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18 条记录 (耗时 0.011 秒)

    COMPOUNDS
    2.
    发明申请
    COMPOUNDS 审中-公开
    化合物

    公开(公告)号：US20020019378A1

    公开(公告)日：2002-02-14

    申请号：US09446585

    申请日：2000-02-11

    发明人： RICHARD MARTYN ANGELL ,  KEITH BIGGADIKE ,  ROSANNE MARY FARRELL ,  DUNCAN STUART HOLMES ,  PANAYIOTIS ALEXANDROU PROCOPIOU ,  USHA V RAMESHI

    IPC分类号： A61K031/58

    CPC分类号： C07J17/00 ,  C07J3/005 ,  C07J31/006 ,  C07J33/005 ,  C07J71/0031 ,  C12Q1/44 ,  G01N2333/918 ,  G01N2500/00

    摘要： A vane pump comprising a central shaft adapted to receive a rotational force from the outside, a ring gear formed in a hollow portion provided in the shaft, a linear gear formed on one end of a constant velocity coupling and meshed with the ring gear, and a ring gear formed in a hollow portion of an inner rotor and meshed with a linear gear formed on the other end of the constant velocity coupling, whereby it is rendered possible to rotate the shaft and inner rotor at an equal speed, insert a circular portion formed at one end of a vane into a circular hollow space of the inner rotor, bring the other end of the vane into contact with an inner surface of an outer rotor, and vary the volumes of a compression chamber and a supply chamber, the air being thereby compressed, so that high-pressure compressed air can be obtained by a small-volume vane pump without encountering the collision of parts causative of noise.

    摘要翻译： 一种叶片泵，包括适于从外部接收旋转力的中心轴，形成在设置在轴中的中空部分中的齿圈，形成在恒速联轴器的一端并与齿圈啮合的线性齿轮，以及 形成在内转子的中空部分并与形成在恒速联轴器的另一端上的线性齿轮啮合的环形齿轮，由此能够以相等的速度旋转轴和内转子，将圆形部分 在叶片的一端形成内转子的圆形中空空间，使叶片的另一端与外转子的内表面接触，并且改变压缩室和供应室的体积，空气 由此被压缩，使得通过小体积叶片泵可以获得高压压缩空气，而不会遇到噪声原因的碰撞。

    Novel 10.beta.-alkynyl-steroids
    4.
    发明授权
    Novel 10.beta.-alkynyl-steroids 失效
    新型10个β-炔基 - 类固醇

    公开(公告)号：US4987128A

    公开(公告)日：1991-01-22

    申请号：US18199

    申请日：1987-02-24

    申请人： Lucien Nedelec ,  Francois Nique ,  Anne-Marie Moura

    发明人： Lucien Nedelec ,  Francois Nique ,  Anne-Marie Moura

    IPC分类号： A61K31/585 ,  A61P9/00 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J43/00 ,  C07J53/00

    CPC分类号： C07J21/006 ,  C07J1/007 ,  C07J21/003 ,  C07J33/005 ,  C07J43/006

    摘要： Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 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 and acetylthio, R.sub.2 is methyl or ethyl, X and Y taken together form a member selected from the group consisting of ##STR2## Alk is alkyl of 1 to 8 carbon atoms or X is hydroxy and Y is ##STR3## or X is optionally acylated or etherified hydroxy and Y is selected from the group consisting of --CH.sub.2 --CH.sub.2 --CH.sub.2 --OH, hydrogen, R.sub.4, and --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, --NH.sub.4 and alkali metal and R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, the dotted lines indicate the optional presence of a second carbon-carbon bond when R.sub.6 and R.sub.7 and the carbon to which they are attached do not form cyclopropyl and the wavy lines indicate that R.sub.6 and R.sub.7 may be in the .alpha. or .beta. position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen, R.sub.2 is methyl, X is optionally acylated or etherified hydroxy, Y is hydrogen or R.sub.4 and the dotted lines are not a second carbon-carbon bond having aldosterone antagonistic activity and increased hydrosodic diuresis with organic potassium conservation with little secondary hormone effects.

    摘要翻译： 新颖的式10的β-炔基 - 类固醇，其中R选自氢，任选取代的烷基和1至8个碳原子的烷氧基，任选取代的碳原子数2〜8的烯基和炔基，任选地 取代的芳基和芳烷基，任意酯化的羧基，二烷基氨基与1至6个碳原子的烷基，卤素和1至7个烷基碳原子的三烷基甲硅烷基，R 6和R 7与它们所连接的碳原子一起形成环丙基或R6是氢 并且R 7是R 1，R 1选自氢，任选取代的1至6个碳原子的烷基，任选取代的烯基和2至6个碳原子的炔基和乙酰硫基，R 2是甲基或乙基，X和Y一起 形成选自由以下组成的组中的一个成员：Alk为1至8个碳原子的烷基或X为羟基，Y为X或X任选被酰化或醚化羟基，Y选自gro 其由-CH 2 -CH 2 -CH 2 -OH，氢，R 4和-CH 2 -CH 2 -COOM组成，M选自氢，-NH 4和碱金属，R 4选自由以下组成的组： 1至6个碳原子和2至6个碳原子的烯基和炔基，虚线表示当R6和R7以及它们所连接的碳不形成环丙基时，任选存在第二碳 - 碳键，波浪线 表示R6和R7可以在α或β位置，条件是当R6和R7是氢时，R不是氢，R2是甲基，X是任选被酰化或醚化羟基，Y是氢或R4，虚线是 不是具有醛固酮拮抗活性的第二个碳 - 碳键和具有少量次生激素效应的有机钾保护的增加的水溶性利尿。

