EOSINOPHIL EOTAXIN RECEPTOR
    1.
    发明申请
    EOSINOPHIL EOTAXIN RECEPTOR 审中-公开
    EOSINOPHIL爱可酮受体

    公开(公告)号:WO1997041154A1

    公开(公告)日:1997-11-06

    申请号:PCT/US1997006568

    申请日:1997-04-24

    发明人: MERCK & CO., INC.

    IPC分类号: C07K14/705

    CPC分类号: C07K14/7158 A61K38/00

    摘要: The eosinophil eotaxin receptor has been isolated, cloned and sequenced. This receptor is a human beta -chemokine receptor and has been designated "CC CKR3". The eosinophil eotaxin receptor may be used to screen and identify compounds that bind to the eosinophil eotaxin receptor. Such compounds would be useful in the treatment and prevention of atopic conditions including allergic rhinitis, dermatis, conjunctivitis, and particularly bronchial asthma.

    摘要翻译: 已经分离,克隆和测序嗜酸性粒细胞嗜酸性粒细胞趋化因子受体。 该受体是人β-胆碱酯受体,被称为“CC CKR3”。 嗜酸性粒细胞嗜酸性粒细胞趋化因子受体可用于筛选和鉴定结合嗜酸性粒细胞嗜酸性粒细胞趋化嗜酸性粒细胞趋化因子受体的化合物。 这些化合物可用于治疗和预防特应性疾病,包括过敏性鼻炎,皮肤病,结膜炎,特别是支气管哮喘。

    ISOMETHEPTENE ISOMER
    2.
    发明申请
    ISOMETHEPTENE ISOMER 审中-公开
    异构体异构体

    公开(公告)号:WO2014113734A3

    公开(公告)日:2014-11-27

    申请号:PCT/US2014012142

    申请日:2014-01-17

    摘要: The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), (Formula (I)) or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)- Isometheptene crystals data of X-ray crystallography are presented.

    摘要翻译: 本发明涉及包含根据式(I),(式(I))的结构或盐酸盐或其药学上可接受的加成盐的纯化的异美汀化合物。 特别地,本公开涉及异美金属异构体粘酸盐晶体2的合成,纯化和表征,其中异美金属异构体2分别立体化学表征为(R) - 对映体。 Isometheptene(R) - 对映体活性表示咪唑啉亚型1(I1)受体位点的选择性中心作用选择性配体; 更具体地说,本公开内容提供了用于治疗偏头痛和其他神经血管疼痛或神经源性疼痛免受腹部痛苦的抗高血压组合物。 (R) - 异美辛对映异构体或异构体2可以是与外消旋体形式相比具有较低副作用的抗高血压剂。 因此(R)-Isometheptene被认为对发作性紧张型头痛(ETTH)有效。 据信(R)-Isometheptene对映异构体或异构体2可有效降低血压,单独使用或与其他头痛改善药物一起使用。 描述了合成和处理的方法。 关于(R) - 异美斯汀晶体的X射线晶体学数据的介绍。

    ISOMETHEPTENE ISOMER
    4.
    发明申请
    ISOMETHEPTENE ISOMER 审中-公开
    异构异构体

    公开(公告)号:WO2014113734A2

    公开(公告)日:2014-07-24

    申请号:PCT/US2014/012142

    申请日:2014-01-17

    摘要: The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), (Formula (I)) or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)- Isometheptene crystals data of X-ray crystallography are presented.

    摘要翻译: 本发明涉及包含根据式(I),(式(I))或盐酸盐的结构或其药学上可接受的加成盐的纯化异构体化合物。 特别地,本公开涉及异葎草酮异构体粘蛋白晶体2的合成,纯化和表征,其中异构异构体异构体2分别被立体化学表征为(R) - 对映异构体。 对映异构体异构体活性表示咪唑啉亚型1(I1)受体位点的选择性中心作用选择性配体; 并且更具体地,本公开提供了用于治疗偏头痛和其他神经血管或神经源性疼痛的抗高血压组合物。 (R) - 异亚丙基对映异构体或异构体2可以是具有低于外消旋形式的副作用的抗高血压剂。 因此(R) - 美沙芬被认为对于发作型紧张型头痛(ETTH)有效。 据信(R) - 异构体异构体2有效地降低血压,单独使用或与其他头痛改善药物一起使用。 描述合成和处理方法。 关于(R) - 异构体色素晶体的X射线晶体学数据。