Sulfonamide containing compounds for treatment of inflammatory disorders
    1.
    发明授权
    Sulfonamide containing compounds for treatment of inflammatory disorders 失效
    含磺酰胺的化合物用于治疗炎症性疾病

    公开(公告)号:US07897776B2

    公开(公告)日:2011-03-01

    申请号:US12148966

    申请日:2008-04-23

    IPC分类号: C07D421/00 C07D207/00

    摘要: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof: wherein: X and Y are independently selected from —CH2— or —CH2—CH2—; Z is selected from S(O)m or Se(O)m and m is 0, 1 or 2; R1 is optionally substituted heteroaryl or heterocyclic; R2 is selected from the group consisting of hydrogen, C1-C6 straight alkyl, and C1-C6 branched alkyl, wherein all may be optionally substituted; and R3 and R4 are alkyl.

    摘要翻译: 提供化合物,药物组合物和治疗或预防炎性病症,特别是哮喘的方法。 所述化合物具有通式I或其药学上可接受的盐,酯,前药或衍生物:其中:X和Y独立地选自-CH 2 - 或-CH 2 -CH 2 - ; Z选自S(O)m或Se(O)m,m为0,1或2; R1是任选取代的杂芳基或杂环; R 2选自氢,C 1 -C 6直链烷基和C 1 -C 6支链烷基,其中全部可以被任选取代; R3和R4是烷基。

    Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
    10.
    发明授权
    Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators 失效
    含有四环衍生物的杂原子作为选择性雌激素受体调节剂

    公开(公告)号:US07329654B2

    公开(公告)日:2008-02-12

    申请号:US10307735

    申请日:2002-12-02

    CPC分类号: C07D493/04

    摘要: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

    摘要翻译: 本发明涉及新颖的含杂原子的四环衍生物,含有它们的药物组合物,它们在治疗和/或预防由一种或多种雌激素受体介导的障碍及其制备方法中的用途。 本发明的化合物可用于治疗和/或预防与雌激素消耗相关的疾病,例如潮热,阴道干燥,骨质减少和骨质疏松症; 激素敏感性癌症和乳腺,子宫内膜,子宫颈和前列腺增生; 子宫内膜异位症,子宫肌瘤,骨关节炎和避孕药,单独或与孕激素或孕激素拮抗剂联合使用。