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    SELECTIVE GLUCOCORTICOID RECEPTOR AGONISTS
    2.
    发明申请
    SELECTIVE GLUCOCORTICOID RECEPTOR AGONISTS 失效
    选择性GLUCOCORTICOID受体激动剂

    公开(公告)号：US20080090792A1

    公开(公告)日：2008-04-17

    申请号：US11737185

    申请日：2007-04-19

    申请人： Stephen Barr ,  Michael McKervey ,  Hughes Miel ,  David Ray ,  Andrew Brass

    发明人： Stephen Barr ,  Michael McKervey ,  Hughes Miel ,  David Ray ,  Andrew Brass

    IPC分类号： A61K31/56 ,  A61K31/58 ,  A61P29/00 ,  A61P37/06 ,  A61P7/00

    CPC分类号： C07J5/0092 ,  C07J3/005 ,  C07J21/003 ,  C07J41/0011 ,  C07J41/0038

    摘要： This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein R═NH2, NHR1, NHOR2, NHNHR2, NHCOR2, and R1═C(1-4)alkyl, C(3-6)cycloalkyl, Cn, where n=1-3, R2=methyl, ethyl, R3=alkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetrecoaryl; wherein R4, R5═C(1-4)alkyl. Novel compounds according to Formula (III), wherein R6 and R7 are any of H, CH3CO, CH3CH2CO, CH3CH2CH2CO provided that R6 and R7 are not both H, or Formula (IV), wherein R5 and R9 are any of H, CH3CO, CH3CH2CO or CH3CH2CH2CO, having use in such methods, are also described.

    摘要翻译： 本发明涉及治疗炎性病症，治疗血液学和其他恶性肿瘤，引起免疫抑制，或预防或治疗人或其他动物中的移植排斥的方法，其包括向患者施用具有式（I）结构的化合物， 或下式定义的式（II）或其药学上可接受的衍生物或其前体药物，其中R-NH 2，NHR 1，NHOR 2， ，NHNHR 2，NHCOR 2和R 1 -C 1-4烷基，（C 1 -C 4）烷基， C 3-6（C 3-6）环烷基，C n为N，其中n = 1-3，R 2 =甲基，乙基， 烷基，环烷基，取代的烷基，取代的环烷基，芳基，杂芳基，取代的芳基或取代的hetrecoaryl; 其中R 4，R 5 -C（1-4） - 烷基）。 根据式（III）的新型化合物，其中R 6和R 7是H，CH 3 CO，CH 3 CH 2 CO 2，CH 3 CH 2 CH 2 CO，条件是R 6 和/或R 7不同时为H或式（Ⅳ），其中R 5和R 9为H， CH 3 CO，CH 3 CH 2 CO或CH 3 CH 2 CH 2 也描述了在这些方法中使用的CO 2。

    Lambda-1,4-pregnadiene-3,20-diones
    4.
    发明授权
    Lambda-1,4-pregnadiene-3,20-diones 失效
    λ-1,4-孕二烯-3,20-二酮

    公开(公告)号：US5451690A

    公开(公告)日：1995-09-19

    申请号：US372647

    申请日：1995-01-13

    申请人： Luc Devocelle ,  Philippe Mackiewicz

    发明人： Luc Devocelle ,  Philippe Mackiewicz

    IPC分类号： A61K31/57 ,  B01J27/10 ,  C07B61/00 ,  C07J5/00 ,  C07J71/00 ,  C07J7/00

    CPC分类号： C07J71/0031 ,  C07J5/0092

    摘要： A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and aralkoxycarbonyl of up to 8 carbon atoms and alkylsulfonyl and arylsulfonyl of up to 8 carbon atoms and their use to prepare substituted 16,17-methylenedioxy-steroids and novel intermediates.

