会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 81. 发明授权
    • Methods for treatment of tumors
    • 肿瘤治疗方法
    • US4932934A
    • 1990-06-12
    • US236603
    • 1988-08-24
    • Thomas J. DoughertyWilliam R. PotterKenneth R. Weishaupt
    • Thomas J. DoughertyWilliam R. PotterKenneth R. Weishaupt
    • A61B5/00A61K31/40A61K41/00A61K49/00A61K51/00A61N5/06A61P35/00A61P43/00C07D487/22C07D519/00C09B47/00G02B6/04G02B6/26G02B6/42
    • A61K31/40A61B5/411A61B5/416A61K41/0071A61N5/0601A61N5/062C07D519/00G02B6/262G02B6/4204A61B5/0071A61B5/0084G02B6/4298Y10S607/901
    • To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs: (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 percent remain self aggregated in serum protein; and (3) are lipophillic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4. Neoplastic tissue retains the drug after it has cleared normal tissues and illumination results in necrosis. Moreover, other photosensitizing materials may be combined with a carrier that enters undesirable tissues and cells of the reticular endothelial system such as macrophages. These photosensitizing materials: (1) must have a triplet energy state above 3.5 kilocalories per mole; (2) cannot be easily oxidized; and (3) not physically quench any required energy state. Preferably, this photosensitizing material should be lipophilic.
    • 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物:(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接 到另一组,并具有高于每摩尔37.5千卡的三线态能量状态; (2)可溶于水,与血清蛋白质相比,在水中形成了超过10,000分子量的聚集体,并且与血清蛋白质具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂肪性的并且能够分解并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。 肿瘤组织清除正常组织后保留药物,照明会导致坏死。 此外,其它光敏材料可以与进入网状内皮系统的不希望的组织和细胞如巨噬细胞的载体组合。 这些光敏材料:(1)必须具有每千克3.5千卡以上的三线态能量状态; (2)不易氧化; 和(3)不能物理地淬灭任何所需的能量状态。 优选地,该光敏材料应该是亲脂的。