公开(公告)号：US08435975B2

公开(公告)日：2013-05-07

申请号：US12733415

申请日：2008-08-14

Applicant: Tilak Raj Bhardwaj ,  Manoj Kumar ,  Neelima Dhingra ,  Neraj Mehta

Inventor： Tilak Raj Bhardwaj ,  Manoj Kumar ,  Neelima Dhingra ,  Neraj Mehta

IPC: A61K31/568 ,  C07J41/00 ,  A61P5/28

CPC classification number: C07J41/0016

Abstract: The present invention relates to steroidal esters of 17-oximino-5-androsten-3-ol, of compound of general formula (A) wherein R is selected from a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from Dehydroandrosterone acetate. The compounds were tested for their antiproliferative activity and 5α-reductase inhibitory activity in comparison to Finasteride. Decreased androgen level have been found in serum of animal treated with newly synthesized compounds. These compounds have also shown better cytotoxicity in comparison to reference drug Finasteride. Thus such compounds can be useful in treatment of androgen dependent disorder of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferative activity.

Abstract translation: 本发明涉及通式（A）化合物，其中R选自芳烷基，芳基，取代芳基的17-肟基-5-雄甾-3-醇类甾体酯。 酯衍生物是从乙酸脱氢睾酮开始合成的。 与非那雄胺相比，测试化合物的抗增殖活性和5α-还原酶抑制活性。 在新合成的化合物处理的动物血清中发现雄激素水平降低。 与参考药物非那雄胺相比，这些化合物也显示出更好的细胞毒性。 因此，这样的化合物可用于治疗前列腺单独的雄激素依赖性病症或通过协同作用，由于它们的抗增殖活性，它们可以减少前列腺的大小。