公开(公告)号：US5220068A

公开(公告)日：1993-06-15

申请号：US649239

申请日：1991-01-29

申请人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

发明人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

IPC分类号： A61K31/135

CPC分类号： A61K31/135

摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient a compound of the Formula I ##STR1## wherein R.sup.1 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms;R.sup.2 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms,with the proviso that groups R.sup.1 and R.sup.2 together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the Formula I by methods known per se. The compounds of the Formula I are phychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficiencies of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.

摘要翻译： 本发明涉及包含作为活性成分的式I化合物（I）的药物组合物，其中R1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R2代表包含1至8个碳原子的直链或支链烷基; 被卤素，羟基，具有1至4个碳原子的烷氧基或一个或两个苯基取代的碳原子数为1〜8的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少3个碳原子。 本发明还涉及通过本身已知的方法制备式I化合物的方法。 式I的化合物是具有新的效应谱的phychostimulants，其可用于增加心理活动（学习和保留）的治疗和用于治疗抑郁症的临床模式和学习和保留的缺陷，如阿尔茨海默病，并且是无效的 的已知兴奋剂的副作用（例如由于儿茶酚胺释放）。

公开(公告)号：US5075338A

公开(公告)日：1991-12-24

申请号：US420058

申请日：1989-10-11

申请人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

发明人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

IPC分类号： C07C211/27 ,  A61K31/135 ,  A61K31/137 ,  A61P25/24

CPC分类号： A61K31/135

摘要： A method of treating a learning deficiency is disclosed wherein a patient in need of stimulating learning ability is treated with a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.8 straight or branched chain alkyl, C.sub.7 to C.sub.10 phenylalkyl, phenyl, or C.sub.3 to C.sub.8 cycloalkyl; andR.sup.2 is C.sub.1 to C.sub.8 straight or branched chain alkyl, unsubstituted or substituted by halogen, hydroxy, C.sub.1 to C.sub.4 alkoxy or by 1 or 2 phenyl groups; or is C.sub.3 to C.sub.8 cycloalkyl;with the proviso that R.sup.1 and R.sup.2 together contain at least 3 carbon atoms; or a pharmaceutically acceptable salt thereof.

摘要翻译： 公开了一种治疗学习缺陷的方法，其中需要刺激学习能力的患者用治疗有效量的式（I）化合物（I）治疗，其中R1为C1至C8直链或支链 烷基，C7至C10苯基烷基，苯基或C3至C8环烷基; R2为C1至C8直链或支链烷基，未取代或被卤素，羟基，C1至C4烷氧基取代或被1或2个苯基取代; 或为C3至C8环烷基; 条件是R1和R2一起含有至少3个碳原子; 或其药学上可接受的盐。