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8 条记录 (耗时 0.023 秒)

    Synthesis and use of .beta.-lapachone analogs
    1.
    发明授权
    Synthesis and use of .beta.-lapachone analogs 失效
    β-apachone类似物的合成和使用

    公开(公告)号：US5763625A

    公开(公告)日：1998-06-09

    申请号：US428574

    申请日：1995-04-25

    申请人： David A. Boothman ,  Benjamin J. Frydman ,  Donald T. Witiak

    发明人： David A. Boothman ,  Benjamin J. Frydman ,  Donald T. Witiak

    IPC分类号： C07D311/92 ,  C07D311/80

    CPC分类号： C07D311/92

    摘要： 3-Substituted-.beta.-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-.beta.-lapachones, 3-alkyl-.beta.-lapachones and 3-halo-.beta.-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.

    摘要翻译： 公开了3-替代的β-大麻素类似物及其单独使用或增加化学疗法或放射疗法诱导程序性肿瘤细胞死亡而不对周围正常细胞表现出毒性的用途。 特别地，发现3-烯丙基-β-倍他乐，3-烷基-β-脂肪酸和3-卤代-β-脂肪酸是拓扑异构酶（Topo I）抑制剂。 当单独使用这些类似物时，在一些细胞中引起细胞凋亡和细胞死亡的肿瘤细胞的DNA中存在可逆的单链断裂。 然而，当这些类似物与化学疗法或X射线照射组合时，实现了不可逆的Topo I介导的断裂。 还公开了化合物的新的和更有效的化学合成。

    Conformationally restricted polyamines
    3.
    发明授权
    Conformationally restricted polyamines 失效
    构象限制多胺

    公开(公告)号：US06392098B1

    公开(公告)日：2002-05-21

    申请号：US09280278

    申请日：1999-03-29

    申请人： Benjamin J. Frydman ,  Laurence J. Marton ,  Venodhar K. Reddy ,  Aldonia L. Valasinas ,  Donald T. Witiak

    发明人： Benjamin J. Frydman ,  Laurence J. Marton ,  Venodhar K. Reddy ,  Aldonia L. Valasinas ,  Donald T. Witiak

    IPC分类号： A61K3113

    CPC分类号： C07C211/18 ,  C07C211/22 ,  C07C211/36 ,  C07C2601/02 ,  C07C2601/04

    摘要： Compounds of Formula I: E—NH—D—NH—B—A—B—NH—D—NH—E  (I) wherein A is C2-C6 alkene, C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C1-C6 alkyl alkenyl; D is independently C1-C6 alkyl or alkenyl, or C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C3-C6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.

    摘要翻译： 式I化合物：其中A是C 2 -C 6烯烃，C 3 -C 6环烷基，环烯基或环芳基; B独立地是单键，C1-C6烷基烯基; D独立地为C 1 -C 6烷基或链烯基，或C 3 -C 6环烷基，环烯基或环芳基; 且E独立地为H，C 3 -C 6烷基或链烯基; 及其药学上合适的盐; 公开了其合成方法，含有这些化合物中的一种以上的药物剂型，以及这些化合物在治疗肿瘤细胞生长中的用途。

    Inhibition of cancer cell growth, proliferation, and metastasis using N,N'-d.alpha.,.omega.-diaminoalkanes
    8.
    发明授权
    Inhibition of cancer cell growth, proliferation, and metastasis using N,N'-d.alpha.,.omega.-diaminoalkanes 失效
    使用N，N'-二苄基-α，ω-二氨基烷烃抑制癌细胞生长，增殖和转移

    公开(公告)号：US5677350A

    公开(公告)日：1997-10-14

    申请号：US472431

    申请日：1995-06-07

    申请人： Benjamin J. Frydman

    发明人： Benjamin J. Frydman

    IPC分类号： A61K31/137 ,  A61K31/13 ,  A61K31/135

    CPC分类号： A61K31/137

    摘要： The present invention relates to the inhibition of cancer cell growth, proliferation, and metastasis by contacting cells with an N,N'-dibenzyl .alpha.,.omega.-diaminoalkane, a derivative of naturally-occurring putrescine. More specifically, the present invention relates to the treatment of cancer in humans by administration of a cancer cell growth-inhibiting amount of an N,N'-dibenzyl .alpha.,.omega.-diaminoalkane to a human cancer patient.

    摘要翻译： 本发明涉及通过使细胞与N，N'-二苄基α，ω-二氨基烷烃（天然存在的腐胺衍生物）接触来抑制癌细胞生长，增殖和转移。 更具体地说，本发明涉及通过向人类癌症患者施用癌细胞生长抑制量的N，N'-二苄基α，ω-二氨基烷烃来治疗人类的癌症。