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1. 发明授权

US5696097A Antineoplastic 5'-diacylglycerylphosphatidyl-2-deoxy-2'-methylenylcytidines and method of making 失效
标题翻译：抗肿瘤性5'-二酰基甘油基磷脂酰基-2-脱氧-2'-亚甲基胞苷及其制备方法
公开(公告)号：US5696097A
公开(公告)日：1997-12-09
申请号：US525606
申请日：1995-09-15
申请人： Akira Matsuda , Takuma Sasaki , Satoshi Shutou , Akihiro Fujii , Takashi Ono , Shinji Sakata , Takanori Miyashita
发明人： Akira Matsuda , Takuma Sasaki , Satoshi Shutou , Akihiro Fujii , Takashi Ono , Shinji Sakata , Takanori Miyashita
IPC分类号： C07H19/10 , A61K31/70 , C07H19/207
CPC分类号： C07H19/10
摘要： Novel 2'-methylidenenucleotide compounds of the formula (I) ##STR1## wherein R is a hydrogen or a halogen, R.sup.1 and R.sup.2 are the same or different and each is a fatty acid residue or a hydrocarbon residue, and R.sup.3 and R.sup.4 are the same or different and each is a hydrogen, a halogen or an alkyl; salts thereof; methods for production thereof; and pharmaceutical use thereof. The compounds and salts thereof show an excellent antitumor effect in mammals. More specifically, they show a remarkable activity of inhibiting growth of mouse tumors, cultured human tumor cells, and human tumors transplanted to nude mice, and are useful for the treatment and prevention of recurrence of lung cancer, gastrointestinal cancer, breast cancer, cervical cancer, gynecological cancer, urinological cancer, leukemia, melanoma, lymphogenous metastatic tumor and the like in mammals. They are also useful as antitumor agents since they have an increased bioavailability and low toxicity. In addition, they have the effects of maintaining and enhancing their activities.
摘要翻译： PCT No.PCT / JP94 / 00427 Sec。 371 1995年9月15日第 102（e）日期1995年9月15日PCT 1994年3月16日PCT公布。第WO94 / 21659号公报日期1994年9月29日新颖的式（I）的2'-亚甲基二核苷酸化合物其中R是氢或卤素，R 1和R 2相同或不同，各自为脂肪酸残基或烃残基，R 3和R 4相同或不同，各自为氢，卤素或烷基; 的盐; 生产方法; 及其药物用途。其化合物和盐在哺乳动物中表现出优异的抗肿瘤效果。更具体地说，它们显示了抑制小鼠肿瘤，培养的人肿瘤细胞和移植到裸鼠的人肿瘤生长的显着活性，并且可用于治疗和预防肺癌，胃肠癌，乳腺癌，宫颈癌的复发，妇科癌症，尿毒症，白血病，黑素瘤，淋巴瘤转移瘤等。它们也可用作抗肿瘤剂，因为它们具有增加的生物利用度和低毒性。此外，它们还具有维护和增强活动的效果。

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