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公开(公告)号：EP1626050B1
公开(公告)日：2009-12-02
申请号：EP04730460.5
申请日：2004-04-30
申请人： East China University of Science and Technology , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Dalian University of Technology
发明人： QIAN, Xuhong , LI, Yonggang , XU, Yufang , DING, Jian , LIN, Liping , MIAO, Zehong , ZHU, Hong , QU, Baoyuan
IPC分类号： C07D495/06 , C07D513/06 , C07D221/14 , A61K31/473 , A61K31/4743 , A61K31/4745 , A61P35/00
CPC分类号： C07D495/06 , C07D221/14 , C07D405/12 , C07D513/06 , C09B57/08 , C09B69/102 , C09B69/109
摘要： The present invention relates to sulfur-containing naphthoylimide derivatives, the preparation and the use thereof. By expanding the conjugate plane of the naphthoylimide with condensed 5- or 6-member aromatic heterocyclic ring and / or introducing a sulfur atom, the antineoplastic activity of the compounds is improved. For inhibition of the proliferation of tumor-cells from different origins, such as lung cancer, carcinoma ventriculi, liver cancer and leucaemia in human beings, the compounds show remarkable effects with clear quantity-effect relationships.
摘要翻译： 含硫萘酰亚胺衍生物及其制备和用途本发明涉及含硫萘酰亚胺衍生物及其制备和用途。 通过用稠合的5-或6-元芳香杂环扩展萘甲酰亚胺的共轭面和/或引入硫原子，可以改善化合物的抗肿瘤活性。 为了抑制来自不同来源的肿瘤细胞的增殖，例如人类的肺癌，胃腔，肝癌和白血病，所述化合物显示出显着的效果，具有明确的量效关系。
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公开(公告)号：EP1626050A1
公开(公告)日：2006-02-15
申请号：EP04730460.5
申请日：2004-04-30
申请人： East China University of Science and Technology , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Dalian University of Technology
发明人： QIAN, Xuhong , LI, Yonggang , XU, Yufang , DING, Jian , LIN, Liping , MIAO, Zehong , ZHU, Hong , QU, Baoyuan
IPC分类号： C07D495/06 , C07D513/06 , C07D221/06 , A61K31/473 , A61K31/4743 , A61K31/4745 , A61P35/00
CPC分类号： C07D495/06 , C07D221/14 , C07D405/12 , C07D513/06 , C09B57/08 , C09B69/102 , C09B69/109
摘要： The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.
摘要翻译： 本发明公开了新型含硫萘二甲酰亚胺衍生物及其制备和用途。 本发明的萘二甲酰亚胺衍生物的共轭平面通过引入5-或6-元杂芳环和/或引入S杂原子而扩大，因此增加了萘二甲酰亚胺的抗肿瘤活性。 本发明的化合物对各种肿瘤细胞如人肺癌，胃癌，肝癌，白血病等的增殖显示出显着的抑制活性。 细胞增殖的抑制是剂量依赖性的。
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公开(公告)号：EP1995249A1
公开(公告)日：2008-11-26
申请号：EP07702109.5
申请日：2007-01-17
发明人： LU, Wei , DING, Jian , GAO, Heyong , LIN, Liping , CHEN, Yi
IPC分类号： C07D491/22 , A61K31/475 , A61P35/00 , C07D221/00 , C07D209/00 , C07D311/00
CPC分类号： C07D491/22
摘要： New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
摘要翻译： 具有以下式（I）结构的新的喜树碱衍生物，它们的用途和含有它们的药物组合物。 本发明化合物具有良好的抗肿瘤活性和在水中的良好溶解性，可用于药物开发。
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公开(公告)号：EP1995249B1
公开(公告)日：2010-11-10
申请号：EP07702109.5
申请日：2007-01-17
发明人： LU, Wei , DING, Jian , GAO, Heyong , LIN, Liping , CHEN, Yi
IPC分类号： C07D491/22 , A61K31/4745 , A61P35/00
CPC分类号： C07D491/22
摘要： New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
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