Formulation containing novel anti-inflammatory androstane derivative
    21.
    发明授权
    Formulation containing novel anti-inflammatory androstane derivative 失效
    含有新型抗炎雄甾烷衍生物的制剂

    公开(公告)号:US06750210B2

    公开(公告)日:2004-06-15

    申请号:US10066964

    申请日:2002-02-04

    申请人: Keith Biggadike

    发明人: Keith Biggadike

    IPC分类号: A61K3158

    摘要: There is provided a pharmaceutical aerosol formulation comprising (i) a compound of formula (I) or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant; and characterized in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.

    摘要翻译: 提供了药物气溶胶制剂,其包含(i)式(I)化合物或其溶剂合物作为药物,(ii)液化氢氟烷烃(HFA)气体作为推进剂; 其特征在于式(I)化合物或其溶剂化物完全溶解在制剂中。

    Anti-inflammatory androstane derivatives
    22.
    发明授权
    Anti-inflammatory androstane derivatives 有权
    抗炎雄甾烷衍生物

    公开(公告)号:US06537983B1

    公开(公告)日:2003-03-25

    申请号:US10066961

    申请日:2002-02-04

    IPC分类号: A61K3158

    摘要: According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and {overscore (-----)} represents a single or a double bond; and salts and solvates thereof together with a long-acting &bgr;2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.

    摘要翻译: 根据本发明的一个方面,提供了一种用于通过吸入给药的药物制剂,其包含式(I)化合物,其中R 1表示C 1-6烷基或C 1-6卤代烷基; R 2表示-C(= O) - 芳基或 -C(= O) - 杂芳基; R 3表示氢,甲基(其可以是α或β构型)或亚甲基; R 4和R 5相同或不同,各自表示氢或卤素; 和(过量的(-----表示单键或双键;以及其与长效β2-肾上腺素受体激动剂的盐和溶剂合物),该制剂在治疗呼吸道炎症性疾病中具有治疗上有用的作用 24小时以上。

    17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
    28.
    发明授权
    17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents 失效
    17β-硫代硫酸钠17α-芳基羰氧基氧基雄甾烷衍生物作为抗炎剂

    公开(公告)号:US07498321B2

    公开(公告)日:2009-03-03

    申请号:US10343842

    申请日:2001-08-03

    CPC分类号: C07J31/006

    摘要: There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and——represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

    摘要翻译: 根据本发明提供式(I)化合物,其中R 1表示C 1-6烷基或C 1-6卤代烷基; R 2表示-C( - ) - 芳基或-C(-O) - 杂芳基; R3表示氢,甲基(其可以是α或β构型)或亚甲基; R4和R5相同或不同,各自表示氢或卤素; 和 - 表示单键或双键; 及其盐和溶剂合物。 还提供了制备式(I)化合物的方法和该化合物在治疗中的用途,特别是用于治疗炎性和过敏性疾病。

    17.Beta.-Fluoromethoxycarbonyl-Androst-4-En-3-One Compounds With a 17.Alpha.-Carbonate Sustituent
    30.
    发明申请
    17.Beta.-Fluoromethoxycarbonyl-Androst-4-En-3-One Compounds With a 17.Alpha.-Carbonate Sustituent 审中-公开
    17.具有17.Alpha.-碳酸酯稳定性的β-甲氧基羰基 - 雄甾-4-烯-3-酮化合物

    公开(公告)号:US20080249077A1

    公开(公告)日:2008-10-09

    申请号:US12093613

    申请日:2006-11-13

    CPC分类号: C07J3/005

    摘要: The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched chain alkyl, C3-C8 cycloalkyl optionally substituted by one or more groups independently selected from C1-C3 alkyl and methoxy, C4-C6 cycloalkylmethyl wherein the methyl group is optionally substituted by a group selected from methyl or ethyl, or a bicycloalkyl group optionally substituted by one or more methyl groups; R2 represents hydrogen, a methyl group, which may be in either the a or D configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; physiologically acceptable solvates thereof, pharmaceutical compositions thereof, methods of treatment using such compounds, and processes for preparing such compounds.

    摘要翻译: 本发明涉及式(I)的化合物:其中R 1表示C 4 -C 7支链烷基,C 表示单键或双键; 其生理上可接受的溶剂化物,其药物组合物,使用这些化合物的治疗方法,以及制备这些化合物的方法。