公开(公告)号：WO2020243049A1

公开(公告)日：2020-12-03

申请号：PCT/US2020/034468

申请日：2020-05-26

Applicant: MERCK SHARP & DOHME CORP. ,  HICKS, Jacqueline, D. ,  DEBENHAM, John, S. ,  ALI, Amjad ,  WEI, Lan ,  JIAN, Tianying ,  YANG, Dexi ,  OGAWA, Anthony, K. ,  FU, Wenlang ,  LOMBARDO, Matthew ,  KUANG, Rongze ,  YANG, Meng ,  SO, Sung-Sau ,  ELLSWORTH, Kenneth ,  NIZNER, Peter ,  TATOSIAN, Daniel, A. ,  WILKENING, Robert, R. ,  WANG, Jun

Inventor： HICKS, Jacqueline, D. ,  DEBENHAM, John, S. ,  ALI, Amjad ,  WEI, Lan ,  JIAN, Tianying ,  YANG, Dexi ,  OGAWA, Anthony, K. ,  FU, Wenlang ,  LOMBARDO, Matthew ,  KUANG, Rongze ,  YANG, Meng ,  SO, Sung-Sau ,  ELLSWORTH, Kenneth ,  NIZNER, Peter ,  TATOSIAN, Daniel, A. ,  WILKENING, Robert, R. ,  WANG, Jun

IPC: A61K31/4162 ,  A61P7/02

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

公开(公告)号：WO2014031468A1

公开(公告)日：2014-02-27

申请号：PCT/US2013/055246

申请日：2013-08-16

Applicant: MERCK SHARP & DOHME CORP. ,  APGAR, James, M. ,  ARASAPPAN, Ashok ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  GUIDRY, Erin ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai

Inventor： APGAR, James, M. ,  ARASAPPAN, Ashok ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  GUIDRY, Erin ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai

IPC: A01N43/50 ,  A61K31/4184

CPC classification number: C07D493/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/454 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

Abstract: The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention 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.

Abstract translation: 本发明的新型苯并咪唑六氢呋喃并[3,2-B]呋喃衍生物是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：WO2005108382A1

公开(公告)日：2005-11-17

申请号：PCT/US2005/015133

申请日：2005-04-29

Applicant: MERCK & CO., INC. ,  XU, Jinyou ,  WEI, Lan ,  MASTRACCHIO, Anthony ,  EDMONDSON, Scott, D.

Inventor： XU, Jinyou ,  WEI, Lan ,  MASTRACCHIO, Anthony ,  EDMONDSON, Scott, D.

IPC: C07D271/06

CPC classification number: C07D271/06 ,  C07D413/06 ,  C07D417/06

Abstract: The present invention is directed to novel 1,2,4-oxadiazole 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.

Abstract translation: 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）的抑制剂的新的1,2,4-恶二唑衍生物，其可用于治疗或预防其中二肽基肽酶 - 涉及IV酶，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：WO2022040070A1

公开(公告)日：2022-02-24

申请号：PCT/US2021/046098

申请日：2021-08-16

Applicant: MERCK SHARP & DOHME CORP. ,  BOGEN, Stephane, L. ,  CLAUSEN, Dane James ,  GUIADEEN, Deodial Guy ,  HAO, Jinsong ,  LIN, Shishi ,  RUDD, Michael, T. ,  WEI, Lan ,  XIAO, Li ,  YANG, Dexi

Inventor： BOGEN, Stephane, L. ,  CLAUSEN, Dane James ,  GUIADEEN, Deodial Guy ,  HAO, Jinsong ,  LIN, Shishi ,  RUDD, Michael, T. ,  WEI, Lan ,  XIAO, Li ,  YANG, Dexi

IPC: C07D403/12 ,  C07D207/14 ,  C07D405/14 ,  C07D417/12 ,  C07D491/04 ,  A61K31/506 ,  A61P43/00

Abstract: The present invention is directed to bicyclo[4.1 0]heptane pyrrolidine compounds of formula (I) which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 diseases in which orexin receptors are involved.

