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1.发明申请4-Amino-3-Arylamino-6-Arylpyrazolo[3,4-D) Pyrimidine Derivatives, Methods for their Preparation and their Use as Antiviral Agents 有权4-氨基-3-芳基氨基-6-芳基吡唑并[3,4-D]嘧啶衍生物，其制备方法及其作为抗病毒剂的用途公开(公告)号：US20100010018A1
公开(公告)日：2010-01-14
申请号：US12308729
申请日：2007-06-20
IPC分类号： A61K31/519 , C07D487/04 , A61P31/12
CPC分类号： C07D487/04
摘要： 4-amino-3-arylamino-6-arylpyrazolo[3,4-d]pyrimidine derivatives of general formula (I), pharmaceutically acceptable salts thereof, method for preparation of the aforesaid compounds and their use as antiviral agents.
摘要翻译： 通式（I）的4-氨基-3-芳氨基-6-芳基吡唑并[3,4-d]嘧啶衍生物，其药学上可接受的盐，上述化合物的制备方法及其作为抗病毒剂的用途。
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![4-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives, their manufacture and their use as antiviral active substances](/abs-image/US/2017/10/17/US09790225B2/abs.jpg.150x150.jpg)
公开(公告)号：US09790225B2
公开(公告)日：2017-10-17
申请号：US14350885
申请日：2012-10-15
申请人： Peter Wutzler , Michaela Schmidtke , Vadim Makarov
发明人： Peter Wutzler , Michaela Schmidtke , Vadim Makarov
IPC分类号： C07D487/04 , A61K31/519 , A61P31/16 , A61K45/06
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06
摘要： The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula I or pharmaceutically acceptable salts or propharmacons thereof, wherein at least one hydrogen atom in at least one of the phenyl groups A and B is substituted by a substituent RH, which has a Hammett constant σp greater than 0.23. The present invention also concerns the method of its manufacture. For corresponding compounds, surprisingly a particularly high activity against viruses, in particular rhinoviruses and picornaviruses was determined. Furthermore, the compounds are tolerated very well. For these reasons the compounds are suitable for the treatment of viral infections and as drugs.
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3.发明申请2-PIPERAZIN-1-YL-4H-1,3-BENZOTHIAZIN-4-ONE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MAMMALIAN INFECTIONS 有权2-PIPERAZIN-1-YL-4H-1,3-苯并噻嗪-4-酮衍生物及其用于治疗哺乳动物感染的用途公开(公告)号：US20130245007A1
公开(公告)日：2013-09-19
申请号：US13884825
申请日：2011-11-21
申请人： Vadim Makarov , Stewart Cole
发明人： Vadim Makarov , Stewart Cole
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D279/08 , C07D417/14
摘要： The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I).
摘要翻译： 本发明涉及新的2-哌嗪-1-基-4H-1,3-苯并噻嗪-4-酮衍生物及其用于治疗由细菌特别是肺结核（TB），布鲁里溃疡和布鲁里溃疡等引起的哺乳动物感染的用途 由于密切相关的分枝杆菌感染引起的麻风病。 （一世）。
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4.发明申请公开(公告)号：US20050032822A1
公开(公告)日：2005-02-10
申请号：US10495651
申请日：2002-11-18
申请人： Ute Mollmann , Vadim Makarov
发明人： Ute Mollmann , Vadim Makarov
IPC分类号： A61K31/505 , A61P31/04 , A61P31/06 , C07D213/71 , C07D239/46 , C07D239/56 , C07D295/08 , A61K31/19 , A61K31/44
CPC分类号： C07D239/56 , C07D213/71 , C07D239/47
摘要： The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.
