Sildenafil-同族物四級銨哌嗪鹽類之製備及醫療用途

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

099137696

專利證號

I 462739

專利獲證名稱

Sildenafil-同族物四級銨哌嗪鹽類之製備及醫療用途

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2014/12/01

技術說明

Sildenafil化合物擁有多元化作用 (Pleitropic activity)，顯示於降低脂質活性、抑制Rho 激酶 (Rho-kinase)表現、內皮型一氧化氮合成酶(eNOS) 之激化作用、3’,5’-cyclic guanosine monophosphate(cGMP) 之活化等活性。因此，本發明提供製備Sildenafil與Statin類或PGI2藥物形成離子性複合物，有益於抑制動物之氣喘、慢性呼吸道阻塞之治療。除可克服目前市售Statin類或PGI2藥物存在著一些不良影響，更促使Sildenafil之哌嗪基團複合鹽類呈現多態樣醫療功能，而減低上述副作用之危險性。 Sildenafil Citrate is pharmacologically active through inhibiting phosphodiesterase and increasing cGMP.Prior studies to directly prove the role of cGMP and PKG-1 signaling could reveal suppression of ventricular hypertrophy. Sildenafil Citrate is indicated in the treatment of male sexual function for improving pulmonary arterial hypertension,erectile dysfunction,and urinary symptoms in men with benign prostatic hyperplasia with lower urinary tract symptom or depression.Patient No.9849166 A1 disclosed the synthesis method of sildenafil,The others with 2 pentanone and diethyl oxalate,as raw material,sildenafil can be synthesized(GONG Ping,2002).Such methods are only based the pyrazolo [4,3d]pyrimidin-7-one moiety structure of sildenafil compounds.The Sildenafil salt discloses in those specification such as the general type of pharmaceutically acceptable salt.Both EP No.2024369 and No.1779852,US PAT.No.7,618,976 disclosed the synthesis method of Sildenafil Citrate

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智財保護與科技管理組

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