申请人:Gyogyszerkutato Intezet Kft.
公开号:US05760235A1
公开(公告)日:1998-06-02
This invention relates to new peptide derivatives of the general formula (I) A-Xaa-Arg-H, wherein A represents a D- or L-isochroman-1-carbonyl, D- or L-isochroman-3-carbonyl group, furthermore an acyl group of the general formula: D- or DL-A'--CH(OH)--CO, wherein A' represents a phenyl, benzyl, 1-naphthyl, 1-naphthylmethyl, 2-naphthyl, 2-naphthylmethyl, 9-fluorenyl, benzhydryl, cyclohexyl, cyclohexylmethyl, 2-pyridyl, 3-pyridyl or 4-pyridyl group, and Xaa represents an L-prolyl or an L-pipecolinic acid residue, and Arg stands for an L-arginine residue, their acid addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. Furthermore the invention relates to a process for preparing them. The compounds of the invention have valuable therapeutic, particularly anticoagulant, properties.
本发明涉及一种新的肽衍生物,其通式为(I)A-Xaa-Arg-H,其中A代表D-或L-异色烷基-1-甲酰基、D-或L-异色烷基-3-甲酰基基团,还包括通式为D-或DL-A'-CH(OH)-CO的酰基基团,其中A'代表苯基、苄基、1-萘基、1-萘甲基、2-萘基、2-萘甲基、9-芴基、苯并苯甲基、环己基、环己基甲基、2-吡啶基、3-吡啶基或4-吡啶基基团,Xaa代表L-脯氨酰基或L-哌嗪酸残基,Arg代表L-精氨酸残基,它们与有机或无机酸形成的酸加成盐以及含有它们的制药组合物。此外,本发明还涉及一种制备它们的方法。本发明所述化合物具有有价值的治疗特性,特别是抗凝血特性。