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    • 4. 发明公开
    • Polycyclic aromatic compounds
    • 多环芳香化合物
    • EP0125702A3
    • 1985-03-13
    • EP84105585
    • 1984-05-16
    • THE WELLCOME FOUNDATION LIMITED
    • Bair, Kenneth Walter
    • C07C91/10C07C93/04C07C93/14C07C91/14C07C89/00C07C47/575A61K31/13A61K31/645A61K31/12C07C119/10C07C103/78
    • A61K31/045C07C205/15C07C215/10C07C215/28C07C215/42C07C217/48C07C217/58C07C255/58C07C317/32C07C323/32C07C2601/14C07C2603/24C07C2603/26C07C2603/40C07C2603/42C07C2603/48C07C2603/50C07D231/12C07D233/56C07D249/08C07D263/52C07D263/64C07D295/135C07D309/12C07D319/06C07J63/008Y10S514/908
    • Compounds of the formula (I)
      or monomethyl or monoethyl ethers thereof, the compounds including their ethers containing no more than 28 carbon atoms in total, or esters or salts thereof; wherein Ar is selected from the group comprising:
      optionally substituted by one or two substituents which taken together contain not more than four carbon atoms in total and which are the same or different and are selected from halo; cyano; Ci-3 alkyl or Ci- 3 alkoxy each optionally substituted by hydroxy or C 1-2 alkoxy; halo substituted C 1-2 alkyl or C 1-2 alkoxy; a group S(O)nR 5 wherein n is an integer 0,1 or 2 and R 5 is C 1-2 alkyl optionally substituted by hydroxy or C 1-2 alkoxy; or Ar is optionally substituted by a group NR 6 R 7 containing not more than 5 carbon atoms wherein R 6 and R 7 are the same or different and each is a C 1-3 alkyl group or NR 6 R 7 forms a five or six membered heterocyclic ring optionally containing one or two additional hetero atoms; R' is Ci-3 alkyl substituted by hydroxy; R 2 is hydrogen, C 1-3 alkyl or hydroxymethyl; R 3 and R 4 are the same or different and each is hydrogen, methyl or ethyl; R 1 , R 2 , R 3 and R 4 taken together containing not more than five carbon atoms; or the group:
      wherein -C-C- is a five or six membered saturated carbocyclic ring containing two or three hydroxy groups; R a is hydrogen, methyl or hydroxymethyl; R 9 and R 10 are the same or different and each is hydrogen or methyl; R 11 is hydrogen, hydroxy, methyl or hydroxymethyl; R 5 , R 9 , R 10 , R 11 and the -C-C- ring taken together containing less than seven carbon atoms which have biocidal, and particularly antitumour, activity are described as are methods for their preparation, their use in medicine and pharmaceutical formulations containing them.
    • 式(I)化合物或其单甲醚或单乙醚,其中包括总共不超过28个碳原子的醚,或其酯或盐; 其中Ar选自包括以下的基团:任选地被一个或两个取代基取代的取代基,它们总共包含不超过四个碳原子,并且相同或不同并且选自卤素; 氰基; 各自任选被羟基或C 1-2烷氧基取代的C 1-3烷基或C 1-3烷氧基; 卤素取代的C 1-2烷基或C 1-2烷氧基; S(O)n R 5基团,其中n是整数0,1或2,R 6是任选被羟基或C 1-2烷氧基取代的C 1-2烷基; 或Ar任选被含有不多于5个碳原子的基团NR 6 R 7取代,其中R 6和R 7相同或不同,并且各自为C 1-3烷基或NR' 6> R 7形成任选地含有一个或两个另外的杂原子的五元或六元杂环; R 1是被羟基取代的C 1-3烷基; R 2是氢,C 1-3烷基或羟甲基; R 3和R 4相同或不同,各自为氢,甲基或乙基; R 1,R 2,R 3和R 4一起含有不超过5个碳原子; 或组; 其中 - @@@ - 是含有两个或三个羟基的五或六元饱和碳环; R 8是氢,甲基或羟甲基; R 9和R 1相同或不同,各自为氢或甲基; R 1是氢,羟基,甲基或羟甲基; R 8,R 9,R 1,O,R 1,和 - @@-环一起含有少于7个具有杀生物活性的碳原子,特别是抗肿瘤活性 被描述为它们的制备方法,它们在医药中的应用和含有它们的药物制剂。