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    NOUVEAUX COMPOSES AYANT UNE ACTIVITE PROTECTRICE VIS-A-VIS DE TOXINES AU MODE D'ACTION INTRACELLULAIRE
    8.
    发明公开
    NOUVEAUX COMPOSES AYANT UNE ACTIVITE PROTECTRICE VIS-A-VIS DE TOXINES AU MODE D'ACTION INTRACELLULAIRE 审中-公开
    有保护作用针对与INTRA细胞活性毒素新的纽带

    公开(公告)号：EP2909184A1

    公开(公告)日：2015-08-26

    申请号：EP13783284.6

    申请日：2013-10-18

    申请人： Commissariat à l'Énergie Atomique et aux Énergies Alternatives ,  Institut Curie ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS

    发明人： GILLET, Daniel ,  BARBIER, Julien ,  JOHANNES, Ludger ,  CINTRAT, Jean-Christophe ,  NOEL, Romain

    IPC分类号： C07D239/91 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  A61K31/427 ,  A61K31/517 ,  A61K31/381 ,  A61K31/4439 ,  A61K31/506 ,  A61P39/02

    CPC分类号： C07D409/04 ,  C07D239/91 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention concerns a new family of 2,3-dihydroquinazolin-4(1
    H) -one compounds of general formula (I), and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as ricin or Shiga toxin, for example, using retrograde transport to intoxicate cells.

    摘要翻译： 2,3-二氢-1H-喹唑啉-4-酮化合物（I）是新的。 2,3-二氢-1H-喹唑啉-4-酮的式（I）的化合物是新的。 R1：H，卤素或1-3C-烷氧基; R2：苯基（被苯基，CF 3，卤素OPTIONALLY substituiertem， - SO 2 - 苯基或-S-X）， - O-X，5-10原子的杂环或杂二环包含两个N原子，优选吡啶，或金刚烷基环被羟基OPTIONALLY substituiertem; X：1-4C-烷基，优选甲基; R3：5或6原子芳族杂环（噻吩由......组成，吡啶（均为优选的），呋喃，吡咯，吡咯啉，吡咯烷，二氧戊环，恶唑，噻唑，咪唑，咪唑啉，咪唑烷，吡唑，异恶唑，异噻唑，吡喃，哌啶，二恶烷 类，吗啉，哒嗪，嘧啶，吡嗪或），或任选被1-3C-烷氧基或N（CH 3）2，其中杂环任选地被（1-3C烷基substituiertem（优选甲基）（优选的）substituiertem， 卤素，苯基-SY1，-CN或5或6原子芳族杂环（噻吩，吡啶，呋喃，吡嗪由......组成（由1-3C-烷氧基，-CN，-NO 2，或--COX -COOX OPTIONALLY substituiertem）（ 所有优选的），吡咯，吡咯啉，吡咯烷，二氧戊环，恶唑，噻唑，咪唑，咪唑啉，咪唑烷，吡唑，异恶唑，异噻唑，吡喃，哌啶，二恶烷，吗啉，哒嗪或嘧啶））; Y1：1-4C-烷基或苯基; 和R4：H或甲基。 提供没有（I）不包括其中R 1 2,3-二氢-1H-喹唑啉-4-酮化合物是H，R 2是苯基，R 3是5-甲基噻吩-2-基和R 4为H. [图像] ACTIVITY ：解毒剂。 作用机理：没有给出。

    INHIBITORS OF THE SHIGA TOXINS TRAFFICKING THROUGH THE RETROGRADE PATHWAY
    9.
    发明公开
    INHIBITORS OF THE SHIGA TOXINS TRAFFICKING THROUGH THE RETROGRADE PATHWAY 审中-公开
    保护反对毒素和病毒的活性作用的新化合物对细胞内的机制DEPLOY

    公开(公告)号：EP2296757A2

    公开(公告)日：2011-03-23

    申请号：EP09766206.8

    申请日：2009-06-17

    申请人： Commissariat à l'Énergie Atomique et aux Énergies Alternatives ,  Institut Curie ,  Centre National de la Recherche Scientifique

    发明人： GILLET, Daniel ,  BARBIER, Julien ,  JOHANNES, Ludger ,  STECHMANN, Bahne ,  BAI, Siau-Kun

    IPC分类号： A61P39/02 ,  A61K31/5513 ,  A61K31/341 ,  A61K31/167

    CPC分类号： C07D453/02 ,  A61K31/167 ,  A61K31/341 ,  A61K31/5513 ,  C07C211/27 ,  C07C211/38 ,  C07C215/10 ,  C07C215/42 ,  C07C215/44 ,  C07C217/16 ,  C07C217/58 ,  C07C229/14 ,  C07C229/22 ,  C07C229/38 ,  C07C229/48 ,  C07C233/06 ,  C07C233/58 ,  C07C233/65 ,  C07C237/40 ,  C07C251/24 ,  C07C271/56 ,  C07C275/28 ,  C07C317/14 ,  C07C335/02 ,  C07C2601/08 ,  C07C2602/46 ,  C07C2603/74 ,  C07D209/14 ,  C07D213/38 ,  C07D215/12 ,  C07D233/10 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D235/08 ,  C07D243/12 ,  C07D243/24 ,  C07D245/06 ,  C07D249/06 ,  C07D307/42 ,  C07D307/52 ,  C07D317/46 ,  C07D317/58 ,  C07D317/62 ,  C07D317/66 ,  C07D333/20 ,  C07D401/04 ,  C07D451/02 ,  C07D471/08 ,  C07D487/04 ,  Y02A50/471 ,  Y02A50/473

