Steroidal esters of 17-oximino-5-androsten-3beta-ol
    1.
    发明授权
    Steroidal esters of 17-oximino-5-androsten-3beta-ol 有权
    17-肟基-5-雄甾-3β-醇的甾体酯

    公开(公告)号:US08435975B2

    公开(公告)日:2013-05-07

    申请号:US12733415

    申请日:2008-08-14

    IPC分类号: A61K31/568 C07J41/00 A61P5/28

    CPC分类号: C07J41/0016

    摘要: 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.

    摘要翻译: 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。

    NOVEL STEROIDAL ESTERS OF 17-OXIMINO-5-ANDROSTEN-3BETA-OL
    2.
    发明申请
    NOVEL STEROIDAL ESTERS OF 17-OXIMINO-5-ANDROSTEN-3BETA-OL 有权
    17-OXIMINO-5-ANDROSTEN-3BETA-OL的新型甾体酯

    公开(公告)号:US20100292201A1

    公开(公告)日:2010-11-18

    申请号:US12733415

    申请日:2008-08-14

    CPC分类号: C07J41/0016

    摘要: 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.

    摘要翻译: 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,测试了这些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。

    Nitric oxide releasing derivatives of paracetamol
    3.
    发明授权
    Nitric oxide releasing derivatives of paracetamol 有权
    扑热息痛的一氧化氮释放衍生物

    公开(公告)号:US08207222B2

    公开(公告)日:2012-06-26

    申请号:US12707410

    申请日:2010-02-17

    IPC分类号: C07C203/04 A61K31/167

    CPC分类号: C07C233/25

    摘要: The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the corresponding nitrate ester derivatives. The nitrate esters of paracetamol are useful as analgesic, anti-inflammatory agents.

    摘要翻译: 本发明特别涉及新型的扑热息痛的硝酸酯。 对乙酰氨基酚的硝酸酯通过使对乙酰氨基酚与二卤烷基化合物反应,随后与硝酸银反应得到相应的硝酸酯衍生物。 对乙酰氨基酚的硝酸酯可用作止痛剂,抗炎剂。

    NITRIC OXIDE RELEASING DERIVATIVES OF PARACETAMOL
    4.
    发明申请
    NITRIC OXIDE RELEASING DERIVATIVES OF PARACETAMOL 有权
    PARACETAMOL的氮氧化物释放衍生物

    公开(公告)号:US20100234472A1

    公开(公告)日:2010-09-16

    申请号:US12707410

    申请日:2010-02-17

    CPC分类号: C07C233/25

    摘要: The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the corresponding nitrate ester derivatives. The nitrate esters of paracetamol are useful as analgesic, anti-inflammatory agents.

    摘要翻译: 本发明特别涉及新型的扑热息痛的硝酸酯。 对乙酰氨基酚的硝酸酯通过使对乙酰氨基酚与二卤烷基化合物反应,随后与硝酸银反应得到相应的硝酸酯衍生物。 对乙酰氨基酚的硝酸酯可用作止痛剂,抗炎剂。

    Polyol oxidases
    10.
    发明授权
    Polyol oxidases 有权
    多元氧化酶

    公开(公告)号:US07919295B2

    公开(公告)日:2011-04-05

    申请号:US11875788

    申请日:2007-10-19

    摘要: The present invention provides compositions and methods for producing a polyol oxidase in microorganisms, and the use of polyol oxidases in cleaning compositions. The invention includes cleaning compositions that contain combinations of two or more POx oxidases, and cleaning compositions that contain combinations of two or more POx oxidases and a perhydrolase. In particular, the invention provides methods for expressing polyol oxidases in bacterial hosts for use in detergent applications for cleaning, bleaching and disinfecting.

    摘要翻译: 本发明提供了用于在微生物中生产多元醇氧化酶的组合物和方法,以及在清洁组合物中使用多元醇氧化酶。 本发明包括含有两种或更多种POx氧化酶的组合的清洁组合物和含有两种或更多种POx氧化酶和过水解酶的组合的清洁组合物。 特别地,本发明提供了用于在洗涤剂应用中用于清洁,漂白和消毒的细菌宿主中表达多元氧化酶的方法。