MASKED CARBOXYLATE NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE
申请人:Jandeleit Bernd
公开号:US20090069419A1
公开(公告)日:2009-03-12
Masked carboxylate neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
本发明公开了一种马来酸阿卡姆普罗酯偶氮磺酸酯前药,其中掩蔽羧酸基的新戊烷磺酰酯前药,以及包含这种前药的制药组合物和使用这种前药及其组合物治疗疾病的方法。具体而言,本发明公开了具有增强口服生物利用度的阿卡姆普罗酯前药及其使用方法,用于治疗神经退行性疾病、精神疾病、情绪障碍、焦虑症、躯体形式障碍、运动障碍、物质滥用障碍、暴食症、皮质扩散性抑制相关障碍、耳鸣、睡眠障碍、多发性硬化和疼痛。