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公开(公告)号：US09604998B2
公开(公告)日：2017-03-28
申请号：US14768245
申请日：2014-02-12
发明人： Alexander Pasternak , Reynalda Keh DeJesus , Fa-Xiang Ding , Shuzhi Dong , Jessica L. Frie , Xin Gu , Jinlong Jiang , Aurash Shahripour , Barbara Pio , Haifeng Tang , Shawn Walsh
IPC分类号： A61K31/401 , C07D498/04 , A61K31/5383 , C07D487/04 , C07D519/00 , A61K31/403 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/4422 , A61K31/4985 , A61K31/55 , A61K31/675 , A61K45/06
CPC分类号： C07D498/04 , A61K31/401 , A61K31/403 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/4422 , A61K31/4985 , A61K31/5383 , A61K31/55 , A61K31/675 , A61K45/06 , C07D487/04 , C07D519/00 , 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, kidney disease, edema, and conditions associated with excessive salt and water retention.
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公开(公告)号：US11306125B2
公开(公告)日：2022-04-19
申请号：US17253815
申请日：2019-06-20
发明人： Yusheng Xiong , Thomas Joseph Tucker , Chengwei Wu , Elisabetta Bianchi , Danila Branca , Angela Dawn Kerekes , Abbas M. Walji , Hubert B. Josien , Fa-Xiang Ding , Hyewon Youm , Alessia Santoprete , Raffaele Ingenito
摘要： Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R4, and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions
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公开(公告)号：US20210069288A1
公开(公告)日：2021-03-11
申请号：US17005686
申请日：2020-08-28
发明人： Hubert Josien , Abbas Walji , Harold B. Wood , Fa-Xiang Ding , Jian Liu , Thomas Joseph Tucker , Michael Man-Chu Lo , Liangqin Guo
摘要： Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
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公开(公告)号：US20190389909A1
公开(公告)日：2019-12-26
申请号：US16446940
申请日：2019-06-20
发明人： Harold B. Wood , Hubert B. Josien , Thomas Joseph Tucker , Angela Dawn Kerekes , Ling Tong , Abbas M. Walji , Anilkumar G. Nair , Fa-Xiang Ding , Elisabetta Bianchi , Danila Branca , Chengwei Wu , Yusheng Xiong , Sookhee Nicole HA , Jian Liu , Sobhana Babu Boga
摘要： Disclosed are compounds of Formula I, or a salt thereof: where A, B, D, X, R1, R2 and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
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公开(公告)号：US09926317B2
公开(公告)日：2018-03-27
申请号：US15323985
申请日：2015-07-09
发明人： Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinglong Jiang , Shuzhi Dong , Xin Gu
IPC分类号： C07D471/10 , A61K31/438 , A61K31/444 , A61K45/06
CPC分类号： C07D471/10 , A61K31/438 , A61K31/444 , A61K45/06
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：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：US20170173035A1
公开(公告)日：2017-06-22
申请号：US15309533
申请日：2015-05-04
发明人： 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分类号： A61K31/546 , A61K31/407 , A61K31/496 , A61K31/43 , A61K31/427 , A61K31/44 , A61K31/41
CPC分类号： 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
摘要： 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.
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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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公开(公告)号：US20140031349A1
公开(公告)日：2014-01-30
申请号：US13951096
申请日：2013-07-25
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： A61K31/5386 , A61K31/435 , C07D451/00 , A61K45/06 , C07D471/20 , A61K31/4995 , C07D498/20 , C07D471/10 , A61K31/46
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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