C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/7.08, 167/10
C07K 7/08 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) C07K 7/06 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2036815
- 1 - BEHRINGWERKE AKTIENGESELLSCHAFT HOE 90/B 007 - Ma 822 Dr. Ha/Bi Abstract of the disclosure Peptides which inhibit blood coagulation, processes for the preparation thereof and the use thereof 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 carbon atoms, an acyl group with 2-10 carbon atoms, an acyl group with 2- 10 carbon 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 carbon atoms, which can also be in the form of a carboxamide group whose hydrogen can - 2 - optionally be replaced by alkyl groups with up to 4 carbon atoms, and a process for the preparation thereof are described. These peptides inhibit blood coagulation and can be used as anticoagulants.
Behringwerke Aktiengesellschaft
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
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