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    THERAPEUTIC USES OF BICYCLIC LIGANDS OF SIGMA 2 RECEPTOR
    3.
    发明申请
    THERAPEUTIC USES OF BICYCLIC LIGANDS OF SIGMA 2 RECEPTOR 有权
    SIGMA 2受体的双相配体的治疗用途

    公开(公告)号：US20100048614A1

    公开(公告)日：2010-02-25

    申请号：US12543647

    申请日：2009-08-19

    Applicant: Robert H. Mach ,  Richard Hotchkiss ,  William Hawkins ,  Rebecca Aft ,  Zhude Tu

    Inventor： Robert H. Mach ,  Richard Hotchkiss ,  William Hawkins ,  Rebecca Aft ,  Zhude Tu

    IPC: A61K31/439 ,  A61P35/00

    CPC classification number: C07D451/14 ,  C07D451/02

    Abstract: A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.

    Abstract translation: 公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3α-基苯基氨基甲酸酯类似物及其制备方法。 描述了它们对西格玛（＆sgr。1和＆sgr; 2）受体的亲和力。 两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对于＆ 1受体。 所公开的化合物中有生物素化和荧光类似物。 这些化合物可以作为第二受体的探针。 此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。 这些化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

    Sigma 2 Receptor Ligands and Therapeutic Uses Therefor
    4.
    发明申请
    Sigma 2 Receptor Ligands and Therapeutic Uses Therefor 有权
    Sigma 2受体配体及其治疗用途

    公开(公告)号：US20080161343A1

    公开(公告)日：2008-07-03

    申请号：US11776533

    申请日：2007-07-11

    Applicant: Robert H. Mach ,  Zhude Tu ,  Wenhua Chu ,  Suwanna Vangveravong ,  Richard Hotchkiss ,  William Hawkins ,  Rebecca Aft

    Inventor： Robert H. Mach ,  Zhude Tu ,  Wenhua Chu ,  Suwanna Vangveravong ,  Richard Hotchkiss ,  William Hawkins ,  Rebecca Aft

    IPC: A61K31/439 ,  C07D453/02 ,  C12N5/06 ,  A61P35/00

    CPC classification number: C07D451/14 ,  C07D451/02

    Abstract: A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.

    Abstract translation: 公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3-基苯基氨基甲酸酯类似物及其制备方法。 描述了它们对西格玛（sigma1和sigma2）受体的亲和力。 两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对sigma2与σ1受体的高亲和力和选择性。 所公开的化合物中有生物素化和荧光类似物。 这些化合物可以作为sigma2受体的探针。 此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。 这些化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

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