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1. 发明申请

US20110160193A1 New Benzothiazinone Derivatives and Their Use as Antibacterial Agents 审中-公开
标题翻译：新的苯并噻嗪酮衍生物及其作为抗菌剂的用途
公开(公告)号：US20110160193A1
公开(公告)日：2011-06-30
申请号：US12976905
申请日：2010-12-22
申请人： A. Vadim Makarov , Stewart T. Cole , Ute Möllmann
发明人： A. Vadim Makarov , Stewart T. Cole , Ute Möllmann
IPC分类号： A61K31/5415 , C07D491/113 , C07D417/04 , A61P31/06 , A61P11/00
CPC分类号： C07D417/04 , C07D491/113
摘要： The present invention relates to novel benzothiazinone derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance. The solution of the present invention is a compound of formula I wherein R1 to R6 are as defined in the specification.
摘要翻译：本发明涉及新的苯并噻嗪酮衍生物及其作为抗菌剂用于由细菌引起的哺乳动物（人和动物）感染性疾病的用途，特别是结核分枝杆菌（TB）和由分枝杆菌引起的麻风病。本发明旨在产生具有抗分枝杆菌活性的新化合物作为潜在的新型结核病药物，以克服有关耐药性和药物不耐受性的问题。本发明的溶液是式I化合物，其中R 1至R 6如说明书中所定义。

2. 发明授权

US07863268B2 Benzothiazinone derivatives and their use as antibacterial agents 有权
标题翻译：苯并噻嗪酮衍生物及其作为抗菌剂的用途
公开(公告)号：US07863268B2
公开(公告)日：2011-01-04
申请号：US12227655
申请日：2006-05-24
申请人： A. Vadim Makarov , Stewart T. Cole , Ute Moellmann
发明人： A. Vadim Makarov , Stewart T. Cole , Ute Moellmann
IPC分类号： C07D417/06 , A61K31/541
CPC分类号： C07D417/04 , C07D491/113
摘要： Disclosed are benzothiazin derivatives of formula (I), preparation methods therefore, and treatment methods employing such compounds as antibacterial agents in treating infectious diseases of mammals caused by bacteria, especially diseases like tuberculosis and leprosy caused by mycobacteria: wherein R1, R2, R3, R4, R5, and R6, and other variables enumerated under one or more of R1, R2, R3, R4, R5, and R6 are as defined.
摘要翻译：公开了式（I）的苯并噻嗪衍生物，其制备方法以及使用抗菌剂等化合物治疗由细菌引起的哺乳动物感染性疾病，特别是结核分枝杆菌和由分枝杆菌引起的麻风病的疾病的治疗方法：其中R1，R2，R3， R4，R5和R6以及R1，R2，R3，R4，R5和R6中的一个或多个下列举的其它变量如上所定义。

3. 发明申请

US20090239851A1 Benzothiazinone Derivatives and their Use as Antibacterial Agents 有权
公开(公告)号：US20090239851A1
公开(公告)日：2009-09-24
申请号：US12227655
申请日：2006-05-24
申请人： A. Vadim Makarov , Stewart T. Cole , Ute Möllmann
发明人： A. Vadim Makarov , Stewart T. Cole , Ute Möllmann
IPC分类号： A61K31/5415 , C07D417/04 , A61P31/06
CPC分类号： C07D417/04 , C07D491/113
摘要： The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria.The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.The solution of the present invention is a compound of the formula I wherein R1 and R2 are, independently each from other, NO2, CN, CONR7R8, COOR9, CHO, halogen, NR7R8, SO2NR7R8, SR9, OCF3, mono-, di or trifluoromethyl; R3 and R4 are, independently each from other, H, a saturated or unsaturated, linear or branched aliphatic radical having 1-7 chain members, cycloalkyl having 3-6 carbon atoms, benzyl, SR9, OR9; R5 and R6 are, independently each from other, a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-8 chain members, cycloalkyl having 3-6 carbon atoms, phenyl, or R5 and R6 together represent a bivalent radical —(CR92)m—, or R5 and R6 together represent bivalent radicals: wherein m is 1-4, or represent bivalent radicals a saturated or unsaturated mono or polyheterocycles with heteroatoms N, S, O and substituted by (R10)x, wherein x is 1-4; R7, R8 and R9 are, independently each from other H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members, mono-, di or trifluoromethyl, halogen, phenyl, or R3 and R4 together represent a bivalent radical —(CH2)n— wherein n is 2-7; R10 is H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members, NO2, NR7R8, CN, CONR7R8, COOR9, CHO, halogen, SO2NR7R8, SR9, OR9, OCF3, mono-, di or trifluoromethyl, benzyl or phenyl.

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