    摘要： Use of aminoadamantane compound (I) and benzodiazepine compound (II) and their salts for the preparation of a composition for the prevention and/or treatment of poisoning at least one toxin intracellular mode of action or at least a virus using the route of internalization to infect eukaryotic cells of mammals, is claimed. Use of aminoadamantane compound of formula (Cy-(-CH 2-) p-NR 2>-X-R 1>) (I) and benzodiazepine compound of formula (II) and their salts for the preparation of a composition for the prevention and/or treatment of poisoning at least one toxin intracellular mode of action or at least a virus using the route of internalization to infect eukaryotic cells of mammals, is claimed. Cy : benzen-1-yl (optionally substituted by W 1>) or adamantane group of formula (a); W 1>H or halo; Y 1>H or OH; Z : C or bond (when Cy is a noradamantyl core); either X : bond, or 1-6C alkyl (optionally saturated and substituted by phenyl, acid and/or 1-3C alkyl ester), where the chain being optionally interrupted by an oxygen atom, -CO-, -O-CO-, -CO-NH- or -S(=O)(=O)-; and R 1>1-21C cyclic or branched radical, optionally saturated, where one or more carbon atoms can be replaced by an atom of nitrogen, oxygen and/or sulfur (where the radical being optionally mono or bi-substituted with a halo, a function-COOH, -OH,-NO 2, 1-3C alkyl, 1-3C alkoxy or 1-3C acyloxy); and R 2>H, 1-3C alkyl (optionally saturated), 2-4C acyl radical, or 1-bromo-3-methyl-benzene moiety; or NXR 1>R 2>a ring, preferably imidazole, oxazole, triazole, benzimidazole, optionally partially saturated, dihydroimidazole, optionally substituted by a phenyl or pyridine radical; p : 0 or 1; A, B 1>C or N, provided that if A is N, then B 1>is C and if A is C, then B is N; R 3>halo, 1-6C alkyl, 1-6C alkoxy, or 1-6C acyloxy (all optionally substituted by 1-6C alkoxy), H, aryloxy or heteroaryloxy; R 4>bond, H, 1-3C acyloxy radical, 1-3C acyloxy radical, or phenyl; and R 5>H, 1-3C alkyl, 1-3C alkoxy, 1-3C acyloxy or phenyl radical (optionally substituted by OH and/or halo, 1-3C alkyl, 1-3C alkoxy, 1-3C acyloxy, NO 2, -CF 3, or group of formula (CH 3-CH=CH-O)). Provided that: when R 2>is a bond, the nitrogen atom bearing R 2>and X or the adjacent carbon atom (when p is 1) are linked by a double bond; when the Cy is adamantyl core, then the chain (-(-CH 2-) p-NR 2>-X-R 1>) is attached to the position 1 or 2; R 4>and R 5>can not simultaneously be a bond and when R 4>or R 5>is a bond, then A and B 1>are linked by a double bound; and when B 1>is a carbon atom, then R 5>may also form with the adjacent hydrogen atom a cycle containing 5-6 atoms (optionally substituted by a phenyl radical, and optionally interrupted by a nitrogen, oxygen or sulfur atom). Independent claims are included for: (1) the compound (I) (where (I) excludes: N-benzyladamantylamine, N-(3-hydroxybenzyl)adamantylamine, N-(3-methoxybenzyl)adamantylamine, N-(4-nitrobenzyl)adamantylamine, N-((pyridin-4-yl)methyl)adamantylamine, N-phenethyladamantylamine, N-(3-phenylpropyl)adamantylamine, N-benzyl-2-adamantylamine, N-(3-bromobenzyl)-2-methylpropan-2-amine, N-(3-bromobenzyl)cyclohexanamine, N-benzyl(3-bromophenyl)methanamine, N-(3-fluorobenzyl)(3-bromophenyl)methanamine, (E)-N-(3-bromobenzylidene)adamantylamine, (E)-N-(3-fluorobenzylidene)adamantylamine, (E)-N-benzylideneadamantylamine, N-1-adamantylbenzamide, N-2-adamantylbenzamide, N-adamantyl benzenesulfonamide, N-2-adamantyl benzenesulfonamide, 1-(adamantyl)-2,5-dihydrooxazole, adamantylamino-4-phenyl-1H-1,2,3-triazole, or (E)-2-(2-(5-methylthiophen-2-yl)vinyl)-N-phenylbenzamide); and (2) the compound (II) (where (II) excludes: 5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one, 7-bromo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one, 7-bromo-5-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-2-one, 4-phenyl-2,3-dihydro-1H-1,5-benzodiazepin-2-one, 4-phenyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one, 4,5-dihydro-7-methoxy-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one, 5-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-2-one, 7-chloro-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one, 7-chloro-5-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-2-one or 7-bromo-5-phenyl-4-propionyl-4,5-dihydro-1H-benzo[e][1,4]diazepin-2(3H)-one). [Image] [Image] ACTIVITY : Antidote. MECHANISM OF ACTION : None given.