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Process for the preparation of pharmaceutical compositions possessing neurogenic or non-neurogenic anti-inflammatory as well as analgetic effects

机译:具有神经源性或非神经源性抗炎以及止痛作用的药物组合物的制备方法

摘要

The invention relates to the use of peptide amides of formula (I) chemistry chemdraw filechemistry mol file;and phenylamino-oxoacetic acid derivatives of formula (II) chemistry chemdraw filechemistry mol file;as well as the salts of the above compounds as active substances for the preparation of pharmaceutical compositions possessing neurogenic and non-neurogenic antiinflammatory as well as analgetic effects. In the above formulae, the most important meanings of the substituents are as follows: ;X1 means an aromatic D-amino acid group; ;X2 stands for an aromatic amino acid group or a derivative thereof ring-substituted by hydroxyl group; ;X3 means aromatic D-amino acid group; ;X4 means threonyl or tryptophyl group; ;k is 0, 1, 2 or 3; ;n is 0, 3 or 4; ;R1 stands for hydrogen or CH3-CO- group, wherein A2 is C1-4 alkyl group; ;R2 means hydrogen, phenyl or carbonyl group; ;R3 represents hydrogen, amino or CF3-CO-NH- group, ;R4 stands for hydrogen, phenyl or amino group; or ;Q1 means hydrogen, halogen, hydroxyl, nitro, amino, C1-4 alkyl or alkoxy group; ;Q2 stands for hydrogen, halogen, hydroxyl, or nitro group; ;Q3 represents hydrogen, halogen, hydroxyl, nitro, CF3, C1-4 alkyl or alkoxy group; ;Q4 and Q5 each represents hydrogen, hydroxyl group, halogen, nitro group, -CF3 group, C1-4 alkyl or C1-4 alkoxy group; or C1-3 dialkylqmino group.
机译:本发明涉及式(I)的肽酰胺的用途 <图像文件=“ US20010009899A1-20010726-C00001.GIF” he =“ 49.69755” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 215.0631” /> 化学chemdraw文件 化学mol文件< / ExternalFileRef> ;以及式(II)的苯基氨基-氧乙酸衍生物 <图像文件=“ US20010009899A1-20010726-C00002.GIF” he =“ 91.4571” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 196.3521” /> 化学chemdraw文件 化学摩尔文件< / ExternalFileRef> ;以及上述化合物的盐,作为制备具有神经源性和非神经源性抗炎以及止痛作用的药物组合物的活性物质。在上式中,取代基的最重要含义如下:; X 1 表示芳族D-氨基酸基团; ; X 2 代表被羟基环取代的芳香族氨基酸基团或其衍生物; ; X 3 表示芳族D-氨基酸基团; ; X 4 表示苏氨酸或色氨酸基团; ; k为0、1、2或3; ; n为0、3或4; ; R 1 代表氢或CH 3 -CO-,其中A 2 是C 1-4 烷基; ; R 2 表示氢,苯基或羰基; ; R 3 代表氢,氨基或CF 3 -CO-NH-基团;; R 4 代表氢,苯基或氨基;或; Q 1 表示氢,卤素,羟基,硝基,氨基,C 1-4 烷基或烷氧基; ; Q 2 代表氢,卤素,羟基或硝基; ; Q 3 代表氢,卤素,羟基,硝基,CF 3 ,C 1-4烷基或烷氧基; ; Q 4 和Q 5 分别代表氢,羟基,卤素,硝基,-CF 3 基团,C < Sub> 1-4 烷基或C 1-4 烷氧基;或C 1-3 二烷基烷基。

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