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2581 条记录 (耗时 0.036 秒)

    Process for 20-oxo-17.alpha.,21-diol steroids
    53.
    发明授权
    Process for 20-oxo-17.alpha.,21-diol steroids 失效
    20-氧代-17α，21-二醇类固醇的方法

    公开(公告)号：US5723638A

    公开(公告)日：1998-03-03

    申请号：US495048

    申请日：1995-06-26

    申请人： Robert Lett ,  Oleg Melnyk

    发明人： Robert Lett ,  Oleg Melnyk

    IPC分类号： C07J5/00 ,  C07J17/00 ,  C07J31/00 ,  C07J75/00

    CPC分类号： C07J5/0053 ,  C07J17/00 ,  C07J31/006

    摘要： The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.

    摘要翻译： 本发明涉及一种制备下式的类固醇的方法，其中R 1是氢或1至4个碳原子的烷基，R 2是1至4个碳原子的烷基，而A，B，C， 和D环系具有至少一个双键，并且任选地被至少一个任选被保护的羟基，任选被保护的酮基，卤素，具有1至4个碳原子的烷基和烷氧基，以及2至4个碳原子的烯基和炔基取代， 相应的17-酮类固醇与式（Ia）化合物反应，然后使所得化合物与芳基硫代卤化物反应。 然后产生的中间体重排，然后用强碱进行差向异构化，得到相应的亚硫酸盐非对映异构体与硫醇化合物反应的混合物。 产生的中间体进行酸水解以提供式I的化合物。

    Process for the preparation of an oxoetiocholenic acid
    54.
    发明授权
    Process for the preparation of an oxoetiocholenic acid 失效
    制备氧代丁酸的方法

    公开(公告)号：US5650526A

    公开(公告)日：1997-07-22

    申请号：US519772

    申请日：1995-08-28

    申请人： Patrick Roussel ,  Michel Vivat

    发明人： Patrick Roussel ,  Michel Vivat

    IPC分类号： C07J3/00 ,  C07J5/00 ,  C07J21/00 ,  C07J41/00 ,  C07J75/00 ,  C07J7/00

    CPC分类号： C07J3/005 ,  C07J41/0094

    摘要： The invention is drawn to a process for the preparation of oxoetiocholenic acid of the formula I ##STR1## by reacting a compound of the formula II ##STR2## with a halonitrile in the presence of a base followed by formation of a 3-ketone group. The intermediate formed is reacted with an acid of the formula HX in an anhydrous medium followed by dehydrohalogenation of the resulting compound in the presence of a base. The intermediate produced then undergoes alkaline hydrolysis followed by a conventional acid treatment to obtain the compound of formula I.

    摘要翻译： 本发明涉及通过在碱存在下使式II的化合物与卤素反应，然后形成3-酮基的方法制备式I的氧代丁烯酸的方法。 所形成的中间体在无水介质中与式HX的酸反应，然后在碱的存在下将所得化合物脱卤化氢。 所生成的中间体经历碱水解，然后进行常规的酸处理，得到式I化合物。

    11,21-bisphenyl-19-norpregnane derivatives
    55.
    发明授权
    11,21-bisphenyl-19-norpregnane derivatives 失效
    11,21-双苯基-19-去甲孕烷衍生物

    公开(公告)号：US5620966A

    公开(公告)日：1997-04-15

    申请号：US445119

    申请日：1995-05-19

    申请人： Ronald Gebhard ,  Hendrikus A. A. van der Voort

    发明人： Ronald Gebhard ,  Hendrikus A. A. van der Voort

    IPC分类号： A61K31/575 ,  A61K31/56 ,  A61K31/58 ,  A61P3/08 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07J5/00 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00 ,  C07J75/00 ,  A61K31/565 ,  C07J1/00

