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2. 发明公开

EP0740649A1 NITROXY-GRUPPEN ENTHALTENDE BENZYLAMINDERIVATE UND IHRE VERWENDUNG ZUR BEHANDLUNG VON CARDIOVASCULÄREN ERKRANKUNGEN SOWIE ERHÖHTEM AUGENINNENDRUCK 失效
标题翻译：硝酰基组含苄胺及其用途疾病和心血管升高的眼内压处理
公开(公告)号：EP0740649A1
公开(公告)日：1996-11-06
申请号：EP95906963.0
申请日：1995-01-18
申请人： Byk Nederland BV
发明人： BRON, Jan , STERK, Geert, Jan , TIMMERMAN, Hendrik , VEERMAN, Meta, E., J. , VAN DER WERF, Jan, Fetze
IPC分类号： C07D295 , A61K31 , A61P1 , A61P7 , A61P9 , A61P11 , A61P27 , C07C213 , C07C217 , C07C323 , C07D213 , C07D221
CPC分类号： C07D295/185 , C07C217/58 , C07C323/25 , C07C2601/14 , C07C2603/32 , C07D213/82 , C07D221/16 , C07D295/088 , C07D295/096
摘要： Compounds have formula (I), in which A1 stands for 1-15C-alkylene, 5-7C-cycloalkylene or di-1-4C-alkylene-5-7C-cycloalkane; R1 stands for hydrogen, 1-7C-alkyl or 3-8C-cycloalkyl; R2 stands for hydrogen, 1-7C-alkyl, 3-8C-cycloalkyl or A2-Y; R1 and R2, together with the nitrogen atom to which both are bound, represent a non-substituted or substituted 5-, 6- or 7-ring heterocycle selected from the group made of pyrrolidine, piperidine, piperazine, morpholine and homopiperazine; A2 stands for 1-15C-alkylene, 5-7C-cycloalkylene or di-1-4C-alkylene-5-7C-cycloalkane; Y stands for R3, NH2, NH-R4 or S-R5. One substituted pyrrolidine residue is substituted by one or two identical or different substituents selected from the group that consists of 1-4C-alkyl, 1-4C-alkoxy and hydroxy. One substituted piperidine residue is substituted by one or two identical or different substituents selected from the group that consists of 1-4C-alkyl, 1-4C-alkoxy and hydroxy. One substituted piperazine residue may be substituted at positions 2, 3, 5 or 6 by a 1-4C-alkyl residue and at position 4 is substituted by a substituent selected from the group that consists of 1-4C-alkyl, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, phenyl substituted by R6, R7 and R8, phenyl-1-4C-alkyl substituted at the phenyl residue by R6, R7 and R8, benzoyl, picolinoyl, nicotinoyl, isonicotinoyl substituted in the phenyl residue by R6, R7 and R8, possibly halogen-substituted or 1-4C-alkyl-substituted benzhydryl and the residue R4. One substituted morpholine residue is substituted by one or two identical or different 1-4C-alkyl residues, and one substituted homopiperazine residue is substituted at position 4 by a substituent selected from the group that consists of 1-4C-alkyl, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, phenyl substituted by R6, R7 and R8, phenyl-1-4C-alkyl substituted in the phenyl residue by R6, R7 and R8 and benzoyl substituted in the phenyl residue by R6, R7 and R8. These compounds are useful for treating cardiovascular diseases and increased intra-ocular pressure.
摘要翻译：化合物具有式（I），1-15C - 亚烷基其中A1代表，5-7C-亚环烷基或二C 1-4 - 亚烷基 - 5-7C - 环烷; R1代表氢，1-7C-烷基或3-8C环烷基; R2代表氢，1-7C-烷基，3-8C环烷基或A2-Y; R1和R2连同氮原子与两者结合，表示非substituiertem奥德substituiertem 5-，从制成吡咯烷，哌啶，哌嗪，吗啉和高哌嗪组成的组中6-或7-环杂环; A2代表1-15C-亚烷基，5-7C-亚环烷基或二C 1-4 - 亚烷基 - 5-7C - 环烷; Y代表R 3，NH 2，NH-R 4或S-R5。一个substituiertem吡咯烷的残余物通过从组中选择的一个或两个相同或不同的取代基取代做1-4C-烷基，1-4C-烷氧基和羟基的besteht。一个substituiertem哌啶残基被选自以下的一个或两个相同或不同的取代基取代做1-4C-烷基，1-4C-烷氧基和羟基的besteht。一个substituiertem哌嗪残基可以在位置2，3，5或6通过1-4C-烷基残基和在4位被选自下列的取代基取代的被substituiertem做1-4C-烷基的besteht，1-4C- 烷氧基羰基，1-4C-烷基羰基，由R6，R7和R8，以由R6，R7和R8，苯甲酰基，吡啶甲酰基，烟酰基，在由R6苯基残基异烟substituiertem苯基残基苯基-1-4C-烷基substituiertem苯基substituiertem ，R7和R8，可能卤素substituiertem或1-4C-烷基substituiertem二苯甲基，残余物R4。一个substituiertem吗啉残基被一个或两个相同或不同的1-4C-烷基残基由选自下组的取代基取代，和一个高哌嗪substituiertem残余物在4位取代的那样1-4C-烷基，1-4C-的besteht 烷氧基羰基，1-4C-烷基羰基，由R6，R7和R8，在由R6，R7和R8的苯基残基由R6，R7和R8和苯甲酰substituiertem苯基残基苯基-1-4C-烷基substituiertem苯基substituiertem。这些化合物可用于治疗心血管疾病和增加的眼内压是有用的。

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