)号：US20180305352A1

公开(公告)日：2018-10-25

申请号：US15769414

申请日：2016-10-25

申请人： MERCK SHARP & DOHME CORP.

发明人： David J. Witter ,  Tesfaye Biftu ,  Purakkattle Biju ,  Stephane L. Bogen ,  Qingmei Hong ,  Chunhui Huang ,  Xianhai Huang ,  Bing Li ,  Min K. Park ,  David L. Sloman

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61P35/02

CPC分类号： C07D471/04 ,  A61P35/02 ,  C07D491/10 ,  C07D498/08 ,  C07D519/00

摘要： The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：US09527839B2

公开(公告)日：2016-12-27

申请号：US14420090

申请日：2013-08-15

申请人： Merck Sharp & Dohme Corp.

发明人： James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Danqing Feng ,  Jacqueline D. Hicks ,  Ahmet Kekec ,  Kenneth J. Leavitt ,  Bing Li ,  Iyassu Sebhat ,  Xiaoxia Qian ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

CPC分类号： C07D417/14 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

摘要： Novel compounds described herein are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPKactivated 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： 本文所述的新型化合物是AMP-蛋白激酶的活化剂，并且可用于治疗，预防和抑制由AMPK活化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：US09278976B2

公开(公告)日：2016-03-08

申请号：US14825535

申请日：2015-08-13

申请人： Merck Sharp & Dohme Corp.

发明人： Tesfaye Biftu ,  Ann E. Weber

IPC分类号： C07D487/04 ,  C07D309/30

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.

公开(公告)号：US09138426B2

公开(公告)日：2015-09-22

申请号：US14591124

申请日：2015-01-07

申请人： Merck Sharp & Dohme Corp.

发明人： Tesfaye Biftu ,  Ann E. Weber

IPC分类号： A61K31/4162 ,  A61K38/17 ,  C07D487/04 ,  A61K45/06 ,  A61K9/20 ,  A61K38/26

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：US20150225402A1

公开(公告)日：2015-08-13

申请号：US14415876

申请日：2013-07-18

申请人： Merck Sharp & Dohme Corp.

发明人： Tesfaye Biftu

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  A61K31/4162 ,  C07D231/00

摘要： The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N 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-N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：US09073930B2

公开(公告)日：2015-07-07

申请号：US14376787

申请日：2013-02-12

申请人： Merck Sharp & Dohme Corp.

发明人： Ann E. Weber ,  Tesfaye Biftu

IPC分类号： A61K31/4439 ,  A61K31/4162 ,  C07D487/04 ,  A61K45/06 ,  A61K31/155

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：US20150099891A1

公开(公告)日：2015-04-09

申请号：US14507001

申请日：2014-10-06

申请人： Merck Sharp & Dohme Corp ,  Merck Sharp & Dohme Ltd.

发明人： Itzia Z. Arroyo ,  Davida Krueger ,  Ping Chen ,  Aaron J. Moment ,  Tesfaye Biftu ,  Faye Sheen ,  Yanfeng Zhang

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/513 ,  C07B2200/13 ,  Y02P20/55

摘要： Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.

摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。

公开(公告)号：US20150099771A1

公开(公告)日：2015-04-09

申请号：US14399762

申请日：2013-05-03

申请人： Merck Sharp & Dohme Corp.

发明人： Ian M. Bell ,  Mark Fraley ,  Tesfaye Biftu ,  Cheng Zhu ,  Anilkumar Nair

IPC分类号： C07D471/20 ,  C07D519/00

CPC分类号： C07D471/20 ,  C07D471/10 ,  C07D519/00

摘要： The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 本发明涉及作为CGRP受体的拮抗剂的吡啶衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US20140051740A1

公开(公告)日：2014-02-20

申请号：US14059638

申请日：2013-10-22

申请人： Merck Sharp & Dohme Corp

发明人： Tesfaye Biftu ,  Ann E. Weber

IPC分类号： A61K31/4162 ,  A61K45/06

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.

公开(公告)号：US11230543B2

公开(公告)日：2022-01-25

申请号：US16912146

申请日：2020-06-25

申请人： Merck Sharp & Dohme Corp.

发明人： Haifeng Tang ,  Weiguo Liu ,  Fa-Xiang Ding ,  Wanying Sun ,  Yi Zang ,  Weidong Pan ,  Anthony Ogawa ,  Linda Brockunier ,  Xianhai Huang ,  Hongwu Wang ,  Rudrajit Mal ,  Tesfaye Biftu ,  Min Park ,  Yan Guo ,  Jinlong Jiang ,  Helen Y. Chen ,  Christopher W. Plummer

IPC分类号： C07D417/14 ,  C07D471/04 ,  C07C53/18 ,  C07F9/6558 ,  A61K31/433 ,  A61K31/444 ,  A61K31/4439 ,  A61K45/06 ,  A61P31/04 ,  A61K31/427 ,  A61K31/424 ,  A61K31/431 ,  A61K31/551

摘要： The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, A2, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.