摘要翻译： 本发明涉及二硫代氨基甲酸酯衍生物用于治疗或预防由细菌引起的哺乳动物（人和动物）感染性疾病的治疗，特别是结核分枝杆菌（TB）和由葡萄球菌引起的分枝杆菌和感染性疾病引起的麻风病。 本发明还涉及式（I）的新型二硫代氨基甲酸酯衍生物，其中X是选自具有优异抗菌活性的式的二价残基和含有该二价残基的药物制剂。
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5.发明授权Antimicrobial compounds, their synthesis and their use for treatment of mammalian infections 有权抗菌化合物，其合成及其用于治疗哺乳动物感染的用途公开(公告)号：US08440842B2
公开(公告)日：2013-05-14
申请号：US12669748
申请日：2008-06-25
申请人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
发明人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
IPC分类号： A61K31/54 , C07D327/06 , C07D409/00
CPC分类号： C07D279/08
摘要： The present invention relates to compounds of Formula (I) or salts thereof wherein R1, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
摘要翻译： 本发明涉及式（I）化合物或其盐，其中R1，R2，R3，R4，R5，R6和其一个或多个下列举的其它变量如本文所定义。 式I的化合物具有作为抗微生物剂的活性。 还公开了使用哺乳动物的微生物感染的药物组合物和方法，例如使用式（I）化合物或其盐的结核病或麻风病感染。
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6.发明授权2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections 有权2-哌嗪-1-基-4H-1,3-苯并噻嗪-4-酮衍生物及其用于治疗哺乳动物感染的用途公开(公告)号：US08796264B2
公开(公告)日：2014-08-05
申请号：US13884825
申请日：2011-11-21
申请人： Vadim Makarov , Stewart Cole
发明人： Vadim Makarov , Stewart Cole
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D279/08 , C07D417/14
摘要： The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria.
摘要翻译： 本发明涉及新的2-哌嗪-1-基-4H-1,3-苯并噻嗪-4-酮衍生物及其用于治疗由细菌特别是肺结核（TB），布鲁里溃疡和布鲁里溃疡等引起的哺乳动物感染的用途 由于密切相关的分枝杆菌感染引起的麻风病。
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7.发明申请ANTIMICROBIAL COMPOUNDS, THEIR SYNTHESIS AND THEIR USE FOR TREATMENT OF MAMMALIAN INFECTIONS 有权抗微生物化合物，其合成及其用于治疗哺乳动物感染的用途公开(公告)号：US20100286130A1
公开(公告)日：2010-11-11
申请号：US12669748
申请日：2008-06-25
申请人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
发明人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
IPC分类号： A61K31/5415 , C07D417/04 , A61P31/06 , A61P31/08
CPC分类号： C07D279/08
摘要： The present invention relates to compounds of Formula (I) or salts thereof wherein R′, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
摘要翻译： 本发明涉及式（I）化合物或其盐，其中R 1，R 2，R 3，R 4，R 5，R 6和其一个或多个下列举的其它变量如本文所定义。 式I的化合物具有作为抗微生物剂的活性。 还公开了使用哺乳动物的微生物感染的药物组合物和方法，例如使用式（I）化合物或其盐的结核病或麻风病感染。
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8.发明申请公开(公告)号：US20080255166A1
公开(公告)日：2008-10-16
申请号：US12155604
申请日：2008-06-06
申请人： Ute Mollmann , Vadim Makarov
发明人： Ute Mollmann , Vadim Makarov
IPC分类号： A61K31/505 , C07D239/38 , A61K31/277 , C07C205/56 , C07D213/70 , A61K31/44
CPC分类号： C07D239/56 , C07D213/71 , C07D239/47
摘要： The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.
摘要翻译： 本发明涉及二硫代氨基甲酸酯衍生物用于治疗或预防由细菌引起的哺乳动物（人和动物）感染性疾病的治疗，特别是结核分枝杆菌（TB）和由葡萄球菌引起的分枝杆菌和感染性疾病引起的麻风病。 本发明还涉及式（I）的新型二硫代氨基甲酸酯衍生物，其中X是选自具有优异抗菌活性的式的二价残基和含有该二价残基的药物制剂。
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