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    • 3. 发明授权
    • Peptides and pharmaceutical compositions comprising same
    • US07196063B1
    • 2007-03-27
    • US10048955
    • 2000-08-01
    • Anat ShirvanIlan Ziv
    • Anat ShirvanIlan Ziv
    • A61K38/00A61K49/00A61K51/00
    • C07K14/4721
    • The present invention relates to an 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 0; 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 6–8 amino acids, of which 4–6 are positively charged and 0–2 are negatively charged, the other amino acid residues being polar uncharged amino acids, wherein the amino acids form 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, aldehydes 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 present also relates to pharmaceutical compositions and methods of using the same.
    • 4. 发明授权
    • Basic peptides and pharmaceutical compositions containing same
    • 碱性肽和含有它们的药物组合物
    • US06602852B1
    • 2003-08-05
    • US09763548
    • 2001-02-23
    • Ilan ZivAnat Shirvan
    • Ilan ZivAnat Shirvan
    • A61K3817
    • C07K14/4721
    • The present invention relates to an NST300 compound of general formula (I): comprising the following components: X1—[(X3)a/(X4)b] in which X1 represents a fatty acid or prenyl group; and X3 represents a domain of positively charged amino acids; and X4 represents a domain containing aromatic amino acids; and a stands for an integer of 1-8; and b stands for an integer of 1-8. The invention relates also to pharmaceutical compositions comprising a compound of general formula (I), the use of the compound and of the 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 the compound and of the pharmaceutical composition for the diagnosis of CMLA loss; as a targeting agent; as targeting drugs to tissues inflicted by CMLA loss; and for basic research in fields of research in which CMLA loss takes place both in vitro and in vivo.
    • 本发明涉及通式(I)的NST300化合物:其中X1表示脂肪酸或异戊烯基,X 1 - [(X 3)a /(X 4)b] X3表示带正电氨基酸的结构域。 X4表示含有芳香族氨基酸的结构域。 a代表1-8的整数; b代表1-8的整数。 本发明还涉及包含通式(I)的化合物的药物组合物,该化合物和药物组合物在制备药物中的用途以及用于治疗或预防与疾病相关的疾病中的血栓前状态的方法 过度促凝活性,由CMLA损失引发或传播。 本发明还涉及化合物和药物组合物用于诊断CMLA损失的用途; 作为靶向剂; 作为CMLA损伤造成的组织靶向药物; 以及在体外和体内发生CMLA损失的研究领域的基础研究。