Methods of preparing and using 2-hydroxy derivatives of sibutramine and its metabolites
申请人:——
公开号:US20030087963A1
公开(公告)日:2003-05-08
The invention is directed, in part, to racemic and stereomerically pure 2-hydroxy derivatives of sibutramine and its metabolites, and 2-hydroxy derivatives of desmethylsibutramine and didesmethylsibutramine in particular. The invention is further directed to novel methods of preparing these derivatives are also disclosed.
The invention is also directed to pharmaceutical compositions and dosage forms that comprise therapeutically or prophylactically effective amounts of the compounds, optionally in combination with an additional pharmacologically active compound. These pharmaceutical compositions and dosage forms can be used in the methods of the invention, which provide for the treatment or prevention of a variety of diseases and disorders.
本发明部分涉及西布曲明及其代谢物的外消旋和立体纯的 2-羟基衍生物,特别是去甲西布曲明和去甲西布曲明的 2-羟基衍生物。本发明还进一步涉及制备这些衍生物的新方法。
本发明还涉及药物组合物和剂型,其中包含治疗或预防有效量的化合物,可选择与其他药理活性化合物结合使用。这些药物组合物和剂型可用于本发明的方法,从而治疗或预防各种疾病和失调。