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1. 发明授权

US08642594B2 Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors 有权
标题翻译：取代噻吩并[2,3-d]嘧啶作为HSP90抑制剂
公开(公告)号：US08642594B2
公开(公告)日：2014-02-04
申请号：US12690983
申请日：2010-01-21
申请人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/497 , A61P25/28 , C07D487/04 , C07D295/04 , C07D295/104
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）化合物是体外或体内HSP90活性的抑制剂，尤其用于治疗癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） r-（Alk2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O）（= S）NRA，-SO2NRA-，-NRAC（= O） - ，-NRASO2-或-NRA-，其中RA是氢或C1-C6烷基，Q是氢或任选取代的碳环或杂环基; R 3是氢，任选的取代基，或任选取代的（C 1 -C 6）烷基，芳基或杂芳基; 并且R 4是羧酸酯，羧酰胺或磺酰胺基。

2. 发明授权

US07820658B2 Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors 有权
标题翻译：取代噻吩并[2,3-d]嘧啶作为HSP90抑制剂
公开(公告)号：US07820658B2
公开(公告)日：2010-10-26
申请号：US10569287
申请日：2004-08-26
申请人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： C07D487/04 , A61K31/519 , C07D295/04 , C07D295/104 , A61K31/5377 , A61K31/497 , A61P25/28
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk 2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)_, —NRASO2- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）的化合物是体外或体内的HSP90活性的抑制剂，并且用于治疗尤其是癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） r-（Alk 2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1 ，Z为-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O）其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; C（= O）NR A - ， - SO 2 NRA-，-NRAC（= O） R 3是氢，任选的取代基，或任选取代的（C 1 -C 6）烷基，芳基或杂芳基; 并且R 4是羧酸酯，羧酰胺或磺酰胺基。

3. 发明申请

US20100120767A1 Pyrimidothiophene Compounds 有权
标题翻译：嘧啶并噻吩化合物
公开(公告)号：US20100120767A1
公开(公告)日：2010-05-13
申请号：US12690983
申请日：2010-01-21
申请人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian William Dymock , Martin James Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： A61K31/5377 , A61K31/519 , A61P29/00 , A61P19/02 , A61P11/06 , C07D495/04
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, -S02-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, -S02NRA—, —NRAC(═O)—, —NRAS02- or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）化合物是体外或体内HSP90活性的抑制剂，尤其用于治疗癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） r-（Alk2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO2-，-C（= O）O-，-C（= O）NRA，-C 其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基;（≡S）NRA-，-SO 2 NR-，-NRAC（= O） - ， - NRASO 2 - 或-NRA- R 3是氢，任选的取代基，或任选取代的（C 1 -C 6）烷基，芳基或杂芳基; 并且R 4是羧酸酯，羧酰胺或磺酰胺基。

4. 发明授权

US07247734B2 3,4-diarylpyrazoles and their use in the therapy of cancer 失效
标题翻译： 3,4-二芳基吡唑及其在癌症治疗中的应用
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。

5. 发明申请

US20110034457A1 Pyridothiophene Compounds 审中-公开
标题翻译：吡啶并噻吩化合物
公开(公告)号：US20110034457A1
公开(公告)日：2011-02-10
申请号：US12909014
申请日：2010-10-21
申请人： Martin James Drysdale , Brian William Dymock , Xavier Barril-Alonso
发明人： Martin James Drysdale , Brian William Dymock , Xavier Barril-Alonso
IPC分类号： A61K31/4365 , C07D471/04 , A61K31/496 , A61K31/5377 , A61P35/00 , A61P37/06 , A61P29/00
CPC分类号： A61K31/4365
摘要： The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): —(Ar1)m-(Alk1)p-(Z)r-(Alk2)S-Q (IA) Ar1, Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.
摘要翻译：式（I）化合物在治疗中的用途，特别是用于治疗由过量或不适当的HSP90活性式（I）介导的病症，其中R2是式（IA）的基团： - （Ar1）m-（Alk1 ）p（Z）r-（Alk2）SQ（IA）Ar1，Alk1，Z，Alk2和Q如说明书中所定义; m，p，r和s独立地为0或1; R 3是氢，任选的取代基，或任选取代的（C 1 -C 6）烷基，芳基或杂芳基; 并且R 4是羧酸酯，羧酰胺或磺酰胺基团; 或其盐，N-氧化物，水合物或溶剂合物。

6. 发明申请

US20070043044A1 Pyrimidothiophene compounds 有权
标题翻译：嘧啶并噻吩化合物
公开(公告)号：US20070043044A1
公开(公告)日：2007-02-22
申请号：US10569287
申请日：2004-08-26
申请人： Brian Dymock , Martin Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
发明人： Brian Dymock , Martin Drysdale , Christofe Fromont , Allan Jordan , Xavier Barril-Alonso
IPC分类号： A61K31/5377 , A61K31/519 , C07D498/02
CPC分类号： C07D495/04 , A61K31/519
摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —0—, —S—, —(C═O)—, —(C═S)—, —S02-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —S02NRA—, —NRAC(═O)_, —NRAS02- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
摘要翻译：式（1）的化合物是体外或体内的HSP90活性的抑制剂，并且用于特别是治疗癌症的用途，其中R 2 2是式 - （Ar 1） - （Z） - （Z） - （Alk＆lt; SUP＆gt; 其中Ar 1是任选取代的芳基或杂芳基，Alk'和Alk 2是任选取代的二价C 1 C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1 中，Z为-O - ， - S - ， - （CO） - ， - （CS） - ， - SO 2 - ， - C（ - -C（-S）NR a - ， - O 2 NR A - ， - O - C（-O） - ， - NR S - 2 - 或-NR A - ，其中R A是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; R 3是氢，任选的取代基或任选取代的（C 1 -C 6 -C 6）烷基，芳基或杂芳基; R 4是羧酸酯，羧酰胺或磺酰胺基。

