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Invention Publication
CN101921164A (-)-β-榄香烯、(-)-β-榄香醛、(-)-β-榄香醇、(-)-β-氟化榄香烯及其类似物、中间体和组合物的合成及应用 无效 - 撤回

(-)-β-榄香烯、(-)-β-榄香醛、(-)-β-榄香醇、(-)-β-氟化榄香烯及其类似物、中间体和组合物的合成及应用
Abstract:
本发明提供了制备(-)-β-榄香烯、(-)-β-榄香醛、(-)-β-榄香醇、(-)-β-氟化榄香烯及其类似物的完整方法，并且提供了用于制备(-)-β-榄香烯的中间体。本发明进一步提供了基于(-)-β-榄香烯、(-)-β-榄香醛、(-)-β-榄香醇和(-)-β-氟化榄香烯的新颖的组合物，以及治疗癌症的方法，如脑肿瘤、肺癌、乳腺癌、前列腺癌、卵巢癌、结肠直肠癌、胃肠癌和胃癌。发明者提出了针对癌症，尤其是对脑肿瘤、肺癌、卵巢癌、膀胱癌、子宫颈癌、结肠癌、乳腺癌和前列腺癌的联合疗法：(1)一种或多种下列抗癌药剂，包括但并不只限于顺铂、5-FU、紫杉醇、紫杉醇衍生物以及任意抗癌药剂；(2)一种或多种下列(-)-β-榄香烯及其类似物，包括(-)-β-榄香烯、(-)-β-榄香醇、(-)-β-榄香醛、(-)-β-氟化榄香烯及其类似物，以及(-)-β-榄香烯化学合成过程中的中间体。
Abstract(English):

The present invention provides convergent processes for preparing (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, and (-)-beta-elemene fluoride and analogues thereof. Also provided are intermediates useful for preparing (-)-beta-elemene. The present invention further provides novel compositions based on analogues of (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride and methods for the treatment of cancer, such as brain tumor, lung cancer, breast cancer, prostate cancer, ovarian cancer, colorectal cancer, gastric intestional cancer, and stomach cancer. The inventors propose a combination therapy using 1) one or more of the following anti-cancer agents: including, but not limited to, Cisplatin, 5-FU, Taxol, Taxol derivatives, and any anti-cancer agent, and 2) one or more of the following (-)-beta-elemene and its analogs, including (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride, and their analogs, and (-)-beta-elemene's intermediate in its chemical synthesis, for the treatment of cancer, especially for the treatment of brain tumor, lung cancer, ovarian cancer, bladder cancer, cervical cancer, colon cancer, breast cancer, and prostate cancer.

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