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    • 10. 发明申请
    • HYDRAZINOMETHYL, HYDR ZONOMETHYL AND 5-MEMBERED HETEROCYLIC COMPOUNDS WHICH ACT AS MTOR INHIBITORS AND THEIR USE AS ANTI CANCER AGENTS
    • 氢化二甲基丙烯酸,氢化二甲基乙烯基醚和作为MT抑制剂的5组分的杂环化合物及其用作抗癌剂
    • WO2006090167A3
    • 2007-05-10
    • PCT/GB2006000668
    • 2006-02-24
    • KUDOS PHARM LTDHUMMERSONE MARC GEOFFREYGOMEZ SYLVIEMENEAR KEITH ALLANCOCKCROFT XIAO-LING FANSMITH GRAEME CAMERON MURRAY
    • HUMMERSONE MARC GEOFFREYGOMEZ SYLVIEMENEAR KEITH ALLANCOCKCROFT XIAO-LING FANSMITH GRAEME CAMERON MURRAY
    • C07D251/70A61K31/506A61K31/517A61K31/53C07D403/04
    • C07D251/70C07D239/48C07D239/50C07D239/94C07D295/135C07D403/04C07D403/12C07D405/04C07D413/12C07D417/04C07D471/04
    • Compounds of formula (I): A-B-C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where R N is H or Me; or B is a divalent C 5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) R A3 and R A5 are independently selected from halo, OR O and R AC , where R O is H or Me, and R AC is H or C 1-4 alkyl; X A is selected from N and CR A4 , where R A4 is selected from H, OR O , CH 2 OH, CO 2 H, NHSO 2 Me and NHCOMe; R A2 and R A6 are independently selected from H, halo and OR O ; or R A3 and R A4 together with the carbon atoms to which they are attached, or RA2 and R A3 together with the carbon atoms to which they are attached, may form a C 5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1 , 2, or 3 of R A2 to R A6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CR C6 ; R C3 is selected from H, halo and an optionally substituted N-containing C 5-7 heterocyclic group; R C5 is a group selected from formula (iv) which group may be selected by one or two C 1-4 alkyl groups or a carboxy group; R C6 is H; or, when X and Y are N, R C5 and R C6 (when Z is CR C6 ) together with the carbon atoms to which they are attached may form a fused C 6 aromatic ring selected from the group consisting of formula (v).
    • 式(I)化合物:ABC及其异构体,盐,溶剂化物,化学保护形式及其前体药物,其中:B选自式(ⅰ),其中R N为H或Me ; 或B是含有一个或两个环杂原子的二价C 5 - 5杂环残基; A是式(ⅱ),R A3和R A5各自独立地选自卤素,O或O, 其中R O是H或Me,且R AC是H或C 1-4烷基; 从其中R A4选自H,OR,O,CH,N, 2 OH,CO 2 H,NHSO 2 Me和NHCOMe; R A2和R A6各自独立地选自H,卤素和ORO; 或R A3与它们所连接的碳原子一起形成,或者与其连接的碳原子一起,或者R A2和R A3与其中的碳原子一起 它们可以形成含有至少一个氮环原子的C 5〜6 - 杂环或杂芳环; 其中如果X不是N,则R A2与R A6之间的1,2或3不是H; C是式(ⅲ)其中X选自N和CH,Y选自N和CH,Z选自N和CR 6 C 6。 R 3选自H,卤素和任选取代的含N C的5-7杂环基; R 5是选自式(ⅳ)的基团,该基团可以被一个或两个C 1-4烷基或羧基选择; C 6 H 6是H; 或者当X和Y为N时,R 5和R 6 C(当Z为CR 6 C 6)时,与它们的碳原子一起 可以形成选自由式(v)组成的组的稠合C 6芳香环。