Hirudin derivatives and process for their preparation.

摘要

Hirudin derivs. of formula (I) and (II) are new. A0-A1-A2-(Hirudin 3-36)-(Y), (Hirudin 37-65) (I) A0-A1-A2-(Hirudin 3-63)-Y (II) in (I) the comma indicates that the 2 hirudin fragments are connected by disulphide bridges. A0, A1 and A2=amino acid (AA) residue; AO may also be H; Y=residue of amines NH2-R-X (IIIa) or A-R1-X (IIIb); A=1-10 AA; R=1-10C alkyl (opt. substd. by 1 or more of phenyl (itself opt. substd. by 1 or more OH), indolyl or imidazolyl), phenyl or naphthyl; R1=H, covalent bond, 1-10 sugar residues (e.g. glucose, fructose, mannose, galactose, ribose, ribulose or xylose), or -(O-(CH2)m)n; m=2-5; n=1-100; X=H, OR2, SR2, NHR2, COOR2 or A; R2=H or as R.