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205 条记录 (耗时 0.018 秒)

    Acyclic amine epoxide process
    51.
    发明授权
    Acyclic amine epoxide process 失效
    非环胺环氧化法

    公开(公告)号：US4442035A

    公开(公告)日：1984-04-10

    申请号：US436219

    申请日：1982-10-25

    申请人： Clifford E. Sacks

    发明人： Clifford E. Sacks

    IPC分类号： C07J71/00

    CPC分类号： C07J71/0015 ,  C07J71/0031

    摘要： Acyclic amines are used to transform 9.alpha.-substituted-11.beta.-hydroxy 21-acyloxy steroids to the corresponding 9.beta.,11.beta.-epoxy 21-acyloxy steroids without removal of the C.sub.17 or C.sub.21 ester. The acyclic amines are cheaper and easier to prepare than previously disclosed dehydrohalogenating agents which do not produce cleavage of the C.sub.21 ester.

    摘要翻译： 使用非环胺将9α-取代-11β-羟基21-酰氧基类固醇转化成相应的9β，11β-环氧型21-酰氧基类固醇而不除去C17或C21酯。 非循环胺比以前公开的不产生C21酯切割的脱卤化氢剂更便宜并且更容易制备。

    4-Pregnene-derivatives, a process for their preparation, composition and method for the treatment of inflammatory conditions
    53.
    发明授权
    4-Pregnene-derivatives, a process for their preparation, composition and method for the treatment of inflammatory conditions 失效
    4-孕烯衍生物，其制备方法，组合物和治疗炎性病症的方法

    公开(公告)号：US4404200A

    公开(公告)日：1983-09-13

    申请号：US322592

    申请日：1981-11-17

    申请人： Bror A. Thalen ,  Ralph L. Brattsand

    发明人： Bror A. Thalen ,  Ralph L. Brattsand

    IPC分类号： C07J5/00 ,  A61K31/573 ,  A61K31/58 ,  A61P29/00 ,  C07J71/00

    CPC分类号： C07J71/0031 ,  Y10S514/863 ,  Y10S514/887

    摘要： The invention refers to compounds having anti-inflammatory activity, characterized by the formula ##STR1## in the form of a stereoisomeric mixture or an epimer of the R or S type regarding the orientation of the substituents at the carbon atom in position 22, in which formula A is n-propyl or n-butyl and Z is hydroxyl or hydroxyl esterified with a fatty acid with a straight or branched hydrocarbon chain having 1-5 carbon atoms.The invention also refers to a process for the preparation of these compounds, a pharmaceutical preparation containing one of the compounds and a method for the treatment and control of inflammatory conditions.

    摘要翻译： 本发明涉及具有抗炎活性的化合物，其特征在于立体异构体混合物或R或S型差向异构体形式的式（I）关于位置22处碳原子上取代基的取向 其中式A为正丙基或正丁基，Z为羟基或羟基酯化为具有1-5个碳原子的直链或支链烃链的脂肪酸。 本发明还涉及制备这些化合物的方法，含有一种化合物的药物制剂和用于治疗和控制炎性病症的方法。

    Prodrugs for the improved delivery of halogen-containing glucocorticosteroids
    56.
    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。

    4-Halo steroids
    57.
    发明授权
    4-Halo steroids 失效
    4-卤素类固醇

    公开(公告)号：US4273770A

    公开(公告)日：1981-06-16

    申请号：US67984

    申请日：1979-08-20

    申请人： Francisco S. Alvarez

    发明人： Francisco S. Alvarez

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J71/00

    CPC分类号： C07J71/0031 ,  C07J21/00 ,  C07J5/0076 ,  C07J7/0085 ,  Y10S514/887

    摘要： Certain pregn-4-ene-3,20-diones or pregn-1,4-diene-3,20-diones 4-substituted with a fluoro or chloro are useful as topical anti-inflammatory steroids. These compounds are substituted at 9.alpha. with hydrogen, fluoro, chloro or bromo; at 6.alpha. with hydrogen, fluoro or chloro; at the 11 position with a keto, a .beta.-hydroxy or a .beta.-chloro (the latter only when there is a 9.alpha.-chloro); at 16.alpha., 17.alpha.-positions with isopropylidenedioxy or at 16.alpha.- (or 16.beta.) with methyl when 17.alpha. is hydroxy (or an ester); and at the 21-position with mono-fluoro, chloro, bromo, hydroxy or alkanoyloxy of 2-6 carbons or difluoro, dichloro, dihydroxy or dimethoxy.

    摘要翻译： 用氟或氯取代的某些妊娠-4-烯-3,20-二氢睾酮或妊娠-1,4-二烯-3,20-二酮可用作局部抗炎类固醇。 这些化合物在9α被氢，氟，氯或溴取代; 在6α与氢，氟或氯; 在11位具有酮基，β-羟基或β-氯（仅当存在9α-氯代时）; 当17α是羟基（或酯）时，在16α，17α-位与异丙烯二氧基或16α-（或16β）与甲基）。 并且在21位上具有2-6个碳的单氟，氯，溴，羟基或烷酰氧基或二氟，二氯，二羟基或二甲氧基。

