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    • 2. 发明申请
    • NEW CHEMICAL INHIBITORS OF BACTERIAL HEPTOSE SYNTHESIS, METHODS FOR THEIR PREPARATION AND BIOLOGICAL APPLICATIONS OF SAID INHIBITORS
    • 细菌肝素合成新化学抑制剂,其抑制剂的制备和生物应用方法
    • WO2008038136A2
    • 2008-04-03
    • PCT/IB2007/003276
    • 2007-09-25
    • MUTABILIS SAESCAICH, SoniaDENIS, AlexisMOREAU, FrançoisGERUSZ, VincentDESROY, Nicolas
    • ESCAICH, SoniaDENIS, AlexisMOREAU, FrançoisGERUSZ, VincentDESROY, Nicolas
    • C07D417/14C07D401/12C07D405/12C07D417/12
    • The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR 1 , C1-C10 alkyl-NR 1 R 1 , alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO 2 R 1 , NR 1 R 1 , NR 1 C(O)R 1 , C(O)NR 1 R 1 , NR 1 C(S)R 1 , C(S)NR 1 R 1 , SO 2 NR 1 R 1 , SO 2 R 1 , NR 1 SO 2 R 1 , NR 1 C(O)NR 1 R 1 , NR 1 C(O)OR 1 , NR 1 C(S)NR 1 R 1 , NR 1 C(S)OR 1 , R 1 C=NOR 1 , C(O)R 1 , aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B 1 , B 2 , B 3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B 4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.
    • 本发明涉及具有式(I)的肝素合成抑制性质的新化合物或其药学上可接受的盐或前药,其中A是芳基或杂环,任选被一个或多个相同或不同的R如H,C1 -C 10烷基,C 1 -C 10烷基-OR 1,C 1 -C 10烷基-NR 1 R 1,烷氧基,羟基,硫代烷基,芳基 ,杂环,卤素,硝基,氰基,CO 2 R 1,NR 1 R 1,NR N, C(O)R 1,C(O)NR 1 R 1,NR 1, C(S)R 1,C(S)NR 1 R 1,SO 2 NR 3, 2个1,1个,1个,1个,2个,1个,1个,1个,1个,1个,3个, NR 1,NR 1,NR 1,NR 1,NR 1, 1个C(O)OR 1,NR 1 C(S)NR 1 R 1, ,NR 1 C(S)OR 1,R 1 C = NOR 1,C(O)R 芳氧基,硫代芳基,烯基,炔基R1相同或相同 不同的是H或C 1 -C 10烷基B 1,B 2,B 3 3相同或不表示C,N,O,S以形成 一个五元芳环,其中一至三个碳原子被选自任选被一个或多个相同或不同的R如上面定义的R 4取代的S,O,N的杂原子取代为C 或NY为H,任选被一个或几个相同或不同的R取代的C 1 -C 10烷基,烷氧基,硫代烷基,W如C,O或N,被一个或多个C 1 -C 10烷基取代或不被 D是任选被一个或多个相同或不同的R取代的杂环,如上所定义。