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    • 5. 发明授权
    • Peptide derivatives
    • 肽衍生物
    • US4439425A
    • 1984-03-27
    • US385594
    • 1982-06-07
    • Lajos TarcsayBruno KamberJaroslav StanekGerhard BaschangAlbert Hartmann
    • Lajos TarcsayBruno KamberJaroslav StanekGerhard BaschangAlbert Hartmann
    • C07K1/113A61K38/00A61P37/04C07J41/00C07K5/083C07K5/103C07K7/06C07K14/245A61K37/00
    • C07K7/06C07K14/245C07K5/081C07K5/1013A61K38/00
    • The present invention relates to new lipopeptides and in particular to compounds of either of the formulae ##STR1## wherein R.sub.1 and R.sub.2 each represent a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical which has 11-21 C atoms and which is also optionally substituted by oxygen functions, R.sub.3 represents hydrogen or the radical R.sub.1 --CO--O--CH.sub.2 --, where R.sub.1 has the same meaning, R.sub.1 ' is a saturated or unsaturated aliphatic hydrocarbon radical of at least 9 C atoms, which is optionally substituted at one of the C atoms non adjacent to the sulfur atom by a free hydroxyl group or a hydroxyl group esterified with a monobasic carboxylic acid and which is optionally interrupted in the C atoms chain by one or more oxygen atoms, and which hydrocarbon is optionally substituted by a maximum of 2 cycloaliphatic hydrocarbon radicals having 5-8 ring C atoms, or R.sub.1 ' is the radical --CO--R.sub.1 ", wherein R.sub.1 " represents a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical of 11-21 C-atoms and which is optionally interrupted in the C atoms chain by oxygen atoms, and X represents an amino acid with free esterified or amidated carboxyl group, or an amino acid sequence of 2-10 aliphatic amino acids, the terminal carboxyl group of which is free or in the ester or amide form, the amino acids being naturals ones in the case of compounds of formula (1).
    • 本发明涉及新的脂肽,特别是涉及式(I)* = R ** = R或S或R / S中的任一个的化合物(I')n = 1,2 * = R / S或R或S,其中R 1和R 2各自表示饱和或不饱和的具有11-21个C原子的脂族或混合的脂族 - 脂环族烃基,并且也可任选被氧官能团取代,R 3表示氢或基团R 1 - CO-O-CH 2 - ,其中R 1具有相同的含义,R 1'是至少9个C原子的饱和或不饱和脂族烃基,其任选地在不与硫原子相邻的C原子之一被自由基 羟基或用一元羧酸酯化的羟基,其任选地在C原子链中被一个或多个氧原子中断,并且该烃任选被具有5-8个环C原子的最多2个脂环族烃基取代 ,或者R1'是-CO-R1“基团,其中R1”表示 是11-21个C原子的饱和或不饱和脂族或混合脂族 - 脂环族烃基,其任选在C原子链中被氧原子中断,X表示具有游离酯化或酰胺化羧基的氨基酸,或 2-10脂肪族氨基酸的氨基酸序列,其末端羧基是游离的或呈酯或酰胺形式,氨基酸在式(1)化合物的情况下是天然的。