首页> 外国专利> THYMOPOIETIN OR THYSPLENIN TETRAPEPTIDE ANALOGUES WITH T-CELL SUPPRESSOR ACTIVITY AND PHARMACEUTICAL COMPOSITIONS

THYMOPOIETIN OR THYSPLENIN TETRAPEPTIDE ANALOGUES WITH T-CELL SUPPRESSOR ACTIVITY AND PHARMACEUTICAL COMPOSITIONS

机译:具有T细胞抑制活性和药物成分的胸腺肽或甲状腺素四肽类似物

摘要

Peptides having the biological activity of the molecule human thymopentin, namely the ability to increase cGMP activity in human T-cell line CEM, have the formula R-Arg-X-Asp-Y-NR1R2 wherein R is H, lower alkyl, acetyl, formyl lower alkanoyl; X is Pro, dehydro-Pro, hydroxyl-Pro, D-Lys, Aib or Lys; Y is Gly or a D or L form of an amino acid selected from Val, Ala, Ile, Leu, Asp, Glu, Gln or Lys; R1 is H and R2 is lower alkyl or alkenyl having 1 to 10 carbon atoms, cyclic alkyl or alkenyl having 4 to 8 carbon atoms, aryl or NHR3, where R3 is a lower alkyl having 1 to 10 carbon atoms, cyclic alkyl or alkenyl having 4 to 8 carbon atoms, or aryl; or R1 and R2 together comprise a methylene chain of 4 to 7 carbon atoms. These peptides can be used in pharmaceutical compositions for regulating a deficiency or excess of T-cell function in human subjects.
机译:具有人胸腺五肽分子生物学活性的肽,即具有提高人T细胞系CEM中cGMP活性的能力的肽,其分子式为R-Arg-X-Asp-Y-NR 1 R 2,其中R为H,低级烷基,乙酰基,甲酰基低级烷酰基; X是Pro,脱氢Pro,羟基Pro,D-Lys,Aib或Lys; Y是甘氨酸或选自Val,Ala,Ile,Leu,Asp,Glu,Gln或Lys的氨基酸的Dly或L形式; R 1为H且R 2为具有1至10个碳原子的低级烷基或烯基,具有4至8个碳原子的环状烷基或烯基,芳基或NHR 3,其中R 3为低级烷基。具有1至10个碳原子的,具有4至8个碳原子的环状烷基或烯基或芳基;或R 1和R 2一起包含4至7个碳原子的亚甲基链。这些肽可用于药物组合物中以调节人类受试者中T细胞功能的不足或过量。

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