17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
    31.
    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
    32.
    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。

    Benzothiophen and thiochrone containing phenethanolamine derivatives for the treatment of respiratory disorders
    34.
    发明申请
    Benzothiophen and thiochrone containing phenethanolamine derivatives for the treatment of respiratory disorders 失效
    苯并噻吩和含硫酚的苯乙醇胺衍生物用于治疗呼吸系统疾病

    公开(公告)号:US20070172385A1

    公开(公告)日:2007-07-26

    申请号:US10595997

    申请日:2004-12-15

    申请人: Keith Biggadike

    发明人: Keith Biggadike

    IPC分类号: A61M1/00

    CPC分类号: C07D333/54 C07D335/06

    摘要: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).

    摘要翻译: 式(I)化合物及其盐,溶剂化物和生理功能衍生物可用于预防或治疗选择性β2 - 肾上腺素受体激动剂的临床病症,例如哮喘 或慢性阻塞性肺疾病(COPD)。

    Glucocorticosteroid compound having anti-inflammatory activity
    38.
    发明授权
    Glucocorticosteroid compound having anti-inflammatory activity 有权
    具有消炎活性的糖皮质激素化合物

    公开(公告)号:US07638508B2

    公开(公告)日:2009-12-29

    申请号:US11863390

    申请日:2007-09-28

    IPC分类号: A61K31/56 C07J3/00

    摘要: A compound of formula (I): wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the α or β configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and  represents a single or a double bond; or a physiologically acceptable salt or solvate thereof, and pharmaceutical formulations and methods of use thereof.

    摘要翻译: 式(I)的化合物:其中X表示O或S; R 1表示C 1-6烷基,C 3-8环烷基,C 3-8环烷基甲基或C 3-8环烯基,其任选可以被一个或多个甲基或卤素原子取代,或者R 1表示芳基,取代的芳基,杂芳基或取代的杂芳基; R 2表示氢,甲基,其可以是α或β构型,或亚甲基; R3和R4相同或不同,各自独立地表示氢,卤素或甲基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”4.57mm“file =”US07638508-20091229-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>表示单键或双键; 或其生理上可接受的盐或溶剂化物,以及药物制剂及其使用方法。

    Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions
    40.
    发明申请
    Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions 审中-公开
    用于治疗炎症和过敏症状的雄激素17-α-碳酸酯

    公开(公告)号:US20090124588A1

    公开(公告)日:2009-05-14

    申请号:US11813230

    申请日:2006-01-01

    CPC分类号: C07J41/0094 C07J3/005

    摘要: The present invention is directed to compounds of formula (I): wherein R1 represents a 1,1-dimethylethyl group or a 1,1-dimethylpropyl group and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

    摘要翻译: 本发明涉及式(I)的化合物:其中R1表示1,1-二甲基乙基或1,1-二甲基丙基及其生理学上可接受的溶剂化物,其生理功能衍生物,包含该化合物的药物组合物, 的用于制造药物的化合物,特别是用于治疗炎性和/或过敏性病症,化合物的制备方法和化合物的制备方法中的化学中间体。