申请人:EGIS Gyogyszergyar Rt.
公开号:US05439940A1
公开(公告)日:1995-08-08
The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases. The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent, R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 4 to 7 membered ring, optionally comprising an oxygen atom or a further nitrogen atom, which latter may carry a phenyl, benzyl, pyridyl, pyrimidinyl or C.sub.1-3 alkyl substituent which substituents may, in turn, bear a hydroxy or methoxy group or a halogen atom or a halophenyl group; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a phthalimido group; or A represents pyrimidino, 2,3-epoxypropyl or a group of the formula --C(O)NHR.sup.3, wherein R.sup.3 stands for C.sub.1-7 alkyl, C.sub.2-7 alkenyl or C.sub.3-8 cycloalkyl; and R denotes hydrogen or C.sub.1-7 alkyl, stereoisomers and optically active isomers and the possible mixtures thereof, further acid addition salts and quaternary ammonium derivatives of these compounds.
该发明涉及新型的具有药用活性的苯并[e]茚衍生物,其制备方法,包含这些衍生物的药物组合物,以及所述苯并[e]茚衍生物在治疗某些疾病和制备适用于治疗这些疾病的药物组合物中的应用。根据该发明的新苯并[e]茚衍生物对应于以下通式##STR1## 其中A代表通式alk-NR.sup.1 R.sup.2的基团,其中alk代表一个C.sub.2-7烷基烃基,可选地携带一个羟基取代基,R.sup.1和R.sup.2分别独立地表示氢、C.sub.1-7烷基、C.sub.2-7烯基、C.sub.2-7炔基、单(C.sub.1-7)烷基氨基(C.sub.1-7)烷基、二(C.sub.1-7)烷基氨基(C.sub.1-7)烷基或C.sub.3-7环烷基;或者R.sup.1和R.sup.2与它们连接的氮原子一起形成一个4到7成员环,可选地包含一个氧原子或另一个氮原子,后者可能携带一个苯基、苄基、吡啶基、嘧啶基或C.sub.1-3烷基取代基,这些取代基反过来可能携带一个羟基或甲氧基或卤原子或卤苯基;或者R.sup.1和R.sup.2与它们连接的氮原子一起形成邻苯二甲酰亚胺基团;或者A代表嘧啶基、2,3-环氧丙基或通式--C(O)NHR.sup.3的基团,其中R.sup.3代表C.sub.1-7烷基、C.sub.2-7烯基或C.sub.3-8环烷基;R代表氢或C.sub.1-7烷基,立体异构体和光学活性异构体及其可能的混合物,以及这些化合物的进一步酸盐和季铵衍生物。