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753 条记录 (耗时 0.033 秒)

    Peptide binding the KLVFF-sequence of amyloid-beta
    97.
    发明申请
    Peptide binding the KLVFF-sequence of amyloid-beta 审中-公开
    肽结合淀粉样蛋白-β的KLVFF序列

    公开(公告)号：US20020094957A1

    公开(公告)日：2002-07-18

    申请号：US09850061

    申请日：2001-05-08

    发明人： Christer Nordstedt ,  Jan Naslund ,  Johan Thyberg ,  Lars O. Tjernberg ,  Lars Terenius

    IPC分类号： A61K038/10 ,  A61K038/08

    CPC分类号： C07K5/0821 ,  A61K38/00 ,  C07K5/0808 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/101 ,  C07K5/1019 ,  C07K5/1021 ,  C07K5/1024 ,  C07K14/4711 ,  G01N33/6896 ,  G01N2800/2821

    摘要： The invention relates to compounds of formula (I) or (II), which are of interest especially for inhibition of polymerization of amyloid null peptide, as model substances for synthesis of amyloid null peptide-ligands, as tools for the identification of other organic compounds with similar functional properties and/or as ligands for detection of amyloid deposits using e.g., positron emission tomography (PET). Formula (II) is: R1-Anull-Ynull-Leu-Xnull-Znull-Bnull-R2 in which Xnull means any group or amino acid imparting to the compound according to formula (I) the ability to bind to the KLVFF-sequence in amyloid null peptide, or two amino acids imparting the same ability, but with the proviso that one is not proline; Ynull means any amino acid; Znull means any non-acidic amino acid; Anull means a direct bond or an null-amino acid bonded at the carboxyl terminal of the null-carboxy group or a di-, tri-, tetra- or pentapeptide bonded at the carboxyl terminal of the null-carboxy group; Bnull means a direct bond or an null-amino acid bonded at the null-nitrogen or a di-, tri-, tetra- or pentapeptide bonded at the null-nitrogen of the N-terminal null-amino acid; R1 is H or nullCOnullR3 bonded at the null-amino group of Anull; R2 is H, nullOR4 or NR5R6, all bonded to the null-carboxyl group of the null-carboxyterminal of Bnull; R3 and R4 are straight or branched carbon chain of 1-4 carbon atoms; R5 and R6 are independently H, alkyl, cycloalkyl, aryl or substituted aryl or together are null(CH2)nnull where n is 4-5; and R1 and R2 together can form a hydrocarbon ring or heterocyclic ring; all null-amino acids being either D- or L-isomers.

    摘要翻译： 本发明涉及式（I）或（II）的化合物，其特别用于抑制淀粉样蛋白β肽的聚合作为淀粉样蛋白β肽配体的合成的模型物质，作为鉴定其它有机化合物的工具 具有类似的功能性质和/或用于使用例如正电子发射断层摄影（PET）检测淀粉样蛋白沉积物的配体。 式（II）是：R1-A'-Y'-Leu-X'-Z'-B'-R2，其中X'表示赋予根据式（I）的化合物的任何基团或氨基酸， 到淀粉样蛋白β肽中的KLVFF序列或赋予相同能力的两个氨基酸，但条件是一个不是脯氨酸; Y'表示任何氨基酸; Z'表示任何非酸性氨基酸; A'是指在α-羧基的羧基末端键合的直接键或α-氨基酸，或在α-羧基的羧基末端键合的二，三，四或五肽; B'是指在α-氮键合键或在N-末端α-氨基酸的α-氮键合的二 - ，三 - ，四 - 或五肽的直接键或α-氨基酸; R1是在A'的α-氨基键合的H或-CO-R3; R2是H，-OR4或NR5R6，均与B'的α-羧基末端的α-羧基键合; R3和R4是1-4个碳原子的直链或支链碳链; R 5和R 6独立地为H，烷基，环烷基，芳基或取代的芳基，或一起为 - （CH 2）n - ，其中n为4-5; 并且R 1和R 2可以一起形成烃环或杂环; 所有α-氨基酸都是D-或L-异构体。

    Melanocortin receptor ligands and methods of using same
    98.
    发明授权
    Melanocortin receptor ligands and methods of using same 失效
    黑皮质素受体配体及其使用方法

    公开(公告)号：US06350430B1

    公开(公告)日：2002-02-26

    申请号：US09027108

    申请日：1998-02-20

    申请人： Colette T. Dooley ,  Beverly E. Girten ,  Richard A. Houghten

    发明人： Colette T. Dooley ,  Beverly E. Girten ,  Richard A. Houghten

    IPC分类号： A61K5100

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/1019 ,  C07K5/1024 ,  C07K5/1027 ,  C07K14/68

    摘要： The invention provides ligands for melanocortin receptors. For example, the invention provides the melanocortin receptor peptide ligand Ac-Nlc-Gln-His-(p(I)-D-Phe)-Arg-(D-Trp)-Cly-NH2, (SEQ ID NO: 1), where the iodo group is unlabeled or radioactively labeled. The invention additionally provides methods of assaying for melanocortin receptors in a cell or tissue such as brain. The invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a melanocortin receptor ligand and to methods of administering the pharmaceutical composition to a subject. The invention further provides tetrapeptide ligands for melanocortin receptors and methods of altering melanocortin receptor activity.

