公开(公告)号：US07247734B2

公开(公告)日：2007-07-24

申请号：US10499030

申请日：2002-12-19

申请人： Martin James Drysdale ,  Brian William Dymock ,  Xavier Barril-Alonso ,  Paul Workman ,  Laurence Harris Pearl ,  Chrisostomos Prodromou ,  Edward McDonald

发明人： Martin James Drysdale ,  Brian William Dymock ,  Xavier Barril-Alonso ,  Paul Workman ,  Laurence Harris Pearl ,  Chrisostomos Prodromou ,  Edward McDonald

IPC分类号： C07D231/10

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-diarylpyazoles 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: Ar3 is independently: a C5-20aryl group, and is optionally substituted; Ar4 is independently: a C5-20aryl group, and is optionally substituted; R5 is independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; R N is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; 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 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（体外和体内）用于抑制热休克蛋白90（HSP90）的用途，以及用于治疗HSP90介导的病症，包括 例如癌症; 其中：Ar 3独立地是C 5-20-20芳基，并且是任选被取代的; Ar 4独立地是C 5-20-20芳基，并且是任选被取代的; R 5独立地为氢; 光环; 羟; 醚; 甲酰基 酰基; 羧基; 酯; 酰氧基 氧羰氧基 氨基酸 酰氨基; 氨基羰基氧基; 四唑基; 氨基; 硝基 氰基; 叠氮 巯基 硫醚 磺酰胺 C 1-7烷基; C 3-20杂环基; 或C 5-20-20芳基; R N 独立地为：-H; C 1-7烷基; C 3-20杂环基; 或C 5-20-20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，这种化合物用于治疗由HSP90介导的病症，包括例如癌症，以及这些化合物在制备药物中的用途 用于治疗。