利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

6 条记录 (耗时 0.022 秒)

    3,3-SUBSTITUTED INDOLINE DERIVATIVES
    3.
    发明公开
    3,3-SUBSTITUTED INDOLINE DERIVATIVES 有权
    3,3-取代的吲哚啉衍生物

    公开(公告)号：EP1175397A1

    公开(公告)日：2002-01-30

    申请号：EP00930201.9

    申请日：2000-05-01

    申请人： AMERICAN HOME PRODUCTS CORPORATION ,  LIGAND PHARMACEUTICALS, INC.

    发明人： ULLRICH, John, W. ,  FENSOME, Andrew ,  ZHI, Lin ,  JONES, Todd, K. ,  WROBEL, Jay, E. ,  TEGLEY, Christopher, M. ,  EDWARDS, James, P.

    IPC分类号： C07D209/08 ,  A61K31/404 ,  A61P5/36

    CPC分类号： C07D209/08

    摘要： A compound of formula (I) and pharmaceutical compositions thereof useful as progesterone receptor antagonist wherein: R1 and R2 are H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, optionally substituted alkyl, O(alkyl), aryl, heteroaryl; or R1 and R2 are joined to form a ring, a double bond to CMe2; C(cycloalkyl), O, C(cycloether); R3 = H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl; RA = H, optionally substituted alkyl, alkoxy, aminoalkyl; R¿4? = H, halo, CN, NH2, optionally substituted alkyl, alkoxy, or aminoalkyl; R5 = optionally substituted phenyl, a 5- or 6-membered heterocycle; a 4- or 7-substituted indole or a substituted benzothiophene.

    摘要翻译： 其中：R1和R2为H，OH，OAc，烷基芳基，烷基杂芳基，1-丙炔基，任选取代的烷基，O（烷基），芳基，杂芳基; 或R1和R2连接形成环，与CMe2形成双键; C（环烷基），O，C（环醚）; R3 = H，OH，NH2，CORA或任选取代的链烯基或炔基; RA = H，任选取代的烷基，烷氧基，氨基烷基; R¿4？ = H，卤素，CN，NH 2，任选取代的烷基，烷氧基或氨基烷基; R5 =任选取代的苯基，5或6元杂环; 4-或7-取代的吲哚或取代的苯并噻吩。

    CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS
    4.
    发明授权
    CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 有权
    CYCLOTHIOCARBAMATDERIVATE孕激素受体调节剂

    公开(公告)号：EP1175411B1

    公开(公告)日：2008-02-20

    申请号：EP00930266.2

    申请日：2000-05-01

    申请人： Wyeth

    发明人： ZHANG, Puwen ,  FENSOME, Andrew ,  TEREFENKO, Eugene, A. ,  ZHI, Lin ,  JONES, Todd, K. ,  COLLINS, MARK, A. ,  TEGLEY, Christopher, M. ,  WROBEL, Jay, E. ,  EDWARDS, James, P.

    IPC分类号： C07D265/18 ,  C07D413/04 ,  A61K31/536 ,  A61P15/00 ,  A61P35/00

    CPC分类号： C07D265/18 ,  C07D413/04

    摘要： The present invention provides compounds which are agonists of the progesterone receptor and have structures (I) or (II) wherein R1 and R2 are independent substituents selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or COR?A or NRBCORA; or R1 and R2¿ are fused to form an optionally substituted 3 to 8 membered Spiro cyclic alkyl or alkenyl ring or a Spiro cyclic ring containing one to three heteroatoms selected from O, S and N; RA is selected from H, amino, or optionally substituted C¿1? to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; R?B¿ is H, C¿1? to C3 alkyl, or substituted C1 to C3 alkyl; R?3¿ is H, OH, NH¿2 COR?C, or optionally substituted C¿1? to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; R?C¿ is selected from H or optionally substituted C¿1? to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; Q?1¿ is S, NR?7; or CR8R9, R5¿ is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring with 1, 2, or 3 ring heteroatoms selected from the group of O, S, SO, SO¿2? or NR?6¿; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds for contraception and the treatment of progesterone-related maladies.

    CYANOPYRROLES AS PROGESTERONE RECEPTOR AGONISTS
    6.
    发明授权
    CYANOPYRROLES AS PROGESTERONE RECEPTOR AGONISTS 有权
    CYANOPYRROLE ALS PROGESTERONREZEPTORAGONISTEN

    公开(公告)号：EP1173433B1

    公开(公告)日：2005-12-28

    申请号：EP00932005.2

    申请日：2000-05-01

    申请人： Wyeth ,  LIGAND PHARMACEUTICALS INCORPORATED

    发明人： COLLINS, Mark, A. ,  MACKNER, Valerie, A. ,  ZHI, Lin ,  JONES, Todd, K. ,  TEGLEY, Christopher, M. ,  WROBEL, Jay, E. ,  EDWARDS, James, P.

    IPC分类号： C07D413/04 ,  C07D403/04 ,  A61K31/40 ,  A61P15/16

    CPC分类号： C07D403/04 ,  A61K31/405 ,  A61K31/5415 ,  C07D413/04

    摘要： This invention provides a progesterone receptor antagonist of formula (1) having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together to form a ring and together contain -CH2(CH2)nCH2-, -CH2CH2CMe2CH2CH2-, -O(CH2)pCH2-, -O(CH2)qO-, -CH2CH2OCH2CH2-, or -CH2CH2NR7CH2CH2-; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R¿4? is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or COR?B; RB¿ is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R¿7? is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.