| 摘要 |
The present invention consists in compound (hereinafter: "NST500 compound") of general formula (I) comprising the following components: X1-X2-{(X3)a/X4/X5}-X6 wherein: X1 stands for a saturated or unsaturated fatty acid residue comprising 6 - 20 carbon atoms; or a cysteine residue bound through a thioether bond to a prenyl group comprising 5 - 20 carbon atoms; said residue being linked to the adjacent component of the compound through an amide bond; X2 is either 0 or consists of a unit of general formula A*2<n>, in which A stands for a branching unit and n stands for 0 - 4; X3 comprises 1 - 6 amino acids, of which 1-6 are positively charged and 0-2 are negatively charged, the other amino acid residues being polar uncharged amino acids; X4 comprises 1-6 amino acids, of which 1-2 are aromatic amino acids, the other amino acids being selected among polar uncharged amino acids and hydrophobic aliphatic amino acids; X5 comprises 1-6 amino acids, of which 1-6 are positevely charged and 0-2 are negatively charged, the other amino acid residues being polar uncharged amino acids, wherein the amino acids have a cyclic structure; X6 is a compound of general formula (II) wherein Z stands for a spacer group selected among alkane and alkene containing 1 - 5 carbon atoms, J stands for a functional group selected among amines, thiols, alcohols, carboxylic acids and esters, aldeydes and alkyl halides; U is 0 or is selected among a labeling group; wherein: a stands for an integer of 1 - 3; and the groups X3, X4 and X5 being located at various places in the compound; as well as functional equivalents thereof and/or compounds having the same biological activity thereto. The invention relates also to pharmaceutical compositions comprising a compound of general formula (I), the use of said compound and of said pharmaceutical composition in the preparation of a medicament and in methods for the treatment or prevention of prothrombic states in disorders which are associated with excessive procoagulant activity, initiated or propagated by CMLA loss. The invention relates also to the use of said compound and of said pharmaceutical composition for the diagnosis of CMLA loss; as a targeting agent; as targeting drugs to tissues inflicted by CMLA loss; as part of affinity filter; and for basic research in which fields of research in CMLA loss takes place both in vitro and in vivo. The invention also relates to a process for the preparation of a NST500 compound of general formula (I).
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