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    Phthalazinone derivatives
    1.
    发明授权
    Phthalazinone derivatives 有权
    酞嗪衍生物

    公开(公告)号：US07750006B2

    公开(公告)日：2010-07-06

    申请号：US11352178

    申请日：2006-02-10

    申请人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Charles Richard White ,  Roger Frank Newton ,  Diane Gillian Douglas ,  Penny Jane Eversley ,  Julia Vile

    发明人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Charles Richard White ,  Roger Frank Newton ,  Diane Gillian Douglas ,  Penny Jane Eversley ,  Julia Vile

    IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D237/26

    CPC分类号： C07D401/12 ,  A61K31/50 ,  A61K31/502 ,  C07D237/32 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by -L-RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(═O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, —(CH2)n3— (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.

    摘要翻译： 一种治疗由PARP介导的人体或动物体的疾病的方法，包括向所述受试者施用治疗有效量的式：或其异构体，盐，溶剂化物，化学保护形式及其前药的化合物，其中： A和B一起表示任选取代的稠合芳环; RC由-L-RL表示，其中L为下式： - （CH2）n1-Qn2-（CH2）n3-，其中n1，n2和n3各自选自0,1,2和3，n1 ，n2和n3是1,2或3，Q选自O，S，NH，C（= O）或-CR1R2-，其中R1和R2独立地选自氢，卤素或任选取代的C 1-7烷基， 或者可以与它们所连接的碳原子一起形成可以是饱和的（C 3-7环烷基）或不饱和的（C 3-7环烯基）或R 1和R 2中的一个的C 3-7环烷基 可以连接到RL中的原子以形成不饱和的C 3-7环烯基，其包含在Q， - （CH 2）n 3-（如果存在）和部分RL中R 1和R 2连接的碳原子; 并且RL是任选取代的C 5-20芳基; 并且RN选自氢，任选取代的C 1-7烷基，C 3-20杂环基和C 5-20芳基，羟基，醚，硝基，氨基，酰胺基，硫醇，硫醚，亚砜和砜。