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    Non-peptide bradykinin antagonists and pharmaceutical compositions therefrom
    2.
    发明授权
    Non-peptide bradykinin antagonists and pharmaceutical compositions therefrom 有权
    非肽缓激肽拮抗剂及其药物组合物

    公开(公告)号：US07645759B2

    公开(公告)日：2010-01-12

    申请号：US11786041

    申请日：2007-04-10

    申请人： Patrizia Felicetti ,  Christopher Ingo Fincham ,  Alessandro Giolitti ,  Carlo Alberto Maggi ,  Laura Quartara ,  Cristina Rossi

    发明人： Patrizia Felicetti ,  Christopher Ingo Fincham ,  Alessandro Giolitti ,  Carlo Alberto Maggi ,  Laura Quartara ,  Cristina Rossi

    IPC分类号： A61K31/4709 ,  C07D405/12 ,  A61K31/47 ,  C07D215/26

    CPC分类号： C07D215/26

    摘要： Non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor are disclosed. The compounds have the general formula (I) in which R is hydrogen or methyl; W is a single bond or an oxygen atom; n=3; X is hydrogen or a —NR1R2 amino group in which R1 and R2 can be independently hydrogen or a group which is methyl, ethyl, n-propyl, or isopropyl; Y is a —NR3R4R5 quaternary ammonium group in which R3, R4, R5 can be independently a group which is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or n-pentyl; and the enantiomers and enantiomeric mixtures thereof. Pharmaceutical compositions containing these compounds and methods of using the compounds to treat patients having conditions, disorders or diseases involving activation of bradykinin B2 receptors are also disclosed.

    摘要翻译： 具有活性作为缓激肽（BK）B2受体的选择性拮抗剂的非肽化合物被公开。 所述化合物具有通式（I），其中R是氢或甲基; W是单键或氧原子; n = 3; X是氢或-NR 1 R 2氨基，其中R 1和R 2可以独立地是氢或甲基，乙基，正丙基或异丙​​基的基团; Y是-NR 3 R 4 R 5季铵基，其中R 3，R 4，R 5可以独立地是甲基，乙基，正丙基，异丙基，正丁基，异丁基或正戊基的基团。 及其对映体和对映体混合物。 还公开了含有这些化合物的药物组合物和使用该化合物治疗患有缓激肽B2受体活化的病症或病症或疾病的患者的方法。