    CPC分类号： C07J71/001 ,  C07J31/006 ,  C07J41/0077 ,  C07J41/0083 ,  C07J43/003

    摘要： The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I ##STR1## wherein R.sub.1 is selected from H, halogen, (1-6C)alkoxy, and NR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being independently hydrogen or (1-6C)alkyl or R.sub.5 and R.sub.6 together are (3-6C)alkylene; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 together are a (1-3C)alkylenedioxy group, optionally substituted by one or more halogen atoms; R.sub.3 is methyl or ethyl; R.sub.4 is selected from C(O)-NR.sub.5 R.sub.6, SO.sub.n -(1-6C)alkyl optionally substituted by one or more halogen atoms, SO.sub.n -(3-6C)cycloalkyl, n being 1 or 2, SO.sub.2 -NR.sub.5 R.sub.6, 2-oxypyrrolidinyl, and NR.sub.5 R.sub.6 ; R.sub.7 is H or (1-6C)alkyl; R.sub.8 is H or carboxy-1-oxo(1-6C)alkyl; and X is selected from (H,OH), O, and NOH; 11 or a pharmaceutically acceptable salt thereof.The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.

    摘要翻译： 本发明涉及式I的11,21-双苯基-19-去甲孕烷衍生物，其中R 1选自H，卤素，（1-6C）烷氧基和NR 5 R 6，R 5和R 6独立地是氢或 （1-6C）烷基或R5和R6一起为（3-6C）亚烷基; R2是氢; 或R 1和R 2一起是（1-3C）亚烷基二氧基，任选被一个或多个卤素原子取代; R3是甲基或乙基; R4选自C（O）-NR5R6，任选被一个或多个卤素原子取代的SO n - （1-6C）烷基，SO n-（3-6C）环烷基，n是1或2，SO 2 -NR 5 R 6，2-氧代吡咯烷基 ，和NR5R6; R7是H或（1-6C）烷基; R8是H或羧基-1-氧代（1-6C）烷基; X选自（H，OH），O和NOH; 11或其药学上可接受的盐。 本发明化合物具有抗糖皮质激素活性，可用于治疗或预防糖皮质激素依赖性疾病。

    Method for enhancement of production of lymphokines and applications thereof
    58.
    发明授权
    Method for enhancement of production of lymphokines and applications thereof 失效
    增强淋巴因子生产的方法及其应用

    公开(公告)号：US5540919A

    公开(公告)日：1996-07-30

    申请号：US18471

    申请日：1993-02-16

    申请人： Raymond A. Daynes ,  Barbara A. Araneo

    发明人： Raymond A. Daynes ,  Barbara A. Araneo

    IPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/59 ,  A61K39/02 ,  A61K39/12 ,  A61K39/395 ,  A61K45/06 ,  A61P37/00 ,  C07J5/00 ,  G01N33/68 ,  A61K31/56 ,  A61K38/20 ,  A61K39/39

    CPC分类号： G01N33/6869 ,  A61K31/565 ,  A61K31/5685 ,  A61K31/57 ,  A61K31/59 ,  A61K45/06 ,  A61K2039/54 ,  A61K2039/55 ,  A61K2039/55511 ,  A61K39/00

    摘要： Disclosed is a method for enhancing the production of T cell lymphokines, which comprises exposing T cell lymphocytes which have a potential to make selected T cell lymphokines to an appropriate concentration of at least one particular steroid hormone prior to cellular activation. Also disclosed are applications of the method for clinically diagnosing abnormal interleukin production, maintaining in vitro tissue cultures of T cells, overcoming certain types of immunosuppression caused by elevated GCS levels, caused by endogenous production or exogenous administration, use as a vaccine adjuvant to selectively direct the vaccine-induced immune response down a protective, rather than a potentially pathologic or non-protective, immunologic pathway, as a treatment for naturally occuring aging-related decreases in immune function, as a treatment for stress or trauma-induced decreases in immune function, and as an agent to facilitate desensitization to agents to which a warm-blooded animal is allergic.