    6-Acyloxy-1,4,6-pregnatrienes, their use as anti-inflammatory agents, methods for their manufacture, and 6-oxo-1,4-pregnadiene intermediates
    58.
    发明授权
    6-Acyloxy-1,4,6-pregnatrienes, their use as anti-inflammatory agents, methods for their manufacture, and 6-oxo-1,4-pregnadiene intermediates 失效
    6-Acyloxy-1,4,6-gestatrienes，它们作为抗炎剂的用途，其制备方法和6-氧代-1,4-孕二烯中间体

    公开(公告)号：US4201778A

    公开(公告)日：1980-05-06

    申请号：US849563

    申请日：1977-11-08

    申请人： Richard W. Draper

    发明人： Richard W. Draper

    IPC分类号： C07J3/00 ,  A61K31/56 ,  A61K31/57 ,  A61K31/58 ,  A61P17/00 ,  A61P29/00 ,  C07J5/00 ,  C07J7/00 ,  C07J31/00 ,  C07J71/00

    CPC分类号： C07J5/0076 ,  C07J31/006 ,  C07J7/0085 ,  C07J71/0026 ,  C07J71/0031 ,  C07J71/0068 ,  C07J71/0089

    摘要： Novel 6-acyloxy-3,20-dioxo-1,4,6-pregnatrienes and 6-acyloxy-3,20-dioxo-4,6-pregnadienes, useful anti-inflammatory agents, are prepared by reaction of the corresponding 3,6,20-trioxo-1,4-pregnadiene or 3,6,20-trioxo-4-pregnene with an acyl halide or an acid anhydride in pyridine. Preferred anti-inflammatory agents are 6-alkanoyloxy-9.alpha.-halogeno-16-methyl-1,4,6-pregnatriene-3,20-diones. Also described are novel 6-oxo-9.alpha.-halogeno-16-substituted-1,4-pregnadienes, useful as intermediates in preparing the corresponding 6-acyloxy-1,4,6-pregnatrienes and which also exhibit anti-inflammatory activity per se.

    摘要翻译： 新型6-酰氧基-3,20-二氧代-1,4,6-孕三烯和6-酰氧基-3,20-二氧代-4,6孕代孕酮是有用的抗炎剂，通过相应的3， 6,20-三氧代-1,4-孕二烯或3,6,20-三氧代-4-孕烯与吡啶中的酰卤或酸酐反应。 优选的抗炎剂是6-烷酰氧基-9α-卤代-16-甲基-1,4,6-孕三烯-3,20-二酮。 还描述了新的6-氧代-9α-卤代-16-取代的-1,4-孕代二烯，其可用作制备相应的6-酰氧基-1,6,6-孕三烯的中间体，并且还表现出抗炎活性 se。

    Triamcinolone acetonide derivative
    59.
    再颁专利
    Triamcinolone acetonide derivative 失效
    曲安奈德衍生物

    公开(公告)号：USRE29799E

    公开(公告)日：1978-10-10

    申请号：US822695

    申请日：1977-08-08

    申请人： Agustin Agusti

    发明人： Agustin Agusti

    IPC分类号： C07J71/00

    CPC分类号： C07J71/0031

    摘要： .[.Triamcinolone.]. .Iadd.Bis(triamcinolone .Iaddend.acetonide.Iadd.) .Iaddend.4,4'-methylene-bis(3-methoxy-2-naphthoate), method of preparing the same by preparing a reactive derivative of 4,4'-methylene-bis(3-methoxy-2-naphthoic) acid and reacting such derivative with triamcinoline acetonide. The triamcinolone acetonide derivative is particularly suitable for use in the treatment of dermatosis, eczema, neurodermatitis, impetigo, psoriasis, pruritis, erythema and the like.

    21,21-Dihalo steroids
    60.
    发明授权
    21,21-Dihalo steroids 失效
    21,21-二卤类固醇

    公开(公告)号：US4065452A

    公开(公告)日：1977-12-27

    申请号：US711042

    申请日：1976-08-02

    申请人： Tsung-tee Li ,  Michael Marx ,  Lewis J. Throop

    发明人： Tsung-tee Li ,  Michael Marx ,  Lewis J. Throop

    IPC分类号： A61K31/57 ,  A61P29/00 ,  C07J71/00 ,  A61K31/58

    CPC分类号： C07J71/0031

    摘要： Novel, topically-active anti-inflammatory steroids are represented by the formula ##STR1## wherein X is fluoro, chloro or hydrogen; X.sup.1 is fluoro, chloro, bromo, or hydrogen; X.sup.2 is hydroxy or may be chloro when X.sup.1 is chloro; and X.sup.3 and X.sup.4 are independently fluoro, chloro or bromo. These steroids are prepared by formylating at the 21-position a 16.alpha.,17.beta.-isopropylidenedioxypregna-1,4,9(11)-triene-3,20-dione or the corresponding 21-fluoro compound, halogenating at the 21 position, deformylating, then reacting to add the desired components at the 9.alpha. and 11.beta. positions.

    摘要翻译： 新型的表面活性抗炎类固醇由式（IMAGE）表示，其中X是氟，氯或氢; X1是氟，氯，溴或氢; X2是羟基或当X1是氯时可以是氯; 且X 3和X 4独立地为氟，氯或溴。 这些类固醇通过在21位甲酰化制备16α，17β-异亚丙基二氧嘧啶-1,4,9（11） - 三烯-3,20-二酮或相应的21-氟化合物，在21位卤化， 然后进行反应，以在9α和11β位置添加所需的组分。