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1. 发明申请

WO2008098138A1 SYNTHETIC MACROCYCLIC COMPOUNDS FOR TREATING CANCER 审中-公开
标题翻译：用于治疗癌症的合成大环化合物
公开(公告)号：WO2008098138A1
公开(公告)日：2008-08-14
申请号：PCT/US2008/053334
申请日：2008-02-07
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES , BEWLEY, Carole, A. , METAFERIA, Belhu, B.
发明人： BEWLEY, Carole, A. , METAFERIA, Belhu, B.
IPC分类号： C07D267/00 , A61K31/395 , A61P35/00
CPC分类号： C07D267/00
摘要： Disclosed herein are macrocyclic compounds that are effective to inhibit cell migration. In one embodiment, the compounds have the structure: or any pharmaceutically acceptable salt or solvate thereof, wherein: m is O or 1; R 1 , R 2 and R 3 independently are H, aralkyl, acyl, lower alkyl or silyl; X is -C(O)N(R 4 )- or -C(S)N(R 4 )-; -C(O)-; -C(S)-; Y is -OC(O)-; -OC(O)N(R 5 )-; -N(R 5 )C(0)-; or -OC(O)O-; G comprises a saturated or unsaturated aliphatic chain having from 2 to about 10 atoms in the chain, the chain optionally including 1, 2, or 3 heteroatoms; the chain optionally being substituted with 1, 2 or 3 substituents independently selected from lower alkyl, -OR 6 , epoxy, aziridinyl, cyclopropyl, -NR 7 R 8 and halo; R 4 , R 5 , R 6 , R 7 and R 8 independently are selected from H, lower alkyl and acyl. Also disclosed are methods for making and using compounds as well as pharmaceutical compositions including one or more of the disclosed macrocycles.
摘要翻译：本文公开了有效抑制细胞迁移的大环化合物。在一个实施方案中，所述化合物具有以下结构：或其任何药学上可接受的盐或溶剂合物，其中：m为O或1; R 1，R 2和R 3独立地是H，芳烷基，酰基，低级烷基或甲硅烷基; X是-C（O）N（R 4） - 或-C（S）N（R 4） - ; -C（O） - ; -C（S） - ; Y为-OC（O） - ; -OC（O）N（R ^{5 ） - ; -N（R ^{5 ）C（O） - ; 或-OC（O）O-; G包含在链中具有2至约10个原子的饱和或不饱和脂族链，该链任选地包括1,2或3个杂原子; 该链任选被1,2或3个独立地选自低级烷基，-OR 6，环氧基，氮丙啶基，环丙基，-NR 7 R 8的取代基取代和光环; R 4，R 5，R 6，R 7和R 8独立地是选自H，低级烷基和酰基。还公开了制备和使用化合物的方法以及包含一种或多种所公开的大环化合物的药物组合物。}}

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