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公开(公告)号：US20170183373A1
公开(公告)日：2017-06-29
申请号：US15461075
申请日：2017-03-16
发明人： Balkrishen Bhat , Anne B. Eldrup , Thazha P. Prakash , Phillip Dan Cook , David B. Olsen , Steven S. Carroll , Malcolm MacCoss
CPC分类号： C07H19/10 , A61K9/4858 , C07D471/04 , C07D473/34 , C07D487/04 , C07H17/02 , C07H19/06 , C07H19/16 , C07H19/207 , Y02P20/582
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
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公开(公告)号：US20210061777A1
公开(公告)日：2021-03-04
申请号：US17093833
申请日：2020-11-10
发明人： Mihir B. Mandal , David B. Olsen , Jing Su , Lihu Yang , Katherine Young , Takao Suzuki , Lanying You
IPC分类号： C07D263/20 , C07D413/14 , A61K31/421 , A61K31/422 , C07D413/10 , A61K45/06 , A61K31/427 , A61K31/4439 , A61K31/541 , C07D413/06 , C07D417/10 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/553 , C07D413/04 , C07D417/14
摘要： The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
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公开(公告)号：US09777035B2
公开(公告)日：2017-10-03
申请号：US14669398
申请日：2015-03-26
IPC分类号： A61K31/7064 , A61K45/06 , C07H19/12 , C07H19/14 , C07H19/06 , C07D487/04
CPC分类号： C07H19/14 , A61K31/7064 , A61K45/06 , C07D487/04 , C07H19/06 , C07H19/12
摘要： The present invention is directed to 4′-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, 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 and/or ARC.
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公开(公告)号：US09765107B2
公开(公告)日：2017-09-19
申请号：US14899008
申请日：2014-06-16
发明人： Stephane Bogen , Vinay Girijavallabhan , Quang Truong , Ping Chen , Frank Bennett , Angela Kerekes , Qun Dang , David B. Olsen , Ian Davies
IPC分类号： A01N43/04 , A61K31/70 , C07H19/10 , A61K45/06 , A61K31/661 , C07F9/6558 , C07F9/6574 , C07H19/11 , A61K31/7072 , A61K31/7068 , A61K31/706 , A61K31/7064
CPC分类号： C07H19/10 , A61K31/661 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K45/06 , C07F9/65586 , C07F9/65744 , C07H19/11 , A61K2300/00
摘要： The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
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公开(公告)号：US20220331321A1
公开(公告)日：2022-10-20
申请号：US17633655
申请日：2020-07-21
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research , MSD R & D (China) Co. LTD.
发明人： John A. McCauley , Alan F. Cowman , Manuel de Lera Ruiz , Paola Favuzza , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , David B. Olsen , Brad Sleebs , Jennifer K. Thompson , Tony Triglia , Dongmei Zhan , Cailing Zhang , Lianyun Zhao
IPC分类号： A61K31/513 , C07D405/14 , C07D493/10 , C07D491/052 , C07D409/14 , C07D239/22 , C07D405/12 , C07D409/04 , A61P33/06 , A61K45/06
摘要： Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
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公开(公告)号：US20220081403A1
公开(公告)日：2022-03-17
申请号：US17422308
申请日：2019-12-19
申请人： Randall R. MILLER , Joseph A. KOZLOWSKI , Philippe NANTERMET , David B. OLSEN , Jing SU , Uihu YANG , Takao SUZUKI , Brendan M. CROWLEY , Nengxue WANG , Lanying YOU , Merck Sharp & Dohme Corp.
发明人： Randall R. Miller , Joseph A. Kozlowski , Philippe Nantermet , David B. Olsen , Jing Su , Lihu Yang , Takao Suzuki , Brendan Crowley , Negxue Wang , Lanying You
IPC分类号： C07D263/06 , C07D471/04 , C07D413/12 , C07D495/04 , C07F9/653 , C07F9/6553 , A61K31/422 , A61K31/421 , A61K31/437 , A61K31/498 , A61K31/4439 , A61K31/541 , A61P31/06 , A61K45/06
摘要： The present invention discloses oxazolidinone compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A and E, are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
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公开(公告)号：US10947205B2
公开(公告)日：2021-03-16
申请号：US16397172
申请日：2019-04-29
发明人： Mihir B. Mandal , David B. Olsen , Jing Su , Lihu Yang , Katherine Young , Takao Suzuki , Lanying You
IPC分类号： A61K31/422 , A61K31/541 , C07D401/14 , C07D413/14 , C07D417/14 , C07D417/10 , C07D413/10 , C07D471/04 , C07D487/04 , C07D263/20 , A61K31/421 , A61K45/06 , A61K31/427 , A61K31/4439 , C07D413/06 , A61K31/437 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/553 , C07D413/04
摘要： The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
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公开(公告)号：US10144741B2
公开(公告)日：2018-12-04
申请号：US15910571
申请日：2018-03-02
发明人： 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分类号： C07D493/08 , C07F7/18 , C07D493/18 , C07C309/06 , C07C53/18
摘要： 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.
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公开(公告)号：US09944654B2
公开(公告)日：2018-04-17
申请号：US15517570
申请日：2015-10-21
发明人： 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分类号： C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07F7/18
CPC分类号： C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07D519/00 , C07F7/1804
摘要： 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.
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公开(公告)号：US20180002366A1
公开(公告)日：2018-01-04
申请号：US15685824
申请日：2017-08-24
IPC分类号： C07H19/14 , C07D487/04 , A61K31/7064 , A61K45/06 , C07H19/12 , C07H19/06
CPC分类号： C07H19/14 , A61K31/7064 , A61K45/06 , C07D487/04 , C07H19/06 , C07H19/12
摘要： The present invention is directed to 4′-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, 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 and/or ARC.
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