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    NOVEL PALLADIUM COMPLEXES INHIBIT N-MYRISTOYLTRANSFERASE ACTIVITY IN VITRO AND CANCER GROWTH IN VIVO
    2.
    发明申请
    NOVEL PALLADIUM COMPLEXES INHIBIT N-MYRISTOYLTRANSFERASE ACTIVITY IN VITRO AND CANCER GROWTH IN VIVO 有权
    新型PADADIUM复合物抑制VIVO中的N-MYRISTOYLTRANSFERASE活性和VIVO中的癌症生长

    公开(公告)号：US20100076076A1

    公开(公告)日：2010-03-25

    申请号：US12470008

    申请日：2009-05-21

    Applicant: Jack Arbiser

    Inventor： Jack Arbiser

    IPC: A61K31/28 ,  A61P35/00 ,  A61P17/00 ,  A61P31/18

    CPC classification number: A61K31/28 ,  C07F15/0066

    Abstract: Melanoma is a solid tumor that is notoriously resistant to chemotherapy, and its incidence is rapidly increasing. Recently, several signaling pathways have been demonstrated to contribute to melanoma tumorigenesis, including constitutive activation of MAP kinase, Akt and stat-3. The activation of multiple pathways may account in part for the difficulty in treatment of melanoma. In a recent screen of compounds, we found that an organopalladium complex showed significant antiproliferative activity against melanoma cells. This complex, tris(dibenzylideneacetone)dipalladium (Tris DBA), has activity against B16 murine and A375 human melanoma in vivo. Tris DBA inhibits several signaling pathways including activation of MAP kinase, Akt, stat-3 and S6 kinase activation. Tris(dibenzylideneacetone)dipalladium is thus a novel compound that is a member of a class of noble metal complexes with potential antitumor activity. Further preclinical evaluation of TrisDBA and related complexes is warranted.

    Abstract translation: 黑色素瘤是一种对化学药物具有抗性的实体肿瘤，其发病率正在迅速增加。 最近，已经证明几种信号通路有助于黑素瘤肿瘤发生，包括MAP激酶，Akt和stat-3的组成型激活。 多种途径的激活可能部分归因于黑色素瘤的治疗难度。 在最近的化合物屏幕中，我们发现有机钯配合物显示出对黑素瘤细胞的显着的抗增殖活性。 这种复合的三（二亚苄基丙酮）二钯（Tris DBA）在体内具有抗B16鼠和A375人黑素瘤的活性。 Tris DBA抑制几种信号通路，包括MAP激酶，Akt，stat-3和S6激酶激活的激活。 因此，三（二亚苄基丙酮）二钯是具有潜在抗肿瘤活性的一类贵金属络合物的成员的新型化合物。 TrisDBA和相关复合物的进一步临床前评估是有必要的。

    Methods and kits for detecting proteins
    4.
    发明申请
    Methods and kits for detecting proteins 审中-公开
    用于检测蛋白质的方法和试剂盒

    公开(公告)号：US20050095657A1

    公开(公告)日：2005-05-05

    申请号：US10945684

    申请日：2004-09-21

    Applicant: Jack Arbiser ,  Cynthia Cohen

    Inventor： Jack Arbiser ,  Cynthia Cohen

    IPC: C12Q1/48 ,  G01N33/574 ,  G01N33/53 ,  G01N33/537 ,  G01N33/543

    CPC classification number: G01N33/57484 ,  C12Q1/485

    Abstract: Briefly described, methods of detecting a phosphorylated mitogen activated protein kinase (P-MAPK), methods of diagnosing cancer, kits for detecting P-MAPK, and kits for diagnosing cancer, are disclosed. One exemplary kit, among others, includes a composition including an antibody that bonds to a phosphorylated mitogen activated protein kinase (P-MAPK) or a variant thereof to form a detectable complex; and a set of printed instructions specifying, in order of implementation, steps to be followed for detecting the P-MAPK or a variant thereof by detecting the complex. The composition and the printed instructions are in packaged combination.

    Abstract translation: 公开了一种检测磷酸化有丝分裂原活化蛋白激酶（P-MAPK）的方法，诊断癌症的方法，用于检测P-MAPK的试剂盒和诊断癌症的试剂盒。 一个示例性试剂盒，其中包括包含与磷酸化有丝分裂原活化蛋白激酶（P-MAPK）或其变体键合以形成可检测复合物的抗体的组合物; 以及一组印刷指令，按照实施的顺序，通过检测复合物来指定检测P-MAPK或其变体的步骤。 组合物和印刷说明书以包装的形式组合。

    Solenopsin a, b and analogs and as novel angiogenesis inhibitors
    5.
    发明申请
    Solenopsin a, b and analogs and as novel angiogenesis inhibitors 有权
    Solenopsin a，b和类似物和新型血管生成抑制剂

    公开(公告)号：US20050038071A1

    公开(公告)日：2005-02-17

    申请号：US10502080

    申请日：2003-01-24

    Applicant: J. Bowen ,  Jack Arbiser ,  David Whitmire ,  M. Furness

    Inventor： J. Bowen ,  Jack Arbiser ,  David Whitmire ,  M. Furness

    IPC: A61K31/445 ,  A61K31/451

    CPC classification number: A61K31/445 ,  A61K31/451

    Abstract: The present invention relates to solenopsin A and its analogs for use as angiogenesis inhibitors. The present compounds unexpectedly exhibit good activity as angiogenesis inhibitors, which find use as antitumor/anticancer agents as well as to treat a number of conditions or disease states in which angiogenesis is a factor.

    Abstract translation: 本发明涉及用于血管生成抑制剂的索伦膦A及其类似物。 本发明化合物意外地表现出作为血管生成抑制剂的良好活性，其可用作抗肿瘤/抗癌剂，以及治疗血管生成是其中一个因素的许多病症或疾病状态。

    Treatment of tuberous sclerosis associated neoplasms
    6.
    发明授权
    Treatment of tuberous sclerosis associated neoplasms 有权
    治疗结节性硬化相关性肿瘤

    公开(公告)号：US08569305B2

    公开(公告)日：2013-10-29

    申请号：US11603747

    申请日：2006-11-22

    Applicant: Jack Arbiser

    Inventor： Jack Arbiser

    IPC: A61K31/497

    CPC classification number: A61K31/505 ,  A61K31/506

    Abstract: The present invention relates to the use of PDGF receptor tyrosine kinase or bcr-abl tyrosine kinase inhibitors, especially of N-phenyl-2-pyrimidine-amine derivatives of formula I, in which the symbols and substituents have the meaning as defined herein in free form or in pharmaceutically acceptable salt form, in the manufacture of a pharmaceutical composition for the treatment of tuberous sclerosis associated neoplasms; to a method of treatment of warm-blooded animals, including humans, suffering from a tuberous sclerosis associated neoplasms.

    Abstract translation: 本发明涉及PDGF受体酪氨酸激酶或bcr-abl酪氨酸激酶抑制剂，特别是式I的N-苯基-2-嘧啶 - 胺衍生物的用途，其中符号和取代基具有如本文所定义的含义， 形式或药学上可接受的盐形式，用于制备用于治疗结节性硬化相关赘生物的药物组合物; 涉及一种治疗患有结节性硬化症相关肿瘤的温血动物，包括人类的方法。

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