Compounds with NEP/MP-inhibitory activity and uses thereof
    1.
    发明申请
    Compounds with NEP/MP-inhibitory activity and uses thereof 审中-公开
    具有NEP / MP抑制活性的化合物及其用途

    公开(公告)号:US20040162345A1

    公开(公告)日:2004-08-19

    申请号:US10715112

    申请日:2003-11-18

    IPC分类号: A61K031/185

    CPC分类号: A61K31/55 A61K31/00

    摘要: Compounds having combined, particularly concurrent, inhibitory activity on neutral endopeptidase (NEP) and on a novel metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, and related methods for treating and for the manufacture of a pharmaceutical composition for a mammal, preferably a larger mammal such as a human, suffering from or being susceptible to a disease or condition which can be alleviated or inhibited by combined or concurrent inhibition of NEP and IGS5. Treatments for diseases or conditions where big-ET-1 levels are elevated, or where ET-1 is upregulated, where such diseases or conditions can be alleviated or inhibited by combined or concurrent inhibition of NEP and IGS5.

    摘要翻译: 对中性内肽酶(NEP)和指定为IGS5的新型金属蛋白酶或其药学上可接受的盐或溶剂合物或生物不稳定酯具有组合,特别并发的抑制活性的化合物,以及用于治疗和制备药物组合物的相关方法 哺乳动物,优选较大的哺乳动物(例如人)患有或易患有疾病或病症,可以通过NEP和IGS5的组合或同时抑制而被缓解或抑制。 治疗大ET-1水平升高或ET-1上调的疾病或病症,其中可以通过NEP和IGS5的组合或同时抑制来缓解或抑制这些疾病或病症。

    3-Phenyl-3,7-diazabicyclo[3.3.1] nonane compounds, process for preparing them, pharmaceutical compositions containing them and use thereof to inhibit cardiac arrhythmia
    2.
    发明申请
    3-Phenyl-3,7-diazabicyclo[3.3.1] nonane compounds, process for preparing them, pharmaceutical compositions containing them and use thereof to inhibit cardiac arrhythmia 有权
    3-苯基-3,7-二氮杂双环[3.3.1]壬烷化合物,其制备方法,含有它们的药物组合物及其用于抑制心律失常的用途

    公开(公告)号:US20030109541A1

    公开(公告)日:2003-06-12

    申请号:US10183038

    申请日:2002-06-27

    IPC分类号: C07D471/02 A61K031/4745

    CPC分类号: C07D471/08 C07D471/10

    摘要: Pharmacologically active compounds of the general formula I 1 wherein R1 is an alkyl group with 1-6 carbon atoms or a cycloalkylalkyl group with 4-7 carbon atoms, R2 is lower alkyl, and R3 is lower alkyl, or R2 and R3 together form an alkylene chain with 3-6 carbon atoms, and R4 represents a phenyl radical monosubstituted in the ortho or para position by nitro, cyano or lower alkanoyl or disubstituted in the ortho and para positions by nitro, and their physiologically compatible acid addition salts are described.

    摘要翻译: 其中R1是具有1-6个碳原子的烷基或具有4-7个碳原子的环烷基烷基的通式I的药理学活性化合物,R 2是低级烷基,R 3是低级烷基,或者R 2和R 3一起形成亚烷基 具有3-6个碳原子的链,R4表示在邻位或对位上由硝基,氰基或低级烷酰基单取代的苯基,或在邻位和对位被二硝基取代,并描述了它们的生理相容的酸加成盐。