    摘要翻译： 本发明提供黑皮质素受体的配体。 例如，本发明提供黑皮质素受体肽配体Ac-Nlc-Gln-His-（p（I）-D-Phe）-Arg-（D-Trp）-Cly-NH 2，（SEQ ID NO：1） 其中碘基团未标记或放射性标记。 本发明另外提供了测定细胞或组织如脑中黑皮质素受体的方法。 本发明还涉及包含药学上可接受的载体和黑皮质素受体配体的药物组合物以及向受试者施用该药物组合物的方法。 本发明还提供了黑皮质素受体的四肽配体和改变黑皮质素受体活性的方法。

    Peptide binding the KLVFF-sequence of amyloid-&bgr;
    100.
    发明授权
    Peptide binding the KLVFF-sequence of amyloid-&bgr; 失效
    肽结合淀粉样蛋白-β的KLVFF序列

    公开(公告)号：US06331440B1

    公开(公告)日：2001-12-18

    申请号：US09095106

    申请日：1998-06-10

    申请人： Christer Nordstedt ,  Jan Näslund ,  Johan Thyberg ,  Lars O. Tjernberg ,  Lars Terenius

    发明人： Christer Nordstedt ,  Jan Näslund ,  Johan Thyberg ,  Lars O. Tjernberg ,  Lars Terenius

    IPC分类号： G01N33566

    CPC分类号： C07K5/0821 ,  A61K38/00 ,  C07K5/0808 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/101 ,  C07K5/1019 ,  C07K5/1021 ,  C07K5/1024 ,  C07K14/4711 ,  G01N33/6896 ,  G01N2800/2821

    摘要： The invention relates to compounds of formula (I) or (II), which are of interest especially for inhibition of polymerization of amyloid &bgr; peptide, as model substances for synthesis of amyloid &bgr; peptide-ligands, as tools for the identification of other organic compounds with similar functional properties and/or as ligands for detection of amyloid deposits using e.g., positron emission tomography (PET). Formula (II) is: R1—A′—Y′—Leu—X′—Z′—B′—R2 in which X′ means any group or amino acid imparting to the compound according to formula (I) the ability to bind to the KLVFF-sequence in amyloid &bgr; peptide, or two amino acids imparting the same ability, but with the proviso that one is not proline; Y′ means any amino acid; Z′ means any non-acidic amino acid; A′ means a direct bond or an &agr;-amino acid bonded at the carboxyl terminal of the &agr;-carboxy group or a di-, tri-, tetra- or pentapeptide bonded at the carboxyl terminal of the &agr;-carboxy group; B′ means a direct bond or an &agr;-amino acid bonded at the &agr;-nitrogen or a di-, tri-, tetra- or pentapeptide bonded at the &agr;-nitrogen of the N-terminal &agr;-amino acid; R1 is H or —CO—R3 bonded at the &agr;-amino group of A′; R2 is H, —OR4 or NR5R6, all bonded to the &agr;-carboxyl group of the &agr;-carboxyterminal of B′; R3 and R4 are straight or branched carbon chain of 1-4 carbon atoms; R5 and R6 are independently H, alkyl, cycloalkyl, aryl or substituted aryl or together are —(CH2)n— where n is 4-5; and R1 and R2 together can form a hydrocarbon ring of heterocyclic ring; all &agr;-amino acids being either D- or L-isomers.

    摘要翻译： 本发明涉及式（I）或（II）的化合物，其特别用于抑制淀粉样蛋白β肽的聚合作为淀粉样蛋白β肽配体的合成的模型物质，作为鉴定其它有机化合物的工具 具有类似的功能性质和/或用于使用例如正电子发射断层摄影（PET）检测淀粉样蛋白沉积物的配体。 式（II）是：R1-A'-Y'-Leu-X'-Z'-B'-R2，其中X'表示赋予根据式（I）的化合物的任何基团或氨基酸， 到淀粉样蛋白β肽中的KLVFF序列或赋予相同能力的两个氨基酸，但条件是一个不是脯氨酸; Y'表示任何氨基酸; Z'表示任何非酸性氨基酸; A'是指在α-羧基的羧基末端键合的直接键或α-氨基酸，或在α-羧基的羧基末端键合的二，三，四或五肽; B'是指在α-氮键合键或在N-末端α-氨基酸的α-氮键合的二 - ，三 - ，四 - 或五肽的直接键或α-氨基酸; R1是在A'的α-氨基键合的H或-CO-R3; R2是H，-OR4或NR5R6，均与B'的α-羧基末端的α-羧基键合; R3和R4是1-4个碳原子的直链或支链碳链; R 5和R 6独立地为H，烷基，环烷基，芳基或取代的芳基，或一起为 - （CH 2）n - ，其中n为4-5; R1和R2一起可以形成杂环的烃环; 所有α-氨基酸都是D-或L-异构体。