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    • 5. 发明申请
      WO0066165A8 CONTRACEPTIVE COMPOSITIONS CONTAINING QUINAZOLINONE AND BENZOXAZINE DERIVATIVES 审中-公开
    • CONTRACEPTIVE COMPOSITIONS CONTAINING QUINAZOLINONE AND BENZOXAZINE DERIVATIVES
    • 含有喹唑啉酮和苯并恶唑衍生物的合成组合物
    • WO0066165A8
    • 2001-11-22
    • PCT/US0011644
    • 2000-05-01
    • AMERICAN HOME PROD , LIGAND PHARM INC , GRUBB GARY S , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , ZHANG PUWEN , FENSOME ANDREW , TEREFENKO EUGENE A , WROBEL JAY E , EDWARDS JAMES P
    • GRUBB GARY S , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , ZHANG PUWEN , FENSOME ANDREW , TEREFENKO EUGENE A , WROBEL JAY E , EDWARDS JAMES P
    • C07D239/80 , A61K31/4704 , A61K31/517 , A61K31/536 , A61K31/565 , A61K31/567 , A61K31/57 , A61K45/06 , A61P15/18 , A61P35/00 , C07D215/22 , C07D265/16
    • A61K31/565 , A61K31/57 , A61K45/06 , A61K2300/00
    • 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 and R are H, COR , or NR COR , alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic; or R and R fuse to form 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; R is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; R is H or alkyl; R is H, OH, NH2, COR or alkyl, alkenyl, or alkynyl; R is H, alkyl, aryl, alkoxy, or aminoalkyl; R is H, halogen, CN, NO2, alkyl, alkynyl, alkoxy, amino or aminoalkyl; R is benzen or 5- or 6-membered heterocyclic ring; R is H or alkyl; G1 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.
    • 本发明涉及利用与孕激素，雌激素或两者结合的孕酮受体拮抗剂组合的循环组合疗法，其通式结构如下：（I）其中：R 1和R 2为H，COR A 或NR C COR A，烷基，烯基，炔基，环烷基，芳基或杂环; 或R 1和R 2融合形成3至8元螺环烷基，烯基或杂环; R AA是H或任选取代的烷基，芳基，烷氧基或氨基烷基; R B是H或烷基; R 3是H，OH，NH 2，COR C或烷基，烯基或炔基; R C是H，烷基，芳基，烷氧基或氨基烷基; R 4是H，卤素，CN，NO 2，烷基，炔基，烷氧基，氨基或氨基烷基; R 5是苯或5-或6-元杂环; R 6是H或烷基; G1是O，NR7或CR7R8; G2为CO或CR7R8; 条件是当G1为O时，G2为CR7R8，G1和G2不能为CR7R8; R 7和R 8是H或任选取代的烷基，芳基或杂环部分; 或其药学上可接受的盐。 这些方法可用于避孕或治疗和/或预防继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症; 多囊卵巢综合征，子宫内膜，卵巢，乳腺，结肠，前列腺的癌和腺癌，或副作用最小化或周期性月经出血。 本发明的额外用途包括刺激食物摄取。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 7. 发明申请
      WO0066164A8 CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC 审中-公开
    • CONTRACEPTIVE COMPOSITIONS CONTAINING ANTIPROGESTINIC AND PROGESTINIC
    • 含有抗菌素和抗生素的合成组合物
    • WO0066164A8
    • 2001-05-03
    • PCT/US0011643
    • 2000-05-01
    • AMERICAN HOME PROD , LIGAND PHARM INC , GRUBB GARY S , ZHI LIN , JONES TODD K , MARSCHKE KEITH B , TEGLEY CHRISTOPHER M , ZHANG PUWEN , TEREFENKO EUGENE A , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P , FLETCHER HORACE A
    • GRUBB GARY S , ZHI LIN , JONES TODD K , MARSCHKE KEITH B , TEGLEY CHRISTOPHER M , ZHANG PUWEN , TEREFENKO EUGENE A , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P , FLETCHER HORACE A
    • A61K31/567 , A61K20060101 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/565 , A61K31/57 , A61K45/06 , A61P20060101 , A61P15/18
    • A61K45/06 , A61K31/565 , A61K31/57 , A61K31/535 , A61K2300/00
    • 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 and R may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, COR ; R is H, C1 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 is H, halogen, CN, NO2, 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 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, SO2 or NR and containing one or two independent substituents from the group including H, halogen, CN, NO2 , amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, COR , or NR COR ; 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.
