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    Small-Molecule HSP90 Inhibitors
    6.
    发明申请
    Small-Molecule HSP90 Inhibitors 有权
    小分子HSP90抑制剂

    公开(公告)号：US20110104054A1

    公开(公告)日：2011-05-05

    申请号：US12939807

    申请日：2010-11-04

    Applicant: Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-bufi ,  Joungnam Kim ,  Steven M. Larson ,  Peter Smith-Jones

    Inventor： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-bufi ,  Joungnam Kim ,  Steven M. Larson ,  Peter Smith-Jones

    IPC: A61K31/52 ,  C07D473/34 ,  A61P35/00 ,  A61K51/00 ,  A61P43/00 ,  C12N5/02

    CPC classification number: C07D473/34 ,  A61K51/0459 ,  C07D491/056 ,  G01N33/60

    Abstract: Hsp90 inhibitors having are provided having the formula: with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

    Abstract translation: 提供具有下式的Hsp90抑制剂：右侧芳基部分具有2'，4'，5'-取代模式。 X1表示在芳基的4'和5'位置上可以相同或不同的两个取代基，其中X 1选自卤素，烷基，烷氧基，卤代烷氧基，羟基烷基，吡咯基，任选取代的芳氧基，烷基氨基 ，二烷基氨基，氨基甲酰基，酰氨基，烷基酰氨基二烷基酰氨基，酰基氨基，烷基磺酰氨基，三卤甲氧基，三卤代烷基，硫代烷基，SO2-烷基，COO-烷基，KH 2，OH，CN，SO 2 X 5，NO 2，NO，C≡SR2 NSO 2 X 5，C = OR 2，其中 X5是F，NH2，烷基或H，R2是烷基，NH2，NH-烷基或O-烷基，C1-C6烷基或烷氧基; 或其中X 1具有式-O-（CH 2）n -O-，其中n是0至2的整数，优选1或2，并且其中一个氧键在5'-位上而另一个在 芳基环的4'-位。 该化合物可用于癌症治疗和放射成像配体。

    Small-molecule Hsp90 inhibitors
    8.
    发明授权
    Small-molecule Hsp90 inhibitors 有权
    小分子Hsp90抑制剂

    公开(公告)号：US07834181B2

    公开(公告)日：2010-11-16

    申请号：US11814506

    申请日：2006-02-01

    Applicant: Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steve M. Larson ,  Peter Smith-Jones

    Inventor： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steve M. Larson ,  Peter Smith-Jones

    IPC: C07D473/34 ,  C07D473/40 ,  A61K31/52 ,  A61P35/00

    CPC classification number: C07D473/34 ,  A61K51/0459 ,  C07D491/056 ,  G01N33/60

    Abstract: Hsp90 inhibitors are provided having the formula: with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2−alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygen is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

    Abstract translation: 提供具有下式的Hsp90抑制剂：右侧芳基部分具有2'，4'，5'-取代模式。 X1表示在芳基的4'和5'位置上可以相同或不同的两个取代基，其中X 1选自卤素，烷基，烷氧基，卤代烷氧基，羟基烷基，吡咯基，任选取代的芳氧基，烷基氨基 ，二烷基氨基，氨基甲酰基，酰氨基，烷基酰氨基二烷基酰氨基，酰基氨基，烷基磺酰氨基，三卤甲氧基，三卤代烷基，硫代烷基，SO2-烷基，COO-烷基，KH 2，OH，CN，SO 2 X 5，NO 2，NO，C≡SR2 NSO 2 X 5，C = OR 2，其中 X5是F，NH2，烷基或H，R2是烷基，NH2，NH-烷基或O-烷基，C1-C6烷基或烷氧基; 或其中X 1具有式-O-（CH 2）n -O-的化合物，其中n为0至2的整数，优选1或2，并且一个氧键在5'位置而另一个在 芳基环的4'-位。 该化合物可用于癌症治疗和放射成像配体。

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