首页> 外国专利> LIPOPEPTIDE CONJUGATES AND THEIR SALTS, METHOD OF MANUFACTURE OF LIPOPEPTIDE CONJUGATES AND THEIR SALTS, PHARMACEUTICAL COMPOSITION COMPRISING A LIPOPEPTIDE CONJUGATE AND ITS SALTS FOR THE TREATMENT OF CHRONIC WOUNDS

LIPOPEPTIDE CONJUGATES AND THEIR SALTS, METHOD OF MANUFACTURE OF LIPOPEPTIDE CONJUGATES AND THEIR SALTS, PHARMACEUTICAL COMPOSITION COMPRISING A LIPOPEPTIDE CONJUGATE AND ITS SALTS FOR THE TREATMENT OF CHRONIC WOUNDS

机译:脂肽缀合物及其盐,脂肽缀合物的制造方法及其盐,包含脂肽缀合物的药物组合物及其盐用于治疗慢性伤口

摘要

Object of the invention ;The object of the invention is a method of obtaining lipopeptide conjugates especially rich in L-hydroxyproline residues described by the general formula Nα-acyl-(AK5-AK4-AK3-AK2-AK1)n-NH2 (I) or their pharmaceutically acceptable salts, wherein: AK1,AK2,AK3,AK4,AK5 denote amino acid residues or their lack; AK1 is a lysine residue of L or D configuration; AK2 is an amino acid residue selected from the group consisting of non-polar neutral amino acids: Phe, Ala, Gly, Ile, Leu, Met, Pro, Val, Trp or its lack; AK3 is an amino acid residue selected from Hyp, Phe, Ala, Gly, Ile, Leu, Met, Pro, Val, Trp; AK4 is an amino acid residue selected from Pro, Hyp or its lack; AK5 is the Gly residue; Nα-acyl group has the formula R1-C(=O), wherein R1 is a saturated carbon chain of length from C7 to C13; n denotes a number of repeat units from 1 to 2 of a general formula: AK5-AK4-AK3-AK2-AK1.;In addition, the invention concerns the use of a pharmaceutical composition containing at least one lipopeptide conjugate or its pharmaceutically acceptable salt or a preparation for the stimulation of proliferation and migration of fibroblasts and keratinocytes, containing the pharmaceutical composition as a basic component for the manufacture of a wound dressing in the form of an aqueous solution, a suspension, an emulsion, an aerosol, a cream, an ointment, a three-dimensional scaffold, a hydrogel in a tube, for the use in the treatment of deep full-thickness wounds, i.e. burn wounds (second and third degree), venous leg ulcers, bedsores or metabolic disorders i.e diabetic foot, being a complication of existing cardiovascular disease or diabetes mellitus.
机译:本发明的目的;本发明的目的是获得特别是富含富含通式Nα-酰基 - (AK5-AK4-AK3-AK2-AK1)N-NH2(I)的脂肽缀合物特别富含L-羟脯氨酸残基的方法或者它们的药学上可接受的盐,其中:ak1,ak2,ak3,ak4,ak5表示氨基酸残基或它们的缺乏; AK1是L或D配置的赖氨酸残留物; AK2是选自非极性中性氨基酸的氨基酸残基:PHE,ALA,GLY,ILE,LEU,MET,PRO,VAL,TRP或其缺乏; Ak3是选自噬菌,Phe,Ala,Gly,Ile,Leu,Met,Pro,Val,TRP的氨基酸残基。 AK4是选自Pro,Hyp或其缺乏的氨基酸残基; Ak5是甘氨酸残留物; Nα-酰基具有式R1-C(= O),其中R1是从C7至C13的长度的饱和碳链; n表示一般式的1至2的重复单元:Ak5-AK4-AK3-AK2-AK1。此外,本发明涉及使用含有至少一种脂肽缀合物或其药学上可接受的盐的药物组合物或者制备刺激成纤维细胞和角质形成细胞的增殖和迁移,含有药物组合物作为制备水溶液,悬浮液,乳液,气溶胶,奶油,奶油,奶油,奶油,奶油软膏,一个三维支架,管中的水凝胶,用于治疗深层全厚伤口,即烧伤伤口(第二和第三度),静脉腿部溃疡,褥疮或代谢障碍,即糖尿病脚,是现有心血管疾病或糖尿病的并发症。

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