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    BETA-HAIRPIN PEPTIDOMIMETICS
    1.
    发明申请
    BETA-HAIRPIN PEPTIDOMIMETICS 有权

    公开(公告)号：US20150218219A1

    公开(公告)日：2015-08-06

    申请号：US14406108

    申请日：2012-06-06

    申请人： Frank Otto Gombert ,  Daniel Obrecht ,  Alexander Lederer ,  Johann Zimmermann ,  Christian Oefner

    发明人： Frank Otto Gombert ,  Daniel Obrecht ,  Alexander Lederer ,  Johann Zimmermann ,  Christian Oefner

    IPC分类号： C07K7/54

    CPC分类号： A61K38/12 ,  A61K38/00 ,  C07K7/08 ,  C07K7/54

    摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.

    摘要翻译： 通式为（-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-）的平滑肽模拟物，Cys4之间的二硫键 和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa3，Xaa6，Xaa8 Xaa13，Xaa14和Xaa15具有有利的药理学性质，并且可用于预防HIV感染 健康个体或减慢和停止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。 这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法来制造。

    Novel factor viia inhibiting compounds
    3.
    发明申请
    Novel factor viia inhibiting compounds 审中-公开
    新型因子viia抑制化合物

    公开(公告)号：US20060084614A1

    公开(公告)日：2006-04-20

    申请号：US10541347

    申请日：2004-01-05

    申请人： Robert Eckl ,  Lutz Weber ,  Christian Oefner

    发明人： Robert Eckl ,  Lutz Weber ,  Christian Oefner

    IPC分类号： A61K31/704 ,  C07H17/00

    CPC分类号： C07H15/203 ,  A61K31/7034

    摘要： The present invention relates to new compounds of formula (I): These compounds are very effective factor VIIa inhibitors and are therefore of interest in the treatment and/or prevention of thromboses, stroke, heart attack, inflammation, arteriosclerosis and tumour conditions.

    摘要翻译： 本发明涉及式（I）的新化合物：这些化合物是非常有效的因子VIIa抑制剂，因此对治疗和/或预防血栓形成，中风，心脏病发作，炎症，动脉硬化和肿瘤状况感兴趣。

    Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
    5.
    发明申请
    Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE) 审中-公开
    抑制二肽基肽酶（DPP-IV）和尿丙氨酸（NEP）和/或血管紧张素转换酶（ACE）的新型化合物

    公开(公告)号：US20060046978A1

    公开(公告)日：2006-03-02

    申请号：US10930606

    申请日：2004-08-31

    申请人： Sabine Pierau ,  Christian Oefner ,  Glenn Dale

    发明人： Sabine Pierau ,  Christian Oefner ,  Glenn Dale

    IPC分类号： A61K31/69 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/4196 ,  A61K31/401 ,  A61K31/165

    CPC分类号： C07D209/20

    摘要： This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.

    摘要翻译： 本发明涉及抑制二肽基肽酶（特别是DPP-IV）和尿丙氨酸（NEP，中性内肽酶）以及二肽基肽酶（特别是DPP-IV）和血管紧张素转化酶（ACE）和/ 或二肽基肽酶（特别是DPP-IV）和血管肽酶（尤其是ACE和NEP）。 这些化合物及其药物组合物可用于治疗以及预防2型糖尿病。