    摘要翻译： 公开了一种用于增强T细胞淋巴因子的产生的方法，其包括将细胞淋巴细胞暴露于在细胞活化之前使选择的T细胞淋巴因子至适合浓度的至少一种特定类固醇激素的潜力。 还公开了用于临床诊断异常白介素产生的方法的应用，保持T细胞的体外组织培养，克服由内源性产生或外源施用引起的由GCS升高引起的某些类型的免疫抑制，用作疫苗佐剂以选择性地直接 疫苗诱导的免疫应答降低了保护性而不是潜在的病理或非保护性免疫途径，作为治疗自然发生老化的免疫功能降低，作为应激或创伤诱导的免疫功能降低的治疗 ，并作为促进对温血动物过敏的药剂脱敏的药剂。

    D-homo-(16-ene)-11.beta.-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents
    59.
    发明授权
    D-homo-(16-ene)-11.beta.-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents 失效
    D-均聚（16-烯）-11β-芳基-4-雌酮，其制备方法以及作为药剂的用途

    公开(公告)号：US5519027A

    公开(公告)日：1996-05-21

    申请号：US78326

    申请日：1994-02-25

    申请人： Wolfgang Schwede ,  Eckhard Ottow ,  Arwed Cleve ,  Walter Elger ,  Krzysztof Chwalisz ,  Martin Schneider

    发明人： Wolfgang Schwede ,  Eckhard Ottow ,  Arwed Cleve ,  Walter Elger ,  Krzysztof Chwalisz ,  Martin Schneider

    IPC分类号： A61K31/57 ,  A61K31/58 ,  A61K31/585 ,  A61P5/38 ,  C07J1/00 ,  C07J3/00 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J41/00 ,  C07J63/00 ,  A61K31/565

    CPC分类号： C07J63/008

    摘要： New D-homo-(16-ene)-11.beta.-aryl-4-estrenes of general formula I ##STR1## as well as their pharmaceutically compatible addition salts with acids are described in whichX stands for an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 stands for an hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,R.sup.11 stands for a fluorine, chlorine or bromine atom, and then R.sup.12 and R.sup.13 together mean an additional bond orR.sup.11 stands for a straight-chain or branched-chain C.sub.1 -C.sub.4 -alkyl radical or a hydrogen atom, and then R.sup.12 and R.sup.13 each mean a hydrogen atom or together mean an additional bond,and R.sup.3 and R.sup.4 have the usual meanings indicated in the description for competitive progesterone antagonists.The invention further relates to a process for the production of new compounds, pharmaceutical preparations containing these compounds, their use for the production of pharmaceutical agents as well as the new intermediate products necessary for the process.The new compounds have a strong affinity to the gestagen receptor and show strong antigestagen as well as antiglucocorticoid, antimineral corticoid and antiandrogenic properties.

    摘要翻译： PCT No.PCT / EP91 / 02495 371日期1994年2月25日 102（e）1994年2月25日PCT PCT 1991年12月21日PCT公布。 出版物WO92 / 11279 日期：1992年7月9日。通式I（I）的新型D-均 - （16-烯）-11β-芳基-4-雌酮及其与酸的药学上相容的加成盐描述于其中 X表示氧原子，羟基亚氨基> N不同OH或两个氢原子，R1表示氢原子或甲基，R2表示羟基，C1-C10烷氧基或C1-C10酰氧基，R11 代表氟，氯或溴原子，然后R 12和R 13一起表示另外的键或R 11表示直链或支链的C 1 -C 4烷基或氢原子，则R 12和R 13各自表示 氢原子或一起表示另外的键，并且R3和R4具有在竞争性孕酮拮抗剂的描述中指出的通常含义。 本发明还涉及生产新化合物的方法，含有这些化合物的药物制剂，其用于生产药物的用途以及该方法所需的新的中间产物。 新化合物对孕激素受体具有强烈的亲和力，并显示出强的抗老化，以及抗糖皮质激素，抗癫痫皮质激素和抗雄激素的特性。