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    Micelles for the solubilization of gossypol
    71.
    发明授权
    Micelles for the solubilization of gossypol 有权
    胶体溶解棉酚

    公开(公告)号：US08945627B2

    公开(公告)日：2015-02-03

    申请号：US13464737

    申请日：2012-05-04

    Applicant: Glen S. Kwon ,  Ho-Chul Shin ,  Hyunah Cho

    Inventor： Glen S. Kwon ,  Ho-Chul Shin ,  Hyunah Cho

    IPC: A61K9/14 ,  A61K31/11 ,  A01N43/42 ,  A61K31/33 ,  A61K47/02 ,  A61K9/00 ,  A61K9/107 ,  A61K47/10 ,  A61K9/12

    CPC classification number: A61K47/02 ,  A61K9/0019 ,  A61K9/1075 ,  A61K9/12 ,  A61K47/10 ,  Y02A50/411 ,  Y10S977/788 ,  Y10S977/906

    Abstract: The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.

    Abstract translation: 本发明提供了装载有一种或多种活性剂的生物相容性胶束。 胶束可以包封抗肿瘤药物如棉酚，以及药物如棉酚和紫杉醇，棉酚和17-AAG，棉酚和环巴胺，棉酚，紫杉醇和17-AAG以及棉酚，紫杉醇和环巴胺的组合。 胶束组合物提供难以溶解药物组合的有效溶解，而不需要对患者有毒性的另外的表面活性剂。 因此，本发明提供稳定和生物相容的药物制剂，其改善生物利用度而不引起毒性。

    Therapeutic uses of steroidal compounds
    75.
    发明授权
    Therapeutic uses of steroidal compounds 有权
    甾体化合物的治疗用途

    公开(公告)号：US08846652B2

    公开(公告)日：2014-09-30

    申请号：US12094079

    申请日：2006-11-17

    Applicant: Ernst Wulfert ,  James Robert Murray ,  David Wynick

    Inventor： Ernst Wulfert ,  James Robert Murray ,  David Wynick

    IPC: A01N43/00 ,  A61K31/33 ,  A61K31/56 ,  A61K31/568 ,  A61K31/573

    CPC classification number: A61K31/568 ,  A61K31/573

    Abstract: A steroid derivative compound of formula (I) in which: one of R1 and R2 is hydroxy and the other is hydrogen; or R1 and R2 together represent oxo; R3 is hydrogen or hydroxy; and the dotted lines represent single or double carbon-carbon bonds; and pharmaceutically acceptable salts and esters thereof are useful for the prevention or treatment of pain, for improving nerve regeneration after nerve injury or damage or disease, for the prevention or treatment of brain injury, damage or disease and for neuroprotection. Particularly useful compounds are 11-hydroxy-Δ4-androstene-3,17-dione and 11-oxo-Δ4-androstene-3,17-dione or their derivatives.

    Abstract translation: 式（I）的类固醇衍生物化合物，其中：R 1和R 2之一是羟基，另一个是氢; 或者R 1和R 2一起代表氧代; R3是氢或羟基; 虚线表示单碳双键; 和其药学上可接受的盐和酯可用于预防或治疗疼痛，用于改善神经损伤或损伤或疾病之后的神经再生，用于预防或治疗脑损伤，损伤或疾病以及用于神经保护。 特别有用的化合物是11-羟基 - 丁基-4-雄甾烯-3,17-二酮和11-氧代-D-四雄甾烯-3,17-二酮或其衍生物。

    Camptothecin derivatives as chemoradiosensitizing agents
    77.
    发明授权
    Camptothecin derivatives as chemoradiosensitizing agents 有权
    喜树碱衍生物作为化学放射增敏剂

    公开(公告)号：US08779138B2

    公开(公告)日：2014-07-15

    申请号：US13012772

    申请日：2011-01-24

    Applicant: Li-Xi Yang

    Inventor： Li-Xi Yang

    IPC: C07D471/00 ,  A61K31/33

    CPC classification number: C07D491/22 ,  A61K45/06

    Abstract: Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.