    Novel 10-substituted steroids and their use in the induction of aldosterone antagonistic activity
    5.
    发明授权
    Novel 10-substituted steroids and their use in the induction of aldosterone antagonistic activity 失效

    公开(公告)号：US4701449A

    公开(公告)日：1987-10-20

    申请号：US768867

    申请日：1985-08-23

    申请人： Vesperto Torelli ,  Lucien Nedelec ,  Martine Moguilewski ,  Anne-Marie Moura

    发明人： Vesperto Torelli ,  Lucien Nedelec ,  Martine Moguilewski ,  Anne-Marie Moura

    IPC分类号： A61K31/58 ,  A61P9/04 ,  A61P9/10 ,  C07J1/00 ,  C07J5/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J53/00 ,  A61K31/585 ,  A61K31/56

    CPC分类号： C07J1/0011 ,  C07J1/0022 ,  C07J1/0033 ,  C07J1/0037 ,  C07J1/0044 ,  C07J21/00 ,  C07J21/003 ,  C07J21/006 ,  C07J31/003 ,  C07J31/006 ,  C07J33/005 ,  C07J41/0038 ,  C07J41/0094 ,  C07J43/006 ,  C07J51/00 ,  C07J53/007

    摘要： Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.2 --CH.sub.2 OH, M is hydrogen, alkali metal or --NH.sub.4 or X and Y together form a member of the group consisting of ##STR2## or X is --OH and Y is ##STR3## R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, Alk is alkyl of 1 to 8 carbon atoms, the dotted lines in the 1(2) and 6(7) indicate the optional presence of a second carbon-carbon bond with the proviso that when R.sub.6 and R.sub.7 form cyclopropyl, there is no 6(7) second bond, the dotted line in 10-substituent indicates the optional presence of a third carbon-carbon bond, the wavy lines at R.sub.6 and R.sub.7 indicate the possible .alpha.- or .beta.-position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen R.sub.2 is methyl, X is hydroxy or acetoxy and Y is hydrogen, the dotted lines at 1(2) and 6(7) do not represent a second bond and the dotted line in the 10-substituent is a third carbon-carbon bond useful as aldosterone antagonists and for increasing hydrosodium diuresis while preserving organic potassium with reduced hormonal side effects.

    Prodrugs for the improved delivery of halogen-containing glucocorticosteroids
    6.
    发明授权
    Prodrugs for the improved delivery of halogen-containing glucocorticosteroids 失效
    用于改善输送含卤素糖皮质激素的前药

    公开(公告)号：US4279900A

    公开(公告)日：1981-07-21

    申请号：US61177

    申请日：1979-07-27

    申请人： Nicholas S. Bodor ,  Kenneth B. Sloan

    发明人： Nicholas S. Bodor ,  Kenneth B. Sloan

    IPC分类号： C07J33/00 ,  C07J71/00

    CPC分类号： C07J33/005 ,  C07J71/0031 ,  Y10S514/887

    摘要： Novel 3,2'-spiro(1',3'-thiazolidine) compounds which are transient prodrug forms of known 6- and/or 9-haloglucocorticosteroids are described. The subject prodrugs provide improved delivery of the prior art steroids for therapeutic purposes, particularly in alleviating inflammation, and can be prepared by known methods, for example, by reacting the corresponding 3-keto steroids with a thiazolidine forming reagent such as an L-cysteine alkyl ester.

    摘要翻译： 描述了已知的6-和/或9-卤素糖皮质激素的瞬时前药形式的新型3,2'-螺（1'，3'-噻唑烷）化合物。 本发明的前药提供了用于治疗目的的现有技术类固醇的改进递送，特别是在减轻炎症中，并且可以通过已知方法制备，例如通过使相应的3-酮类固醇与形成噻唑烷的试剂例如L-半胱氨酸 烷基酯。

    Novel 17-spirosultines
    10.
    发明授权
    Novel 17-spirosultines 失效
    小说17-spirosultines

    公开(公告)号：US4154730A

    公开(公告)日：1979-05-15

    申请号：US843962

    申请日：1977-10-20

    申请人： Vesperto Torelli ,  Daniel Philibert

    发明人： Vesperto Torelli ,  Daniel Philibert

    IPC分类号： A61K31/565 ,  A61K31/58 ,  A61P5/38 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J17/00

    CPC分类号： C07J31/006 ,  C07J21/006 ,  C07J33/005 ,  Y10S514/899

    摘要： Novel 17-spirosultines of steroids and the corresponding .gamma.-hydroxy acids of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms, A is hydrogen and B is hydrogen or hydroxyl of .beta.configuration or A and B together form a double bond, X and Y together form the group ##STR2## or X is --OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, --NH.sub.4 and an alkali metal having a remarkable progestomimetic and antialdosteronic activity and a novel process for their preparation and novel intermediates.

    摘要翻译： 类固醇的新型17-螺旋体和相应的式（I）的γ-羟基酸，其中R 1是1至4个碳原子的烷基，A是氢，B是氢或β构型的羟基或A和B一起形成 双键，X和Y一起形成基团，或X是-OH，Y是，M选自氢，-NH 4和具有显着的假动物模拟和反向递质活性的碱金属，和 新型制备方法及新型中间体。