公开(公告)号：US10968193B2

公开(公告)日：2021-04-06

申请号：US15328735

申请日：2015-08-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Helen Chen ,  Steven L. Colletti ,  Duane DeMong ,  Yan Guo ,  Michael Miller ,  Anilkumar Nair ,  Christopher W. Plummer ,  Dong Xiao ,  De-Yi Yang

IPC: C07D491/06 ,  C07D311/60 ,  C07D405/14 ,  C07D491/08 ,  C07D405/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107 ,  A61K31/4985 ,  C07D451/02 ,  A61K31/397 ,  A61K45/06 ,  A61K31/366 ,  C07D413/14 ,  C07D413/12 ,  C07D471/08

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US10662171B2

公开(公告)日：2020-05-26

申请号：US15328908

申请日：2015-08-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harry Chobanian ,  Duane DeMong ,  Yan Guo ,  Barbara Pio ,  Christopher W. Plummer

IPC: C07D335/06 ,  C07D213/64 ,  C07D311/04 ,  A61K45/06 ,  A61K31/453 ,  A61K31/44 ,  A61K31/353 ,  A61K31/192 ,  A61K31/352 ,  C07D311/20 ,  A61K31/366 ,  A61K31/382 ,  C07D405/04 ,  A61K31/444 ,  C07D405/10

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US09957219B2

公开(公告)日：2018-05-01

申请号：US15034189

申请日：2014-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Thomas Bara ,  Harry R. Chobanian ,  Yan Guo ,  Hubert Josien ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Cangming Yang ,  Dong Xiao

IPC: C07C59/72 ,  A61K45/06 ,  A61K31/192 ,  A61K31/404 ,  A61K31/435 ,  C07D221/04 ,  C07D231/12 ,  C07D207/333 ,  C07D277/42 ,  C07D209/12 ,  A61K31/277 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/437 ,  A61K31/44 ,  C07C255/59 ,  C07D209/08 ,  C07D213/64 ,  C07D249/04 ,  C07D333/24 ,  C07D417/04 ,  C07D471/04

CPC classification number: C07C59/72 ,  A61K31/192 ,  A61K31/277 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/44 ,  A61K45/06 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/06 ,  C07C2602/08 ,  C07D207/333 ,  C07D209/08 ,  C07D209/12 ,  C07D213/64 ,  C07D221/04 ,  C07D231/12 ,  C07D249/04 ,  C07D277/42 ,  C07D333/24 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US09840512B2

公开(公告)日：2017-12-12

申请号：US14767815

申请日：2014-02-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Linda L. Brockunier ,  Helen Chen ,  Harry R. Chobanian ,  Matthew J. H. Clements ,  Alejandro Crespo ,  Duane E. DeMong ,  Yan Guo ,  William K. Hagmann ,  Karen M. Marcantonio ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Dong Xiao

IPC: C07D311/04 ,  C07D311/28 ,  C07D491/052 ,  C07D493/04 ,  C07D201/00 ,  C07D405/14 ,  C07D319/20 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D413/10 ,  C07D417/04 ,  C07D491/048 ,  A61K31/352 ,  A61K31/416 ,  A61K31/422 ,  A61K31/427 ,  A61K31/436 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/497 ,  A61K31/538 ,  A61K45/06

CPC classification number: C07D493/04 ,  A61K31/352 ,  A61K31/416 ,  A61K31/422 ,  A61K31/427 ,  A61K31/436 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/497 ,  A61K31/538 ,  A61K45/06 ,  C07D201/00 ,  C07D311/04 ,  C07D311/28 ,  C07D319/20 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D413/10 ,  C07D417/04 ,  C07D491/048 ,  C07D491/052

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US20160002255A1

公开(公告)日：2016-01-07

申请号：US14767815

申请日：2014-02-20

Applicant: Linda L. BROCKUNIER ,  Helen CHEN ,  Harry R. CHOBANIAN ,  Matthew J. CLEMENTS ,  Alejandro CRESPO ,  Duane E. DEMONG ,  Yan GUO ,  William K. HAGMANN ,  Karen M. MARCANTONIO ,  Michael MILLER ,  Barbara PIO ,  Christopher W. PLUMMER ,  Dong XIAO ,  MERCK SHARP & DOHME CORP.

