利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

23 条记录 (耗时 0.022 秒)

    3,3-SUBSTITUTED INDOLINE DERIVATIVES
    1.
    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
    5.
    发明公开
    CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 有权
    CYCLOTHIOCARBAMATDERIVATE孕激素受体调节剂

    公开(公告)号：EP1175411A1

    公开(公告)日：2002-01-30

    申请号：EP00930266.2

    申请日：2000-05-01

    申请人： American Home Products Corporation ,  LIGAND PHARMACEUTICALS INCORPORATED

    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.

    CYCLOCARBAMATE AND CYCLIC AMIDE DERIVATIVES
    7.
    发明公开
    CYCLOCARBAMATE AND CYCLIC AMIDE DERIVATIVES 审中-公开
    环磷酰胺和ZYCLISCHE氨基酸

    公开(公告)号：EP1185535A1

    公开(公告)日：2002-03-13

    申请号：EP00928691.5

    申请日：2000-05-01

    申请人： American Home Products Corporation ,  LIGAND PHARMACEUTICALS INCORPORATED

    发明人： SANTILLI, Arthur, A. ,  VIET, Andrew, Q. ,  ZHANG, Puwen ,  FENSOME, Andrew ,  ZHI, Lin ,  JONES, Todd, K. ,  TEGLEY, Christopher, M. ,  WROBEL, Jay, E. ,  EDWARDS, James, P.

    IPC分类号： C07D498/04 ,  A61K31/535 ,  A61P15/18 ,  A61P35/00

    CPC分类号： C07D498/04 ,  A61K31/5365

    摘要： This invention provides compounds of formula (I) wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with a C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, COR?A, or NRBCORA; or R1 and R2¿ are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. The compounds of this invention are useful as agonists and antagonists of the progesterone receptor and in methods of inducing contraception and in the treatment or prevention of benign or malignant neoplastic diseases.

    CONTRACEPTIVE COMPOSITIONS CONTAINING 3,3-SUBSTITUTED INDOLINE DERIVATIVES AND USES THEREOF
    10.
    发明公开
    CONTRACEPTIVE COMPOSITIONS CONTAINING 3,3-SUBSTITUTED INDOLINE DERIVATIVES AND USES THEREOF 审中-公开
    避孕组合物，其3,3-取代衍生物。包含吲哚啉

    公开(公告)号：EP1173211A1

    公开(公告)日：2002-01-23

    申请号：EP00928667.5

    申请日：2000-05-01

    申请人： American Home Products Corporation ,  LIGAND PHARMACEUTICALS INCORPORATED

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

    IPC分类号： A61K45/06 ,  A61P15/18

    CPC分类号： A61K31/57 ,  A61K45/06 ,  A61K2300/00

    摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having general structure (I) wherein: R1, and R2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R1 and R2 are joined to form a ring comprising -CH2(CH2)nCH2- where n = 0-5; -CH2CH2CMe2CH2CH2-; -O(CH2)mCH2- where m = 1-4; O(CH2)pO- where p = 1-4; -CH2CH2OCH2CH2-; -CH2CH2N(H or alkyl)CH2CH2-; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl groups; RA = H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R¿4? = H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is selected from optionally substituted benzene ring; a five or six membered heterocyclic ring; a 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt thereof. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.