公开(公告)号：US20040023968A1

公开(公告)日：2004-02-05

申请号：US10426147

申请日：2003-04-29

申请人： KuDOS Pharmaceuticals Limited ,  Maybridge plc

发明人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Penny Jane Eversley ,  Xiao-Ling Cockcroft ,  Frank Kerrigan ,  Janet Hoare ,  Lesley Dixon

IPC分类号： A61K031/502 ,  C07D43/02

CPC分类号： C07D401/10 ,  C07D237/32 ,  C07D403/10 ,  C07D495/04

摘要： A compound of formula: 1 or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is a C5-7 aryl group substituted in the meta position by the group R2, and optionally further substituted; wherein R2 is selected from: 2 and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP.

摘要翻译： 下式化合物或其异构体，盐，溶剂合物，化学保护形式或前药，其中A和B一起表示任选取代的稠合芳环; R L是由R 2基团在间位取代的任选进一步取代的C 5-7芳基; 其中R 2选自：及其作为药物的用途，特别是用于治疗通过抑制PARP的活性而改善的疾病。

公开(公告)号：US20020183325A1

公开(公告)日：2002-12-05

申请号：US10021506

申请日：2001-10-30

申请人： KuDOS Pharmaceuticals Limited

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： A61K031/502

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: 1 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 nullLnullRL, where L is of formula: null(CH2)n1nullQn2null(CH2)n3nullwherein 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(nullO) or nullCR1R2null, 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, null(CH2)n3null (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：<段落lvl =“0”> in-line-formula> - （CH2）n1-Qn2-（CH2）n3 - 其中n1，n2和n3各自选自0,1,2和3，n1，n2和n3的和为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C 3-7环状烷基，其可以是饱和的（a C 3-7环烷基）或不饱和（C 3-7环烯基），或者R 1和R 2中的一个可以连接到RL中的原子上以形成不饱和的C 3-7环烯基，其包含其中R 1和R 2 连接在Q， - （CH2）n3-（如果存在）和部分RL; 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。