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![Substituted imidazo[1,2-a]pyrazines as soluble guanylate cyclase activators](/abs-image/US/2019/04/02/US10245264B2/abs.jpg.150x150.jpg)
公开(公告)号：US10245264B2
公开(公告)日：2019-04-02
申请号：US15575978
申请日：2016-05-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： Joie Garfunkle , Olga Ornoski , Dann L. Parker, Jr. , Subharekha Raghavan , Libo Xu
IPC: A61K31/4985 , C07D487/04 , A61K31/519 , A61K45/06 , C07D519/00 , A61P9/08
Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating 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 furthermore relates to processes for preparing compounds of Formula I, or pharmaceutically acceptable salt thereofs, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or pharmaceutically acceptable salts thereof.
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公开(公告)号：US20180193343A1
公开(公告)日：2018-07-12
申请号：US15575989
申请日：2016-05-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： Joie Garfunkle , Olga Ornoski , Dann L. Parker, JR. , Subharekha Raghavan , Libo Xu , Zhiqiang Yang
CPC classification number: A61K31/519 , A61K45/06 , A61P1/16 , A61P3/10 , A61P9/04 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/10 , C07D519/00
Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating 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 furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US10548910B2
公开(公告)日：2020-02-04
申请号：US15775966
申请日：2016-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley , Andrew Stamford , Wensheng Liu , Jay A. Grobler , Libo Xu
IPC: A61K31/675 , A61P31/18 , A61K31/683 , A61K31/34 , A61K31/426 , A61K31/44 , A61K31/513 , A61K31/52 , A61K31/535 , A61K31/7068
Abstract: The present invention relates to Amido-Substituted Pyridotriazine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, R, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Pyridotriazine Derivative, and methods of using the Amido-Substituted Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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4.发明授权Glucokinase activator compounds, compositions containing such compounds, and methods of treatment 有权葡糖激酶活化剂化合物，含有这些化合物的组合物和治疗方法公开(公告)号：US09453038B2
公开(公告)日：2016-09-27
申请号：US14652883
申请日：2013-12-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： Songnian Lin , Rui Zhang , Brian Campbell , Sunita V. Dewnani , Jiayi Xu , Libo Xu , Emma R. Parmee , Roman Kats-Kagan
IPC: C07F9/6539 , A61K31/4439 , C07D401/04 , A61K31/444 , C07D471/04 , A61K31/437 , C07F9/58 , A61K31/675 , A61K31/497 , A61K31/427 , C07F9/6558 , C07F7/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/14
CPC classification number: C07F9/6539 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/675 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/14 , C07D471/04 , C07F7/0812 , C07F9/58 , C07F9/65583
Abstract: Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included.
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公开(公告)号：US20180009796A1
公开(公告)日：2018-01-11
申请号：US15104537
申请日：2015-01-20
Applicant: Merck Sharp & Dohme Corp.
Inventor： Richard Berger , Timothy A. Blizzard , Brian T. Campbell , Helen Y. Chen , John S. Debenham , Sunita V. Dewnani , Byron Dubois , Candido Gude , Zack Zhiqiang Guo , Bart Harper , Zhiyong Hu , Songnian Lin , Ping Liu , Ming Wang , Feroze Ujjainwalla , Jiayi Xu , Libo Xu , Rui Zhang
IPC: C07D413/14 , C07D417/14 , C07D413/12 , C07D471/04 , C07D401/12
CPC classification number: C07D413/14 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/14 , C07D471/04
Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
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Patent Agency Ranking
公开(公告)号：US20180325926A1
公开(公告)日：2018-11-15
申请号：US15775871
申请日：2016-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley , Andrew Stamford , Wengsheng Liu , Jay A. Grobler , Libo Xu
IPC: A61K31/675 , A61P31/18
CPC classification number: A61K31/675 , A61K31/426 , A61K31/513 , A61K31/52 , A61K2300/00 , A61P31/18 , C07D491/20 , C07F9/6561
Abstract: The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R16 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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7.发明授权公开(公告)号：US09649294B2
公开(公告)日：2017-05-16
申请号：US15030779
申请日：2014-10-30
Applicant: Merck Sharp & Dohme Corp.
Inventor： Songnian Lin , Libo Xu , Emma R. Parmee , Xibin Liao
IPC: A61K31/404 , C07D209/18 , A61K45/06 , A61K31/397 , A61K31/4035 , C07D209/20
CPC classification number: A61K31/404 , A61K31/397 , A61K31/4035 , A61K45/06 , C07D209/18 , C07D209/20 , A61K2300/00
Abstract: Glucagon receptor antagonist compounds are disclosed which are of long duration of action. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
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8.发明申请NOVEL GLUCOKINASE ACTIVATOR COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT 有权新型GLUCOKINASE激活剂化合物，包含这些化合物的组合物和处理方法公开(公告)号：US20150336991A1
公开(公告)日：2015-11-26
申请号：US14652883
申请日：2013-12-12
Applicant: Emma R. PARMEE , Songnian LIN , Brian CAMPBELL , Sunita V. DEWNANI , Roman KATS-KAGAN , Jiayi XU , Libo XU , Rui ZHANG , MERCK SHARP & DOHME CORP.
Inventor： Songnian Lin , Rui Zhang , Brian Campbell , Sunita V. Dewnani , Jiayi Xu , Libo Xu , Emma R. Parmee , Roman Kats-Kagan
IPC: C07F9/6539 , A61K31/4439 , C07D401/04 , A61K31/444 , C07D471/04 , A61K31/427 , C07F9/58 , A61K31/675 , C07D403/14 , A61K31/497 , C07D417/14 , C07D401/14 , A61K31/437
CPC classification number: C07F9/6539 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/675 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/14 , C07D471/04 , C07F7/0812 , C07F9/58 , C07F9/65583
Abstract: Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included.
Abstract translation: 公开了式I的新型吡啶-2-甲酰胺衍生物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病症。 这些化合物作为葡萄糖激酶活化剂是有效的。 还包括药物组合物和治疗方法。
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公开(公告)号：US10213429B2
公开(公告)日：2019-02-26
申请号：US15575989
申请日：2016-05-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： Joie Garfunkle , Olga Ornoski , Dann L. Parker, Jr. , Subharekha Raghavan , Libo Xu , Zhiqiang Yang
Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating 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 furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20180325927A1
公开(公告)日：2018-11-15
申请号：US15775966
申请日：2016-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley , Andrew Stamford , Wengsheng Liu , Jay A. Grobler , Libo Xu
IPC: A61K31/675 , A61K31/683 , A61P31/18
CPC classification number: A61K31/675 , A61K31/34 , A61K31/426 , A61K31/44 , A61K31/513 , A61K31/52 , A61K31/535 , A61K31/683 , A61K31/7068 , A61K45/06 , A61K2300/00 , A61P31/18 , C07D471/04 , C07F9/6561
Abstract: The present invention relates to Amido-Substituted Pyridotriazine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, R, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Pyridotriazine Derivative, and methods of using the Amido-Substituted Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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