7. 发明申请

US20090069336A1 PYRIMIDOTHIOPHENE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：US20090069336A1
公开(公告)日：2009-03-12
申请号：US11632969
申请日：2005-07-18
申请人： Xavier Barril-Alonso , Paul Andrew Brough , Martin James Drysdale , Paul Webb
发明人： Xavier Barril-Alonso , Paul Andrew Brough , Martin James Drysdale , Paul Webb
IPC分类号： A61K31/519 , C07D495/04 , A61K31/496 , A61P35/00 , A61P31/12 , A61P17/00 , A61P3/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are inhibitors of HSP90, and useful in the treatment of, for example, cancers: wherein R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q (IA) wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is (i) hydrogen, a —CN group, a nitro group —NO2, or a —C(═NOH)(NH2) group, or (ii) an optionally substituted C1-C6alkyl, aryl, heterocyclic, aryl(C1-C6alkyl)-, or heterocyclic(C1-C6alkyl)- group, or (iii) a group of formula —C(═O)R5 wherein R5 is hydroxyl, optionally substituted C1-C6alkyl, C1-C6alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C1-C6alkyl)-, aryl(C1-C6alkoxy)-, heteroaryl(C1-C6alkyl)-, or heteroaryl(C1-C6alkoxy)-, or (iv) a group of formula —C(═O)NHR6 wherein R6 is primary, secondary, tertiary or cyclic amino, or hydroxyl, optionally substituted C1-C6alkyl, C1-C6alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C1-C6alkyl)-, aryl(C1-C6alkoxy)-, heteroaryl(C1-C6alkyl)-, or heteroaryl(C1-C6alkoxy)-.
摘要翻译：式（I）化合物是HSP90的抑制剂，可用于治疗例如癌症：其中R2是式（IA）的基团：<？在线公式描述=“在线公式”末端 =“引线”→（Ar1）m-（Alk1）p-（Z）r-（Alk2）sQ（IA）<？in-line-formula description =“In-line Formulas”end =“tail”？其中在任何相容的组合中，Ar1是任选取代的芳基或杂芳基，Alk1和Alk2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m，p，r和s独立地为0或1，Z为 - （-S） - ， - （CO） - ， - （CS） - ， - SO 2 - -SO 2 NR - ， - NRAC（-O） - ， - NRASO 2 - 或-NRA-，其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; R 3是氢，任选的取代基，或任选取代的（C 1 -C 6）烷基，芳基或杂芳基; 和（i）氢，-CN基，硝基-NO 2或-C（-NOH）（NH 2）基团，或（ii）任选取代的C 1 -C 6烷基，芳基，杂环，芳基 -C 1-6烷基） - 或杂环（C 1 -C 6烷基） - 基团，或（iii）式-C（ - ） - R 5基团，其中R 5是羟基，任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基，芳基，芳氧基，杂芳基，杂芳基（C 1 -C 6烷基） - ，芳基（C 1 -C 6烷氧基） - ，杂芳基（C 1 -C 6烷基） - 或杂芳基（C 1 -C 6烷氧基） - 或（ⅳ）式-C NHR 6，其中R 6是伯，仲，叔或环状氨基，或羟基，任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基，芳基，芳氧基，杂芳基，杂芳氧基，芳基（C 1 -C 6烷基）杂芳基（C 1 -C 6烷基） - 或杂芳基（C 1 -C 6烷氧基） - 。

8. 发明申请

US20070213328A1 Pyridothiophene Compounds 审中-公开
标题翻译：吡啶并噻吩化合物
公开(公告)号：US20070213328A1
公开(公告)日：2007-09-13
申请号：US10574788
申请日：2004-10-05
申请人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso
发明人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso
IPC分类号： A61K31/4365 , A61P35/00
CPC分类号： A61K31/4365
摘要： The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q (IA) Ar1, Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.
摘要翻译：式（I）化合物在治疗中的用途，特别是用于治疗由过量或不适当的HSP90活性式（I）介导的病症，其中R 2是式（IA）的基团： - （Z 1） - （Z 1） - （Z 1） - （Z 1） Z（Alk），（Z），Al（k）＆lt; SUP＆gt;和Q如说明书中所定义; m，p，r和s独立地为0或1; R 3是氢，任选的取代基或任选取代的（C 1 -C 6 -C 6）烷基，芳基或杂芳基; R 4是羧酸酯，羧酰胺或磺酰胺基; 或其盐，N-氧化物，水合物或溶剂合物。

9. 发明申请

US20050222230A1 3,4-diarylpyrazoles and their use in the therapy of cancer 失效
标题翻译： 3,4-二芳基吡唑及其在癌症治疗中的应用
公开(公告)号：US20050222230A1
公开(公告)日：2005-10-06
申请号：US10499030
申请日：2002-12-19
申请人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso , Paul Workman , Laurence Pearl , Chrisostomos Prodromou , Edward Macdonald
发明人： Martin Drysdale , Brian Dymock , Xavier Barril-Alonso , Paul Workman , Laurence Pearl , Chrisostomos Prodromou , Edward Macdonald
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/428 , A61K31/506 , A61P35/00 , A61P43/00 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/22 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D417/04 , A61K31/4152
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: 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; hydroxy; ether; formyl; acyl; carboxy; ester, acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamido; 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 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; 羟基; 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，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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