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    • 6. 发明申请
    • NOVEL CURCUMIN-ANTIBODY CONJUGATES AS ANTI-CANCER AGENTS
    • 作为抗癌剂的新型CURCUMIN-ANTIBODY缀合物
    • WO2011068894A2
    • 2011-06-09
    • PCT/US2010058588
    • 2010-12-01
    • UNIV CITY NEW YORK RES FOUNDBANERJEE PROBALKRISHNASWAMI RAJA
    • BANERJEE PROBALKRISHNASWAMI RAJA
    • A61K39/395A61K39/44A61K47/48A61P35/00C07D207/40
    • A61K47/48384A61K47/50A61K47/6803A61K47/6849A61K47/6865
    • The invention relates to curcumin derivatives having the formula I: wherein: Z represents: H3CO A represents -CH2-CH2- or -CH=CH-;L represents-C(O)-(NH)n1-R-(NH)n2-C(O)-; R represents a saturated or unsaturated, branched or unbranched hydrocarbyl chain having a minimum of 3 carbon atoms in the chain; wherein the maximum number of carbon atoms in the chain is 24; and wherein the carbon atoms of the chain can be replaced by at least one heteroatom, wherein the heteroatoms are independently -O- or - NH2-, with the proviso that each heteroatom is separated from each other heteroatom by at least two carbon atoms;n1 and n2 independently represent 0 or 1; and Y represents an antibody that binds specifically to a target antigen of a tumor cell. The invention further relates to methods of method of inhibiting the growth of tumors in a human by administering an effective amount of the curcumin derivative, and to methods of producing the curcumin derivative.
    • 本发明涉及具有式I的姜黄素衍生物:其中:Z表示:H 3 CO A表示-CH 2 -CH 2 - 或-CH = CH-; L表示-C(O) - (NH)n1-R-(NH)n2 -C(O) - ; R代表在链中具有最少3个碳原子的饱和或不饱和的支链或非支链烃基链; 其中链中碳原子的最大数目是24; 并且其中所述链的碳原子可以被至少一个杂原子替代,其中所述杂原子独立地为-O-或-NH 2 - ,条件是每个杂原子彼此隔开至少两个碳原子; n 1 和n2独立地表示0或1; Y代表特异性结合肿瘤细胞的靶抗原的抗体。 本发明还涉及通过施用有效量的姜黄素衍生物来抑制人类肿瘤生长的方法,以及生产姜黄素衍生物的方法。
    • 7. 发明申请
    • USE OF CURCUMIN TO BLOCK BRAIN TUMOR FORMATION IN VIVO
    • 莪术素在体内阻断脑肿瘤形成的研究
    • WO2009073050A2
    • 2009-06-11
    • PCT/US2008009053
    • 2008-07-25
    • RES FOUNDATION OF CITY UNIVERSBANERJEE PROBALRAJA KRISHNASWAMI SAMBASIVAN
    • BANERJEE PROBALRAJA KRISHNASWAMI SAMBASIVAN
    • A61K31/12
    • A61K36/9066
    • The présent invention provides compositions and methods of using curcumin or curcumin derivatives or analogs to activate the pro-apoptotic enzymes caspase-3/7 in cancer cells. The présent invention also provides formulations of curcumin or derivatives or analogs with increased solubility or improved bioavailability. The formulations may be administered to a subject such that high concentrations of therapeutically effective curcumin compounds resuit in the subject' s bloodstream. The invention thus involves the use of curcumin or curcumin derivatives or analogs to diminish cancer cell growth, decrease tumor size, prevent tumor formation, and to reduce or prevent cancer or tumor cell invasion or metastasis into a tissue, e.g., into the nervous System and especially the brain, of a subject. The instant invention may be used prophylactically to prevent tumor formation or metastasis, as a monotherapy to treat existing tumors, after surgery to prevent récurrence of tumors or in conjunction with conventional cancer thérapies to improve patient prognosis and reduce side-effects.
    • 本发明提供了使用姜黄素或姜黄素衍生物或类似物来激活癌细胞中的促凋亡酶胱天蛋白酶-3/7的组合物和方法。 本发明还提供具有增加的溶解度或改善的生物利用度的姜黄素或衍生物或类似物的制剂。 该制剂可以施用于受试者,使得高浓度的治疗有效的姜黄素化合物在受试者的血流中结果。 因此,本发明涉及使用姜黄素或姜黄素衍生物或类似物来减少癌细胞生长,减小肿瘤尺寸,防止肿瘤形成,以及减少或预防癌症或肿瘤细胞侵入或转移到组织中,例如进入神经系统和 特别是大脑,一个主题。 本发明可以预防性地用于预防肿瘤形成或转移,作为治疗现有肿瘤的单一疗法,手术后预防肿瘤发生或与常规癌症疗法结合以改善患者预后并减少副作用。