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公开(公告)号：US20180290987A1
公开(公告)日：2018-10-11
申请号：US15766395
申请日：2016-10-17
申请人： Mihir B. MANDAL , David B. OLSEN , Jing SU , Lihu YANG , Katherine YOUNG , Takao SUZUKI , Lanying YOU , Merck Sharp & Dohme Corp.
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 , C07D471/04 , C07D413/10 , C07D417/10 , C07D413/04 , C07D487/04 , C07D413/06 , C07D417/14 , C07D413/14 , A61K31/421 , A61K31/437 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/506 , A61K31/553 , A61K31/4985 , A61K31/541 , A61K31/5377 , A61K45/06
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：US20170275283A1
公开(公告)日：2017-09-28
申请号：US15505277
申请日：2015-10-26
申请人： Alexander PASTERNAK , Fa-Xiang DING , Shuzhi DONG , Jinlong JIANG , Haifeng TANG , Xin GU , Reynalda K. DEJESUS , Jessica FRIE , Qinghong FU , Takao SUZUKI , Zhifa PU , Merck Sharp & Dohme Corp.
发明人： Alexander Pasternak , Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Haifeng Tang , Xin Gu , Reynalda K. DeJesus , Jessica Frie , Qinghong Fu , Takao Suzuki , Zhifa Pu
IPC分类号： C07D471/10 , C07D498/10 , A61K31/5386 , A61K45/06 , A61K31/435 , A61K31/537 , C07D498/20 , A61K31/553 , A61K31/499 , A61K31/55
CPC分类号： C07D471/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/499 , A61K31/537 , A61K31/5386 , A61K31/55 , A61K31/553 , A61K45/06 , C07D487/10 , C07D498/10 , C07D498/20 , A61K2300/00
摘要： The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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13.发明授权公开(公告)号：US11339156B2
公开(公告)日：2022-05-24
申请号：US16621953
申请日：2018-06-22
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Timothy J. Henderson , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Meng Na , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang , Takao Suzuki
IPC分类号： C07D471/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D417/14
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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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：US20200010463A1
公开(公告)日：2020-01-09
申请号：US16490958
申请日：2018-03-15
发明人： Jing Su , Lihu Yang , Takao Suzuki
IPC分类号： C07D413/14 , A61P31/06 , A61K9/00 , C07D413/10 , C07D263/22 , C07D417/14
摘要： The present invention relates to oxazolidinone Compounds of Formula (I): (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：US09862720B2
公开(公告)日：2018-01-09
申请号：US15505620
申请日：2015-10-26
发明人： Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Takao Suzuki , Joseph P. Vacca , Shouning Xu
IPC分类号： C07D471/10 , A61K31/435 , A61K31/444 , A61K31/501
CPC分类号： C07D471/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/444 , A61K31/501 , A61K31/55 , A61K2300/00
摘要： The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号：US09839629B2
公开(公告)日：2017-12-12
申请号：US15101481
申请日：2014-12-19
发明人： Shuzhi Dong , Alexander Pasternak , Xin Gu , Qinghong Fu , Jinlong Jiang , Fa-Xiang Ding , Haifeng Tang , Reynalda K. DeJesus , Takao Suzuki
IPC分类号： C07D471/10 , C07D498/10 , A61K31/4545 , A61K31/537 , A61K31/4745 , A61K31/435 , A61K31/497 , A61K31/501 , A61K31/506 , C07D519/00 , A61K31/437 , A61K31/438 , A61K31/444 , A61K45/06
CPC分类号： A61K31/435 , A61K31/437 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/537 , A61K45/06 , C07D471/10 , C07D498/10 , C07D519/00 , A61K2300/00
摘要： Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included.
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公开(公告)号：US20150099729A1
公开(公告)日：2015-04-09
申请号：US14569858
申请日：2014-12-15
发明人： Fa-Xiang Ding , Shuzhi Dong , Jessica Frie , Xin Gu , Jinlong Jiang , Alexander Pasternak , Haifeng Tang , Zhicai Wu , Yang Yu , Takao Suzuki
IPC分类号： C07D498/20 , C07D471/20 , C07D471/10
CPC分类号： C07D498/20 , A61K31/435 , A61K31/46 , A61K31/4995 , A61K31/5386 , A61K45/06 , C07D451/00 , C07D471/10 , C07D471/20 , C07D519/00
摘要： The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
摘要翻译： 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 该化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭以及与过量盐和水滞留有关的病症的医学病症。
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