    Abstract translation: 喜树碱类化合物可用于治疗哺乳动物受试者的肿瘤，其通过与受试者联合放射治疗，即用放射性物质治疗肿瘤或从受试者外部的来源辐射来治疗肿瘤。 通过在喜树碱结构周围定位至少一个电子亲和基团来改善喜树碱类化合物，以增强其与放射治疗相结合的价值。 公开了新的喜树碱类化合物，其可用于通过单独施用新化合物或与放射治疗组合来治疗癌症。

    METHODS AND COMPOSITIONS FOR INHIBITING INTEGRINS USING TELLURIUM-CONTAINING COMPOUNDS
    79.
    发明申请
    METHODS AND COMPOSITIONS FOR INHIBITING INTEGRINS USING TELLURIUM-CONTAINING COMPOUNDS 审中-公开
    使用含有含碲化合物抑制整合剂的方法和组合物

    公开(公告)号：US20140194496A1

    公开(公告)日：2014-07-10

    申请号：US14208104

    申请日：2014-03-13

    Applicant: BIOMAS LTD.

    Inventor： Benjamin SREDNI ,  Michael ALBECK

    IPC: C07D517/22 ,  A61K45/06 ,  A61K31/33 ,  C07D329/00

    CPC classification number: C07D517/22 ,  A61K31/095 ,  A61K31/33 ,  A61K31/555 ,  A61K45/06 ,  C07D329/00 ,  Y02A50/393

    Abstract: Methods and compositions for inhibiting integrin and treating integrin-related conditions, utilizing tellurium-containing compounds, are disclosed. The tellurium-containing compounds comprise at least one tellurium dioxo moiety and may have any one of Formulae I to IV as defined in the specification. Further disclosed are methods and compositions for treating a neoplastic condition characterized by a resistance to an anti-neoplastic agent and by a high level of expression of an integrin by neoplastic cells.

    Abstract translation: 公开了使用含碲化合物抑制整联蛋白和治疗整联蛋白相关病症的方法和组合物。 含碲化合物包含至少一个碲二氧代部分，并且可以具有本说明书中定义的任何一种式I至IV。 进一步公开的是用于治疗以抗肿瘤剂的抗性为特征的肿瘤状态的方法和组合物，以及通过肿瘤细胞的整合素的高水平表达。

    Anti-cancer compositions and methods
    80.
    发明授权
    Anti-cancer compositions and methods 有权
    抗癌成分和方法

    公开(公告)号：US08772274B1

    公开(公告)日：2014-07-08

    申请号：US13659501

    申请日：2012-10-24

    Applicant: The Penn State Research Foundation

    Inventor： Gavin P. Robertson ,  Subbarao V. Madhunapantula ,  Shantu Amin ,  Dhimant Desai

    IPC: A01N43/00 ,  A61K31/33 ,  A01N31/00 ,  A61K31/095 ,  C07C391/00 ,  C07C395/00 ,  A61K31/155 ,  A61K8/23

    CPC classification number: C07C391/00 ,  A61K8/23 ,  A61K31/095 ,  A61K31/155 ,  A61K31/33

    Abstract: Anti-cancer compositions and methods are described including one or more compounds having the structural formula I: R2-R—R1, where R is phenyl, where R1 is (CH2)n—Se—C(═NH)—NH2, where R2 is (CH2)n—Se—C(═NH)—NH2 or R2 is H, and where each n is independently 2, 3, 4, 5, 6, 7, or 8. Methods of treating a subject are provided according to embodiments of the present invention which include administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject having a condition characterized by Akt dysregulation. Administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject detectably increases apoptosis and/or decreases proliferation of cancer cells, particularly cancer cells characterized by Akt dysregulation. Compositions of the present invention inhibit Akt enzymes, iNOS, and increase MAP kinase activity such that cancer cells contacted with the compositions are inhibited.

    Abstract translation: 描述了抗癌组合物和方法，其包括一种或多种具有结构式I的化合物：其中R是苯基，其中R1是（CH2）n-Se-C（= NHN）-NH2，其中R2 是（CH2）n-Se-C（= NH）-NH2或R2是H，并且其中每个n独立地是2,3,4,5,6,7或8.治疗受试者的方法根据 本发明的实施方案包括将具有结构式I的治疗有效量的包含一种或多种具有结构式I的化合物的组合物施用于具有由Akt调节异常表征的病症的受试者。 向受试者施用治疗有效量的包含一种或多种具有结构式I的化合物的组合物可检测地增加癌细胞，特别是Akt失调特征的癌细胞的凋亡和/或降低增殖。 本发明的组合物抑制Akt酶，iNOS，并且增加MAP激酶活性，使得与组合物接触的癌细胞被抑制。

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