STRUKTURMIMETIKA PROLINREICHER PEPTIDE UND IHRE VERWENDUNG

    公开(公告)号:EP2747764A1

    公开(公告)日:2014-07-02

    申请号:EP12753111.9

    申请日:2012-08-24

    摘要: The invention relates to compounds that can be used in particular as structural mimetics of proline-rich peptides and accordingly are able to bind PRM (proline-rich motif) binding domains of proteins. The invention further relates to the use of said compounds as pharmaceutical active ingredients and to the use of the pharmaceutical active ingredients to treat bacterial diseases, neurodegenerative diseases, and tumors.

    摘要翻译: 取代的桥接肽化合物(I)是新的。 式(I)的取代的桥连肽化合物是新的。 X:O或S; A1,B1:环桥; Y1:H,烷基,氟烷基或(杂)芳基; Z 1,Z 2:H,羰基,OH,O-烷基,O-酰基或N-R 11 R 12; R11,R12:H,烷基,酰基,磺酰基,烷基,酰基,氟烷基或(杂)芳基; R1:烷基,酰基,烷氧基羰基,芳氧基羰基或氨基羰基; 和R 2:H,烷基,芳基,烷基羰基,芳基羰基,烷氧基羰基,氨基羰基,芳氧基羰基,烷基磺酰基,芳基磺酰基,氨基酰基或肽基。 对于包含(I)和载体的组合物,包括独立权利要求。 活动:神经保护; 抗菌; 解热; 内分泌根; 妇科; 止泻; 精神药物; 抗帕金森氏病; 镇惊; 抑制细胞生长。 作用机理:Src同源性3结构域结构; WW域粘合剂,Ena-VASP同源性1结构域结合物; GYF结构域结合剂; UEV域绑定器 Profilin粘合剂

    INHIBITOREN ZUR HEMMUNG DER TUMORMETASTASIERUNG
    2.
    发明公开
    INHIBITOREN ZUR HEMMUNG DER TUMORMETASTASIERUNG 审中-公开
    INHIBITORENZEN ZUR HEMMUNG DER TUMORMETASTASIERUNG

    公开(公告)号:EP3230300A1

    公开(公告)日:2017-10-18

    申请号:EP15808218.0

    申请日:2015-12-11

    IPC分类号: C07K5/12 A61K31/55 A61P35/00

    CPC分类号: C07K7/06 A61K38/00 C07D519/00

    摘要: The invention relates to chemical compounds that can be used in particular as structural mimetics of proline-rich peptides. The compounds of the invention are capable of selectively inhibiting ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of said compounds as pharmaceutical active substances and to the use of the pharmaceutical active substances to treat tumor diseases. The chemical compounds of the invention can strongly inhibit the chemotaxis and motility of invasive tumor cells and thus can be used in the treatment and/or prevention of tumor metastases.

    摘要翻译: 本发明涉及可特别用作富含脯氨酸肽的结构模拟物的化学化合物。 本发明的化合物能够选择性地抑制ena / VASP-EVH1介导的蛋白质 - 蛋白质相互作用。 本发明进一步涉及所述化合物作为药物活性物质的用途以及药物活性物质用于治疗肿瘤疾病的用途。 本发明的化学化合物可强烈抑制侵袭性肿瘤细胞的趋化性和运动性,因此可用于治疗和/或预防肿瘤转移。

    VORRICHTUNG UND VERFAHREN ZUR ZUORDNUNG DER NMR-SIGNALE VON POLYPETIDEN
    5.
    发明公开
    VORRICHTUNG UND VERFAHREN ZUR ZUORDNUNG DER NMR-SIGNALE VON POLYPETIDEN 审中-公开
    装置和方法进行分配POLYPETIDEN的NMR信号的

    公开(公告)号:EP1425571A1

    公开(公告)日:2004-06-09

    申请号:EP02777009.8

    申请日:2002-09-05

    IPC分类号: G01N24/08 G01R33/465

    CPC分类号: G01R33/465 G01N24/08

    摘要: NMR spectroscopy is being used increasingly to determine the structure of proteins. According to the invention, cross-signal pattern search masks are used to jointly evaluate 3D triple resonance experiments and the amino acid type-specific 2D spectra. By means of pattern identification, the inventive cross-signal pattern search masks allow all signal peaks caused by one or a group of amino acids, whose exact sequence has previously been derived from the protein sequence and which form the basis for the specific pattern identification, to be jointly detected and evaluated. The invention permits the fully-automated assignment of the signal peaks occurring in the various spectra to the magnetically active nuclei of the protein.