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康子圣

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虫号: 1813224
注册: 2012-05-12
性别: GG
专业: 合成药物化学

[求助] 重金求翻译！！！请高手帮忙已有1人参与

肺动脉高压防治新药CPU86017-RS

肺动脉高压是由各种原因所引起的肺动脉压力持久性增高，超过正常最高值，是多病因、发病机理复杂的一种疾病。持续的肺动脉高压会引起右心室肥厚，进而导致右心衰竭，是重要的死亡原因之一。目前临床用药有:口服内皮素受体拮抗剂；吸入NO；静滴注前列环素的衍生物；硝苯地平等，但这些药物对肺动脉高压只有辅助治疗作用。

本项目研制的CPU86017-RS为CPU86017的一个光学异构体，CPU86017为中国药科大学自主创新的一类抗心律失常新药，已完成全部临床前研究。研究证明：CPU86017对治疗肺动脉高压也有明显的疗效，但它存在水溶性差；生物利用度较低，约10%；并且有较强阻断a-受体活性，不适于静脉给药等局限。为了克服CPU86017的局限，本课题组研制出CPU86017的异构体CPU86017-RS。实验结果表明：CPU86017-RS治疗肺动脉高压作用机制明确，与临床用药硝苯地平比，除了具有硝苯地平的扩血管作用外，还具有肺动脉重构，这是硝苯地平所不具有的；与内皮素受体拮抗剂相比，还具有钙拮抗作用，这是内皮素受体拮抗剂所不具有的。与消旋体CPU86017相比具有以下优点：治疗缺氧性肺动脉高压的药效更明显；可增强钙拮抗作用；减弱了 a- 阻断作用；药动学和生物利用度均有明显改善（20%）；溶解度提高；毒性降低等。而且消旋体CPU86017的代谢途径和代谢产物已明确，对于CPU86017-RS来说是不会改变的，应与消旋体相同。
本项目采用的原料为中草药有效成分小檗碱（黄连素），来源广泛，价格低廉。通过还原、手性拆分、季铵化和柱层析分离得到，方法简单易行。而且消旋体CPU86017的相关研究对本项目的研究提供基础，如CPU86017代谢途径和代谢产物已明确，对于其异构体CPU86017-RS来说是不会改变的，应与消旋体相同。
RS-异构体的优势：原料易得,工艺成熟；具有优良的药效学基础药动学研究基础；毒理学研究基础，毒性比消旋物低，低风险；有消旋物CPU86017的前期研究支持。目前已进行CPU86017-RS异构体的合成工艺、治疗肺动脉高压主要药效学、毒理学初步研究以及 iv和po 各3种剂量的药动学及生物利用度研究。
商业化前景良好
已获得中国专利（02138325.1 CN）。

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康子圣: 金币+150, ★★★★★最佳答案, 昨晚我就已经把自己翻译的交上去了，不过还是谢谢你，翻译的很棒 2014-10-10 07:54:34

New Drug (CPU86017-RS) for Prevention and treatment of pulmonary hypertension

Pulmonary hypertension is the persistent hypertension of pulmonary artery above the normal maximum level. It is a multi-etiology disease with a complicated pathogenesis. Persistent pulmonary hypertension causes right ventricular hypertrophy, subsequently leading to right heart failure, which is one of the important causes of death. Current clinical drugs include oral endothelin receptor antagonists; inhaled NO; intravenous administration of prostacyclin derivatives, and nifedipine. But all these drugs can only be used as an adjuvant therapy for pulmonary hypertension.

CPU86017-RS, developed in this project, is an optical isomer of CPU86017. CPU86017 is a class of anti-arrhythmic drugs innovated independently by China Pharmaceutical University. All pre-clinical studies of CPU86017 have been completed. Studies have shown that CPU86017 had a significant therapeutic effect on treatment of pulmonary hypertension. However, the poor aqueous solubility, low bioavailability (about 10%), and its strong α-receptor antagonistic effects make it unsuitable for intravenous administration. To overcome the limitations of CPU86017, our group developed CPU86017-RS, an isomer of CPU86017. Experimental results showed that mechanism of action of CPU86017-RS in the treatment of pulmonary hypertension is clear, and that as compared with clinical drug nifedipine, CPU86017-RS not only has the vasodilating effect, but also has the effect on pulmonary artery reconstruction, which nifedipine does not have. As compared with the endothelin receptor antagonists, CPU86017-RS has calcium antagonistic effect, of which endothelin receptor antagonists is lack. Compared with racemic CPU86017, CPU86017-RS has the following advantages: the efficacy of the treatment of hypoxic pulmonary hypertension is more obvious; enhancement of calcium antagonistic effect; weakened α-blocking effect; significantly improved pharmacokinetics and bioavailability (20 %); increased solubility; and decreased toxicity. The metabolic pathways and its metabolites have been well-documented for racemate CPU86017. It should be reasonable to suppose that the isomer CPU86017-RS has the same metabolic pathways as racemate CPU86017.

This project uses the raw materials for the herbal active ingredient berberine (berberine), wide variety of sources, low prices. By reducing, chiral separation, quaternary ammonium and column chromatography to obtain, the method is simple. And related research racemic CPU86017 provides the basis for the study of the project, such as CPU86017 metabolic pathways and metabolites has been clear for its isomer CPU86017-RS is not going to change, should be the same as the racemate.

Advantages of RS-isomers: Readily available raw materials, matured process; excellent foundation for pharmacodynamic and pharmacokinetic research; toxicology research foundation, lower toxicity than racemate, low risk; support from the preliminary studies on racemate CPU86017. Currently, the synthesis process of CPU86017-RS isomer has been started, the preliminary studies on the major pharmacodynamics, toxicology of treatment of pulmonary hypertension have been under investigation, the pharmacokinetics and bioavailability are being studied by intravenous or intraperitoneal injections of three dosages of CPU86017-RS.

China patent obtained: 02138325.1 CN

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