申请人:Cyogyszerkutato Intezet KFT
公开号:US05639751A1
公开(公告)日:1997-06-17
The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) R stands for a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms; R.sup.1 means hydrogen; or R.sup.1 is absent when a double bond exists between the N(3) and C(4) atoms; R.sup.2 means a C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms; R.sup.3 means hydrogen or a C.sub.1-4 alkanoyl group; R.sup.4 represents hydrogen; a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group or by one or more halogen(s); as well as a benzoyl, palmitoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; and the dotted lines represent valence bonds optionally being present, with the proviso that no double bond exists between the N(3) and C(4) atoms when both R.sup.3 and R.sup.4 stand for hydrogen. The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.
本发明涉及一种新型的N-酰基-2,3-苯并二氮平衍
生物,其通式为(I),其立体异构体和酸加成盐,以及包含它们的制药组合物和制备它们的方法。在通式(I)中,R代表C.sub.1-6脂肪酰基,其可由甲氧基,
氰基,羧基,
氨基,C.sub.1-4烷基
氨基,二(C.sub.1-4烷基)
氨基,
吡咯烷基,邻苯二甲
酰亚胺或苯基取代,或由一个或多个卤素取代;或R是苯甲酰基,
环丙烷羧酰基,C.sub.1-5烷基
氨基甲酰基或苯基
氨基甲酰基;或当N(3)和C(4)原子之间存在双键时,R不存在;R.sup.1表示氢;或当N(3)和C(4)原子之间存在双键时,R.sup.1不存在;R.sup.2表示C.sub.1-3烷基;或R.sup.1和R.sup.2一起表示亚甲基,且N(3)和C(4)原子之间不存在双键;R.sup.3表示氢或C.sub.1-4脂肪酰基;R.sup.4代表氢;C.sub.1-6脂肪酰基,其可由甲氧基,
氰基,羧基,
氨基,C.sub.1-4烷基
氨基,二(C.sub.1-4烷基)
氨基,
吡咯烷基,邻苯二甲
酰亚胺或苯基取代,或由一个或多个卤素取代;以及苯甲酰基,棕榈酰基,
环丙烷羧酰基,C.sub.1-5烷基
氨基甲酰基或苯基
氨基甲酰基;虚线代表可能存在的价键,但前提是当R.sup.3和R.sup.4都代表氢时,N(3)和C(4)原子之间不存在双键。通式(I)化合物具有有价值的中枢神经系统作用,特别是肌肉松弛,抗惊厥和神经保护作用。因此,它们可能对于治疗各种中枢神经系统起源的疾病有用。