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    • 3. 发明授权
    • Peptide enzyme inhibitors
    • 肽类酶抑制剂
    • US3832337A
    • 1974-08-27
    • US25871472
    • 1972-06-01
    • SQUIBB & SONS INC
    • ONDETTI MPLUSCEC J
    • A61K8/64A61K38/00A61Q17/04C07K5/04C07K5/113C07K5/117C07K7/04C07K7/06A61K27/00C07C103/52
    • A61Q17/04A61K8/64A61K38/00C07K5/1021C07K5/1024C07K7/06
    • WHEREIN Y IS LYS OR GLU, 11. AN UNDECAPEPTIDE OF THE FORMULA

      PGLU-TRP-PRO-ARG-PRO-V-PRO-W-ILE-PRO-PRO

      WHEREIN V IS THR OR GLY AND W IS GLN OR GLU, 12 A. TRIDECAPEPTIDE OF THE FORMULA
      PGLU-TRP-PRO-NLE-T-PRO-PRO

      WHEREIN T IS AS DEFINED ABOVE,

      PGLU-TRP-PRO-ARG-PRO-GLU-PHE-PRO-PRO, PGLU-TRP-PRO-ARG-PRO-LYS-PHE-ALA-PRO, PGLU-TRP-PRO-D-ARG-PRO-GLN-ILLE-PRO-PRO, PGLU-TRP-PRO-AGR-PRO-GLN-PHE-PRO-PRO, PGLU-TRP-PRO-GLY-PRO-GLU-ILE-PRO-PRO, PGLU-LYS-PHE-ALA-PRO-GLN-ILE-PRO-PRO,

      10. A DECAPEPTIDE OF THE FORMULA

      PGLU-K-TRP-PRO-ARG-PRO-GLN-ILE-PRO-PRO

      WHEREIN K, P AND Q ARE AS DEFINED ABOVE,
      PGLU-U-TRP-PRO-ARG-PRO-GLN-ILE-PRO-PRO

      THE ENZYMATIC CONVERSION OF ANGIOSTENSIN I INTO ANTIOTENSIN II IS INHIBITED BY A PEPTIDE OR AN ACYLATED PEPTIDE HAVING ONE OF THE FOLLOWING AMINO ACID SEQUENCES:

      1. AN ACYLATED TRIPEPTIDE OF THE FORMULA

      CHC-PHE-ALA-PRO

      WHEREIN CAC IS CHLOROACETIC ACID, 2. A TETRAPEPTIDE OF THE FORMULA

      PGLU-TRP-ALA-PRO OR PGLU-LYS-TRP-PRO,

      3. AN ACYLATED TETRAPEPTIDE OF THE FORMULA

      DAC-FLY-ALA-PRO OR A-LYS-PHE-ALA-PRO

      WHEREIN DAC IS DIAZOACETIC ACID, AND A IS CHLOROACETIC ACID, CYCLOBUTYLCARBOXYLIC ACID, CYCLOPENTYLCARBOXYLIC ACID OR CYCLOHEXYLCARBOXYLIC ACID, 4. A PENTAPEPTIDE OF THE FORMULA

      PGLU-C-TRP-ALA-PRO

      WHEREIN B IS LYS, NLE, GLU OR GIN,

      PGLU-C-TRP-ALA-PRO

      WHEREIN C IS NLE, HIS, ORN OR ARG, N''PGLU-LYS-TRP-ALA-PRO,PGLU-LYS-E-ALA-PRO WHEREIN E IS HIS , ILE, PRO, SER OR 3-AMINO-4-PHENYL-BUTYRIC ACID,

      PGLU-LYS-PHE-F-PRO

      WHEREIN G IS ALA, ASP OR GLU,

      PGLU-LYS-PHE-ALA-G



      WHEREIN W IS AS DEFINED ABOVE.

      WHEREIN G IS ALA, ASP OR GLU,

      PGLU-LYS-TRP-H

      WHEREIN H IS ILE-PRO, THR-PRO-ALA-GLY OR ALA-SAR,

      PGLU-TRP-PRO-J-PRO

      WHEREIN J IS HIS, LYS OR GLY, 5. AN ACYLATED PENTAPEPTIDE OF THE FORMULA

      DAC-GLY-GLY-PHE-ALA-PRO

      WHEREIN DAC IS DIAZOACETIC ACID, 6. A HEXAPEPTIDE OF THE FORMULA

      PGLU-LYS-PHE-ALA-PRO-PRO, PGLU-K-TRP-PRO-ARG-PRO

      WHEREIN K IS ASN, NLE OR SER,

      PGLU-NLE-TRP-PRO-L-PRO

      WHEREIN L IS HIS OR GLY,

      PGLU-ASN-TRP-PRO-M-PRO

      WHEREIN M IS LYS OR GLY, 7. AN OCTAPEPTIDE OF THE FORMULA

      PGLU-ILE-PRO-PRO-LYS-PHE-ALA-PRO,

      8. AN ACYLATED OCTAPEPTIDE OF THE FORMULA

      N-O-PRO-ARG-PRO-GLN-ILE-PRO-PRO

      WHEREIN N IS CYCLOBUTYLCARBOXYLIC ACID, CYCLOPENTYLCARBOXYLIC ACID OR CYCLOHEXYLCARBOXYLIC ACID AND O IS TRP, TYR,

      -TYR(-BZL)-

      PHE, GLY, LEU, OR D-TRP,

      N-TRP-PRO-GLY-PRO-LYS-SHPHE-ALA-PRO

      WHEREIN N IS AS DEFINED ABOVE AND SHPE IS 3-AMINO-4 PHENYLBUTYRIC ACID, 9. A NONAPEPTIDE OF THE FORMULA

      PGLU-TRP-PRO-P-PRO-Q-ILE-PRO-PRO

      WHEREIN P IS ARG, HIS, LYS OR GLY AND Q IS GLN OR ASN,

      PGLU-TRP-PRO-R-PRO-S-T-ALA-PRO

      WHEREIN R IS ARG OR ORN, S IS NLE OR GLN AND T IS ILE OR PHE,

      PGLU-TRP-PRO-ORN-PRO-S-T-PRO-PRO

      WHEREIN S AND T ARE AS DEFINED ABOVE,

      PGLU-O-PRO-ARG-PRO-GLN-ILE-PRO-PRO

      WHEREIN O IS AS DEFINED ABOVE,
      PGLU-GLY-GLY-TRP-PRO-ARG-PRO-GLY-PRO-W-ILEPRO-PRO