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109 条记录 (耗时 0.024 秒)

    Anti-cancer compositions and methods
    6.
    发明授权
    Anti-cancer compositions and methods 有权
    抗癌成分和方法

    公开(公告)号：US08309541B1

    公开(公告)日：2012-11-13

    申请号：US13107494

    申请日：2011-05-13

    申请人： Gavin P. Robertson ,  SubbRao V. Madhunapantula ,  Shantu Amin ,  Dhimant Desai

    发明人： Gavin P. Robertson ,  SubbRao V. Madhunapantula ,  Shantu Amin ,  Dhimant Desai

    IPC分类号： A01N43/00 ,  A01N31/00 ,  A61K31/33 ,  A61K31/095 ,  C07C391/00 ,  C07C395/00

    CPC分类号： C07C391/00 ,  A61K8/23 ,  A61K31/095 ,  A61K31/155 ,  A61K31/33

    摘要： 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)nSe—C(═NH)—NH2, where R2 is (CH2)nSe—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.

    摘要翻译： 描述了抗癌组合物和方法，包括一种或多种具有结构式I的化合物：R2-R-R1，其中R是苯基，其中R1是（CH2）nSe-C（= NHN）-NH2，其中R2是（ CH2）nSe-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.根据本发明的实施方案提供了治疗受试者的方法 其包括将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。

    Multi-substituted selective androgen receptor modulators and methods of use thereof
    9.
    发明申请
    Multi-substituted selective androgen receptor modulators and methods of use thereof 有权
    多取代的选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US20060183931A1

    公开(公告)日：2006-08-17

    申请号：US10371155

    申请日：2003-02-24

    申请人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka ,  Dong Hwang ,  Jiyun Chen

    发明人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka ,  Dong Hwang ,  Jiyun Chen

    IPC分类号： C07F9/02 ,  C07F7/22 ,  C07C395/00 ,  C07C255/60 ,  C07C237/10

    CPC分类号： C07C235/24

    摘要： This invention provides androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer

    摘要翻译： 本发明提供雄激素受体靶向剂（ARTA）。 这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。 已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。 已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血， 肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌 癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; 和/或g）降低前列腺癌的发生率，停止或导致消退

    Process for the production of living radical polymers and polymers
    10.
    发明申请
    Process for the production of living radical polymers and polymers 审中-公开
    生产活性自由基聚合物和聚合物的方法

    公开(公告)号：US20060135711A1

    公开(公告)日：2006-06-22

    申请号：US10545310

    申请日：2004-02-17

    申请人： Shigeru Yamago ,  Junichi Yoshida ,  Takashi Kameshima

    发明人： Shigeru Yamago ,  Junichi Yoshida ,  Takashi Kameshima

    IPC分类号： C07C395/00 ,  C08F4/00

    CPC分类号： C07C395/00 ,  C08F4/04 ,  C08F4/42

    摘要： A process for producing a living radical polymer characterized in that a vinyl monomer is polymerized with use of an organotellurium compound represented by the formula (1) and an azo type polymerization initiator, and the living radical polymer obtainable by the process wherein R1 is C1-C8 alkyl, aryl, substituted aryl or an aromatic heterocyclic group, R2 and R3 are each a hydrogen atom or C1-C8 alkyl, and R4 is aryl, substituted aryl, an aromatic heterocyclic group, acyl, oxycarbonyl or cyano.

    摘要翻译： 一种活性自由基聚合物的制造方法，其特征在于，使用由式（1）表示的有机碲化合物和偶氮型聚合引发剂使乙烯基单体聚合，得到的活性自由基聚合物，其中R 1是C 1 -C 8烷基，芳基，取代的芳基或芳族杂环基，R 2和R 2 > 3个各自为氢原子或C 1 -C 8烷基，R 4为芳基，取代的芳基， 芳族杂环基，酰基，氧羰基或氰基。