Novel 17.alpha.-aryl-steroids
    1.
    发明授权
    Novel 17.alpha.-aryl-steroids 失效
    新型17α-芳基类固醇

    公开(公告)号:US4242335A

    公开(公告)日:1980-12-30

    申请号:US955403

    申请日:1978-10-27

    IPC分类号: A61K31/565 C07J1/00 C07J21/00

    CPC分类号: C07J1/0088 C07J21/006

    摘要: Novel 17.alpha.-aryl-steroids of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, R.sub.3 is aryl of 6 to 12 carbon atoms optionally substituted with at least one substituent selected from the group consisting of --OH, halogen, alkoxy and alkyl of 1 to 4 carbon atoms and --CF.sub.3, the dotted line in the B ring indicating an optional double bond in the 9(10)-position, and A and B are hydrogen and when there is a double bond in the 9(10)-position, A and B form a double bond in the 11(12) position or B is hydrogen and A is an 11.beta.-hydroxy having progestomimetic activity activity without androgenic activity and a process for their preparation and novel intermediates produced therein.

    摘要翻译: 新型17α-芳基 - 类固醇,其中R 1为1至3个碳原子的烷基,R 2选自氢,1至12个碳原子的烷基和有机羧酸的酰基 1至18个碳原子,R3是任选被至少一个选自-OH,卤素,烷氧基和1至4个碳原子的烷基和-CF 3的取代基取代的6至12个碳原子的芳基,虚线在 B环表示9(10)位中任选的双键,A和B是氢,当在9(10)位具有双键时,A和B在11(10) - 位上形成双键, 12)位置或B是氢,A是具有没有雄激素活性的模拟活动活性的11β-羟基,其制备方法和其中产生的新的中间体。

    Method of controlling fertility in males with 20-substitute of steroids
    2.
    发明授权
    Method of controlling fertility in males with 20-substitute of steroids 失效
    用20替代类固醇控制男性生育能力的方法

    公开(公告)号:US5679668A

    公开(公告)日:1997-10-21

    申请号:US691667

    申请日:1996-08-02

    摘要: The invention is a method of controlling fertility in male warm-blooded animals by administering a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R.sub.3 is an .alpha.-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R.sub.4 is alkyl of 1 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20- asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts.

    摘要翻译: 本发明是通过给予式Ⅰ化合物来控制雄性温血动物的生殖力的方法,其中R1和R2分别选自1至12个碳原子的烷基和7至15个的芳烷基 碳原子或一起形成5至6个环成员的饱和杂环,任选具有选自硫,氧和氮的第二个环杂原子,R 3是1至8个碳原子的α-烷基,n是整数 2至15,R 4为1至12个碳原子的烷基,R 5选自氢,1至12个碳原子的烷基和至多12个碳原子的有机羧酸的酰基,波浪线表示 17和20-不对称中心独立于绝对的R和S构型及其无毒的药学上可接受的酸加成盐。

    19-nor-3-keto steroids
    4.
    发明授权
    19-nor-3-keto steroids 失效
    19-NOR-3-KETO STEROIDS

    公开(公告)号:US5108996A

    公开(公告)日:1992-04-28

    申请号:US497562

    申请日:1990-03-21

    摘要: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.2 and R'.sub.2 are individually hydrogen or methyl, R.sub.11 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom adjacent to the 11-carbon atom being a carbon, the wavy lines at the 13 and 17-positions indicate that when the 13-methyl is .alpha., R'.sub.17 group is .beta. and R.sub.17 is .alpha. and when the 13-methyl is .sub..beta., R.sub.17 is .sub..beta. and R'.sub.17 is .alpha., R.sub.17 is --OH or acyloxy of 1 to 18 carbon atoms and R'.sub.17 is ##STR2## is hydrogen or --OH or acyloxy of 1 to 18 carbon atoms, Z is selected from the group consisting of a single bond, alkylene of 1 to 5 carbon atoms and alkenylene and alkynylene of 2 to 5 carbon atoms and P is selected from the group consisting of pyrimidinyl and pyridyl optionally substituted with 1 or 2 individual members of the group consisting of amino, alkylamino and dialkylamino of 1 to 4 alkyl carbon atoms and (B aminated 5- or 6-membered heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms) and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and anti-oxidant activity.