    摘要翻译： 式Ⅰ化合物，其中R选自氢，碳原子数1〜8的有机羧酸的酰基，高达8个碳原子的烷氧羰基和芳烷氧基羰基，烷基磺酰基和芳基磺酰基 至8个碳原子，并用于制备取代的16,17-亚甲二氧基类固醇和新型中间体。

    Pregnanoic acid derivatives and process for the preparation thereof
    5.
    发明授权
    Pregnanoic acid derivatives and process for the preparation thereof 失效
    孕酸衍生物及其制备方法

    公开(公告)号：US3919421A

    公开(公告)日：1975-11-11

    申请号：US42670273

    申请日：1973-12-20

    申请人： SCHERING AG

    发明人： LAURENT HENRY ,  WIECHERT RUDOLF ,  HOFMEISTER HELMUT ,  MENGEL KLAUS ,  WENDT HANS ,  ANNEN KLAUS

    IPC分类号： C07J5/00 ,  C07J71/00 ,  C01B7/00

    CPC分类号： C07J5/0092 ,  C07J71/0031

    摘要： Pharmacologically active pregnanoic acid derivatives of the Formula I

    wherein -A-B- is -CH2-CH2-, -CH CH-, or -CCl CH-; X is a hydrogen atom, a halogen atom, or methyl; -Y-Z- is -CH-CH2-, C CH-, -CV-CHOU-, -CV-CO-, -CW-CHW''-, wherein U is a hydrogen atom or acyl, V is a hydrogen atom or a halogen atom, and W and W'' each are a halogen atom; R1 is alkyl; R2 is alkyl or aryl; or, R1 and R2 together represent a tetramethylene group or pentamethylene group; R3 is a hydrogen atom, an alkali metal atom, or a hydrocarbon. The invention also comprises the process of producing the compounds by various procedures.

    摘要翻译： 其中-A-B-是-CH 2 -CH 2 - ， - CH = CH-或-CCl = CH-的式I的药理学活性孕酸衍生物; X是氢原子，卤素原子或甲基; -YZ-是-CH-CH2-，-C = CH-，-CV-CHOU-，-CV-CO-，-CW-CHW'-，其中U是氢原子或酰基，V是氢原子或 卤素原子，W和W'各自为卤素原子; R1是烷基; R2是烷基或芳基; 或者R1和R2一起表示四亚甲基或五亚甲基; R3是氢原子，碱金属原子或烃。

    Selective glucocorticoid receptor agonists
    6.
    发明申请
    Selective glucocorticoid receptor agonists 审中-公开
    选择性糖皮质激素受体激动剂

    公开(公告)号：US20040102425A1

    公开(公告)日：2004-05-27

    申请号：US10415711

    申请日：2003-12-05

    发明人： Alexander Stephen Barr ,  Michael Anthony McKervey ,  Hughes Jean-Pierre Miel ,  David William Ray ,  Andrew Michael Brass

    IPC分类号： A61K031/58 ,  A61K031/573

    CPC分类号： C07J5/0092 ,  C07J3/005 ,  C07J21/003 ,  C07J41/0011 ,  C07J41/0038

    摘要： This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein RnullNH2, NHR1, NHOR2, NHNHR2, NHCOR2, and R1nullC(1-4)alkyl, C(3-6)cycloalkyl, Cn, where nnull1-3, R2nullmethyl, ethyl, R3nullalkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetreoaryl; wherein R4, R5nullC(1-4)alkyl. Novel compounds according to Formula (III), wherein R6 and R7 are any of H, CH3CO, CH3CH2CO, CH3CH2CH2CO provided that R6 and R7 are not both H, or Formula (IV), wherein R8 and R9 are any of H, CH3CO, CH3CH2CO or CH3CH2CH2CO, having use in such methods, are also described.

    摘要翻译： 本发明涉及治疗炎性病症，治疗血液学和其他恶性肿瘤，引起免疫抑制，或预防或治疗人或其他动物中的移植排斥的方法，其包括向患者施用具有式（I）结构的化合物， 或下式定义的式（II）或其药学上可接受的衍生物或其前体药物，其中R = NH 2，NHR 1，NHOR 2，NHNHR 2，NHCOR 2和R 1 = C（1-4）烷基，C（3-6）环烷基，Cn，其中n = 1-3，R2 =甲基，乙基，R3 =烷基，环烷基，取代的烷基，取代的环烷基，芳基， 芳基或取代的杂芳基; 其中R 4，R 5 = C（1-4）烷基。 根据式（III）的新化合物，其中R 6和R 7是H，CH 3 CO，CH 3 CH 2 CO，CH 3 CH 2 CH 2 CO 2中的任何一个，条件是R 6和R 7不同时为H或式（IV） 其中R 8和R 9是在这些方法中使用的H，CH 3 CO，CH 3 CH 2 CO或CH 3 CH 2 CH 2 CO中的任何一种。

    Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions
    8.
    发明授权
    Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions 失效
    前草-1,4-二烯-3,20-二酮-16-17-乙缩醛-21酯，其制备方法，组合物和治疗炎性病症的方法

    公开(公告)号：US5482934A

    公开(公告)日：1996-01-09

    申请号：US278112

    申请日：1994-07-20

    申请人： Jose Calatayud ,  Jose R. Conde ,  Manuel Luna

    发明人： Jose Calatayud ,  Jose R. Conde ,  Manuel Luna

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

    CPC分类号： C07J5/0092 ,  C07J71/0031

    摘要： The present invention relates to compounds of the formula: ##STR1## in which X.sub.1 and X.sub.2 correspond to H or F without distinction; R.sub.1 represents the following radicals: ##STR2## and R.sub.2 represents the radicals ##STR3## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, novel intermediates and a method of their preparation by hydrolysis-ketalization, and use of such compounds as drugs and/or therapeutic agents.

    摘要翻译： 本发明涉及下式的化合物：其中X1和X2不区分对应于H或F; R1表示以下基团：R 1和R 2分别代表取代基的R取代基的取代基的R差向异构体，S差向异构体或立体异构体混合物的形式的基团 在22位的碳原子上，新的中间体及其通过水解缩醛化制备的方法，以及使用这些化合物作为药物和/或治疗剂。

    Anti-inflammatory carboxycyclic acetal pregnane derivatives
    9.
    发明授权
    Anti-inflammatory carboxycyclic acetal pregnane derivatives 失效
    抗炎性羧基环缩醛孕烷衍生物

    公开(公告)号：US5200518A

    公开(公告)日：1993-04-06

    申请号：US658542

    申请日：1991-02-21

    申请人： Hyun P. Kim ,  Kwan S. Sin ,  Chang M. Kim ,  Moon Y. Heo ,  Henry J. Lee

    发明人： Hyun P. Kim ,  Kwan S. Sin ,  Chang M. Kim ,  Moon Y. Heo ,  Henry J. Lee

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J13/00 ,  C07J21/00 ,  C07J41/00 ,  C07J71/00

    CPC分类号： C07J13/005 ,  C07J21/00 ,  C07J41/005 ,  C07J5/0092 ,  C07J7/0095 ,  C07J71/0031

    摘要： Compounds of the formula: ##STR1## wherein X is H, F, Cl, or CH.sub.3and Y is ##STR2## wherein R.sub.1 is H, alkyl of 1-5 carbon atoms, phenyl, or benzyl;R.sub.2 is COOR.sub.6, R.sub.5 COOR.sub.6, or R.sub.5 CONHR.sub.6 ;R.sub.3 is H, F, OH, or CH.sub.3 ;R.sub.4 is CH.sub.2 OH, CH.sub.2 OCOR.sub.6, COOR.sub.6, or CONHR.sub.6 ;R.sub.5 is alkyl of 1-3 carbon atoms;R.sub.6 is alkyl of 1-5 carbon atoms, or benzyl; represents a single or double bond;.about. represents .alpha.-position, .beta.-position, or a mixture of both .alpha.- and .beta.-positions; and-- represents .alpha.-position;and methods for preparing the same.

    摘要翻译： 其中X是H，F，Cl或CH 3，Y是下式的化合物：其中R 1是H，1-5个碳原子的烷基，苯基或苄基; R2是COOR6，R5 COOR6或R5CONHR6; R3是H，F，OH或CH3; R4是CH2OH，CH2OCOR6，COOR6或CONHR6; R5是1-3个碳原子的烷基; R6是1-5个碳原子的烷基，或苄基; 代表单键或双键; 差异表示α位，β位，或α和β位的混合物; 和 - 表示α位; 及其制备方法。