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公开(公告)号：US10544130B2
公开(公告)日：2020-01-28
申请号：US16244876
申请日：2019-01-10
发明人： Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu
IPC分类号： C07D403/10 , C07D403/12 , C07D413/14 , C07D401/10 , C07D403/14 , C07D407/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , A61P31/04 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D487/04 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/431 , A61K31/439 , A61K31/496 , A61K31/541 , A61K31/546 , C07D405/14 , C07D453/02 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
摘要： The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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公开(公告)号：US10428076B2
公开(公告)日：2019-10-01
申请号：US16019964
申请日：2018-06-27
发明人： Raphaelle Berger , Yi-Heng Chen , Guoqing Li , Joie Garfunkle , Hong-Dong Li , Shouwu Miao , Subharekha Raghavan , Cameron J. Smith , John Stelmach , Alan Whitehead , Rui Zhang , Yong Zhang , Jianmin Fu , Gang Ji , Falong Jiang
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61K45/06
摘要： The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US20180305366A1
公开(公告)日：2018-10-25
申请号：US16019964
申请日：2018-06-27
发明人： Raphaelle Berger , Yi-Heng Chen , Guoqing Li , Joie Garfunkle , Hong-Dong Li , Shouwu Miao , Subharekha Raghavan , Cameron J. Smith , John Stelmach , Alan Whitehead , Rui Zhang , Yong Zhang , Jianmin Fu , Gang Ji , Falong Jiang
IPC分类号： C07D487/04 , A61K31/519 , C07D519/00 , A61K45/06
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , C07D519/00
摘要： The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US10030027B2
公开(公告)日：2018-07-24
申请号：US15384429
申请日：2016-12-20
发明人： Raphaelle Berger , Yi-Heng Chen , Guoqing Li , Joie Garfunkle , Hong-Dong Li , Shouwu Miao , Subharekha Raghavan , Cameron J. Smith , John Stelmach , Alan Whitehead , Rui Zhang , Yong Zhang , Jianmin Fu , Gang Ji , Falong Jiang
IPC分类号： C07D487/04 , C07D519/00 , A61K45/06 , A61K31/519
摘要： The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US20180179190A1
公开(公告)日：2018-06-28
申请号：US15737334
申请日：2016-06-24
发明人： Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , David Hunter , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu , Yunfeng Bai , Zhixiang Zheng , Xu Zhang
IPC分类号： C07D403/14 , A61K45/06 , A61K31/4184 , C07D401/14 , A61K31/454 , C07D471/04 , A61K31/437 , A61K31/4545 , C07D487/04 , A61K31/5025 , C07D403/10 , A61K31/416 , A61K31/4439 , C07D417/14 , A61K31/428 , A61K31/4375 , C07D413/14 , A61K31/423 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/506 , A61K31/498 , A61K31/5377 , A61P31/04
CPC分类号： C07D403/10 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/431 , A61K31/437 , A61K31/4375 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/546 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
摘要： The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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公开(公告)号：US20180134712A1
公开(公告)日：2018-05-17
申请号：US15574411
申请日：2016-05-24
申请人： Dong-Ming SHEN , Michael P. DWYER , Christopher J. SINZ , Deping WANG , Shawn J. STACHEL , Daniel V. PAONE , Ashley FORSTER , Richard BERGER , William D. SHIPE , Yili CHEN , Yimin QIAN , Shimin XU , Chunmei HU , Jianmin FU , Zhigang GUO , Haitang LI , Yingjian BO , Merck Sharp & Dohme Corp. , MSD R & D (China) Co., LTD.
发明人： Dong-Ming Shen , Michael P. Dwyer , Christopher J. Sinz , Deping Wang , Shawn J. Stachel , Daniel V. Paone , Ashley Forster , Richard Berger , Yilli Chen , Yimin Qian , Shimin Xu , Chunmel Hu , William D. Shipe , Jianmin Fu , Zhigang Guo , HAITANG LI , Yingjian Bo
CPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28
摘要： The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.
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公开(公告)号：US10780092B2
公开(公告)日：2020-09-22
申请号：US16301935
申请日：2017-05-11
申请人： Merck Sharp & Dohme Corp. , Alan Whitehead , Olga Ornoski , Subharekha Raghavan , Raphaelle Berger , Joie Garfunkle , Zhiqiang Yang , Gang Ji , Falong Jiang , Jianmin Fu
发明人： Alan Whitehead , Olga Ornoski , Subharekha Raghavan , Raphaelle Berger , Joie Garfunkle , Zhiqiang Yang , Gang Ji , Falong Jiang , Jianmin Fu
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P9/12
摘要： The invention provides certain fused pyrazine compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, R1, R3, R4a, R5a, R5b, R6, and the subscript t are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases or disorders which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and disorders and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US10100064B2
公开(公告)日：2018-10-16
申请号：US15318483
申请日：2015-06-09
发明人： Meredeth Ann McGowan , Kin Chiu Fong , Neville John Anthony , Hua Zhou , Jason D. Katz , Lihu Yang , Chaomin Li , Yuan Tian , Changwei Mu , Baijun Ye , Feng Shi , Xiaoli Zhao , Jianmin Fu , Yabin Li
IPC分类号： C07D473/30 , C07D473/34 , C07D519/00 , A61K31/52
摘要： The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
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公开(公告)号：US20180244656A1
公开(公告)日：2018-08-30
申请号：US15737351
申请日：2016-06-24
发明人： Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu
IPC分类号： C07D403/10 , A61K31/4184 , C07D401/10 , A61K31/4709 , A61K31/416 , C07D413/10 , A61K31/423 , C07D417/10 , A61K31/428 , C07D417/14 , A61K31/496 , A61K31/5377 , A61K31/454 , C07D471/04 , C07D495/08 , C07D487/10 , A61K31/541 , C07D493/04 , C07D493/08 , C07D453/02 , C07D403/14 , C07D405/14 , A61K31/41 , A61K31/4245 , A61K31/4192 , A61K31/421 , A61K31/4196 , A61K31/198 , A61K31/431 , A61K31/546 , A61K31/4545 , A61K31/439 , A61K31/407 , A61P31/04
CPC分类号： C07D403/10 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/431 , A61K31/437 , A61K31/4375 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/546 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
摘要： The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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公开(公告)号：US09884048B2
公开(公告)日：2018-02-06
申请号：US15531759
申请日：2015-12-10
发明人： Phieng Siliphaivanh , Joey Methot , Kathryn Ann Lipford , Danielle Molinari , David L. Sloman , David Witter , Hua Zhou , Christopher Boyce , Xianhai Huang , Jongwon Lim , David Guerin , Ganesh Babu Karunakaran , Raman Kumar Bakshi , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu
IPC分类号： A61K31/437 , A61K31/4545 , A61K31/444 , C07D471/04 , C07D519/00
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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