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89 条记录 (耗时 0.033 秒)

    3-Nitrogen-6, 7-dioxygen steroids and uses related thereto
    5.
    发明申请
    3-Nitrogen-6, 7-dioxygen steroids and uses related thereto 失效
    3-氮-6,7-二氧类固醇及其相关用途

    公开(公告)号：US20050215534A9

    公开(公告)日：2005-09-29

    申请号：US10624946

    申请日：2003-07-21

    申请人： Jeffery Raymond ,  Claudia Kasserra ,  Yaping Shen

    发明人： Jeffery Raymond ,  Claudia Kasserra ,  Yaping Shen

    IPC分类号： A61K31/56 ,  A61K31/566 ,  A61K31/57 ,  A61K31/58 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/02 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00

    CPC分类号： C07J41/00 ,  C07J41/0005 ,  C07J41/0011 ,  C07J43/00 ,  C07J71/0047 ,  C07J71/0063 ,  Y02P20/55

    摘要： A compound of the formula and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R1 and R2 are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R1 and R2 may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R1 may be a 2, or 3 atom chain to numeral 2 so that —N—R1— forms part of a fused bicyclic structure to ring A; R3 and R4 are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups, hydrogen, or a protecting group such that R3 and/or R4 is part of hydroxyl or carbonyl protecting group; numerals 1 through 17 each represent a carbon having substitution as described. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.

    摘要翻译： R 1和R 2各自独立地是分别地或以混合物形式的式及其药学上可接受的盐，溶剂合物，立体异构体和前药的化合物，其中每次出现：R 1和 选自氢，氧，以形成硝基或肟，氨基，硫酸根和磺酸，以及具有1-30个碳原子并且任选地含有1-6个选自氮，氧，磷，硅和硫的杂原子的有机基团，其中 R 1和R 2可以与它们都键合的N一起形成可以是具有1-30个碳的有机基团的一部分的杂环结构，以及 任选地含有1-6个选自氮，氧和硅的杂原子，并且其中R 1可以是2或3个原子链至2，使得-NR 1 - 形成环A的稠合双环结构的一部分; R 3和R 4分别选自6和7的直接键，以便形成羰基，氢或保护基，使得R 3， 和/或R 4是羟基或羰基保护基的一部分; 数字1至17各自表示如上所述具有取代的碳。 化合物可以配制成药物组合物，并用于治疗和/或预防各种病症，包括炎症，哮喘，过敏性疾病，慢性阻塞性肺病，特应性皮炎，实体瘤，AIDS，局部缺血和心律失常。

    19,11 .beta.-bridged steroids, their manufacture and pharmaceutical preparations containing them
    7.
    发明授权
    19,11 .beta.-bridged steroids, their manufacture and pharmaceutical preparations containing them 失效
    19,11（BETA） - 混合型STEROIDS，其制造和含有它们的药物制剂

    公开(公告)号：US5095129A

    公开(公告)日：1992-03-10

    申请号：US283632

    申请日：1988-12-09

    申请人： Eckhard Ottow ,  Rudolf Wiechert ,  Gunter Neef ,  Sybille Beier ,  Walter Elger ,  David A. Henderson

    发明人： Eckhard Ottow ,  Rudolf Wiechert ,  Gunter Neef ,  Sybille Beier ,  Walter Elger ,  David A. Henderson

    IPC分类号： A61K31/565 ,  A61K31/58 ,  A61P5/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J53/00 ,  C07J63/00 ,  C07J71/00

    CPC分类号： C07J71/0063 ,  C07J21/006 ,  C07J31/006 ,  C07J41/0038 ,  C07J53/002 ,  C07J71/0005 ,  C07J71/0047

    摘要： New 19,11.beta.-bridged steroids of the general formula I ##STR1## where R.sup.1 stands for a methyl or ethyl radical,R.sup.2 for a hydrogen or chlorine atom or a C.sub.1 -C.sub.4 -alkyl radical,B and G, which are the same or different, respectively for a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl radical or, together, for a second bond between the carbon atoms 6 and 7,B and R.sup.2 together for a methylene or an ethylene group,Z for the radical of a pentagonal or hexagonal ring, which is possibly substituted and possibly unsaturated,V stands for a possibly substituted carbocyclic or heterocyclic aryl radical,the ring A for ##STR2## M and N together meaning a second bond or M a hydrogen atom and N a hydroxy group,X means an oxygen atom, two hydrogen atoms or a hydroxyimino grouping N.about.OH,R.sup.3 and D, which are the same or different, respectively a hydrogen atom, a nitrile radical or a C.sub.1 -C.sub.4 -alkyl radical or, together, a methylene or ethylene group,E a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl radical,D and E together meaning a second bond between carbon atoms 1 and 2 or together a methylene group ##STR3## with R.sup.11 in the meaning of a hydrogen atom or a C.sub.1 -C.sub.8 -alkyl radical,are described as well as their pharmaceutically tolerated addition salts with acids. The new compounds possess valuable pharmacological properties.

