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59 条记录 (耗时 0.021 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。

    QUINAZOLINONE AND BENZOXAZINE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS
    4.
    发明公开
    QUINAZOLINONE AND BENZOXAZINE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 审中-公开
    喹唑啉酮和苯并恶嗪衍生物孕激素受体调节剂

    公开(公告)号：EP1175404A1

    公开(公告)日：2002-01-30

    申请号：EP00930288.6

    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. ,  EDWARDS, James, P. ,  TEGLEY, Christopher, M. ,  WROBEL, Jay, E.

    IPC分类号： C07D215/22 ,  C07D413/04 ,  C07D239/80 ,  C07D265/14 ,  C07D239/78 ,  A61K31/517 ,  A61P5/00

    摘要： This invention provides compounds which are agonists and antagonists of the progesterone receptor having general structure (I): wherein R?1 and R2¿ are independently selected from H, COR?A, or NRBCORA¿, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic moieties; or R?1 and R2¿ are fused to form: 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; RB 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 alkyl, alkenyl, or alkynyl; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO¿2?, or optionally substituted alkyl, alkynyl, alkoxy, amino or aminoalkyl; R?5¿ is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO¿2? or NR?6; R6¿ is H or C¿1? to C3 alkyl; G1 is O, NR7, or CR7R8; G2 is CO, CS, or CR7R8; provided that when G1 is O, G2 is CR7R8, and G1 and G2 cannot both be CR7R8; R7 and R8 are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof, and methods using these compounds in mammals as agonists or antagonists of the progesterone receptor.

    CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC
    5.
    发明公开
    CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC 有权
    避孕孕激素的组合物和孕激素拮抗剂含

    公开(公告)号：EP1173210A1

    公开(公告)日：2002-01-23

    申请号：EP00928611.3

    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 ,  EDWARDS, James, P. ,  FLETCHER, Horace, A. ,  WROBEL, Jay, E. ,  FENSOME, Andrew ,  ZHANG, Puwen ,  TEREFENKO, Eugene, A.

    IPC分类号： A61K45/06 ,  A61K31/57 ,  A61K31/565 ,  A61P15/18

    CPC分类号： A61K45/06 ,  A61K31/565 ,  A61K31/57 ,  A61K31/535 ,  A61K2300/00

    摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (I): wherein R?1 and R2¿ may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, COR?C; RC¿ is H, C¿1? to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R?4¿ is H, halogen, CN, NO¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R?5¿ is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO¿2? or NR?6¿ and containing one or two independent substituents from the group including H, halogen, CN, NO¿2? , amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, COR?F, or NRGCORF¿; 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 endormetrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention inlcude stimulation of food intake.

    CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS
    8.
    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.