HOMOLOGUES FROM APROTININE WHOSE LYS 15 AMINO ACID IS SUBSTITUTED BY OTHER AMINO ACIDS, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

摘要

Homologues replaced by one of (all L forms where applicable) Gly, Ala, Val, Leu, Ile, Met, Arg, alpha-aminobutyric acid, norvaline, Nle, dehydroalanine or homoserine are new. Also new are the intermediate (I) derivs. in which (1) 15-Lys is replaced by one of the specified amino acids or their alkyl esters and any additional COOH in side chains or terminal position are partly or completely esterified; (2) the bond between 15-Lys and 16-Ala is open and only 15-Lys COOH is in free form, all other side chain COOH (3- and 50-Asp; 7- and 49-Glu) and (-terminal COOH (58-Ala) are present as alkyl esters; (3) the 15/16 bond is broken; 15-Lys is absent, the side-chain and terminal COOH are esterified and only 14-Cys has a COOH in free form.