    摘要翻译： 新的19,11个β-桥连类固醇，其通式为Ⅰ（Ⅰ），其中R1代表甲基或乙基，R2代表氢或氯原子或C1-C4烷基，B和G，其中 分别对于氢原子，C 1 -C 4 - 烷基或碳原子6和7之间的第二个键，B和R 2一起为亚甲基或亚乙基，Z为相同或不同的 可能被取代且可能不饱和的五角或六方环的基团V代表可能被取代的碳环或杂环芳基，A，A，M和N一起表示第二个键或M是氢原子 和N是羟基，X表示氧原子，两个氢原子或羟基亚氨基基团N分别OH，R3和D分别相同或不同，分别为氢原子，腈基或C1-C4烷基 或者一起是亚甲基或亚乙基，E是氢原子或C 1 -C 4烷基，D和E togeth 呃意指碳原子1和2之间的第二个键或一起与氢原子或C 1 -C 8 - 烷基的含义中的R 11一起形成的亚甲基基团b）或者c），以及 它们与酸的药学上耐受的加成盐。 新化合物具有宝贵的药理性质。

    -Azido-4,6-pregnadieno(3,2-c)pyrazoles, processes for their preparation and intermediates useful therein
    9.
    发明授权
    -Azido-4,6-pregnadieno(3,2-c)pyrazoles, processes for their preparation and intermediates useful therein 失效
    （3,2-c）吡唑，其制备方法和其中有用的中间体

    公开(公告)号：US3932388A

    公开(公告)日：1976-01-13

    申请号：US462687

    申请日：1974-04-22

    申请人： Thomas L. Popper ,  Richard W. Draper ,  Elliot L. Shapiro ,  Arthur S. Watnick

    发明人： Thomas L. Popper ,  Richard W. Draper ,  Elliot L. Shapiro ,  Arthur S. Watnick

    IPC分类号： C07J71/00 ,  C07J1/00

    CPC分类号： C07J71/0047 ,  Y10S514/899 ,  Y10S514/96 ,  Y10S514/962 ,  Y10S514/969

    摘要： Steroidal 6-azido-4,6-pregnadieno[3,2-c]pyrazoles having glucocorticoid activity are prepared by treating a 6-unsubstituted-4,6-pregnadieno[3,2-c]pyrazole with a halogen azide followed by treatment of the thereby formed 6-azido-7-halogeno-6,7-dihydro-4-pregnene[3,2-c]pyrazole with a dehydrohalogenating agent. Other methods of preparing these compounds are described, including the process of treating a 6-azido-17.alpha.,20; 20,21-bismethylenedioxy-4,6-pregnadiene-3-one with an alkyl formate in the presence of base followed by treatment of the resulting 2-hydroxymethylene derivative with a hydrazine or, alternatively, by converting said 2-hydroxymethylene to a 2-alkoxymethylene derivative followed by treatment thereof with a hydrazine.Preferred compounds include 6-azido-11.beta.,17.alpha.,21-trihydroxy-20-keto-4,6-pregnadieno[3,2-c]pyrazoles, particularly 2'-phenyl-9.alpha.-fluoro(and 9.alpha.-chloro)-16-methyl-derivatives thereof which possess potent anti-inflammatory activity. Of interest is 2'-phenyl-6-azido-9.alpha.-fluoro-11.beta.,17.alpha.,21-trihydroxy-16.alpha.-methyl-20-keto-4,6-pregnadieno[3,2-c]pyrazole.

    摘要翻译： 具有糖皮质激素活性的甾体6-叠氮基-4,6-孕雌二烯并[3,2-c]吡唑通过用卤素叠氮化物处理6-未取代的4,6孕烯二烯并[3,2-c]吡唑，然后进行处理 由此形成的6-叠氮基-7-卤代-6,7-二氢-4-孕烯[3,2-c]吡唑与脱卤化氢剂反应。 描述了制备这些化合物的其它方法，包括处理6-叠氮基-17α，20; 在碱的存在下，与甲酸烷基酯反应，然后用肼处理所得2-羟基亚甲基衍生物，或者通过将所述2-羟基亚甲基转化为2 - 烷氧基亚甲基衍生物，随后用肼处理。