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    • 57. 发明申请
    • THROMBIN RECEPTOR ANTAGONISTS
    • 硫蛋白受体拮抗剂
    • WO1994003479A1
    • 1994-02-17
    • PCT/US1993006428
    • 1993-07-08
    • COR THERAPEUTICS, INC.SCARBOROUGH, Robert, M.
    • COR THERAPEUTICS, INC.
    • C07K05/00
    • C07K7/06A61K38/00C07K5/06078C07K5/1016C07K7/02
    • Peptide derivatives serving as thrombin receptor antagonists are disclosed, which bear specificity for the cellular thrombin receptor without interfering with the catalytic activities of thrombin. The derivatives generally have formula (I) in which R1 and R3 are amide linkages, N-alkylamide linkages, or isosteric replacements of such linkages; R2 is either a neutral amino acid side chain or a hydrophobic radical; R4 is hydrophobic radical; R5 is CO, CH2 or SO; X is either of formula (II) in which R6 and R7 are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R8 is a hydrophobic radical, or a hydrophobic residue; Y is alkoxy, hydroxy, amino, alkylamino, dialkylamino, in which any of the alkyl groups may be substituted with a basic moiety; Z is an amino acid or peptide residue; and m is zero or one.
    • 公开了用作凝血酶受体拮抗剂的肽衍生物,其对细胞凝血酶受体具有特异性,而不干扰凝血酶的催化活性。 衍生物通常具有式(I),其中R 1和R 3是酰胺键,N-烷基酰胺键或这种键的等排取代基; R2是中性氨基酸侧链或疏水基团; R4是疏水基; R5是CO,CH2或SO; X为式(Ⅱ)中R6和R7为H,烷基,环烷基烷基,烷氧基烷基,烷硫基烷基或芳基烷基,R8为疏水基团或疏水残基; Y是烷氧基,羟基,氨基,烷基氨基,二烷基氨基,其中任何烷基可被碱部分取代; Z是氨基酸或肽残基; m为0或1。