首页> 外国专利> Peptide-inhibitor TGF-β1 and a cyclodextrin or a derivative thereof, emulsions Peptide inhibitors of TGF-β1, PHARMACEUTICALS ON THEIR BASE, METHODS FOR THE ABOVE SET and emulsions, products obtained by the aforementioned method, and methods of treating diseases and / or conditions mediated by TGF-β1

Peptide-inhibitor TGF-β1 and a cyclodextrin or a derivative thereof, emulsions Peptide inhibitors of TGF-β1, PHARMACEUTICALS ON THEIR BASE, METHODS FOR THE ABOVE SET and emulsions, products obtained by the aforementioned method, and methods of treating diseases and / or conditions mediated by TGF-β1

机译:肽抑制剂TGF-β1及其环糊精或其衍生物,乳剂TGF-β1的肽抑制剂,其基础上的药物,上述方法和乳剂,通过上述方法获得的产品以及治疗疾病和/或方法TGF-β1介导的疾病

摘要

1. The complex of the peptide inhibitor of TGF-β1 and cyclodextrin or its derivative, consisting of a peptide that inhibits TGF-β1, the sequence of which is at least 70% identical to one of the amino acid sequences of SEQ ID NO: 1-23, or its salts , functional derivatives, variants, analogues or fragments thereof with the ability to inhibit TGF-β1 and cyclodextrin selected from the group of cyclodextrins, including β-cyclodextrin and γ-cyclodextrin. 2. The complex according to claim 1, wherein the β-cyclodextrin is selected from the group of β-cyclodextrins, including mono (C-C) hydroxyalkylated β-cyclodextrin and poly (C-C) hydroxyalkylated β-cyclodextrin. The complex according to claim 1 or 2, which contains a peptide that inhibits TGF-β1, in a mass ratio of from about 0.002: 1 to about 0.024: 1 relative to cyclodextrin. A pharmaceutical preparation comprising the complex according to any one of claims 1 to 3, wherein the TGF-β1 inhibiting peptide is present in a therapeutically effective amount and the cyclodextrin is a pharmaceutically acceptable cyclodextrin. 5. The drug according to claim 4, which further comprises cetyl PEG / PPG-10/1 dimethicone. TGF-β1 inhibitor peptide emulsion comprising cetyl PEG / PPG-10/1 dimethicone. 7. The emulsion according to claim 6, in which the sequence of the peptide inhibiting TGF-β1 is at least 70% identical to one of the amino acid sequences of SEQ ID NO: 1-23.8. The emulsion according to claim 7, in which the peptide inhibiting TGF-β1 forms a complex with cyclodextrin or its derivative. The emulsion of claim 8, wherein the TGF-β1 inhibiting peptide is present in a weight ratio of from about 0.002: 1 to about 0.024: 1 relative to cyclodextrin. Pharmaceutical
机译:1.TGF-β1肽抑制剂与环糊精或其衍生物的复合物,由抑制TGF-β1的肽组成,该肽的序列与SEQ ID NO:1的氨基酸序列至少有70%相同: 1-23或其具有抑制TGF-β1和环糊精的能力的盐,功能衍生物,变体,类似物或片段,选自环糊精,包括β-环糊精和γ-环糊精。 2.根据权利要求1的配合物,其中所述β-环糊精选自β-环糊精,包括单(C-C)羟烷基化的β-环糊精和聚(C-C)羟烷基化的β-环糊精。 3.根据权利要求1或2所述的复合物,其含有相对于环糊精以约0.002∶1至约0.024∶1的质量比抑制TGF-β1的肽。 4.一种药物制剂,其包含根据权利要求1至3中任一项所述的复合物,其中所述TGF-β1抑制肽以治疗有效量存在,并且所述环糊精为药学上可接受的环糊精。 5.根据权利要求4的药物,其进一步包含鲸蜡基PEG / PPG-10 / 1二甲聚硅氧烷。包含鲸蜡基PEG / PPG-10 / 1二甲聚硅氧烷的TGF-β1抑制剂肽乳液。 7.根据权利要求6的乳液,其中抑制TGF-β1的肽的序列与SEQ ID NO:1-23.8的氨基酸序列之一至少70%相同。 8.根据权利要求7所述的乳液,其中,所述抑制TGF-β1的肽与环糊精或其衍生物形成复合物。 9.权利要求8的乳液,其中相对于环糊精,TGF-β1抑制肽以约0.002∶1至约0.024∶1的重量比存在。制药业

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