Inventor： Linda L. Brockunier ,  Helen Chen ,  Harry R. Chobanian ,  Matthew J. H. Clements ,  Alejandro Crespo ,  Duane E. DeMong ,  Yan Guo ,  William K. Hagmann ,  Karen M. Marcantonio ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Dong Xiao

IPC: C07D493/04 ,  A61K31/352 ,  C07D405/04 ,  A61K31/4433 ,  C07D311/28 ,  C07D417/04 ,  A61K31/427 ,  C07D491/052 ,  A61K31/436 ,  C07D405/14 ,  A61K31/444 ,  C07D413/10 ,  A61K31/422 ,  C07D405/10 ,  A61K31/416 ,  A61K31/497 ,  A61K31/538 ,  A61K45/06 ,  C07D311/04

CPC classification number: C07D493/04 ,  A61K31/352 ,  A61K31/416 ,  A61K31/422 ,  A61K31/427 ,  A61K31/436 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/497 ,  A61K31/538 ,  A61K45/06 ,  C07D201/00 ,  C07D311/04 ,  C07D311/28 ,  C07D319/20 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D413/10 ,  C07D417/04 ,  C07D491/048 ,  C07D491/052

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract translation: 结构式（I）的新型化合物及其药学上可接受的盐是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制G蛋白偶联受体 受体40.本发明的化合物可用于治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和 高甘油三酯血症

公开(公告)号：US20230054411A1

公开(公告)日：2023-02-23

申请号：US17294836

申请日：2019-11-26

Applicant: Yonglian ZHANG ,  Amjad ALI ,  Jared CUMMING ,  Duane DEMONG ,  Qiaolin DENG ,  Thomas H. GRAHAM ,  Elisabeth HENNESSY ,  Matthew A. LARSEN ,  Kun LIU ,  Ping LIU ,  Umar Faruk MANSOOR ,  Jianping PAN ,  Christopher W. PLUMMER ,  Aaron SATHER ,  Uma SWAMINATHAN ,  Huijun WANG ,  Merck Sharp & Dohme Corp.

Inventor： Yonglian Zhang ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Matthew A. Larsen ,  Kun Liu ,  Ping Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang

IPC: A61K31/519 ,  A61K39/395 ,  C07D471/04 ,  C07D519/00 ,  A61K31/55

Abstract: In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US11161819B2

公开(公告)日：2021-11-02

申请号：US16935565

申请日：2020-07-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： Gregory L. Adams ,  Jason M. Cox ,  John S. Debenham ,  Scott Edmondson ,  Eric J. Gilbert ,  Yan Guo ,  Yu Jiang ,  Hubert Josien ,  Hyunjin M. Kim ,  Ping Lan ,  Shouwu Miao ,  Christopher W. Plummer ,  Murali Rajagopalan ,  Unmesh Shah ,  Zhongxiang Sun ,  Quang T. Truong ,  Feroze Ujjainwalla ,  Francisco Velazquez ,  Srikanth Venkatraman ,  Takao Suzuki ,  Nengxue Wang

IPC: C07D217/04 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D417/12 ,  C07D417/14 ,  C07D401/06 ,  C07D417/04 ,  A61K31/4725 ,  C07D417/06 ,  C07D217/22 ,  A61K45/06 ,  A61K31/472 ,  A61K9/48 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P29/00

Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.

公开(公告)号：US20170217942A1

公开(公告)日：2017-08-03

申请号：US15328913

申请日：2015-08-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harry Chobanian ,  Duane DeMong ,  Christopher W. Plummer ,  Minghai Fang ,  Bin Hu

IPC: C07D405/14 ,  C07D405/04 ,  C07D313/08 ,  C07D405/10

CPC classification number: C07D405/14 ,  A61K31/335 ,  A61K31/397 ,  A61K31/4427 ,  A61K31/444 ,  A61K45/06 ,  C07D313/08 ,  C07D405/04 ,  C07D405/10 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US20170210727A1

公开(公告)日：2017-07-27

申请号：US15328672

申请日：2015-08-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Helen Chen ,  Duane DeMong ,  Paul E. Finke ,  Christopher W. Plummer

IPC: C07D405/04 ,  C07D405/10 ,  C07D307/80

CPC classification number: C07D405/04 ,  A61K31/343 ,  A61K31/443 ,  A61K45/06 ,  C07D307/80 ,  C07D405/10 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US20220220117A1

公开(公告)日：2022-07-14

申请号：US17657515

申请日：2022-03-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： Matthew A. Larsen ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Andrew J. Hoover ,  Ping Liu ,  Kun Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang ,  Yonglian Zhang

IPC: C07D487/04

Abstract: In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.