    • 本发明涉及使用具有通式结构（I）的孕酮受体的拮抗剂的取代的二氢吲哚衍生物化合物的环状组合疗法和方案：其中R 1和R 2可以是单个取代基或稠合形成螺环或异 - 螺环; R 3是H，OH，NH 2，C 1至C 6烷基，取代的C 1 -C 6烷基，C 3至C 6烯基，取代的C 1至C 6烯基，炔基或取代的炔基。 R C是H，C 1至C 3烷基，取代的C 1至C 3烷基，芳基，取代的芳基，C 1至C 3的烷氧基，取代的C 1至C 3的烷氧基，C 1至C 3的氨基烷基或取代的C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2，C 1至C 6烷基，取代的C 1 -C 6烷基，炔基或取代的炔基，C 1至C 6烷氧基，取代的C 1至C 6烷氧基，氨基，C 1至C 6氨基烷基或取代 C1至C6氨基烷基; R 5选自具有1,2或3个杂原子的五元或六元环的三取代苯环，所述杂原子包括O，S，SO，SO 2或NR 6，并含有一个或两个独立的取代基 包括H，卤素，CN，NO 2，氨基和C 1至C 3烷基，C 1至C 3烷氧基，C 1至C 3氨基烷基，COR F或NR G COR F; 或其药学上可接受的盐。 这些治疗方法可用于避孕或治疗和/或预防继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症; 多囊卵巢综合征，宫内膜，卵巢，乳腺，结肠，前列腺的癌和腺癌，或副作用或周期性月经出血的最小化。 本发明的另外用途包括刺激食物摄取。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO0066225A8 CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC CARBAMATES AND AMIDE DERIVATIVES 审中-公开
    • CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC CARBAMATES AND AMIDE DERIVATIVES
    • 含有环状碳酸酯和酰胺衍生物的合成组合物
    • WO0066225A8
    • 2002-05-30
    • PCT/US0011846
    • 2000-05-01
    • AMERICAN HOME PROD , LIGAND PHARM INC , GRUBB GARY S , ZHI LIN , JONES TODD K , SANTILLI ARTHUR A , TEGLEY CHRISTOPHER M , VIET ANDREW Q , ZHANG PUWEN , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P
    • GRUBB GARY S , ZHI LIN , JONES TODD K , SANTILLI ARTHUR A , TEGLEY CHRISTOPHER M , VIET ANDREW Q , ZHANG PUWEN , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P
    • C07D498/04 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/5365 , A61K31/56 , A61K45/06 , A61P15/18 , A61K31/565 , A61K31/57
    • A61K31/56 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/565 , A61K45/06 , A61K2300/00
    • This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, estrogens, or both, substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (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 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 , or NR COR ; or R and R 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. 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.
    • 本发明涉及利用与孕激素，雌激素或两者作为孕酮受体的拮抗剂的代用药物，其具有一般结构（I）的循环组合疗法和方案，其中A和B是选自S，CH 或N; 条件是当A为S时，B为CH或N; 当B为S时，A为CH或N; A和B不能同时为CH; 并且当A和B均等于N时，一个N可以任选地被C 1至C 6烷基取代; R1和R2是选自H，C1至C6烷基，取代C1至C6烷基，C2至C6烯基，取代C2至C6烯基，C2至C6炔基，取代C2至C6炔基，C3至C8环烷基的独立取代基 取代的C 3至C 8环烷基，芳基，取代的芳基，杂环基，取代的杂环基，COR A或NR C CORA; 或R 1和R 2稠合形成任选取代的3至8元螺环烷基，烯基或杂环，所述杂环含有一至三个选自O，S和N的杂原子; 或其药学上有用的盐。 这些治疗方法可用于避孕或治疗和/或预防继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症; 多囊卵巢综合征，子宫内膜，卵巢，乳腺，结肠，前列腺的癌和腺癌，或副作用最小化或周期性月经出血。 本发明的额外用途包括刺激食物摄取。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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