公开(公告)号：US11498923B2

公开(公告)日：2022-11-15

申请号：US16769603

申请日：2018-12-10

申请人： Merck Sharp & Dohme Corp.

发明人： Yeon-Hee Lim ,  Gioconda V. Gallo-Etienne ,  Joseph Michael Kelly ,  Michael Berlin ,  Pauline Ting ,  Hongwu Wang

IPC分类号： C07D487/04 ,  C07D519/00

摘要： Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: “Z” and R1 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：US20200261421A1

公开(公告)日：2020-08-20

申请号：US16461952

申请日：2017-12-19

申请人： Merck Sharp & Dohme Corp.

发明人： Brian McKittrick ,  John P. Caldwell ,  John A. McCauley ,  Henry Vaccaro ,  Tin-Yau Chan ,  Hyunjin Kim ,  Elizabeth Smith ,  Liwu Hong ,  Tanweer Khan ,  Shihong Ying ,  Hongwu Wang

IPC分类号： A61K31/4168 ,  A61K45/06 ,  A61K31/497 ,  C07D233/72 ,  C07D403/12 ,  C07D401/12 ,  A61P31/18

摘要： The present invention is directed to compounds of Formula I, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

公开(公告)号：US20200069691A1

公开(公告)日：2020-03-05

申请号：US16461899

申请日：2017-12-19

申请人： Merck Sharp & Dohme Corp.

发明人： Brian McKittrick ,  John P. Caldwell ,  John McCauley ,  Henry Vaccaro ,  Tin-Yau Chan ,  Hyunjin Kim ,  Elizabeth Smith ,  Liwu Hong ,  Tanweer Khan ,  Shihong Ying ,  Hongwu Wang ,  Peter D. Williams ,  Jae-Hun Kim ,  M. Brad Nolt ,  Maryann Caplen

IPC分类号： A61K31/519 ,  A61K45/06 ,  C07D487/04 ,  A61K31/4985 ,  C07D519/00 ,  C07D413/14 ,  A61K31/496 ,  C07D498/04 ,  C07D403/14 ,  C07D413/10 ,  C07D498/14 ,  A61K31/5383 ,  A61K31/4178 ,  A61K31/4188 ,  A61K31/424 ,  A61K31/4355 ,  A61K31/429 ,  C07D513/04 ,  A61P31/18

摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

公开(公告)号：US11180504B2

公开(公告)日：2021-11-23

申请号：US16083980

申请日：2017-03-15

申请人： ORCHID PHARMA LTD. ,  MERCK SHARP & DOHME CORP.

发明人： Gopalan Balasubramanian ,  Maneesh Paul-Satyaseela ,  Chidambaram Venkateswaran Srinivasan ,  Sridhar Ramanathan Iyer ,  Hariharan Periasamy ,  Venkatesan Parameswaran ,  Bharani Thirunavukkarasu ,  Prabhakar Rao Gunturu ,  Manjula Devi Deshkumar ,  Venkateshwarlu Jakkala ,  Michael Miller ,  Ravi P. Nargund ,  Sheo Singh ,  Shuzhi Dong ,  Hongwu Wang ,  Katherine Young

IPC分类号： A61K31/407 ,  C07D487/04 ,  C07D519/00

摘要： This invention relates to carbapenem compounds of the following formula: wherein A, Z, X, R1, and R4 are as described herein, as well as stereoisomers, pharmaceutically acceptable salts or N-oxides thereof, which may be useful for the treatment of bacterial infections, particularly drug-resistant bacterial infections, as well as the processes for the preparation of compounds, the pharmaceutical compositions of these compounds and their use in the treatment of bacterial infection.

公开(公告)号：US11542505B1

公开(公告)日：2023-01-03

申请号：US17047271

申请日：2019-04-15

申请人： Merck Sharp & Dohme Corp. ,  Craig A. Parish ,  Hongwu Wang ,  Wonsuk Chang ,  Quang T. Truong ,  Tony Siu ,  Anne Mai Wassermann

发明人： Craig A. Parish ,  Hongwu Wang ,  Wonsuk Chang ,  Quang T. Truong ,  Tony Siu ,  Anne Mai Wassermann

IPC分类号： C12N15/113 ,  C07H21/02

摘要： This invention provides compositions, compounds, and uses thereof, wherein said compounds comprise a single strand oligonucleotide that may form a short oligonucleotide hairpin or stem loop molecule with self complementary base pairing of less than 12 base pairs that bind to RIG-I and activate the RIG-I pathway.

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.

公开(公告)号：US10472347B2

公开(公告)日：2019-11-12

申请号：US15525788

申请日：2015-11-13

申请人： Merck Sharp & Dohme Corp.

发明人： Rongze Kuang ,  Pauline Ting ,  Amjad Ali ,  Heping Wu ,  Michael Berlin ,  Andrew Stamford ,  Hongwu Wang ,  Gang Zhou ,  David Kim ,  Qiaolin Deng ,  Yeon-Hee Lim ,  Younong Yu

IPC分类号： A61K31/497 ,  C07D401/14 ,  C07D241/26 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04 ,  A61P25/16

摘要： Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, 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：US20180339983A1

公开(公告)日：2018-11-29

申请号：US15775487

申请日：2016-12-12

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 ,  A61K31/427 ,  A61P31/04

摘要： The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, 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.

公开(公告)号：US20180327385A1

公开(公告)日：2018-11-15

申请号：US15525788

申请日：2015-11-13

申请人： Merck Sharp & Dohme Corp.

发明人： Rongze KUANG ,  Pauline Ting ,  Amjad Ali ,  Heping Wu ,  Michael Berlin ,  Andrew Stamford ,  Hongwu Wang ,  Gang Zhou ,  David Kim ,  Qiaolin Deng ,  Yeon-Hee Lim ,  Younong Yu

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, 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：US20200291029A1

公开(公告)日：2020-09-17

申请号：US16083980

申请日：2017-03-15

申请人： ORCHID PHARMA LTD. ,  MERCK SHARP & DOHME CORP.

发明人： Gopalan Balasubramanian ,  Maneesh Paul-Satyaseela ,  Chidambaram Venkateswaran Srinivasan ,  Sridhar Ramanathan Iyer ,  Hariharan Periasamy ,  Venkatesan Parameswaran ,  Bharani Thirunavukkarasu ,  Prabhakar Rao Gunturu ,  Manjula Devi Deshkumar ,  Venkateshwarlu Jakkala ,  Michael Miller ,  Ravi P. Nargund ,  Sheo Singh ,  Shuzhi Dong ,  Hongwu Wang ,  Katherine Young

IPC分类号： C07D487/04 ,  C07D519/00

摘要： This invention relates to carbapenem compounds, their stereoisomers, pharmaceutically acceptable salts or N-oxides thereof, which may be useful for the treatment of bacterial infections, particularly drug-resistant bacterial infections, as well as the processes for the preparation of compounds, the pharmaceutical compositions of these compounds and their use in the treatment of bacterial infection.