公开(公告)号：US10138212B2

公开(公告)日：2018-11-27

申请号：US15549242

申请日：2016-02-01

申请人： Merck Sharp & Dohme Corp.

发明人： Amjad Ali ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Purakkattle Biju ,  Manuel de Lera Ruiz ,  Sylvia J. Degrado ,  Alexander L. Tung ,  Timothy J. Henderson ,  Liwu Hong ,  Jae-Hun Kim ,  Dong Won-Shik Kim ,  Joe Lee ,  Jie Wu ,  Heping Wu ,  Yushi Xiao ,  Tao Yu ,  Gang Zhou ,  Xiaohong Zhu ,  Kevin D. McCormick ,  Jayaram R. Tagat ,  Dong Xiao ,  Tanweer Khan ,  Jianhua Cao ,  Michael Berlin ,  Yonglian Zhang

IPC分类号： C07D239/84 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61P25/14 ,  A61K31/517

摘要： The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

公开(公告)号：US20180193314A1

公开(公告)日：2018-07-12

申请号：US15815212

申请日：2016-06-06

申请人： Merck Sharp & Dohme Corp.

发明人： Junying Zheng ,  Walter Won ,  Michael Berlin ,  Pauline Ting ,  Guoqing Li ,  Dong Xiao ,  Hongwu Wang ,  Robert Aslanian

IPC分类号： A61K31/4162 ,  A61K31/519 ,  A61K31/497 ,  A61P25/00

CPC分类号： A61K31/4162 ,  A01N43/80 ,  A61K31/497 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04 ,  C07D487/10 ,  A01N25/04

摘要： Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: “Z”, R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US20150361101A1

公开(公告)日：2015-12-17

申请号：US14766462

申请日：2014-02-03

申请人： Xing DAI ,  Anandan PALANI ,  Shuwen HE ,  Linda L. BROCKUNIER ,  Ravi NARGUND ,  Karen MARCANTONO ,  Nicolas Zorn ,  Dong XIAO ,  Xuanjia PENG ,  Tao GUO ,  MERCK SHARP & DOHME CORP.

发明人： Xing Dai ,  Hong Liu ,  Anandan Palani ,  Shuwen He ,  Linda L. Brockunier ,  Ravi Nargund ,  Karen Marcantonio ,  Nicolas Zorn ,  Dong Xiao ,  Xuanjia Peng ,  Peng Li ,  Tao Guo

IPC分类号： C07D519/00 ,  C07D471/14 ,  A61K31/4375 ,  A61K31/5025 ,  A61K31/438 ,  A61K31/55 ,  C07D471/22 ,  C07D471/04 ,  C07D471/20 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D519/00 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/20 ,  C07D471/22 ,  C07D487/14 ,  A61K2300/00

摘要： The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的用途的式I化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。

公开(公告)号：US11352320B2

公开(公告)日：2022-06-07

申请号：US17057921

申请日：2019-05-28

申请人： Merck Sharp & Dohme Corp.

发明人： Shuwen He ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Dong Xiao ,  Li Xiao ,  Feng Ye ,  Hongjun Zhang

IPC分类号： C07C13/06 ,  C07C233/65 ,  C07C233/80 ,  A61K31/166 ,  C07C271/14 ,  A61P35/00 ,  C07D213/74 ,  C07D237/34 ,  C07D239/42 ,  C07D239/94 ,  C07D241/20 ,  C07D471/04 ,  A61K45/06

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20210198190A1

公开(公告)日：2021-07-01

申请号：US17057921

申请日：2019-05-28

申请人： Merck Sharp & Dohme Corp.

发明人： Shuwen He ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Dong Xiao ,  Li Xiao ,  Feng Ye ,  Hongjun Zhang

IPC分类号： C07C271/14 ,  C07D239/42 ,  C07D237/34 ,  C07D241/20 ,  C07D239/94 ,  C07D213/74 ,  C07D471/04 ,  A61P35/00

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US10968193B2

公开(公告)日：2021-04-06

申请号：US15328735

申请日：2015-08-06

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： 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

摘要： 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：US20200206350A1

公开(公告)日：2020-07-02

申请号：US16644107

申请日：2018-08-31

申请人： Merck Sharp & Dohme Corp.

发明人： Lin Chu ,  Nathalie Y. Toussaint ,  Dong Xiao ,  Petr Vachal ,  Ramesh S. Kashi ,  Annette Bak

IPC分类号： A61K47/22 ,  C07K16/28 ,  A61K47/26 ,  C07D233/64 ,  C07C279/14 ,  C07C235/12 ,  C07C229/36 ,  A61K47/18

摘要： The present invention relates to pegylated amino acid compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3A, R3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.

公开(公告)号：US10011615B2

公开(公告)日：2018-07-03

申请号：US15423238

申请日：2017-02-02

申请人： Merck Sharp & Dohme Corp.

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Xianhai Huang ,  Timothy J. Henderson ,  Jae-Hun Kim ,  Christopher Boyce ,  Pauline Ting ,  Junying Zheng ,  Edward Metzger ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Qiaolin Deng

IPC分类号： A01N43/00 ,  A01N43/46 ,  C07D519/00 ,  C07D487/04

CPC分类号： C07D519/00 ,  C07D487/04

摘要： Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

公开(公告)号：US09957219B2

公开(公告)日：2018-05-01

申请号：US15034189

申请日：2014-12-01

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： 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分类号： 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

摘要： 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

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： 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分类号： 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

摘要： 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.