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1.3 thiazole Derivatives, inhibitors of DNA gyrase and topoisomerase IV / or

机译:1.3噻唑衍生物,DNA回旋酶和拓扑异构酶IV的抑制剂

摘要

It also describes the process of preparing these drugs, the pharmaceutical ingredients that contain them, how they are used as drugs, and how they are used to treat bacterial infections. Claim 1: a compound classified as formula (1): (I) R1 is Cl, R2 is br or CF, R3 is CH3, (II) R1 is br, R2 is Cl, Br, CN or CF3, R3 is CH3, (III) R1 is CN, R2 is br or CF3, R3 is CH3, or (IV) R1 is CH3, R2 and R3 are CL; R4 is h, fluoride, methyl, methoxi, etoxi, cycloxi, proposxi, aliloxi and benloxi; R5 is hydrogen or C1-4 tar; y = n or CRA, where RA is h, CH3, F, CF3 or CN; R6 is selected from any 1-4 tar, halogen-1-4 alquiniloc2-4, alquiniloc2-4,C3-6cycloalkyl, (cycloalkylC3-6) alkyl, (C1-4alkoxy) alkyl, (cycloalkoxyC3-6) alkyl, (haloalkoxyC1-4) alkyl, N- (C1-4alkyl) alkyl, N, N- ( C1-4alkyl) 2alkyl, carbocyclyl-R7- or heterocyclyl-R8; R7 and R8 are independently selected from a direct bond, -O-,-N (R9) --C (O) --N (R10) C (O) --C (O) N (R11) --S (O) p--SO2N (R12) - o -N (R13) SO2-In this case, R9, R10, R11, R12 and R13 are independently selected from hydrogen or hydrocarbon 1-4 and p; their salts are pharmaceutically acceptable.
机译:它还描述了这些药物的制备过程,包含这些药物的药物成分,如何将它们用作药物以及如何将它们用于治疗细菌感染。 1.根据权利要求1所述的化合物,其被分类为式(1):(I)R1为Cl,R2为br或CF,R3为CH3,(II)R1为br,R2为Cl,Br,CN或CF3,R3为CH3, (III)R1为CN,R2为br或CF3,R3为CH3,或(IV)R1为CH3,R2和R3为CL; R4为h,氟,甲基,甲氧基,依托克西,环氧基,普罗泊西,阿利洛西和本洛西; R5是氢或C1-4焦油; y = n或CRA,其中RA为h,CH3,F,CF3或CN; R 6选自任何1-4焦油,卤素1-4 Alquiniloc2-4,Alquiniloc2-4,C3-6环烷基,(环烷基C3-6)烷基,(C1-4烷氧基)烷基,(环烷氧基C3-6)烷基,(卤代烷氧基C1 -4)烷基,N-(C 1-4烷基)烷基,N,N-(C 1-4烷基)2烷基,碳环基-R 7-或杂环基-R 8; R7和R8独立选自直接键,-O-,-N(R9)-C(O)-N(R10)C(O)-C(O)N(R11)-S( O)对-SO 2 N(R 12)-邻-N(R 13)SO 2-在这种情况下,R 9,R 10,R 11,R 12和R 13独立地选自氢或烃1-4和p;它们的盐是药学上可接受的。

著录项

  • 公开/公告号AR074721A1

    专利类型

  • 公开/公告日2011-02-09

    原文格式PDF

  • 申请/专利权人 ASTRAZENECA AB;

    申请/专利号AR2009P104827

  • 发明设计人 PEER MOHAMED SHAHUL HAMEED;WATERSON DAVID;

    申请日2009-12-11

  • 分类号C07D417/14;A61K31/427;A61P31/04;

  • 国家 AR

  • 入库时间 2022-08-21 18:07:29

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