申请人:Carlsson; Per A. E.
公开号:US05286747A1
公开(公告)日:1994-02-15
Compounds of the formula ##STR1## wherein R.sup.3 and the NR.sup.1 R.sup.2 group are in a cis-position to each other and wherein Y is OH, R.sup.4 COO, (R.sup.5).sub.2 NCOO or R.sup.6 O either in position 5 or position 7, whereby R.sup.4 is an alkyl group having 1-5 carbon atoms or a possibly substituted phenyl group, R.sup.5 is an alkyl group having 1-5 carbon atoms and R.sup.6 is an allyl or benzyl group, R.sup.1 is hydrogen or an alkyl group having 1-3 carbon atoms, R.sup.2 is an alkyl group having 1-6 carbon atoms, a phenylalkyl- or m-hydroxyphenylalkyl group with 2-4 carbon atoms in the alkyl part, or an alkenyl group with 3-6 carbon atoms other than 1-alkenyl, and R.sup.3 is an alkyl group having 1-3 carbon atoms, processes and intermediates for their preparation, pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.
化合物的式子为##STR1## 其中R.sup.3和NR.sup.1 R.sup.2基团相对为顺式,Y为OH,R.sup.4 COO,(R.sup.5).sub.2 NCOO或R.sup.6 O,位置在5或7,其中R.sup.4是具有1-5个碳原子的烷基或可能被取代的苯基,R.sup.5是具有1-5个碳原子的烷基,R.sup.6是烯丙基或苄基,R.sup.1为氢或具有1-3个碳原子的烷基,R.sup.2是具有1-6个碳原子的烷基,苯基烷基或m-羟基苯基烷基,其烷基部分具有2-4个碳原子,或具有3-6个碳原子的烯烃基,不包括1-烯烃基。为其制备过程和中间体,制备药物制剂和使用这种化合物的治疗方法。这些化合物对于治疗目的特别有用,尤其是用于治疗中枢神经系统紊乱。