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81. 发明专利

AU4682000A Contraceptive compositions containing antiprogestinic and progestinic 未知
公开(公告)号：AU4682000A
公开(公告)日：2000-11-17
申请号：AU4682000
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： GRUBB GARY S , ZHI LIN , JONES TODD K , MARSCHKE KEITH B , TEGLEY CHRISTOPHER M
IPC分类号： A61K31/567 , A61K20060101 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/565 , A61K31/57 , A61K45/06 , A61P20060101 , A61P15/18

82. 发明专利

CA2372768A1 CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC UREA AND AMIDE DERIVATIVES 未知
公开(公告)号：CA2372768A1
公开(公告)日：2000-11-09
申请号：CA2372768
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： GRUBB GARY S , ZHI LIN , VIET ANDREW Q , JONES TODD K , TEREFENKO EUGENE A , TEGLEY CHRISTOPHER M , WROBEL JAY E , EDWARDS JAMES P , SANTILLI ARTHUR A , PUWEN ZHANG , FENSOME ANDREW
IPC分类号： C07D498/04 , A61K31/5365 , A61K31/565 , A61K31/57 , A61K45/06 , A61P5/32 , A61P5/36 , A61P15/08 , A61P15/18 , A61P35/00 , A61K31/12 , A61K31/495
摘要： This invention concerns cyclic combination therapies using indoline derivatives which are progesterone receptor antagonists of general structure (I) wherein: A, B and D are N or CH, though not all can be CH; R1 and R2 are H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R1 and R2 form a spirocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, alkyl alkyl; R3 is H, OH, NH2, alkyl, alkenyl, or CORC; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is benzene or a 5 or 6 memebered heteroaromatic ring; RF is H, alkyl, aryl, alkoxy, or aminoalkyl; RG is H or alkyl; R5 is H or alkyl; W is O or a chemical bond; or a 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 o f the invention include stimulation of food intake.

83. 发明专利

CA2372595A1 CONTRACEPTIVE COMPOSITIONS CONTAINING INDOLINE DERIVATIVES AND PROGESTATIONAL AGENTS 未知
公开(公告)号：CA2372595A1
公开(公告)日：2000-11-09
申请号：CA2372595
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC
发明人： ZHI LIN , TEGLEY CHRISTOPHER M , JONES TODD K , BENDER REINHOLD H W , ZHANG PUWEN , ULLRICH JOHN W , GRUBB GARY S , MILLER LORI L , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P
IPC分类号： C07D401/04 , A61K31/403 , A61K31/404 , A61K31/4439 , A61K31/535 , A61K31/56 , A61K31/57 , A61K45/06 , A61P15/18 , C07D209/34 , C07D209/96 , C07D405/04 , C07D409/04 , A61K31/40 , A61K31/565
摘要： This invention relates to cyclic combination therapies and regimens utilizin g substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (1), wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. 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 bleedin g. Additional uses of the invention include stimulation of food intake.

84. 发明专利

NO20003550D0 未知
公开(公告)号：NO20003550D0
公开(公告)日：2000-07-10
申请号：NO20003550
申请日：2000-07-10
申请人： LIGAND PHARM INC
发明人： JONES TODD K , POOLEY CHARLOTTE L F , EDWARDS JAMES E , TEGLEY CHRISTOPHER M , HAMANN LAWRENCE G , DAVIS ROBERT J , GOLDMAN MARK E , WINN DAVID T , WEST SARAH J , ZHI LIN , FARMER LUC J
IPC分类号： A61K31/435 , A61K31/47 , A61K31/473 , A61K31/4741 , A61P5/00 , A61P5/24 , C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/044 , C07D491/052 , C07D493/04 , C07D495/04 , A61K

