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26 条记录 (耗时 0.039 秒)

    QUINAZOLINONE AND BENZOXAZINE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS
    12.
    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
    13.
    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.

    CYANOPYRROLES AS PROGESTERONE RECEPTOR AGONISTS
    16.
    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.

    CYCLIC UREA AND CYCLIC AMIDE DERIVATIVES
    20.
    发明公开
    CYCLIC UREA AND CYCLIC AMIDE DERIVATIVES 审中-公开
    环状脲和酰胺基

    公开(公告)号：EP1173443A1

    公开(公告)日：2002-01-23

    申请号：EP00928699.8

    申请日：2000-05-01

    申请人： American Home Products Corporation ,  LIGAND PHARMACEUTICALS INCORPORATED

    发明人： ZHANG, Puwen ,  SANTILLI, Arthur, A. ,  FENSOME, Andrew ,  TEREFENKO, Eugene, A. ,  VIET, Andrew Q. ,  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

    摘要： This invention provides compounds of formula (I) wherein: A, B and D are N or CH, with the proviso that A, B and D can not all be CH; R?1 and R2¿ are independent substituents selected from H, COR?A, NRBCORA¿, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or groups; or R?1 and R2¿ are fused to form an optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, C¿1? to C3 alkyl, or substituted C1 to C3 alkyl; R?3¿ is H, OH, NH¿2?, or optionally substituted alkyl, or alkenyl, or COR?C; Rc¿ is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is a substituted benzene ring or a five or six membered ring with 1, 2 or 3 heteroatoms from the group including O, S, SO, SO¿2? or NR?5; RF¿ is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RG is H, alkyl, or substituted alkyl; R5 is H or alkyl; Q is O, S, NR?6, or CR7R8; R6¿ is CN, SO¿2?CF3, or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic ring; R?7 and R8¿ are H, NO¿2?, CN CO2R?9¿, or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic; R9 is C1 to C3 alkyl; or CR7R8 form a six membered ring of structure (a): W is O or a chemical bond; or a pharmaceutically acceptable salt thereof, as well as their use and pharmaceutical compositions as agonists and antagonists of the progesterone receptor.