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    • 40. 发明公开
    • DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES
    • DIAZENIUMDIOLAT环己基衍生物
    • EP2571351A1
    • 2013-03-27
    • EP11784021.5
    • 2011-05-16
    • Merck Sharp & Dohme Corp.
    • ALI, AmjadYAN, LinHUO, PeiNARGUND, Ravi
    • A01N33/26A61K31/13A61K31/15
    • C07C291/02C07B59/001C07C2601/14
    • A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R
      3 is hydrogen, deuterium, -OH, -OC
      1-6 alkyl, or halogen; R
      8 is hydrogen, deuterium, or C
      1-6 alkyl; R
      11 and R
      12 are independently hydrogen, -C
      1-6 alkyl, -OH, -OC
      1-6 alkyl, or halogen; R
      13 and R
      14 are independently -C
      1-6 alkyl, -(CH
      2 )
      1-2 OH, or -OC
      1-6 alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or -C
      1-6 alkyl; R
      15 is (CR
      1 R
      2 )
      n C(O)OR
      16 , wherein n is 0, 1 or 2, -C(O)NHCH(R
      17 )OR
      16 , or -C(O)NHCH(R
      17 )C(O)NHCH(R
      18 )C(O)OR
      16 ; R
      16 is hydrogen, C
      1-6 alkyl, or (CH
      2 )
      1-2 N+R
      19 R
      20 R
      21 ; R
      1 , R
      2 , R
      4 , R
      5 , R
      6 , R
      7 , R
      9 , R
      10 , R
      17 , R
      18 , R
      19 , R
      20 , and R
      21 are independently hydrogen or -C
      1-6 alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.
    • 具有结构(I)的化合物或其药学上可接受的盐,其中R 3是氢,氘,-OH,-OC 1-6烷基或卤素; R8是氢,氘或C1-6烷基; R 11和R 12独立地是氢,-C 1-6烷基,-OH,-OC 1-6烷基或卤素; R 13和R 14独立地是C 1-6烷基, - (CH 2)1-2 OH或-OC 1-6烷基,或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环 原子和0或1个氧原子,其中所述环是未取代的或被卤素或-C 1-6烷基单取代或二取代或三取代; R 15是-C(O)OH,-C(O)OCH 2 CH 2 N + CH 3)3,其中n是0,1或2,-C(O)NHCH(R 17)OR 16或-C(O)NHCH(R 17)C (O)NHCH(R 18)C(O)OR 16; R16是氢,C1-6烷基或(CH2)1-2N + R19R20R21; R 1,R 2,R 4,R 5,R 6,R 7,R 9,R 10,R 17,R 18,R 19,R 20和R 21独立地为氢或-C 1-6烷基; 及其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。