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    • 5. 发明授权
    • Anti-cancer activity of carvedilol and its isomers
    • 卡维地洛及其异构体的抗癌活性
    • US06632832B1
    • 2003-10-14
    • US10238992
    • 2002-09-10
    • Anand C. BurmanRama MukherjeeManu JaggiAnu T. Singh
    • Anand C. BurmanRama MukherjeeManu JaggiAnu T. Singh
    • A61K3140
    • A61K31/403A61K31/00Y10S436/813Y10S514/908
    • The present invention provides for pharmaceutical compositions comprising carvedilol for treatment of cancer. More particularly the invention relates to the use of carvedilol for treatment of cancers of the colon, ovary, breast, prostate, pancreas, lung, melanoma, glioblastoma, oral cancer and leukemias. Although not bound to any theory, the anticancer activity of carvedilol appears to be attributed to the inhibition of Epidermal Growth Factor and Platelet derived growth factor dependent proliferation of cancer cells. Further, carvedilol exerts anticancer effect by inhibition of the Protein kinase C (PKC) activity and that of the cyclooxygenase 2 enzyme. The invention also relates to the anticancer activity of the optically pure isomers S(−) and R(+) of carvedilol and the use of carvedilol and its isomers in pharmaceutical compositions for the treatment of cancer.
    • 本发明提供包含用于治疗癌症的卡维地洛的药物组合物。 更具体地,本发明涉及卡维地洛用于治疗结肠,卵巢,乳腺,前列腺,胰腺,肺,黑素瘤,成胶质细胞瘤,口腔癌和白血病的癌症的用途。 虽然不受任何理论的约束,卡维地洛的抗癌活性似乎归因于表皮生长因子和血小板衍生生长因子依赖性增殖的癌细胞的抑制。 此外,卡维地洛通过抑制蛋白激酶C(PKC)活性和环加氧酶2酶的活性而发挥抗癌作用。 本发明还涉及卡维地洛的光学纯异构体S( - )和R(+)的抗癌活性以及用于治疗癌症的药物组合物中卡维地洛及其异构体的用途。