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公开(公告)号：EP1682486A1
公开(公告)日：2006-07-26
申请号：EP04790064.2
申请日：2004-10-28
IPC分类号： C07C225/22 , C07C225/16 , C07C217/22 , C07D295/10 , A61K31/14 , A61K31/4965 , A61P31/04
CPC分类号： C07D295/112 , C07C217/22 , C07C225/16 , C07C225/22
摘要： The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y1)m-Ar1(X1)-C(=O)Var2(X2)-(Y2)p (I), wherein V designates -CH2-CH2-, -CH=CH-or -C=C; Ar1 and Ar2 independently are aryl and heteroary.; m=0, 2, p=0, 1, 2, m+p>0; each Y1 and Y2 independently is -Z-N+(R1)(R2)R4 Q-(A); -NR3-Z-N+(R1)(R2)R4 Q- (B), or O-Z-N+(R1)(R2)R4 Q- (C), R1, R2, R3, R4, X1, X2 are substituents, and Q- is an anion. The present invention also relates to the compounds for sue as pharmaceutically active agents, in particular against bacterial infections (such as Gram-negative and Gram-positive bacteria, including antibiotic-sensitive or resistant strains), and in the medical treatment of bacterial infections in mammals.
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公开(公告)号：EP2074085A2
公开(公告)日：2009-07-01
申请号：EP07821261.0
申请日：2007-10-12
IPC分类号： C07C335/16 , A61K31/17 , A61P31/00
CPC分类号： A61K31/17 , C07C335/16
摘要： The present application discloses thiourea compounds for use in the treatment of infections. The thiourea compounds have formula (I) wherein X1 and X2 each designate one or more substituents; and Z is-(CHR)-, -(CHR)2-, -O-(CHR)2-, -NH-(CHR)2-, or -S-(CHR)2-; including salts thereof.
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公开(公告)号：EP1506157A2
公开(公告)日：2005-02-16
申请号：EP03722316.1
申请日：2003-05-19
发明人： NIELSEN, Simon, Feldbaek , KROMANN, Hasse , LARSEN, Mogens , HANSEN, Majbritt,c/o Anette Hansen , BOESEN, Thomas
IPC分类号： C07C225/16 , C07D295/116 , A61K31/5375 , A61P31/04 , C07D295/16
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel amino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, and bacteriocidal agents.
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公开(公告)号：EP1515940A2
公开(公告)日：2005-03-23
申请号：EP03722317.9
申请日：2003-05-19
发明人： NIELSEN, Simon, Feldbaek , BOESEN, Thomas , LARSEN, Mogens , NIELSEN, Mette, Bjerg , KROMANN, Hasse
IPC分类号： C07C217/18 , A61K31/135 , A61P31/04
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel alkoxyaminochalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, bacteriostatic, and bacteriocidal agents.
摘要翻译： 本发明提供了新的烷氧基氨基查耳酮衍生物及其类似物。 还公开了化合物或包含它们的组合物作为药物活性剂，特别是抗细菌和寄生虫感染的用途。 本发明进一步涉及用于检测针对例如细菌，寄生虫，真菌和蠕虫的抑制作用的方法。 本发明的查耳酮含有氨基取代基并且表现出增强的生物效应以及改善的代谢和物理化学性质，使得该化合物可用作药物，特别是作为抗寄生虫剂，抑菌剂和杀菌剂。
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公开(公告)号：EP1506158A2
公开(公告)日：2005-02-16
申请号：EP03722318.7
申请日：2003-05-19
发明人： NIELSEN, Simon, Feldbaek , SCHOENNING, Kristian , KROMANN, Hasse , BOESEN, Thomas , LARSEN, Mogens
IPC分类号： C07C225/22 , A61K31/136 , A61P31/04
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel diamino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic and bacteriostatic agents.
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公开(公告)号：EP0634927B1
公开(公告)日：2001-07-04
申请号：EP93907809.3
申请日：1993-03-08
IPC分类号： A61K31/12 , A61K31/135 , C07C49/84 , C07C69/007 , C07C225/22 , C07C323/22
CPC分类号： C07D207/333 , A61K31/12 , A61K31/135 , A61K31/165 , A61K31/22 , A61K31/27 , A61K31/34 , C07C45/00 , C07C45/62 , C07C45/67 , C07C45/673 , C07C45/71 , C07C45/74 , C07C45/78 , C07C47/575 , C07C49/835 , C07C49/84 , C07C69/24 , C07C271/44 , C07C323/59 , C07D303/32 , C07D307/46 , C07D311/64 , C07K5/0215 , Y02A50/409 , Y02A50/411 , Y02A50/478 , Y02A50/481 , Y02A50/488 , Y10S977/775 , Y10S977/907 , C07C47/565
摘要： The invention is drawn to novel bis-aromatic a,beta-unsaturated ketones. The compounds are useful in the treatment and prophylaxis of diseases caused by parasites or bacteria.
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