3-Aminomethyl derivatives of indane, indoline and dihydrobenzofurane and dihydrobenzothiophene
申请人:H. LUNDBECK A/S
公开号:EP0281261A2
公开(公告)日:1988-09-07
Indane-, dihydrobenzofurane-, dihydrobenzothiophene-, and indoline- derivatives of the following formula:
wherein X, R¹, R², R³ and R⁴ are as defined in Claim 1,
are effective at presynaptic DA receptors, or both at pre- and postsynaptic DA receptors, indicating usefulness in the treatment of disorders of the central nervous system (CNS) such as schizophrenia or Parkinson's disease.
The 1-aminomethyl derivatives of Formula I exist as optical isomers, and the useful effects are often found in the single enantiomers to a different degree.
A method for the preparation of compounds of Formula I is described.
下式中的茚满-、二氢苯并呋喃-、二氢苯并噻吩-和吲哚啉-衍生物: 其中X、R¹、R²、R³和R⁴如权利要求1中所定义,对突触前DA受体有效,或对突触前和突触后DA受体均有效,表明在治疗精神分裂症或帕金森病等中枢神经系统(CNS)疾病方面有用。 式I的1-氨基甲基衍生物以光学异构体形式存在,其有用的效果通常在单一对映体中以不同程度存在。 描述了一种制备式I化合物的方法。