11.beta.-Substituted-.DELTA..sup.4,9 -estradienes
    1.
    发明授权
    11.beta.-Substituted-.DELTA..sup.4,9 -estradienes 失效
    11β-取代-TATA 4,9-雌二醇

    公开(公告)号:US4233296A

    公开(公告)日:1980-11-11

    申请号:US867485

    申请日:1978-01-06

    摘要: Novel steroids of the formula ##STR1## wherein R.sub.1 is linear or branched alkyl of 1 to 12 carbon atoms, unsaturated alkyl of 2 to 8 carbon atoms optionally substituted, optionally substituted aryl of 6 to 12 carbon atoms, optionally substituted aralkyl of 7 to 13 carbon atoms and a heterocycle with at least one sulfur or oxygen atom, R.sub.2 is alkyl of 1 to 4 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, hydroxy, acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms, alkoxy of 1 to 8 carbon atoms and acyl of an organic carboxylic acid of 1 to 18 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxy of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms and acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms, with the proviso that R.sub.4 is not hydrogen when R.sub.1 is allyl, R.sub.2 is methyl and R.sub.3 is hydroxy having progestomimetic properties and their preparation.

    摘要翻译: 式中,R1是1-12个碳原子的直链或支链烷基,任意取代的2-8个碳原子的不饱和烷基,任选被取代的6-12个碳原子的芳基,任意取代的7〜7个芳烷基的新型类固醇 13个碳原子和具有至少一个硫或氧原子的杂环,R 2是1至4个碳原子的烷基,R 3选自具有1至18个碳原子的有机羧酸的氢,羟基,酰氧基, 1至8个碳原子的烷氧基和1至18个碳原子的有机羧酸的酰基,R 4选自氢,羟基,1至8个碳原子的烷基和烷氧基,2至8的烯基和炔基 碳原子和具有1至18个碳原子的有机羧酸的酰氧基,条件是当R 1是烯丙基时,R 4不是氢,R 2是甲基,R 3是具有假动物性质的羟基及其制备。

    Steroids
    3.
    发明授权
    Steroids 失效
    类固醇

    公开(公告)号:US4519946A

    公开(公告)日:1985-05-28

    申请号:US614440

    申请日:1984-05-25

    摘要: Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbons atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C=A group at position 3 is selected from the group consisting of C-O, ketal, which may be open or closed ##STR2## --C.dbd.NOH,--C--NOAlK.sub.3 and C--CH.sub.2,AlK.sub.1, AlK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocoritcoid activity and a process for their preparation.

    摘要翻译: 具有式“IMAGE”I的新型19-或类固醇和19-去甲基-D-同型甾族化合物,其中R 1是含有至少一个选自氮,磷和 具有与碳原子紧邻的原子的硅为碳,R2为碳原子数为1〜8的烃基,X选自五价环和任意含有双键的六角环, B和C一起形成双键或环氧基,第3位的C = A基团选自CO,缩酮,其可以是开或关的-C = NOH,-C-NOAlK3 和C-CH 2,AlK1,AlK 2和AlK 3选自由1至8个碳原子的烷基和7至15个碳原子的芳烷基组成的组及其无毒的药学上可接受的具有抗葡糖聚糖活性的酸加成盐和 他们的准备过程。

    Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids

    公开(公告)号:US5064822A

    公开(公告)日:1991-11-12

    申请号:US438359

    申请日:1989-11-16

    摘要: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.3 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms, --OH, acetyl, hydroxyacetyl, carboxyalkoxy of 2 to 4 carbon atoms optionally esterified or salified and hydroxyalkyl of 1 to 6 carbon atoms optionally esterified, R.sub.4 is selected from the group consisting of hydrogen, alkylthio and alkoxy of 1 to 12 carbon atoms, trialkylsilyl of 1 to 6 carbon atoms, --CN, --OH and alkyl, alkenyl and alkynyl of up to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkylamino and dialkylamino of 1 to 6 alkyl carbon atoms, R.sub.5 is selected from the group consisting of hydrogen and methyl in the .alpha.- or .beta.-position, X is .dbd.0 or hydroxyimino or alkoxyimino of 1 to 4 carbon atoms in the syn or anti form and A and B are an epoxy or a second bond in the 9(10) position and their non-toxic, pharmaceutically acceptable acid addition salts where R.sub.4 is an amino group, with the proviso that A and B are not a second bond in the 9(10)-position when X is .dbd.0 and R.sub.5 is hydrogen and a) R.sub.2 is methyl and .alpha.) R.sub.3 is --OH and i) R.sub.1 is ethyl or phenyl and R.sub.4 is hydrogen or ii) R.sub.1 is ethyl, propyl, isopropyl, vinyl, allyl, isopropenyl, phenyl, 4-fluorophenyl, methoxyphenyl or thienyl and R.sub.4 is ethynyl or iii) R.sub.1 is propyl, isopropyl, vinyl, allyl, isopropenyl, 4-methoxyphenyl or thienyl and R.sub.4 is methyl and .beta.) R.sub.3 is acetyl and i) R.sub.1 is ethyl, vinyl or phenyl and R.sub.4 is --OH or ii) R.sub.1 is vinyl and R.sub.4 is methyl and b) R.sub.2 is ethyl and R.sub.1 is vinyl, R.sub.3 is --OH and R.sub.4 is hydrogen possessing a remarkable antiglucocorticoidal activity.

    .DELTA..sup.1,3,5(10) -Estratrienes
    8.
    发明授权
    .DELTA..sup.1,3,5(10) -Estratrienes 失效
    DELTA 1,3,5(10)-Estratrienes

    公开(公告)号:US4272530A

    公开(公告)日:1981-06-09

    申请号:US867486

    申请日:1978-01-06

    摘要: Novel 11.beta. -substituted-.DELTA. .sup.1,3,5(10) -estratrienes of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of optionally substituted unsaturated alkyl of 2 to 8 carbon atoms, optionally substituted aryl of 6 to 12 carbon atoms, optionally substituted aralkyl of 7 to 13 carbon atoms and heterocycle with at least one sulfur or oxygen heteroatom, R.sub.2 is alkyl of 1 to 4 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 9 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, hydroxy, acyl of an organic carboxylic acid of 1 to 18 carbon atoms and acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxy of 1 to 8 carbon atoms, acyloxy of an organic carboxylic acid of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, with the proviso that R.sub.1 is not allyl when Z is hydrogen, R.sub.2 is methyl, R.sub.3 is hydroxy and R.sub.4 is hydrogen having estrogenic activity and their preparation.

    摘要翻译: 新颖的11β-取代的-TATA 1,3,5(10) - 结构式Ⅰ'的三亚甲基,其中R 1选自任选取代的2至8个碳原子的不饱和烷基,任选取代的6至 12个碳原子,任选取代的7至13个碳原子的芳烷基和与至少一个硫或氧杂原子杂环,R 2是1至4个碳原子的烷基,Z选自氢,1至12个碳的烷基 原子和7至9个碳原子的芳烷基,R3选自氢,羟基,1至18个碳原子的有机羧酸的酰基和1至18个碳原子的有机羧酸的酰氧基,R4是 选自氢,羟基,具有1至8个碳原子的烷基和烷氧基,具有1至8个碳原子的有机羧酸的酰氧基和2至8个碳原子的链烯基和炔基,条件是R1不是 Z为氢时为烯丙基,R2为甲基 R3是羟基,R4是具有雌激素活性的氢及其制备。

    Steroid derivatives
    9.
    发明授权
    Steroid derivatives 失效
    类固醇衍生物

    公开(公告)号:US4634695A

    公开(公告)日:1987-01-06

    申请号:US693682

    申请日:1985-01-22

    摘要: Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, which may be open or closed ##STR2## are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.

    摘要翻译: 具有式“IMAGE”I的新型19-或类固醇和19-去甲基-D-同型甾族化合物,其中R 1是含有至少一个选自氮,磷和 具有与碳原子紧邻的原子的硅为碳,R2为碳原子数为1〜8的烃基,X选自五价环和任意含有双键的六角环, B和C一起形成双键或环氧基,第3位的C = A基团选自C = O,缩酮,其可以是开放的或闭合的。图中,TRCOAlK3和CCH2,AlK1 ,AlK 2和AlK 3选自具有1至8个碳原子的烷基和7至15个碳原子的芳烷基及其无毒的药学上可接受的具有抗糖皮质激素活性的酸加成盐及其制备方法。