INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL
    12.
    发明公开
    INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL 审中-公开
    IONENKANALHEMMUNG DESÜBERGANGSREZEPTORPOTENTIALSA1

    公开(公告)号:EP2945947A4

    公开(公告)日:2016-07-27

    申请号:EP14741091

    申请日:2014-01-17

    申请人: CUBIST PHARM INC

    IPC分类号: C07D473/08 C07F9/00

    CPC分类号: C07D473/08 C07F9/092

    摘要: Provided herein are pharmaceutical compositions and methods for the treatment of pain, respiratory conditions, including chronic or inflammatory pain, asthma or COPD as well as inhibiting the Transient Receptor Potential Al (TRPA1 ) ion channel. The compounds include tetrahydropurinyl alpha-methyl amide derivatives containing heterocyclic moieties such as pyridinyl, pyrimidinyl, pyrazinyl, and pyrrolidinyl. One such example includes (S)-2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-((S)-2-(trifluoromethyl)pyrrolidin-1-yl)pyrimidin-5-yl)pyrazin-2-yl)propanamide.

    摘要翻译: 本文提供了用于治疗疼痛,呼吸病症(包括慢性或炎性疼痛,哮喘或COPD)以及抑制瞬时受体电位Al(TRPA1)离子通道的药物组合物和方法。 所述化合物包括含有杂环部分的四氢嘌呤基α-甲基酰胺衍生物,例如吡啶基,嘧啶基,吡嗪基和吡咯烷基。 一个这样的实例包括(S)-2-(1,3-二甲基-2,6-二氧代-1,2,3,6-四氢-7H-嘌呤-7-基)-N-(6-(2- ((S)-2-(三氟甲基)吡咯烷-1-基)嘧啶-5-基)吡嗪-2-基)丙酰胺。