Chemical compounds
    7.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号:US08354406B2

    公开(公告)日:2013-01-15

    申请号:US13273408

    申请日:2011-10-14

    IPC分类号: C07D401/04 A61K31/445

    摘要: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    摘要翻译: 本发明涉及新的吲哚甲酰胺衍生物。 具体地说,本发明涉及式I化合物:其中R1,R2,R3,U和V定义如下,及其药学上可接受的盐。 本发明的化合物是IKK2的抑制剂,并且可用于治疗与不适当的IKK2(也称为IKK&bgr)活性相关的疾病,例如类风湿性关节炎,哮喘和COPD(慢性阻塞性肺疾病)。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

    Dual pharmacophores—PDE4-muscarinic antagonistics
    9.
    发明授权
    Dual pharmacophores—PDE4-muscarinic antagonistics 失效
    双重药效学 - PDE4-毒蕈碱拮抗剂

    公开(公告)号:US08067408B2

    公开(公告)日:2011-11-29

    申请号:US12365934

    申请日:2009-02-05

    CPC分类号: C07D471/04

    摘要: The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

    摘要翻译: 本发明涉及式(I)的新型化合物,其药物组合物及其在治疗中的用途,例如作为IV型磷酸二酯酶(PDE4)的抑制剂和毒蕈碱性乙酰胆碱受体(mAChR)的拮抗剂,用于治疗和/ 或预防呼吸系统疾病,包括抗炎和/或过敏性疾病如慢性阻塞性肺疾病(COPD),哮喘,鼻炎(例如过敏性鼻炎),特应性皮炎或牛皮癣。