公开(公告)号：WO2014031517A1

公开(公告)日：2014-02-27

申请号：PCT/US2013/055531

申请日：2013-08-19

Applicant: MERCK SHARP & DOHME CORP. ,  APGAR, James, M. ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai ,  ARASAPPAN, Ashok

Inventor： APGAR, James, M. ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai ,  ARASAPPAN, Ashok

IPC: A61P3/10 ,  A61K31/4184 ,  A61K31/415 ,  A61K31/454

CPC classification number: C07D471/04 ,  A61K31/19 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  C07C53/18 ,  C07D519/00 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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：WO2014031465A1

公开(公告)日：2014-02-27

申请号：PCT/US2013/055240

申请日：2013-08-16

Applicant: MERCK SHARP & DOHME CORP. ,  APGAR, James, M. ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai

Inventor： APGAR, James, M. ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai

IPC: A61P3/10 ,  A61K31/4184 ,  A61K31/415 ,  A61K31/454

CPC classification number: C07D471/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4985 ,  A61K45/06 ,  A61K2300/00

Abstract: 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 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.

Abstract translation: 结构式（I）的新化合物是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：WO2014031445A1

公开(公告)日：2014-02-27

申请号：PCT/US2013/055177

申请日：2013-08-15

Applicant: MERCK SHARP & DOHME CORP. ,  APGAR, James, M. ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai

Inventor： APGAR, James, M. ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  HICKS, Jacqueline, D. ,  KEKEC, Ahmet ,  LEAVITT, Kenneth, J. ,  LI, Bing ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert, R. ,  WU, Zhicai

IPC: A01N43/50 ,  A61K31/4184

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

Abstract: 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.

Abstract translation: 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：WO2002073208A2

公开(公告)日：2002-09-19

申请号：PCT/CA2002/000363

申请日：2002-03-13

Applicant: QUEEN'S UNIVERSITY AT KINGSTON ,  NEUROCHEM INC. ,  WEAVER, Donald, F. ,  TAN, Christopher, Y., K. ,  KIM, Stephen, T. ,  KONG, Xianqi ,  WEI, Lan ,  CARRAN, John, R.

Inventor： WEAVER, Donald, F. ,  TAN, Christopher, Y., K. ,  KIM, Stephen, T. ,  KONG, Xianqi ,  WEI, Lan ,  CARRAN, John, R.

IPC: G01N33/68

CPC classification number: C07D239/54 ,  A61K31/195 ,  C07D239/553 ,  C07D239/557 ,  C07D239/96 ,  C07D405/04 ,  C07D473/06 ,  C07D491/04 ,  G01N33/6896 ,  G01N33/9406 ,  G01N2500/00

Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described.

Abstract translation: 公开了用于抑制惊厥性疾病（包括癫痫）的方法和化合物。 本发明的方法和化合物抑制或预防发热和/或癫痫发生。 还描述了制备本发明化合物的方法。

公开(公告)号：WO2022119888A1

公开(公告)日：2022-06-09

申请号：PCT/US2021/061344

申请日：2021-12-01

Applicant: MERCK SHARP & DOHME CORP. ,  BOGEN, Stephane, L. ,  CHEN, Ping ,  CLAUSSEN, Dane James ,  HUANG, Xianhai ,  RUDD, Michael, T. ,  WALSH, Shawn, P. ,  WEI, Lan ,  YANG, Dexi

Inventor： BOGEN, Stephane, L. ,  CHEN, Ping ,  CLAUSSEN, Dane James ,  HUANG, Xianhai ,  RUDD, Michael, T. ,  WALSH, Shawn, P. ,  WEI, Lan ,  YANG, Dexi

IPC: A61K31/454 ,  A61P25/20 ,  C07D405/14

Abstract: The present invention is directed to 3-heteroaryl pyrrolidine and piperidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 diseases in which orexin receptors are involved.

公开(公告)号：WO2014031515A1

公开(公告)日：2014-02-27

申请号：PCT/US2013/055528

申请日：2013-08-19

Applicant: MERCK SHARP & DOHME CORP. ,  APGAR, James, M. ,  ARASAPPAN, Ashok ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  GUIDRY, Erin ,  HICKS, Jacqueline ,  KEKEC, Ahmet ,  LEAVITT, Kenneth ,  LI, Bing ,  MCCRACKEN, Troy ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert ,  WU, Zhicai

Inventor： APGAR, James, M. ,  ARASAPPAN, Ashok ,  BIFTU, Tesfaye ,  CHEN, Ping ,  FENG, Danqing ,  GUIDRY, Erin ,  HICKS, Jacqueline ,  KEKEC, Ahmet ,  LEAVITT, Kenneth ,  LI, Bing ,  MCCRACKEN, Troy ,  SEBHAT, Iyassu ,  QIAN, Xiaoxia ,  WEI, Lan ,  WILKENING, Robert ,  WU, Zhicai

IPC: A61P3/10 ,  A61K31/4184 ,  A61K31/415 ,  A61K31/454

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

Abstract: 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.

Abstract translation: 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。