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1. 发明申请

US20090325983A1 NEW PURINE DERIVATIVES 有权
标题翻译：新的嘌呤衍生物
公开(公告)号：US20090325983A1
公开(公告)日：2009-12-31
申请号：US12489663
申请日：2009-06-23
申请人： Peter Martin FISCHER , Michael JARMAN , Edward MCDONALD , Bernard NUTLEY , Florence RAYNAUD , Stuart WILSON , Paul WORKMAN
发明人： Peter Martin FISCHER , Michael JARMAN , Edward MCDONALD , Bernard NUTLEY , Florence RAYNAUD , Stuart WILSON , Paul WORKMAN
IPC分类号： A61K31/52 , C07D473/16 , C12Q1/48
CPC分类号： C07D473/16 , A61K31/52 , Y02A50/411
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病中的用途。

2. 发明授权

US5721265A Fluorinated 2-nitroimidazole analogs for detecting hypoxic tumor cells 失效
标题翻译：用于检测缺氧性肿瘤细胞的氟化2-硝基咪唑类似物
公开(公告)号：US5721265A
公开(公告)日：1998-02-24
申请号：US458178
申请日：1995-06-02
申请人： Michael Tracy , Andrew B. Kelson , Paul Workman , Alexander D. Lewis , Eric O. Aboagye
发明人： Michael Tracy , Andrew B. Kelson , Paul Workman , Alexander D. Lewis , Eric O. Aboagye
IPC分类号： A61K49/00 , A61K49/06 , C07D233/91 , C07H13/04 , C07H15/04 , C07D233/02 , A61K31/415 , C07D233/04 , C07D233/28 , C07D233/54 , C07D233/68
CPC分类号： C07H13/04 , A61K49/06 , C07D233/91 , C07H15/04
摘要： Agents useful for detecting hypoxic tumor cells are provided. The compounds have the structural formula (I) ##STR1## Methods of using the compounds to detect hypoxic tumor cells are also provided, as are pharmaceutical compositions formulated with the novel compounds.
摘要翻译：提供了可用于检测缺氧性肿瘤细胞的药剂。化合物具有结构式（I）（I）也提供了使用化合物检测缺氧性肿瘤细胞的方法，以及与新化合物一起配制的药物组合物。

3. 发明授权

US07612079B2 2,6,9-substituted purine derivatives and their use in the treatment of proliferative disorders 失效
标题翻译： 2,6,9-取代的嘌呤衍生物及其在治疗增殖性疾病中的用途
公开(公告)号：US07612079B2
公开(公告)日：2009-11-03
申请号：US10742237
申请日：2003-12-18
申请人： Peter Martin Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , C07C215/08 , A61P17/06 , A61P35/02
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein R3 is hydrogen or methyl and R4 is methyl, ethyl or isopropyl; R6 is 3-nitrophenylamino, 3,4-dimethoxybenzylamino, 3-iodobenzyl-amino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino; R9 is isopropyl or cyclopentanyl. In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R2是2-羟甲基吡咯烷-1-基或NHCH（R4）CH（R3）OH，其中R3是氢或甲基，R4是甲基，乙基或异丙基 R6是3-硝基苯基氨基，3,4-二甲氧基苄基氨基，3-碘苄基 - 氨基，吡啶-2-基 - 甲基氨基，吡啶-4-基 - 甲基氨基或茚满-5-氨基; R9是异丙基或环戊基。在另一方面，本发明涉及包含所述化合物的药物组合物及其在治疗抗增生性疾病和/或病毒性疾病中的用途。

4. 发明授权

US07582642B2 Purine derivatives 有权
标题翻译：嘌呤衍生物
公开(公告)号：US07582642B2
公开(公告)日：2009-09-01
申请号：US11033692
申请日：2005-01-11
申请人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Martin Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , A61P31/14 , A61P31/20 , C07D473/40
CPC分类号： C07D473/16 , A61K31/52 , Y02A50/411
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病中的用途。

5. 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。

6. 发明申请

US20060183760A1 New purine derivatives 有权
标题翻译：新嘌呤衍生物
公开(公告)号：US20060183760A1
公开(公告)日：2006-08-17
申请号：US11238533
申请日：2005-09-28
申请人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , C07D473/12
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or un branched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, CNS disorders, diabetes, stroke, alopecia or neurodegenerative disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R 1和R 2中的一个为甲基，乙基或异丙基，另一个为H; R 3和R 4各自独立地为H，支链或非支链C 1 -C 6烷基，或芳基，并且其中R 3和R 4中的至少一个不是H; R 5是支链或非支链C 1 -C 5烷基或C 1 -C 3亚烷基其中每一个可以任选地被一个或多个OH基团取代; R 6，R 7，R 8和R 9各自独立地为H，卤素，NO 3， 2，OH，OMe，CN，NH 2，COOH，CONH 2或SO 2 NH 2， / SUB>。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中枢神经系统疾病，糖尿病，中风，脱发或神经变性疾病中的用途。

