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2. 发明申请

WO2003055860A1 3,4-DIARYLPYRAZOLES AND THEIR USE IN THE THERAPY OF CANCER 审中-公开
标题翻译： 3,4-DIARYLPYRAZOLES及其在癌症治疗中的应用
公开(公告)号：WO2003055860A1
公开(公告)日：2003-07-10
申请号：PCT/GB2002/005778
申请日：2002-12-19
申请人： RIBOTARGETS LIMITED , CANCER RESEARCH TECHNOLOGY LTD. , THE INSTITUTE OF CANCER RESEARCH , DRYSDALE, Martin, James , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier , WORKMAN, Paul , PEARL, Laurence, Harris , PRODROMOU, Chrisostomos , MACDONALD, Edward
发明人： DRYSDALE, Martin, James , DYMOCK, Brian, William , BARRIL-ALONSO, Xavier , WORKMAN, Paul , PEARL, Laurence, Harris , PRODROMOU, Chrisostomos , MACDONALD, Edward
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D231/16 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D417/04
摘要： The present invention pertains to the use of certain 3,4-diarylpyrazoles of formula (I), both in vitro and in vivo , to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar 3 is independently: a C 5-20 aryl group, and is optionally substituted; Ar 4 is independently: a C 5-20 aryl group, and is optionally substituted; R 5 is independently: hydrogen; halo; hydroxy; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamido; C 1-7 alkyl; C 3-20 heterocycyl; or C 5-20 aryl; R N is independently: -H; C 1-7 alkyl; C 3-20 heterocycyl; or, C 5-20 aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, such compounds for medical use, such compounds for use in the treatment of conditions mediated by HSP90, including, for example, cancer, and use of such compounds in the preparation of medicaments for such treatments.
摘要翻译：本发明涉及式（I）的某些3,4-二芳基吡唑（体外和体外）均用于抑制热休克蛋白90（HSP90），以及治疗由HSP90介导的病症，包括例如癌症; 其中：Ar 3独立地为：C 5-20芳基，并且是任选取代的; Ar 4独立地是C 5-20芳基，并且任选被取代; R 5独立地为：氢; 光环; 羟基; 醚; 甲酰基; 酰基; 羧基; 酯; 酰氧基; 氧羰基氧; 酰胺基; 酰氨基; 羰基氨基; 四唑基; 氨基; 硝基; 氰基; 叠氮; 巯基; 硫醚; 磺酰; ç 1-7 烷基; ç 3-20 杂环基; 或C 15-20芳基; R N 独立地为：-H; ç 1-7 烷基; ç 3-20 杂环基; 或者C 15-20芳基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及这样的化合物，包含这种化合物的药物组合物，用于医疗用途的这种化合物，用于治疗由HSP90介导的病症包括例如癌症的化合物，以及这些化合物在制备药物用于治疗。

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