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    BASIC PEPTIDES AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    4.
    发明公开
    BASIC PEPTIDES AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
    碱性肽和药物含有活性化合物

    公开(公告)号：EP1107985A1

    公开(公告)日：2001-06-20

    申请号：EP99939587.4

    申请日：1999-08-23

    申请人： NST Neurosurvival Technologies Ltd.

    发明人： ZIV, Ilan ,  SHIRVAN, Anat

    IPC分类号： C07K14/47 ,  A61K38/17 ,  G01N33/68

    CPC分类号： C07K14/4721

    摘要： 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 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; and for basic research in fields of research in which CMLA loss takes place both in vitro and in vivo.

    PEPTIDES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
    9.
    发明公开
    PEPTIDES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME 审中-公开
    含有肽和YOU药物组合物

    公开(公告)号：EP1226165A2

    公开(公告)日：2002-07-31

    申请号：EP00948239.9

    申请日：2000-08-01

    申请人： NST Neurosurvival Technologies Ltd.

    发明人： SHIRVAN, Anat ,  ZIV, Ilan

    IPC分类号： C07K14/47 ,  A61K38/17 ,  G01N33/68 ,  A61P7/02

    CPC分类号： C07K14/4721

    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*2n, in which A stands for a branching unit and n stands for 0 - 4; X¿3? 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).

    PEPTIDES FOR INHIBITION OF APOPTOSIS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    10.
    发明公开
    PEPTIDES FOR INHIBITION OF APOPTOSIS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
    肽阻止细胞凋亡，并含有组合物PHARMAZEUTSCHE

    公开(公告)号：EP1056772A2

    公开(公告)日：2000-12-06

    申请号：EP99905151.9

    申请日：1999-02-16

    申请人： NST Neurosurvival Technologies Ltd.

    发明人： ZIV, Ilan ,  SHIRVAN, Anat

    IPC分类号： C07K14/47 ,  G01N33/68 ,  A61K38/17

    CPC分类号： C07K14/4747 ,  A61K38/00

    摘要： The present invention relates to an isolated and purified peptide of the RY domain having an amino acid sequence of general formula (I) comprising a sequence of the following amino acids: X1 - X2 - X3 - X4 - X1 - X4 - X4 - X3 - X1, X1 = Phe, Tyr, or any amino acid having a substituted aromatic residue; X2 = Glu, Asp, Ser, or any amino acid having a -(CH2)n-COO residue, wherein n = 0-3; X3 = Asp, Thr, any aliphatic amino acid, or any of amino acids X4; and X4 = Arg, Lys, or any amino acid having a -(CH2)n-NH3+ residue, or a -(CH¿2?)n-NH-C(NH3?+)NH¿2 residue wherein n = 0-4; as well as functional equivalents thereof. The invention relates also to pharmaceutical compositions comprising a compound of general formula (I), the use of said RY peptide and of said pharmaceutical composition in the preparation of a medicament and in methods for the treatment of disorders of inappropriate activation of apoptosis; for increasing the number of viable cells in a biological tissue; and in a method for the enhancement for the survival of biological cells. The invention also relates to a method for the preparation of a RY-peptide of general formula (I). Furthermore, the invention also relates to an in vitro assay system for the regulation of cell death by the Bcl-2 family of test compounds (as hereinbefore defined).