7. 发明授权

US07674823B2 DNA-PK inhibitors 失效
标题翻译： DNA-PK抑制剂
公开(公告)号：US07674823B2
公开(公告)日：2010-03-09
申请号：US11758332
申请日：2007-06-05
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
IPC分类号： A61K31/351
CPC分类号： C07D417/04 , C07D309/38 , C07D311/22 , C07D311/92 , C07D471/04
摘要： The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR′4 and NR″4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R′4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R′4 is H, or R3 and R4 or R″4 together are —A—B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
摘要翻译：本发明涉及式（I）化合物及其异构体，盐，溶剂合物，化学保护形式及其前药在制备用于抑制DNA-PK活性的药物中的用途，其中R1和R2独立地为氢，任选取代的C 1-7烷基，C 3-20杂环基或C 5-20芳基，或者可以与它们所连接的氮原子一起形成任选取代的具有4-8个环的杂环原子 X和Y选自CR4和O，O和CR'4和NR "4和N，其中不饱和键在环中的适当位置，并且其中R3和R4或R'4之一是任选取代的C3 -20杂芳基或C5-20芳基，R3和R4或R'4中的另一个为H，或R3和R4或R“4一起为-A-B-，它们共同表示稠合的任选取代的芳环。与PI3-激酶和/或ATM相比，化合物还选择性地抑制DNA-PK的活性。

8. 发明申请

US20070238729A1 DNA-PK INHIBITORS 失效
标题翻译： DNA-PK抑制剂
公开(公告)号：US20070238729A1
公开(公告)日：2007-10-11
申请号：US11758332
申请日：2007-06-05
申请人： Niall Martin , Graeme Smith , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Laurent Rigoreau , Xiao-ling Cockcroft , Vincent Junior Loh , Paul Workman , Florence Raynaud , Bernard Nutley
发明人： Niall Martin , Graeme Smith , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Laurent Rigoreau , Xiao-ling Cockcroft , Vincent Junior Loh , Paul Workman , Florence Raynaud , Bernard Nutley
IPC分类号： A61K31/351 , A61K31/519 , A61K31/5377 , A61P35/00
CPC分类号： C07D417/04 , C07D309/38 , C07D311/22 , C07D311/92 , C07D471/04
摘要： The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR′4 and NR″4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R′4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R′4 is H, or R3 and R4 or R″4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
摘要翻译：本发明涉及式（I）化合物及其异构体，盐，溶剂合物，化学保护形式及其前药在制备用于抑制DNA-PK活性的药物中的用途，其中R 1， R 2和R 2各自独立地为氢，任选取代的C 1-7 - 烷基，C 3-20杂环基或C 或者可以与它们所连接的氮原子一起形成具有4至8个环原子的任选取代的杂环; X和Y选自CR 4和O，O和CR'4和NR“4和N，其中不饱和键处于 R 2中的一个是R 3，R 4，R 4和R 4中的一个是任选取代的C 3 -20个杂芳基或C 5-20-20芳基，R 3和R 4中的另一个或R' > 4 是H，或R 3和R 4或R“4”一起是-AB-，它们共同表示稠合的任选取代的芳环。与PI3-激酶和/或ATM相比，化合物还选择性地抑制DNA-PK的活性。

9. 发明授权

US07226918B2 DNA-PK inhibitors 有权
标题翻译： DNA-PK抑制剂
公开(公告)号：US07226918B2
公开(公告)日：2007-06-05
申请号：US10486816
申请日：2002-08-14
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
IPC分类号： A61K31/353 , A61K31/5377 , C07D265/30 , C07D311/58
CPC分类号： C07D417/04 , C07D309/38 , C07D311/22 , C07D311/92 , C07D471/04
摘要： The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR′4 and NR″4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R′4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R′4 is H, or R3 and R4 or R″4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
摘要翻译：本发明涉及式（I）化合物及其异构体，盐，溶剂合物，化学保护形式及其前药在制备用于抑制DNA-PK活性的药物中的用途，其中R 1， R 2和R 2各自独立地为氢，任选取代的C 1-7 - 烷基，C 3-20杂环基或C 或者可以与它们所连接的氮原子一起形成具有4-8个环原子的任选取代的杂环; X和Y选自CR 4和O，O和CR'4和NR“4和N，其中不饱和键处于 R 2中的一个是R 3，R 4，R 4和R 4中的一个是任选取代的C 3 -20个杂芳基或C 5-20-20芳基，R 3和R 4中的另一个或R' > 4 是H，或R 3和R 4或R“4”一起是-AB-，它们共同表示稠合的任选取代的芳环。与PI3-激酶和/或ATM相比，化合物还选择性地抑制DNA-PK的活性。

10. 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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