85. 发明专利

NZ300739A Steroid receptor modulator compounds 未知
公开(公告)号：NZ300739A
公开(公告)日：2000-05-26
申请号：NZ30073995
申请日：1995-12-13
申请人： LIGAND PHARM INC
发明人： JONES TODD K , GOLDMAN MARK E , POOLEY CHARLOTTE L , WINN DAVID T , EDWARDS JAMES E , WEST SARAH J , TEGLEY CHRISTOPHER M , ZHI LIN , HAMANN LAWRENCE G , FARMER LUC J , DAVIS ROBERT J
IPC分类号： A61K31/435 , A61K31/47 , A61K31/473 , A61K31/4741 , A61P5/00 , A61P5/24 , C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/044 , C07D491/052 , C07D493/04 , C07D495/04
摘要： The steroid receptor modulator compounds have the formulae (I) to XVIII wherein: R1 is an optionally substituted heterocycle attached through a carbon or nitrogen atom; R3 is H, alkyl, perfluoroalkyl, hydroxymethyl, aryl, heteroaryl or optionally substituted allyl, arylmethyl, alkynyl or alkenyl; R4 to R6 and R11 to R15 are independently H, halo, NO2, CO2R2, COR2, CN, CF3, CH2OH, alkyl, perfluoroalkyl, OR2, S(O)2R2, SO3H, S(NR2R7)R2, S(O)(NR2R7)R2 ,NR2R7, aryl, heteroaryl or optionally substituted allyl, arylmethyl, alkynyl or alkenyl; R9 and R10 are independently H, alkyl, perfluoroalkyl, aryl, heteroaryl or optionally substituted allyl, arylmethyl, alkynyl or alkenyl or together are an optionally substituted three to seven membered ring; W is O, NR7, CH2, CHOH, C(O), O-C(O), (O)C-O, NR7CO, OCNR7, SC(O), (O)CS or CHO(CO)R7; X is CH2, O, S or NR7; R16 is H, OR17, SR17, NR2R7, optionally substituted allyl, arylmethyl, alkynyl, alkenyl, heteroaryl or aryl; R18 and R19 are independently H, alkyl, perfluoroalkyl aryl, heteroaryl or optionally substituted allyl, arylmethyl, alkynyl or alkenyl or together are an optionally substituted three to seven membered ring; R20 and R21 are independently alkyl or optionally substituted allyl, arylmethyl, alkynyl, aryl, heteroaryl or alkenyl; R22 is H, alkyl, halo, OR2, NR2R7 or SR2; R23 is H, halo, OR8, NR2R7, alkyl or perhaloalkyl or is optionally substituted allyl, arylmethyl, alkynyl, aryl, heteroaryl or alkenyl; R24 is H, halo, alkyl, perhaloalkyl, aryl, heteroaryl, CF3, CF2OR25, CH2OR25 or OR25; R26 is H, alkyl, halo, OR2, NR2R7 or SR2; R27 and R28 are independently H, alkyl, perfluoroalkyl, heteroaryl or optionally substituted allyl, arylmethyl, alkynyl, aryl or alkenyl or together are an optionally substituted three to seven membered ring; R29 is H, alkyl or optionally substituted allyl, arylmethyl, aryl or heteroaryl; R30 and R31 are independently H, alkyl or optionally substituted allyl, arylmethyl, alkynyl, aryl or alkenyl or together are an optionally substituted three to seven membered ring; R32 and R33 are independently H, alkyl or optionally substituted aryl or together are an optionally substituted three to seven membered ring; n is 0 or 1; Y is O or S; Z is O, S, NR2 or NCOR2; R2 and R7 are independently H or are as defined in the specification and R8, R25 and R17 are as defined in the specification limited by the provisos defined in the specification. A pharmaceutical composition thereof is useful as a PR or AR antagonist or as an estrogen, glucocorticoid or mineralocortocoid receptor agonist or antagonist.

86. 发明专利

ZA9901156B Glucocortiocoid-selective antiinflammatory agents. 未知
公开(公告)号：ZA9901156B
公开(公告)日：1999-08-12
申请号：ZA9901156
申请日：1999-02-12
申请人： ABBOTT LAB , LIGAND PHARM INC
发明人： COGHLAN MICHAEL J , ELMORE STEVEN W , KORT MICHAEL E , KYM PHILIP R , MOORE JIMMIE L , PRATT JOHN K , WANG ALAN X , EDWARDS JAMES P , JONES TODD K
IPC分类号： A61K20060101 , C07D20060101 , C07D , A61K

87. 发明专利

BR9510486A 未知
公开(公告)号：BR9510486A
公开(公告)日：1998-06-02
申请号：BR9510486
申请日：1995-12-13
申请人： LIGAND PHARM INC
发明人： FARMER LUC J , HAMANN LAWRENCE G , ZHI LIN , TEGLEY CHRISTOPHER M , WEST SARAH J , EDWARDS JAMES E , WINN DAVID T , POOLEY CHARLOTTE L F , GOLDMAN MARK E , DAVIS ROBERT J , JONES TODD K
IPC分类号： A61K31/435 , A61K31/47 , A61K31/473 , A61K31/4741 , A61P5/00 , A61P5/24 , C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/044 , C07D491/052 , C07D493/04 , C07D495/04

88. 发明专利

MX9704640A COMPUESTO MODULADORES DE LOS RECEPTORES DE LOS ESTEROIDES Y METODOS PARA SU PREPARACION. 未知
公开(公告)号：MX9704640A
公开(公告)日：1997-10-31
申请号：MX9704640
申请日：1995-12-13
申请人： LIGAND PHARM INC
发明人： JONES TODD K , GOLDMAN MARK E , CHARLOTTE POOLEY L F , WINN DAVID T , EDWARDS JAMES E , WEST SARAH J , TEGLEY CHRISTOPHER M , ZHI LIN , HAMANN LAWRENCE G
IPC分类号： C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D491/02 , C07D215/16
摘要： Se describen compuestos no esteroides que son moduladores de alta selectividad, alta afinidad para los receptores de esteroides. También se describen composiciones farmacéuticas que incorporan tales compuestos, métodos para emplear los compuestos y composiciones descritos para tratar pacientes que requieren terapia de agonista o antagonista del receptor de esteroides, intermediarios utiles en la preparacion de los compuestos y procesos para la preparacion de los compuestos moduladores de los receptores de esteroides.

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