16-Keto-17-substituted thia-17-alkyl(or alkenyl or alkynyl) androstenes
    82.
    发明授权
    16-Keto-17-substituted thia-17-alkyl(or alkenyl or alkynyl) androstenes 失效
    16-酮17取代的硫杂-17-烷基(或烯基或炔基)雄甾烯

    公开(公告)号:US4528138A

    公开(公告)日:1985-07-09

    申请号:US622509

    申请日:1984-06-20

    CPC分类号: C07J31/003

    摘要: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, mono-, di- or trifluoroalkyl, ##STR2## aryl or alkylthioalkyl, wherein R.sub.6 is alkyl or aryl and m is 1, 2, 3 or 4;R.sub.2 is ##STR3## wherein R.sub.7, R.sub.8 and R.sub.9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2;with the proviso that if R.sub.1 is alkylthioalkyl, n is 0.

    摘要翻译: 抗炎活性由具有下式的类固醇及其1,2-脱氢衍生物显示,其中R 1为烷基,单 - ,二 - 或三氟烷基,芳基或烷硫基烷基,其中R 6为烷基或芳基,m 是1,2,3或4; R 2是,其中R 7,R 8和R 9各自独立地是氢或1至4个碳原子的烷基; R3是羰基或β-羟基亚甲基; R4是氢或卤素; R5是氢,甲基或氟; 且n为0,1或2; 条件是如果R1是烷硫基烷基,n是0。

    [16,17-a]Cyclopentano pregnenes
    84.
    发明授权
    [16,17-a]Cyclopentano pregnenes 失效
    [16,17-a]环戊烯孕烯

    公开(公告)号:US4474702A

    公开(公告)日:1984-10-02

    申请号:US572495

    申请日:1984-01-20

    CPC分类号: C07J53/002

    摘要: Antiinflammatory activity is exhibited by pregnenes having the structural formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, halogen, or acyloxy;R.sub.2 and R.sub.3 are each hydrogen, R.sub.2 and R.sub.3 are each methyl, R.sub.2 and R.sub.3 are each alkylthio, R.sub.2 is hydrogen and R.sub.3 is alkyl, R.sub.2 is hydroxyl and R.sub.3 is alkyl, or R.sub.2 and R.sub.3 taken together are --(CH.sub.2).sub.2 --, methylene, or oxo; andR.sub.4 is hydrogen, fluorine, chlorine or bromine.

    摘要翻译: 抗炎活性由结构式为“IMAGE”的孕烯显示,其中R1是氢,羟基,卤素或酰氧基; R2和R3各自为氢,R2和R3各自为甲基,R2和R3各自为烷硫基,R2为氢,R3为烷基,R2为羟基,R3为烷基,R2和R3一起为 - (CH2)2- ,亚甲基或氧代; R4是氢,氟,氯或溴。

    Androstene-17-dithioketals
    85.
    发明授权
    Androstene-17-dithioketals 失效
    雄甾烯-17-二硫酮缩酮

    公开(公告)号:US4427592A

    公开(公告)日:1984-01-24

    申请号:US462164

    申请日:1983-04-07

    摘要: Topical antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro, and 6,7-dehydro derivatives thereof, wherein one of R.sub.1 and R.sub.2 is alkyl, aryl, arylalkyl, or cycloalkyl, and the other is alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, mono-, di- or trifluoroalkyl, cyanoalkyl, alkanoylalkyl or ##STR2## wherein n is 1, 2, 3 or 4 and Y.sub.1 and Y.sub.2 are the same or different and each is hydrogen or alkyl;R.sub.3 is hydrogen, hydroxy, alkoxy, aryloxy, oxo, methylene, alkylthio, arylthio, alkanoyl, alkanoyloxy, or fluorine;R.sub.4 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene;R.sub.5 is hydrogen or halogen; andR.sub.6 is hydrogen, methyl, hydroxy, alkanoyl, alkanoyloxy or halogen.

    摘要翻译: 具有式“IMAGE”的类固醇及其1,2-二氢和6,7-脱氢衍生物可表现出局部抗炎活性,其中R1和R2之一为烷基,芳基,芳基烷基或环烷基,另一个为 链烯基,取代的烯基,炔基,取代的炔基,单 - ,二 - 或三氟烷基,氰基烷基,烷酰基烷基或其中n为1,2,3或4,并且Y 1和Y 2相同或不同,各自为氢或烷基 ; R3是氢,羟基,烷氧基,芳氧基,氧代,亚甲基,烷硫基,芳硫基,烷酰基,烷酰氧基或氟; R4是羰基,β-羟基亚甲基或β-乙酰氧基亚甲基; R5是氢或卤素; R 6为氢,甲基,羟基,烷酰基,烷酰氧基或卤素。