NITRIC OXIDE RELEASING STEROIDS
    44.
    发明申请
    NITRIC OXIDE RELEASING STEROIDS 有权
    硝酸氧化物释放甾体

    公开(公告)号:US20100093685A1

    公开(公告)日:2010-04-15

    申请号:US12525970

    申请日:2008-01-28

    CPC分类号: C07J41/005

    摘要: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R-(Z)a-Rx  (I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position α or β; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

    摘要翻译: 本发明涉及通式(I)的糖皮质激素及其药学上可接受的盐或立体异构体的硝基氧基衍生物R-(Z)a-Rx(I)其中R是式(II)的皮质类固醇残基:其中:R1是OH,R2 -CH 3或R 1和R 2一起形成式(III)的基团,R 3为Cl或F; R4是H或F; 其中R 1,R 2,R 3和R 4可以连接到甾族结构在位置α或bgr中的相应碳原子。 条件是:当R 1和R 2是式(III)的基团时,R 3是F且R 4是H或F; 该化合物可用于治疗呼吸系统疾病,炎性疾病,皮肤病和眼部疾病。

    NITRIC OXIDE RELEASING STEROIDS
    47.
    发明申请
    NITRIC OXIDE RELEASING STEROIDS 审中-公开
    硝酸氧化物释放甾体

    公开(公告)号:US20100041633A1

    公开(公告)日:2010-02-18

    申请号:US12526005

    申请日:2008-01-28

    CPC分类号: C07J41/005

    摘要: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof wherein R is a corticosteroid residue selected from: The compounds are useful in the treatment of respiratory diseases.

    摘要翻译: 本发明涉及通式(I)的皮质类固醇及其药学上可接受的盐或立体异构体的硝基氧基衍生物,其中R是选自以下的皮质类固醇残基:该化合物可用于治疗呼吸系统疾病。

    Statin derivatives
    48.
    发明申请
    Statin derivatives 有权
    他汀衍生物

    公开(公告)号:US20070072942A1

    公开(公告)日:2007-03-29

    申请号:US11590770

    申请日:2006-11-01

    IPC分类号: A61K31/21 C07C203/00

    摘要: Statin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for treating and/or preventing several diseases, in particular coronary syndromes, neurodegenerative disorders as well as for reducing cholesterol levels.

    摘要翻译: 描述了具有改善的药理活性和增强的耐受性的他汀类硝基衍生物。 它们可用于治疗和/或预防多种疾病,特别是冠状动脉综合征,神经变性疾病以及降低胆固醇水平。

    Process for the preparation of naproxene nitroxyalkylesters
    49.
    发明申请
    Process for the preparation of naproxene nitroxyalkylesters 有权
    制备萘普生硝基烷基酯的方法

    公开(公告)号:US20050119339A1

    公开(公告)日:2005-06-02

    申请号:US10625558

    申请日:2003-07-24

    CPC分类号: C07C201/02 C07C203/04

    摘要: A process for obtaining nitroxyalklesters of the 2(S)(6-methoxy-2-naphthyl)-propanoic acid having an enantiomeric excess higher than or equal to 95%, preferably higher than or equal to 98%, characterized in that an halide of the 2-(S)-(6 methoxy-2-naphthyl)propanoic acid of formula A-Hal, wherein A is the acid acyl residue, is reacted in an inert orgariic solvent with an aliphatic nitroxyalkanol HO—Y—ONO2, wherein Y is a C2-C20 alkylene or a cycloalkylene from 3 to 8 carbon atoms, or an alkylene as defined containing a cycloalkylene as defined, in the presence of an inorganic base.

    摘要翻译: 一种获得具有高于或等于95%,优选高于或等于98%的对映异构体过量的2(S)(6-甲氧基-2-萘基) - 丙酸的硝基螺旋体的方法,其特征在于, 其中A是酸酰基残基的式A-Hal的2-(S) - (6-甲氧基-2-萘基)丙酸在惰性溶剂中与脂族硝基链烷醇HO-Y-ONO 2,其中Y是C 2 -C 20亚烷基或3至8个碳原子的亚环烷基,或如所定义的含有如所定义的亚环烷基的亚烷基 在无机碱存在下进行。