首页> 外国专利> CONDENSED PYRIDAZINE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, AN AGENT SHOWING INHIBITORY ACTIVITY WITH RESPECT TO CYCLIC GMP-PHOSPHODIESTERASE

CONDENSED PYRIDAZINE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, AN AGENT SHOWING INHIBITORY ACTIVITY WITH RESPECT TO CYCLIC GMP-PHOSPHODIESTERASE

机译:缩合哒嗪或其药学上可接受的盐,一种与循环GMP-磷酸酯酶有关的抑制剂,具有抑制活性

摘要

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to condensed pyridazine of the general formula (I) where n = 1 or 2; R1- - hydrogen, halogen atom, nitro-, cyano-, amino-group or 4-hydroxypiperidine-1-yl; R2 and R3- - halogen atom or lower alkoxy-group, or R2 and R3 form together methylenedihydroxy- -group; symbol ___ means double or simple bond; when ___ is a double bond then X - nitrogen atom and Y means =C-Z where Z - halogen atom, group of the formulas (a), (b), (c), (d), (e), (f); p = 0 or 1; m = 0, 1, 2; R4 means carbamoyl-, carboxy-, carboxylate-group with cation, alkoxycarbonyl- or dialkylamino-group; R5 or R6 means H and other - hydroxyl; R7 means pyridyl, pyrimidyl or lower hydroxyalkyl; R8- means H, lower alkyl; R9- means pyridyl, lower hydroxyalkyl, carboxyalkyl, lower alkoxy-, lower hydroxyalkoxy-group, hydroxymethylpyrrolidinyl, imidazolyl, morpholinyl, pyridylmethyl; when ___ means a simple bond then X means NR10 where R10 means H, carboxymethyl, lower alkoxycarbonylmethyl, tetrahydropyranylalkyl or hydroxyalkyl; Y means carbonyl. Synthesized compounds show inhibitory activity with respect to cyclic GMP-phosphodiesterase. EFFECT: improved method of synthesis. 13 cl, 1 tbl, 73 ex
机译:领域:有机化学,生物化学,药学。物质:本发明涉及通式(I)的缩合哒嗪。<图像文件=“ 00000010.GIF” he =“ 85” id =“ imag0.10” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 77” />其中n = 1或2; R 1 --氢,卤素原子,硝基,氰基,氨基或4-羟基哌啶-1-基; R 2 和R 3 --卤原子或低级烷氧基,或R 2 和R 3 形式亚甲基二羟基-基团;符号&lowbar;&lowbar;&lowbar;表示双键或单键;当&lowbar;&lowbar;&lowbar;是一个双键,则X-氮原子,Y表示= C-Z,其中Z-卤素原子是式(a),(b),(c),(d),(e),(f)的基团; p = 0或1; m = 0,1,2; R 4 是指具有阳离子的氨基甲酰基,羧基,羧酸酯基,烷氧基羰基或二烷基氨基。 R 5 或R 6 是指H和其他羟基; R 7 是指吡啶基,嘧啶基或低级羟烷基; R 8 -是指H,低级烷基; R 9 -是指吡啶基,低级羟烷基,羧烷基,低级烷氧基-,低级羟基烷氧基,羟甲基吡咯烷基,咪唑基,吗啉基,吡啶基甲基;当&lowbar;&lowbar;&lowbar;表示单键,则X表示NR 10 ,其中R 10 表示H,羧甲基,低级烷氧羰基甲基,四氢吡喃基烷基或羟烷基; Y表示羰基。合成的化合物对环状GMP-磷酸二酯酶显示抑制活性。效果:改进的合成方法。 13厘升,1汤匙,73前

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