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    Modulators of GTPase and Use In Relevant Treatment
    2.
    发明申请
    Modulators of GTPase and Use In Relevant Treatment 有权
    GTPase调节剂和相关治疗用途

    公开(公告)号：US20130345277A1

    公开(公告)日：2013-12-26

    申请号：US13867658

    申请日：2013-04-22

    Applicant: STC.UNM ,  Kansas University Center for Technology Commercialization, Inc.

    Inventor： Angela Wandinger-Ness ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea ,  Laurie Hudson ,  Jeffrey Aube ,  Jennifer E. Golden ,  Chad E. Schroeder ,  Denise S. Simpson ,  Julica J. Noth

    IPC: A61K31/415 ,  A61K45/06 ,  C07D231/06

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

    Abstract: The present invention relates to molecules which function as selective modulators of the Ras-homologous (Rho) family of small GTPases, in particular, Cdc42 GTPase and their use to treat diseases, for example cancers, including metastatic cancer, genetic and acquired diseases where activation of Cdc42 GTPase plays a pivotal role, such as neurodegenerative diseases, rheumatoid arthritis, atherosclerosis, diabetes type I, autosomal polycystic kidney disease, cystic kidney disease, precystic kidney disease, microbial infections, including Chlamydia infections, E. coli infections, H. pylori infections and its secondary effects including gastric ulcers, Coxiella Brunetti (Q-fever) infections and Streptococcus pneumonia infections, fungal infections including Paracoccidiodes brasiliensis and Candida albicans and their secondary effects including lung edema. Additionally, compounds according to the present invention may be used to inhibit rejection in transplant patients (pursuant to transplantation), to promote immunosuppression, anti-inflammatory response and to mobilize stem cell (migration) in patients in need, among others.

    Abstract translation: 本发明涉及用作小GTP酶的Ras同源（Rho）家族，特别是Cdc42GTP酶的选择性调节剂的分子及其用于治疗疾病的用途，例如癌症，包括转移性癌症，遗传和获得性疾病，其中激活 的Cdc42 GTPase起着关键的作用，如神经退行性疾病，类风湿关节炎，动脉粥样硬化，I型糖尿病，常染色体多囊肾病，囊性肾病，前期肾脏疾病，微生物感染，包括衣原体感染，大肠杆菌感染，幽门螺杆菌 感染及其次要作用包括胃溃疡，布氏梭菌（Qex fever）感染和肺炎链球菌感染，包括巴西隐孢子虫和白色念珠菌在内的真菌感染及其副作用，包括肺水肿。 此外，根据本发明的化合物可以用于抑制移植患者的排斥（根据移植），以促进免疫抑制，抗炎反应和在需要的患者中调动干细胞（迁移）等。

    ARSENIC-BASED TREATMENT OF CANCERS AND INFLAMMATORY DISORDERS
    3.
    发明申请
    ARSENIC-BASED TREATMENT OF CANCERS AND INFLAMMATORY DISORDERS 审中-公开
    基于ARSENIC的癌症治疗和炎症性疾病

    公开(公告)号：US20160184356A1

    公开(公告)日：2016-06-30

    申请号：US14776929

    申请日：2014-03-14

    Applicant: Ke Jian Jim LIU ,  Laurie HUDSON ,  Karen COOPER ,  Xixi ZHOU ,  STC.UNM

    Inventor： Ke Jian Jim Liu ,  Laurie Hudson ,  Karen Cooper ,  Xixi Zhou

    IPC: A61K33/36 ,  A61K45/06 ,  A61K41/00

    CPC classification number: A61K33/36 ,  A61K31/166 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/454 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/55 ,  A61K31/555 ,  A61K31/7068 ,  A61K41/0038 ,  A61K45/06 ,  A61N2005/1098 ,  A61K2300/00

    Abstract: In one embodiment, the invention provides a method of treating a subject who suffers from a cancer (particularly a chemotherapeutic or radiotherapeutic-resistant cancer) or from an inflammatory disorder, the method comprising co-administering to the subject a pharmaceutically-effective amount of: (a) one or more elements or compounds selected from the group consisting of arsenic, an arsenite and arsenic trioxide (ATO); and optionally (b) at least one anticancer agent (preferably a DNA damaging agent); and/or (c) at least one or more Poly(ADP-ribose) polymerase (PARP) inhibitors other than arsenic, an arsenite and arsenic trioxide (ATO). In preferred embodiments, the arsenic for the treatment of cancer, arsenite and ATO serve as radio sensitizers for concomitant radiotherapy as well as PARP inhibitors. Methods for treating inflammatory disease are also disclosed. Related pharmaceutical formulations are also provided.

    Abstract translation: 在一个实施方案中，本发明提供了治疗患有癌症（特别是化学治疗或放射治疗耐药性癌症）或炎症性疾病的受试者的方法，所述方法包括向受试者共同施用药物有效量的： （a）选自砷，亚砷酸钠和三氧化二砷（ATO）中的一种或多种元素或化合物; 和（b）至少一种抗癌剂（优选DNA损伤剂）; 和/或（c）至少一种或多种除砷以外的聚（ADP-核糖）聚合酶（PARP）抑制剂，亚砷酸钠和三氧化二砷（ATO））。 在优选实施方案中，用于治疗癌症，亚砷酸盐和ATO的砷用作伴随放射治疗的放射敏化剂以及PARP抑制剂。 还公开了治疗炎性疾病的方法。 还提供了相关的药物制剂。

    Modulators of GTPases and Their Use
    5.
    发明申请
    Modulators of GTPases and Their Use 审中-公开
    GTPases的调制器及其使用

    公开(公告)号：US20150335619A1

    公开(公告)日：2015-11-26

    申请号：US14813874

    申请日：2015-07-30

    Applicant: STC.UNM

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

    IPC: A61K31/407 ,  A61K45/06

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

    Abstract: 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.

    Abstract translation: 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。 或棘阿米巴属 感染，特别是包括溶组织内阿米巴（Entamoeba histolytica）。

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