PEPTIDES INHIBITING THE BLOOD COAGULATION, THEIR PROCESS OF PREPARATION AND THEIR USE

摘要

Peptides of the formula I A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15 in which A1 is hydrogen, cysteine, acetylcysteine, one or two alkyl groups with 1-4 C atoms, an acyl group with 2-10 C atoms, an acyl group with 2-10 C atoms and another carboxyl group, or a protective group customary in peptide chemistry, A2 is a bond, Asn, Asp, Gln or Glu, A3 is a bond, Gly or Ala, A4 is Glu or Asp, A5 is Phe, Tyr, Trp, Pgl (phenylglycine) or Nal (naphthylalanine), A6 is Glu or Asp, A7 is Glu, Asp, Pro or Ala, A8 is Ile, Leu, Val, Nle or Phe, A9 is Pro or Hyp, A10 is Glu or Asp, A11 is Glu or Asp, A12 is Phe(SO3H) or Phe(PO3H2) (preferably in the p position) or Pgl(SO3H) or Pgl(PO3H2) (preferably in the p position), A13 is a bond, Leu, Ile, Val or Ala, A14 is a bond, Gln, Asn, Glu, Asp or Cys and A15 is Cys, Cys-amide, an OH group of the alpha-carboxyl group, free or esterified with a lower alcohol with up to 4 C atoms, which can also be in the form of the carboxamide functionality whose hydrogens can optionally be replaced by alkyl groups with up to 4 C atoms, and a process for the preparation thereof are described. These peptides inhibit blood coagulation and can be used as anticoagulants.