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公开(公告)号：US20210079018A1
公开(公告)日：2021-03-18
申请号：US16764563
申请日：2018-11-15
发明人： Steven J. Ferrara , Michael H. Serrano-Wu , Christopher Lemke , David McKinney , Mark Fitzgerald , Christopher Nasveschuk , Kiel Lazarski , Laura Furst , Guo Wei , Patrick Ryan MacCarren , Kai Thede , Anne Mengel , Clara Christ , Joachim Kuhnke , Sarah Anna Liesa Johannes , Philipp Buchgraber , Ulrich Klar , Ulrike Sack , Stefan Kaulfuss , Amaury Ernesto Fernandez-Montalvan , Nicolas Werbeck , Ursula Mönning
IPC分类号： C07D498/14 , C07D487/14 , A61P35/00
摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
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![Azabicyclo[4.1.0]heptane allosteric modulators of the M4 muscarinic acetylcholine receptor](/abs-image/US/2021/03/16/US10945771B2/abs.jpg.150x150.jpg)
42.发明授权公开(公告)号：US10945771B2
公开(公告)日：2021-03-16
申请号：US16620046
申请日：2018-06-04
IPC分类号： A61B17/70 , A61B17/17 , A61B17/34 , A61B17/86 , C07D471/04 , C07D471/14 , C07D498/14 , A61B17/56 , A61B90/00
摘要： The present invention is directed to azabicyclo[4.1.0]heptane 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：US20200339598A1
公开(公告)日：2020-10-29
申请号：US16924390
申请日：2020-07-09
IPC分类号： C07D498/14 , C07D471/04 , C07D471/14 , C07D498/04 , C07D471/22 , C07D498/20 , C07D498/22 , A61K31/4985 , A61K31/5365 , A61K45/06 , A61K9/00 , A61K31/519 , A61K31/551
摘要： The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
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公开(公告)号：US20200283405A1
公开(公告)日：2020-09-10
申请号：US16702891
申请日：2019-12-04
发明人： Timothy Alcacio , Minson Baek , Peter Grootenhuis , Sara Sabina Hadida Ruah , Robert M. Hughes , Ali Keshavarz-Shokri , Rachel McAuley-Aoki , Jason McCartney , Mark Thomas Miller , Fredrick Van Goor , Beili Zhang , Corey Anderson , Thomas Cleveland , Bryan A. Frieman , Haripada Khatuya , Pramod Virupax Joshi , Paul John Krenitsky , Vito Melillo , Fabrice Jean Denis Pierre , Andreas P. Termin , Johnny Uy , Jinglan Zhou , Alexander Russell Abela , Brett Bradley Busch , Prasuna Paraselli
IPC分类号： C07D401/14 , C07D471/14 , C07D498/14 , C07B59/00
摘要： Compounds of Formula I: pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
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公开(公告)号：US10752642B1
公开(公告)日：2020-08-25
申请号：US16399357
申请日：2019-04-30
发明人： Mikell Paige , Yun Michael Shim , Young-Ok You
IPC分类号： C07D498/14
摘要： The present compositions and methods generally relate to the treatment of diseases, such as idiopathic pulmonary fibrosis (IPF) and neurodegenerative diseases related to tau aggregation. In particular, the compositions relate to compounds or pharmaceutically acceptable salts of Formula I:
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46.发明申请公开(公告)号：US20200255421A1
公开(公告)日：2020-08-13
申请号：US16639394
申请日：2018-08-14
申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMYOF SCIENCES , TOPHARMAN SHANGHAI CO., LTD.
发明人： Yang HE , Xiangrui JIANG , Jianfeng LI , Yu WANG , Zhen WANG , Weiming CHEN , Fuqiang ZHU , Chunhui WU , Rongxia ZHANG , Jingshan SHEN , Hualiang JIANG
IPC分类号： C07D455/03 , A61P25/20 , C07D498/14
摘要： The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.
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公开(公告)号：US10682350B2
公开(公告)日：2020-06-16
申请号：US13011407
申请日：2011-01-21
申请人： Rajinder Singh , Ankush Argade , Donald Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossi
发明人： Rajinder Singh , Ankush Argade , Donald Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossi
IPC分类号： C07D498/04 , A61K31/505 , A61K31/519 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D239/48 , C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D265/36 , A61K31/5395 , C07D495/04 , C07F5/02 , C07D498/14 , C07D407/14
摘要： The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
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公开(公告)号：US20200157118A1
公开(公告)日：2020-05-21
申请号：US16742326
申请日：2020-01-14
申请人： Laurus Labs Limited
发明人： Ram THAIMATTAM , Rajesh Edupuganti , Venkata Sunil Kumar Indukuri , Srihari Raju Kalidindi , Satyanarayana Chava
IPC分类号： C07D498/14 , A61K31/5365
摘要： The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
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公开(公告)号：US10654872B1
公开(公告)日：2020-05-19
申请号：US16732992
申请日：2020-01-02
申请人： Laurus Labs Limited
发明人： Ram Thaimattam , Rajesh Edupuganti , Venkata Sunil Kumar Indukuri , Srihari Raju Kalidindi , Satyanarayana Chava
IPC分类号： C07D498/14 , A61K31/5365
摘要： The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
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公开(公告)号：US10647729B1
公开(公告)日：2020-05-12
申请号：US16742326
申请日：2020-01-14
申请人： Laurus Labs Limited
发明人： Ram Thaimattam , Rajesh Edupuganti , Venkata Sunil Kumar Indukuri , Srihari Raju Kalidindi , Satyanarayana Chava
IPC分类号： C07D498/14 , A61K31/5365
摘要： The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
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