首页> 外国专利> SUBSTITUTED HETEROCYCLYLCARBONYLAMINO-ACETIC-ACID-DERIVATIVES AS INHIBITORS OF BACTERIAL HEPTOSE SYNTHESIS, METHODS FOR THEIR PREPARATION AND BIOLOGICAL APPLICATIONS OF SAID INHIBITORS

SUBSTITUTED HETEROCYCLYLCARBONYLAMINO-ACETIC-ACID-DERIVATIVES AS INHIBITORS OF BACTERIAL HEPTOSE SYNTHESIS, METHODS FOR THEIR PREPARATION AND BIOLOGICAL APPLICATIONS OF SAID INHIBITORS

机译:取代的杂环碳酰氨基乙酸衍生物作为细菌庚糖合成的抑制剂,其制备方法和所述抑制剂的生物学应用

摘要

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-OR1, C1-C10 alkyl-NR1R1, alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO2R1, NR1R1, NR1C(O)R1, C(O)NR1R1, NR1C(S)R1, C(S)NR1R1, SO2NR1R1, SO2R1, NR1SO2R1, NR1C(O)NR1R1, NR1C(O)OR1, NR1C(S)NR1R1, NR1C(S)OR1, R1C-NOR1, C(O)R1, aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B1, B2, B3 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 B4 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.
机译:本发明涉及式(I)的具有庚糖合成抑制特性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,任选地被一个或几个相同或不同的R例如H,C1取代-C10烷基,C1-C10烷基-OR1,C1-C10烷基-NR1R1,烷氧基,羟基,硫代烷基,芳基,杂环,卤素,硝基,氰基,CO2R1,NR1R1,NR1C(O)R1,C(O)NR1R1, NR1C(S)R1,C(S)NR1R1,SO2NR1R1,SO2R1,NR1SO2R1,NR1C(O)NR1R1,NR1C(O)OR1,NR1C(S)NR1R1,NR1C(S)OR1,R1C-NOR1,C(O) R1,相同或不同的芳氧基,硫代芳基,烯基,炔基R1为H或C1-C10烷基B1,B2,B3相同或不代表C,N,O,S,形成五元芳环,其中1至3个碳原子被选自以下的杂原子取代:S,O,N,任选地被一个或几个相同或不同的R取代,例如以上定义的B4为C或NY为H,C1-C10烷基,烷氧基,硫代烷基,任选被一个或多个取代或几个身份证如上定义的直链或不同的R W是被一个或多个C 1 -C 10烷基取代或未被取代的C,O或N D是任选被一个或几个以上定义的相同或不同的R取代的杂环。

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