公开(公告)号：US20170173035A1

公开(公告)日：2017-06-22

申请号：US15309533

申请日：2015-05-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Haifeng Tang ,  Shu-Wei Yang ,  Mihir Mandal ,  Jing Su ,  Guoqing Li ,  Weidong Pan ,  Haiqun Tang ,  Reynalda DeJesus ,  Jianping Pan ,  William Hagmann ,  Fa-Xiang Ding ,  Li Xiao ,  Alexander Pasternak ,  Yuhua Huang ,  Shuzhi Dong ,  Dexi Yang

IPC: A61K31/546 ,  A61K31/407 ,  A61K31/496 ,  A61K31/43 ,  A61K31/427 ,  A61K31/44 ,  A61K31/41

CPC classification number: A61K31/546 ,  A61K31/407 ,  A61K31/41 ,  A61K31/427 ,  A61K31/43 ,  A61K31/44 ,  A61K31/496 ,  A61K45/06 ,  A61K2121/00 ,  C07D257/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

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：US09839642B2

公开(公告)日：2017-12-12

申请号：US15309533

申请日：2015-05-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Haifeng Tang ,  Shu-Wei Yang ,  Mihir Mandal ,  Jing Su ,  Guoqing Li ,  Weidong Pan ,  Haiqun Tang ,  Reynalda DeJesus ,  Jianping Pan ,  William Hagmann ,  Fa-Xiang Ding ,  Li Xiao ,  Alexander Pasternak ,  Yuhua Huang ,  Shuzhi Dong ,  Dexi Yang

IPC: A61K31/407 ,  A61K31/41 ,  A61K31/427 ,  A61K31/43 ,  A61K31/44 ,  A61K31/496 ,  A61K31/546

CPC classification number: A61K31/546 ,  A61K31/407 ,  A61K31/41 ,  A61K31/427 ,  A61K31/43 ,  A61K31/44 ,  A61K31/496 ,  A61K45/06 ,  A61K2121/00 ,  C07D257/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

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.

公开(公告)号：US11141403B2

公开(公告)日：2021-10-12

申请号：US16061481

申请日：2016-12-13

Applicant: MERCK SHARP & DOHME CORP. ,  John P. Caldwell ,  Ginny Dai Ho ,  Sookhee N. Ha ,  Sandra J. Koseoglu ,  Marc A. Labroli ,  Sang Ho Lee ,  Christina Madsen-Duggan ,  Mihir Mandal ,  Jianping Pan ,  Weidong Pan ,  Terry Roemer ,  Jing Su ,  Christopher Michael Tan ,  Zheng Tan ,  Hao Wang ,  Christine Yang ,  Shu-Wei Yang

Inventor： John P. Caldwell ,  Ginny Dai Ho ,  Sookhee N. Ha ,  Sandra J. Koseoglu ,  Marc A. Labroli ,  Sang Ho Lee ,  Christina Madsen-Duggan ,  Mihir Mandal ,  Jianping Pan ,  Weidong Pan ,  Terry Roemer ,  Jing Su ,  Christopher Michael Tan ,  Zheng Tan ,  Hao Wang ,  Christine Yang ,  Shu-Wei Yang

IPC: A61K31/397 ,  A61P31/04 ,  A61K31/407 ,  C07D235/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D471/04

Abstract: Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.

公开(公告)号：US20210107904A1

公开(公告)日：2021-04-15

申请号：US16695367

申请日：2019-11-26

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.

公开(公告)号：US11752128B2

公开(公告)日：2023-09-12

申请号：US17385194

申请日：2021-07-26

Applicant: MERCK SHARP & DOHME CORP.

Inventor： John P. Caldwell ,  Ginny Dai Ho ,  Sookhee N. Ha ,  Sandra J. Koseoglu ,  Marc A. Labroli ,  Sang Ho Lee ,  Christina Madsen-Duggan ,  Mihir Mandal ,  Jianping Pan ,  Weidong Pan ,  Terry Roemer ,  Jing Su ,  Christopher Michael Tan ,  Zheng Tan ,  Hao Wang ,  Christine Yang ,  Shu-Wei Yang

IPC: A61K31/397 ,  A61P31/04 ,  A61K31/407 ,  C07D235/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D471/04

CPC classification number: A61K31/397 ,  A61K31/407 ,  A61P31/04 ,  C07D235/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D471/04

Abstract: Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.

公开(公告)号：US11312719B2

公开(公告)日：2022-04-26

申请号：US16695367

申请日：2019-11-26

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 ,  C07K16/28

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.