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    Rab7 GTPase Inhibitors and Related Methods of Treatment
    1.
    发明申请
    Rab7 GTPase Inhibitors and Related Methods of Treatment 有权
    Rab7 GTPase抑制剂及相关治疗方法

    公开(公告)号：US20140248268A1

    公开(公告)日：2014-09-04

    申请号：US14278468

    申请日：2014-05-15

    申请人： Angela Wandinger-Ness ,  Larry Sklar ,  Jacob Agola ,  Zurab Surviladze ,  Jeffrey Aube ,  Jennifer Golden ,  Chad E. Schroeder ,  Denise S. Simpson

    发明人： Angela Wandinger-Ness ,  Larry Sklar ,  Jacob Agola ,  Zurab Surviladze ,  Jeffrey Aube ,  Jennifer Golden ,  Chad E. Schroeder ,  Denise S. Simpson

    IPC分类号： C07D495/04 ,  A61K45/06 ,  A61K31/381

    CPC分类号： C07D495/04 ,  A61K31/381 ,  A61K45/06

    摘要： This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.

    摘要翻译： 本发明涉及化合物及其作为Rab7 GTPase的抑制剂或活化剂的用途，用于治疗或预防Rab 7 GTP酶相关疾病如神经病变，癌症，骨骼和脂质储存代谢疾病的发生。 本发明也适用于Rab7灭活或其蛋白质 - 蛋白质相互作用被调节以促进病原体的细胞内存活的感染性疾病。 所描述的化合物作为核苷酸结合的竞争性抑制剂，因此也可用作靶向其他小GTP酶的支架。 一方面，本发明的治疗方法用于治疗或预防遗传性感觉神经病发作，例如Charcot-Marie-Tooth 2B型疾病。 还提供了相关的药物组合物，测定和药物筛选。

    Rab7 GTPase inhibitors and related methods of treatment
    2.
    发明授权
    Rab7 GTPase inhibitors and related methods of treatment 有权
    Rab7 GTPase抑制剂及相关治疗方法

    公开(公告)号：US08765803B1

    公开(公告)日：2014-07-01

    申请号：US13404921

    申请日：2012-02-24

    申请人： Angela Wandinger-Ness ,  Larry Sklar ,  Jacob Agola ,  Zurab Surviladze ,  Jeffrey Aubé ,  Jennifer Golden ,  Chad E. Schroeder ,  Denise S. Simpson

    发明人： Angela Wandinger-Ness ,  Larry Sklar ,  Jacob Agola ,  Zurab Surviladze ,  Jeffrey Aubé ,  Jennifer Golden ,  Chad E. Schroeder ,  Denise S. Simpson

    IPC分类号： A01N43/10 ,  A01N43/16

    CPC分类号： C07D495/04 ,  A61K31/381 ,  A61K45/06

    摘要： This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.

    摘要翻译： 本发明涉及化合物及其作为Rab7 GTPase的抑制剂或活化剂的用途，用于治疗或预防Rab 7 GTP酶相关疾病如神经病变，癌症，骨骼和脂质储存代谢疾病的发生。 本发明也适用于Rab7灭活或其蛋白质 - 蛋白质相互作用被调节以促进病原体的细胞内存活的感染性疾病。 所描述的化合物作为核苷酸结合的竞争性抑制剂，因此也可用作靶向其他小GTP酶的支架。 一方面，本发明的治疗方法用于治疗或预防遗传性感觉神经病发作，例如Charcot-Marie-Tooth 2B型疾病。 还提供了相关的药物组合物，测定和药物筛选。

    Modulators of GTPases and their use
    3.
    发明授权
    Modulators of GTPases and their use 有权
    GTPases的调制器及其用途

    公开(公告)号：US09125899B1

    公开(公告)日：2015-09-08

    申请号：US13161766

    申请日：2011-06-16

    申请人： Angela-Wandinger Ness ,  Laurie Hudson ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea

    发明人： Angela-Wandinger Ness ,  Laurie Hudson ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea

    IPC分类号： A61K31/403

    CPC分类号： A61K31/407 ,  A61K31/403 ,  A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/573 ,  Y02A50/473 ,  Y02A50/486 ,  A61K2300/00

    摘要： The present invention relates to molecules which function as modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases (e.g. Rac, Cdc42 and Rho GTPases) and their use to treat diseases, including cancers (including solid tumors-medulloblastoma, ovarian, breast, head and neck, testicular, prostate among others and hematologic malignancies-B cell lymphoma, where these GTPases are overexpressed or hyperactivated), sporadic and genetic diseases where activation of Rho GTPases plays a pivotal role (Menkes disease, rheumatoid arthritis, atherosclerosis, diabetes (type 1), Huntington's disease and Alzheimer's disease) which are mediated through these proteins. Compounds according to the present invention may also be used as a therapy for the treatment of Entamoeba spp. or Acanthamoeba spp, infections, especially including Entamoeba histolytica.

    摘要翻译： 本发明涉及用作小GTP酶（例如Rac，Cdc42和Rho GTP酶）的Ras同源（Rho）家族的调节剂（即抑制剂和激动剂）的分子及其用于治疗疾病的用途，包括癌症（包括固体 肿瘤 - 成神经管细胞瘤，卵巢癌，乳腺癌，头颈部，睾丸癌，前列腺癌和血液恶性肿瘤--B细胞淋巴瘤，其中这些GTP酶过度表达或过度活化），其中Rho GTP酶的活化起关键作用的散发性和遗传性疾病（Menkes disease ，类风湿性关节炎，动脉粥样硬化，糖尿病（1型），亨廷顿氏病和阿尔茨海默氏病）。 根据本发明的化合物也可以用作治疗阿米巴疫霉的疗法。 或Acanthamoeba spp，感染，特别是包括溶组织内阿米巴（Entamoeba histolytica）。