    摘要翻译: 选自下式的化合物的化合物其中R 2和R 12独立地是氢或甲基,R 11是具有1至18个碳原子的有机基团,任选地含有至少一个与原子相邻的原子的杂原子 11碳原子是碳,13位和17位的波浪线表示当13-甲基是α时,R'17基团是β,R17是α,当13-甲基是β时,R17是 β和R'17是α,R17是-OH或1至18个碳原子的酰氧基,R'17是氢或-OH或含1至18个碳原子的酰氧基,Z选自 由单键键合,1至5个碳原子的亚烷基和2至5个碳原子的亚烯基和亚炔基组成的组,P选自嘧啶基和吡啶基,任选被1或2个独立成员取代的氨基 ,烷基氨基和1至4个烷基碳原子的二烷基氨基和(B胺化的5或6元环 任选被1至3个碳原子的烷基取代的杂环)及其无毒的药学上可接受的具有抗炎和抗氧化活性的酸加成盐。

    Steroid derivatives
    5.
    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。

    Vibratory cleaner for endless belt conveyor
    7.
    发明授权
    Vibratory cleaner for endless belt conveyor 失效
    环形皮带输送机的振动清洁器

    公开(公告)号:US4174030A

    公开(公告)日:1979-11-13

    申请号:US891387

    申请日:1978-03-29

    申请人: Daniel Philibert

    发明人: Daniel Philibert

    IPC分类号: B65G45/00 B65G45/10

    CPC分类号: B65G45/105

    摘要: A device for clearing residues of pulverulent or particulate product from a belt conveyor includes a vibrating roller freely rotatably mounted between an upper carrier run and a lower return run of said conveyor belt and biased into engagement with the inner side of the return run, the vibrating roller being sealed against ingress of dust and other foreign matter and enclosing a vibration generator motor. In such a device the vibration generator motor is protected from the effects of dust and climatic variations and is of compact form. The vibrating roller is resiliently supported by coil springs which thrust the roller against the inside face of the return run of the conveyor belt to ensure that contact is maintained between the vibrating roller and the return run of the conveyor belt even when the conveyor belt is circulating at a high linear speed.

    摘要翻译: 用于从带式输送机清除粉状或颗粒状产物残留物的装置包括一个可自由旋转地安装在所述传送带的上部载体行程和下部回程之间的振动辊,并被偏压成与返回行程的内侧接合, 辊子被密封以防止灰尘和其他异物进入并且包围振动发生器电机。 在这种装置中,振动发生器马达被保护免受灰尘和气候变化的影响,并且具有紧凑的形式。 振动辊由螺旋弹簧弹性地支撑,螺旋弹簧将辊推压抵靠传送带的返回行程的内表面,以确保即使当传送带循环时也能够在传送带之间保持接触保持在振动辊和传送带的回程之间 以高线速度。

    20-substituted steroids
    9.
    发明授权
    20-substituted steroids 失效
    20-取代的类固醇

    公开(公告)号:US06437157B1

    公开(公告)日:2002-08-20

    申请号:US08403276

    申请日:1995-03-13

    IPC分类号: C07J300

    摘要: A compound selected from the group consisting of a compound of the formula wherein R1 and R2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R3 is an &agr;-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R4 is alkyl of 1 to 12 carbon atoms, R5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20-asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts useful for controlling fertility in male warm-blooded animals.

    摘要翻译: 选自由下列化合物组成的组的化合物,其中R 1和R 2的化合物分别选自1至12个碳原子的烷基和7至15个碳原子的芳烷基,或者一起形成5至6个饱和杂环 任选具有选自硫,氧和氮的第二环杂原子的环成员,R 3是1至8个碳原子的α-烷基,n是2至15的整数,R 4是1至12个碳的烷基 原子,R5选自氢,1至12个碳原子的烷基和至多12个碳原子的有机羧酸的酰基,波浪线表示17和20不对称中心独立于 绝对R和S构型及其无毒的药学上可接受的酸加成盐,用于控制雄性温血动物的生育力。