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1. 发明授权

US07148228B2 Pyrazolopyrimidines and related analogs as HSP90-inhibitors 有权
标题翻译：吡唑并嘧啶类和相关类似物作为HSP90-抑制剂
公开(公告)号：US07148228B2
公开(公告)日：2006-12-12
申请号：US10946637
申请日：2004-09-20
申请人： Srinivas Rao Kasibhatla , Marco A. Biamonte , Kevin D. Hong , David Hurst , Marcus F. Boehm
发明人： Srinivas Rao Kasibhatla , Marco A. Biamonte , Kevin D. Hong , David Hurst , Marcus F. Boehm
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P37/06 , A61P29/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00
摘要： A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R1 is halogen, —OR1, —SR11 or lower alkyl; R2 is —NHR8; R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —CO2H, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R4 is —CHR12—, —C(O), —C(S), —S(O)—, or —SO2—; R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents.
摘要翻译：由式I表示的化合物或其多晶型物，酯，互变异构体，对映异构体，药学上可接受的盐或前体药物：其中：R 1是卤素，-OR 1， - 或低级烷基; R 2是-NHR 8; R 3选自氢，卤素，-SR 8，-OR 8，-CN，-C（O） R 9，-CO 2 H，-NO 2，-NR 8 R 10，低级烷基，低级链烯基，低级炔基，低级全卤代烷基，芳基，杂芳基，脂环族和杂环基，全部是任选取代的，其中：芳基，杂芳基，脂环族和杂环基团任选是单，双或三环的R 4 > - > - ， - C（O）， - （S），-S（O） - 或-SO 2 - 。 R 5是芳基，杂芳基，脂环族或杂环基，其中芳基被3〜5个取代基取代，杂芳基被2〜5个取代基取代，脂环基被3〜 5个取代基，杂环基团被3至5个取代基取代。

2. 发明授权

US07138401B2 2-aminopurine analogs having HSP90-inhibiting activity 有权
标题翻译：具有HSP90抑制活性的2-氨基嘌呤类似物
公开(公告)号：US07138401B2
公开(公告)日：2006-11-21
申请号：US10946645
申请日：2004-09-20
申请人： Srinivas Rao Kasibhatla , Kevin D. Hong , Marcus F. Boehm , Marco A. Biamonte , Lin Zhang
发明人： Srinivas Rao Kasibhatla , Kevin D. Hong , Marcus F. Boehm , Marco A. Biamonte , Lin Zhang
IPC分类号： C07D473/40 , C07D473/16 , C07D473/18 , C07D473/24 , A61K31/52
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00
摘要： 2-Aminopurine analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.
摘要翻译： 2-氨基嘌呤类似物被描述和证实或预测可用作热休克蛋白90（HSP90）抑制剂用于治疗和预防各种HSP90介导的病症，例如增殖性疾病。还描述和要求保护这些化合物的合成和使用方法。

3. 发明授权

US07129244B2 Triazolopyrimidines and related analogs as HSP90-inhibitors 有权
标题翻译：三唑并嘧啶和相关类似物作为HSP90-抑制剂
公开(公告)号：US07129244B2
公开(公告)日：2006-10-31
申请号：US10946628
申请日：2004-09-20
申请人： Srinivas Rao Kasibhatla , Kevin D. Hong , Marcus F. Boehm
发明人： Srinivas Rao Kasibhatla , Kevin D. Hong , Marcus F. Boehm
IPC分类号： C07D487/04 , A61P37/06 , A61P35/00 , A61P29/00 , A61K31/519
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00
摘要： A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, diastereomer, pharmaceutically acceptable salt or prodrug thereof, Wherein R1 is halogen, —OR11, —SR11 or lower alkyl; R2 is —NHR8; R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —S2—; and R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 4 to 5 substituents, the heteroaryl group is substituted with 3 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, and the heterocyclic group is substituted with 3 to 5 substituents.
摘要翻译：由式I表示的化合物或其多晶型物，酯，互变异构体，对映体，非对映异构体，药学上可接受的盐或前药，其中R 1是卤素，-OR 11， -SR 11或低级烷基; R 2是-NHR 8; R 4是-CHR 12 - ， - C（O） - ， - C（S） - ， - S（O） - 或-S < / SUB> - ; R 5是芳基，杂芳基，脂环族或杂环基，其中芳基被4〜5个取代基取代，杂芳基被3〜5个取代基取代，脂环基被3个至5个取代基，并且杂环基团被3至5个取代基取代。

4. 发明授权

US07138402B2 Pyrrolopyrimidines and related analogs as HSP90-inhibitors 有权
标题翻译：吡咯并嘧啶类和相关类似物作为HSP90-抑制剂
公开(公告)号：US07138402B2
公开(公告)日：2006-11-21
申请号：US10945851
申请日：2004-09-20
申请人： Srinivas R. Kasibhatla , Jiandong Shi , Jean-Yves Le Brazidec , Marco A. Biamonte , Kevin D. Hong , Marcus F. Boehm
发明人： Srinivas R. Kasibhatla , Jiandong Shi , Jean-Yves Le Brazidec , Marco A. Biamonte , Kevin D. Hong , Marcus F. Boehm
IPC分类号： C07D487/04 , A61K31/519 , A61P19/02 , A61P35/00 , A61P31/16
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00
摘要： The present invention provides compounds represented by Formula I. R0 is selected from hydrogen, halogen, lower alkyl, —SR8, —OR8, —CN, and —NHR8, R1 is halogen, or lower alkyl; R2 is —NHR8; R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —C(O)OH, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, and R5 is aryl, heteroaryl, alicyclic, or heterocyclic:
摘要翻译：本发明提供由式I表示的化合物。R 0选自氢，卤素，低级烷基，-SR 8，-OR 8，，-CN和-NHR 8，R 1是卤素或低级烷基; R 2是-NHR 8; R 3选自氢，卤素，-SR 8，-OR 8，-CN，-C（O） R 9，-C（O）OH，-NO 2，-NR 8 R 10，低级烷基，低级烯基，低级炔基，低级全卤代烷基，芳基，杂芳基，脂环族和杂环基，全部被取代，R 5是芳基，杂芳基，脂环族或杂环基：

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