Abstract:
Improved synthesis of peptides by the carbodiimide method in which an amino-protected amino acid or peptide having a reactive carboxy group is condensed with a carboxy-protected amino acid or peptide having a reactive amino group in the presence of a 1hydroxy-benzotriazole or a substituted 1-hydroxy-benzotriazole of the formula
AS WELL AS IN THE PRESENCE OF A CARBODIIMIDE SUCH AS DICYCLOHEXYL CARBODIIMIDE.
Abstract:
NW-4,4''-DIMETHOXYBENZYL-PROTECTED ASPARAGINE AND GLUTAMINE COMPOUNDS USEFUL AS INTERMEDIATES IN THE SYNTHESIS OF THERAPEUTICS BY PEPTIDE CONDENSATION REACTIONS.
Abstract:
IMPROVED SYNTHESIS OF PEPTIDES BY THE CARBODIIMIDE METHOD IN WHICH AN AMINO-PROTECTED AMINO ACID OR PEPTIDE HAVING A REACTIVE CARBOXY GROUP IS CONDENSED WITH A CARBOXY-PROTECTED AMINO ACID OR PEPTIDE HAVING A REACTIVE AMINO IN THE PRESENCE OF 3-HYDROXY-4-OXO3,4-DIHYDRO-1,2,3-BENZOTRIAZINE AS WELL AS IN THE PRESENCE OF A CARBODIIMIDE SUCH AS DICYCLOHEXYL CARBODIIMIDE.
Abstract:
The invention relates to peptides of the formula in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R1), beta -Asn, beta -Asp-OMe, D-Thi or -NH-CH(CH2R2)-CO-; F is Ser(R1), Leu, Trp or Phe; G is Gly-NH2, Aza-Gly-NH2, D-Ala-NH2 or NH-alkyl; R1 is glycosyl and R2 is hydrogen, acyl, aryl or heteroaryl. The invention also relates to methods for the preparation of these peptides, agents containing them and their use.
Abstract:
A process for the purification of secretin by chromatography on an alkylated dextran gel is disclosed, as is a method of its manufacture appropriate for preparing larger amounts of secretin.
Abstract:
The present invention relates to peptides having strong LH-RH/FSH-RH activity, wherein Gly in the 6-position is replaced by different substituted amino acids and in the 10-position there is glycinamide or glycine in the 10-position is replaced by a NH-alkyl group with 1-3 carbon atoms or a NH-cyclopropyl group. The invention relates as well to a process for manufacturing said peptides, and to pharmaceutical preparations containing said peptides.
Abstract:
The present invention relates to peptides having strong LH-RH/FSH-RH activity, wherein Gly in the 6-position is replaced by different substituted amino acids and in the 10-position there is glycinamide or glycine in the 10-position is replaced by a NH-alkyl group with 1-3 carbon atoms or a NH-cyclopropyl group. The invention relates as well to a process for manufacturing said peptides, and to pharmaceutical preparations containing said peptides.