FDA批准他达拉非用于治疗良性前列腺增生
作者：admin信息来源：www点击数：196 更新时间：2011-10-27
2011年10月6日，美国食品药品管理局（FDA）批准他达拉非(tadalafi，商品名Cialis)用于治疗良性前列腺增生(benign prostatic hyperplasia ，BPH)，该疾病表现为前列腺增大。
他达拉非于2003年被批准用于治疗ED，在我国
也已获准进口，商品名：西力士。
BPH的常见症状包括排尿困难、尿无力、尿急、包括夜间在内的尿频。
在两项临床试验中，根据国际前列腺症状分级标准(the International Prostate Symptom Score ，IPSS)评估BPH症状，与安慰剂组患者相比，每天服用一次5mg他达拉非的患者BPH症状上有显著统计学差异。
上述试验基于IPSS总分减少的研究结果。
在第三项试验中，同时患有ED和BPH的患者每天服用一次5mg他达拉非，与安慰剂组患者相比，患者的ED和BP H症状均有改善。
测定ED的改善程度采用国际勃起功能指数（the International Index of Erectile Function）的评级标准。
服用硝酸盐类的患者应禁用他达拉非，例如硝酸甘油，因为联合用药可导致血压降低的危险性。
也不推荐他达拉非与α受体阻断剂联合用药，因为在联合用药治疗BPH方面也没有足够的研究，且也存在血压降低的风险。
FDA批准的其他8种用于治疗BPH的药物：保列治（非那雄胺）、适尿通（度他雄胺）、Jalyn（度他雄胺附加坦索罗辛）和α受体阻断剂类：高特灵（特拉唑嗪）、可多华（多沙唑嗪）、坦洛新（坦索罗辛）、Uroxatral（阿夫唑嗪）、R apaflo（西罗多辛）。
Cialis相当于伟哥，一种治疗性功能障碍的药物。
临床证明，药效可长达36小时，30分钟起效。
由于cialis的药效可延续性，不需要担心几小时内失效。
你和你的伴侣可以好好放松并且享受。
cialis的好处：
药效长达36小时
快速见效
很管用
使你准备好
不必就餐而食
百万人使用
可以在网上买
【药物名称】Tadalafil, GF-196960, IC-351, Cialis
化学结构式(Chemical Structure):
参考文献No.27672
标题: Tetracyclic derivs., process of preparation and use
作者: Daugan, A.C.-M. (Icos Corp.)
来源: EP 0740668; JP 1997508113; US 5859006; US 6025494; US 6127542; WO 9519978
合成路线图解说明:
Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.
参考文献No.32434
标题: Use of cGMP-phosphodiesterase inhibitors to treat impotence
作者: Daugan, A.C.-M. (Icos Corp.)
来源: JP 1999509221; US 6140329; WO 9703675
合成路线图解说明:
Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.
参考文献No.46213
标题: Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use
作者: Gellibert, F.; Daugan, A.C.-M. (Icos Corp.)
来源: US 6143746
合成路线图解说明:
Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.
参考文献No.606182
标题: IC-351
作者: Mart韓, L.; Sorbera, L.A.; Leeson, P.A.; Casta馿r, J.
来源: Drugs Fut 2001,26(1),15
合成路线图解说明:
Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.
参考文献No.757016
标题: The discovery of tadalafil: A novel and highly selective PDE5 inhibitor. 2:
2,3,6,7,12,12a-Hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues
作者: Daugan, A.; Grondin, P.; Ruault, C.; Le Monnier de Gouville, A.C.; Coste, H.; Linget, J.M.; Kirilovsky, J.;
Hyafil, F.; Labaudiniere, R.
来源: J Med Chem 2003,46(21),4533
合成路线图解说明:
Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.。