Abstract:
L-PYROGLUTAMYL-2,5-DIIODO-L-HISTIDYL-PROLINAMIDE AND ITS ACID ADDITION SALTS ARE ACTIVE AS THYROIDAL AGENTS, SUCH AS FOR EXAMPLE IN THE TREATMENTOF HYPERTHYREOSIS. THE IODINATED TRIPEPTIDE IS CONVENIENTLY PREPARED BY IODINATING 1PYROGLUTAMYL-L-HISTIDYL-PROLINAMIDE.
Abstract:
DIURETICALLY ACTIVE NONAPEPTIDES WHICH ARE ANALOGS OF VASOPRESSIN ARE DISCLOSED. PARTICULAR EMBODIMENTS INCLUDE (ILE3,LEU4) - ARGINING-VASOPRESSIN AND (ILE3,LEU4)-LYSINEVASOPRESSIN. INTERMEDIATES USEFUL IN THE PREPARATION OF THE ABOVE COMPOUNDS ARE ALSO DISCLOSED.
Abstract:
PEPTIDES ARE PREPARED IN A HOMOGENEOUS SYSTEM BY COUPLING A FIRST AMINO ACID TO A SOLUBLE POLYMER SUPPORT AND THEREAFTER COUPLING ADDITIONAL AMINO ACIDS IN DESIRED SEQUENCE UNTIL THE ULTIMATE PEPTIDE IS OBTAINED. REAGENTS USED IN THE INTERMEDIATE STEPS ARE READILY SEPARATED FROM THE COUPLED POLYMER-AMINO ACID CHAIN BY SELECTIVE FILTRATION TECHNIQUES. IN THE FINAL STEP THE DESIRED PEPTIDE IS CLEAVED FROM THE POLYMER SUPPORT AND SEPARATED FROM THE SOLUBLE POLYMER BY USE OF ULTRAFILTRATION.
Abstract:
The novel title polypeptides are of formula (where X is the radical of an aminoacid or a linear peptide contg. 2-6 aminoacids, and Q is Arg or Lys), all the aminoacids having the 1-configuration, together with their pharmaceutically acceptable acid addn. salts. They may be prepd. by removal of the protecting gps. from peptides of formula (where R1 is an opt. protected aminoacid or a 2-6 aminoacid linear peptide, R2 is H or an amide protecting gp, Q' is -NHCH (CH2)3NH-C(=NH)-NHR3 CO- or NHCH -(CH2)4NHR4-CO-, where R3 is H or a guanidine-protecting gp. and R4 is H or a lysine-protecting gp).