, (IIb) , (IIc) , (IId) and (IIe) ; k = 0-3; m = 1, 2; q = 0, 1, 2 or 3; R1 - H, C1-4-alkyl, R11-OOC-alkyl (other values see p. 1 of the invention claim). Compounds of the formula (I) are effective inhibitors of serine proteases, especially thrombin and kininogenases, for example, kallikrein. EFFECT: improved method of synthesis, enhanced effectiveness of compounds as inhibitors of enzymes. 38 cl, 2 tbl, 91 ex"/> PEPTIDE DERIVATIVES, THEIR STEREOISOMERS OR PHYSIOLOGICALLY ACCEPTABLE SALTS SHOWING ANTITHROMBOSIS, ANTICOAGULATING OR ANTI-INFLAMMATORY ACTIVITY, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF SUPPRESSION OF THROMBIN ACTIVITY, METHOD OF INHIBITION OF KININOGENASES ACTIVITY, USE OF COMPOUNDS AS PARENT SUBSTANCES FOR SYNTHESIS OF THROMBIN INHIBITOR
首页> 外国专利> PEPTIDE DERIVATIVES, THEIR STEREOISOMERS OR PHYSIOLOGICALLY ACCEPTABLE SALTS SHOWING ANTITHROMBOSIS, ANTICOAGULATING OR ANTI-INFLAMMATORY ACTIVITY, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF SUPPRESSION OF THROMBIN ACTIVITY, METHOD OF INHIBITION OF KININOGENASES ACTIVITY, USE OF COMPOUNDS AS PARENT SUBSTANCES FOR SYNTHESIS OF THROMBIN INHIBITOR

PEPTIDE DERIVATIVES, THEIR STEREOISOMERS OR PHYSIOLOGICALLY ACCEPTABLE SALTS SHOWING ANTITHROMBOSIS, ANTICOAGULATING OR ANTI-INFLAMMATORY ACTIVITY, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF SUPPRESSION OF THROMBIN ACTIVITY, METHOD OF INHIBITION OF KININOGENASES ACTIVITY, USE OF COMPOUNDS AS PARENT SUBSTANCES FOR SYNTHESIS OF THROMBIN INHIBITOR

机译:肽衍生物,其立体异构体或生理上可接受的盐,显示出抗细菌病,抗凝或抗炎活性,其合成方法,药物组成,抑制癌变活性的方法,其整合性,癌变活性的抑制方法,凝血酶抑制剂

摘要

FIELD: organic chemistry, derivatives of peptides. SUBSTANCE: invention relates to peptide derivative of the general formula (I): A1-A2-NH-(CH)n-D where A1 is a structural fragment of the formulas (IIa) , (IIb) , (IIc) , (IId) and (IIe) ; k = 0-3; m = 1, 2; q = 0, 1, 2 or 3; R1 - H, C1-4-alkyl, R11-OOC-alkyl (other values see p. 1 of the invention claim). Compounds of the formula (I) are effective inhibitors of serine proteases, especially thrombin and kininogenases, for example, kallikrein. EFFECT: improved method of synthesis, enhanced effectiveness of compounds as inhibitors of enzymes. 38 cl, 2 tbl, 91 ex
机译:领域:有机化学,肽的衍生物。物质:本发明涉及通式(I)的肽衍生物:A 1 -A 2 -NH-(CH) n -D其中A 1 是公式(IIa)的结构片段,(IIb)<图像文件=“ 00000003.GIF” he =“ 30” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 26” />,(IIc)<图像文件=“ 00000004.GIF”他=“ 33” imgContent =“未定义” imgFormat =“ GIF” wi =“ 24” />,(IId)<图像文件=“ 00000005.GIF” he =“ 33” imgContent =“未定义” imgFormat =“ GIF” wi =“ 24” />和(IIe)<图像文件=“ 00000006.GIF” he =“ 22” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 41” />; k = 0-3; m = 1,2; q = 0、1、2或3; R 1 -H,C 1-4 -烷基,R 11 -OOC-烷基(其他值请参见本发明的第1页)。式(I)化合物是丝氨酸蛋白酶特别是凝血酶和激肽原酶例如激肽释放酶的有效抑制剂。效果:改进的合成方法,增强了化合物作为酶抑制剂的有效性。 38厘升,2汤匙,91前

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