公开(公告)号：US20210115044A1

公开(公告)日：2021-04-22

申请号：US17048811

申请日：2019-04-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： Tao Yu ,  James M. Apgar ,  Alan Whitehead ,  Yonglian Zhang ,  Zhiyong Hu ,  Valerie W. Shurtleff ,  John A. McCauley ,  Izzat T. Raheem

IPC: C07D471/16 ,  A61K31/4985 ,  A61P31/18 ,  A61K31/52 ,  A61K31/435 ,  A61K31/5383 ,  A61K31/506 ,  A61K31/513 ,  A61K31/685 ,  A61K31/427

Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US09868733B2

公开(公告)日：2018-01-16

申请号：US14419825

申请日：2013-08-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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 ,  Ashok Arasappan

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/366 ,  A61K31/397 ,  A61K31/4985 ,  A61K31/19 ,  A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  C07C53/18

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.

公开(公告)号：US10786488B2

公开(公告)日：2020-09-29

申请号：US16479997

申请日：2018-01-23

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Tao Yu ,  John A. McCauley ,  Alan Whitehead ,  James M. Apgar ,  Izzat T. Raheem ,  Guizhen Dong ,  Sherman T. Waddell ,  Hong Li

IPC: A61K31/4375 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/47 ,  A61K31/506 ,  A61K31/5365 ,  A61K31/675 ,  A61K31/7068 ,  A61K31/7076 ,  C07D491/147

Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

公开(公告)号：US20150284411A1

公开(公告)日：2015-10-08

申请号：US14419774

申请日：2013-08-19

Applicant: 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.

Inventor： 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: C07D519/00 ,  A61K31/438 ,  A61K45/06 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/437 ,  A61K31/506

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。

公开(公告)号：US10144741B2

公开(公告)日：2018-12-04

申请号：US15910571

申请日：2018-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Katherine Young ,  David B. Olsen ,  Sheo B. Singh ,  Jing Su ,  Robert R. Wilkening ,  James M. Apgar ,  Dongfang Meng ,  Dann Parker ,  Mihir Mandal ,  Lihu Yang ,  Ronald E. Painter ,  Qun Dang ,  Takao Suzuki

IPC: C07D493/08 ,  C07F7/18 ,  C07D493/18 ,  C07C309/06 ,  C07C53/18

Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

公开(公告)号：US09944654B2

公开(公告)日：2018-04-17

申请号：US15517570

申请日：2015-10-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： Katherine Young ,  David B. Olsen ,  Sheo B. Singh ,  Jing Su ,  Robert R. Wilkening ,  James M. Apgar ,  Dongfang Meng ,  Dann Parker ,  Mihir Mandal ,  Lihu Yang ,  Ronald E. Painter ,  Qun Dang ,  Takao Suzuki

IPC: C07D493/08 ,  C07C53/18 ,  C07C309/06 ,  C07D493/18 ,  C07F7/18

CPC classification number: C07D493/08 ,  C07C53/18 ,  C07C309/06 ,  C07D493/18 ,  C07D519/00 ,  C07F7/1804

Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

公开(公告)号：US09527839B2

公开(公告)日：2016-12-27

申请号：US14420090

申请日：2013-08-15

Applicant: Merck Sharp & Dohme Corp.

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

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：US20180186808A1

公开(公告)日：2018-07-05

申请号：US15910571

申请日：2018-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Katherine Young ,  David B. Olsen ,  Sheo B. Singh ,  Jing Su ,  Robert R. Wilkening ,  James M. Apgar ,  Dongfang Meng ,  Dann Parker ,  Mihir Mandal ,  Lihu Yang ,  Ronald E. Painter ,  Qun Dang ,  Takao Suzuki

IPC: C07D493/08 ,  C07F7/18 ,  C07C53/18 ,  C07C309/06 ,  C07D493/18

CPC classification number: C07D493/08 ,  C07C53/18 ,  C07C309/06 ,  C07D493/18 ,  C07D519/00 ,  C07F7/1804

Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

公开(公告)号：US09382243B2

公开(公告)日：2016-07-05

申请号：US14419842

申请日：2013-08-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07D471/02 ,  A61K31/00 ,  C07D471/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/4985 ,  A61K31/437 ,  A61K31/444 ,  A61K45/06

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 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。

公开(公告)号：US20150218149A1

公开(公告)日：2015-08-06

申请号：US14420024

申请日：2013-08-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07D417/14 ,  A61K31/4184 ,  C07D405/14 ,  A61K31/4192 ,  C07D413/14 ,  A61K31/4985 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/506 ,  A61K31/366 ,  A61K31/397 ,  C07D405/12 ,  A61K31/5377

CPC classification number: C07D417/14 ,  A61K31/366 ,  A61K31/397 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

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。