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    CONTRACEPTIVE COMPOSITIONS CONTAINING 3,3-SUBSTITUTED INDOLINE DERIVATIVES AND USES THEREOF
    1.
    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.

    CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC
    2.
    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.

    COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS
    6.
    发明公开
    COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS 审中-公开
    苯并咪唑酮组合物和孕激素CONTAIN

    公开(公告)号：EP1173213A1

    公开(公告)日：2002-01-23

    申请号：EP00932006.0

    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. ,  MARSCHKE, Keith, B. ,  TEGLEY, Christopher, M. ,  ZHANG, Puwen ,  BENDER, Reinhold,H.,W. ,  EDWARDS, JAMES, P. ,  WROBEL, Jay, E. ,  BENDER, Reinhold, H., W.

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

    CPC分类号： A61K45/06 ,  A61K31/415 ,  A61K31/535 ,  A61K31/54 ,  A61K31/56 ,  A61K31/57 ,  A61K31/565 ,  A61K31/495 ,  A61K31/425 ,  A61K31/42 ,  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 (1) wherein: A is O, S, or NR4; B is a bond between A and C=Q, or the moiety CR?5R6; R4, R5, R6¿ are independently selected from H or optionally substituted C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R?4 and R5¿ to form a 5 to 7 membered ring; R1 is selected from H, OH, NH¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alkynyl, -COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 to C3 aminoalkyl) groups; R?2¿ is selected from H, halogen, CN, NO¿2?, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R?3¿ is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both 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. These combinations may also be used in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.

    CONTRACEPTIVE COMPOSITIONS CONTAINING QUINAZOLINONE AND BENZOXAZINE DERIVATIVES
    8.
    发明公开
    CONTRACEPTIVE COMPOSITIONS CONTAINING QUINAZOLINONE AND BENZOXAZINE DERIVATIVES 审中-公开
    避孕组合物和喹唑酮衍生物苯并恶嗪包

    公开(公告)号：EP1173206A1

    公开(公告)日：2002-01-23

    申请号：EP00926488.8

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

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

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

    摘要： This invention relates to cyclic combination therapies utilizing, in combination with progestins, estrogens, or both, compounds which are progesterone receptor antagonists of general structure: (I) wherein: R?1 and R2¿ are H, COR?A, or NRBCORA¿, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic; or R?1 and R2¿ fuse 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 or alkyl; R3 is H, OH, NH¿2, COR?C or alkyl, alkenyl, or alkynyl; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO¿2?, alkyl, alkynyl, alkoxy, amino or aminoalkyl; R?5¿ is benzen or 5- or 6-membered heterocyclic ring; R6 is H or alkyl; G¿1? is O, NR7, or CR7R8; G2 is CO 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. These methods may be used for contraception or 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.

    CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC
    9.
    发明授权
    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：EP1173210B1

    公开(公告)日：2004-09-15

    申请号：EP00928611.3

    申请日：2000-05-01

    申请人： Wyeth ,  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.