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126 条记录 (耗时 0.089 秒)

    3,3-substituted indoline derivatives
    52.
    发明授权
    3,3-substituted indoline derivatives 失效
    3,3-取代的二氢吲哚衍生物

    公开(公告)号：US06835744B2

    公开(公告)日：2004-12-28

    申请号：US10131379

    申请日：2002-04-24

    申请人： John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    发明人： John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    IPC分类号： A61K31403

    CPC分类号： C07D209/08

    摘要： This invention provides compounds of the formula I: wherein: R1 and R2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl), aryl, or heteroaryl; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2C(CH3)2CH2CH2—; —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 C(CH3)2, 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; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is optionally substituted benzene ring; five or six membered heterocyclic ring; 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds as progesterone receptor antagonists.

    摘要翻译： 本发明提供式I化合物：其中：R 1和R 2独立地是H，OH，OAc，烷基芳基，烷基杂芳基，1-丙炔基，3-丙炔基和取代的烷基，O（烷基），芳基或杂芳基;或R 1 并且R 2连接形成包含-CH 2（CH 2）n CH 2 - 的环，其中n = 0-5; -CH 2 CH 2 C（CH 3）2 CH 2 CH 2 - ; -O（CH 2）m CH 2 - ，其中m = 1-4; O（CH 2）p O-，其中p = 1-4; -CH2CH2OCH2CH2-; -CH 2 CH 2 N（H或烷基）CH 2 CH 2 - ;或R 1和R 2一起包含与C（CH 3）2，C（环烷基），O或C（环醚）的双键; R 3是H，OH，NH 2， 或任选取代的烯基或炔基; R A = H或任选取代的烷基，烷氧基或氨基烷基; R 4 = H，卤素，CN，NH 2或任选取代的烷基，烷氧基或氨基烷基; 取代苯环; 五元或六元杂环; 4或7-取代的吲哚或取代的苯并噻吩;或其药学上可接受的盐，以及使用该化合物作为孕酮受体拮抗剂的药物组合物和方法。

    Cyclocarbamate derivatives as progesterone receptor modulators
    55.
    发明授权
    Cyclocarbamate derivatives as progesterone receptor modulators 失效
    环丙氨酸衍生物作为孕酮受体调节剂

    公开(公告)号：US06566358B2

    公开(公告)日：2003-05-20

    申请号：US09948309

    申请日：2001-09-06

    申请人： Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    发明人： Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    IPC分类号： A61K31536

    CPC分类号： C07D265/18 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04

    摘要： This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 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, CORC; RC 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; R4 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 R5 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 NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alky, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.

    摘要翻译： 本发明提供式（I）化合物：其中R 1和R 2可以是单个取代基或稠合形成螺环或杂 - 六环环; R 3是H，OH，NH 2，C 1 -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，CORC; RC为H，C1至C3烷基，取代C1至C3烷基，芳基，取代芳基，C1至C3烷氧基，取代C1至C3烷氧基，C1至C3氨基烷基或取代C1至C3氨基烷基; R4为H，卤素，CN 取代的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氨基烷基或取代的C 1至C 6氨基烷基; 并且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，并且包含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，CORF或NRGCORF; 或其药学上可接受的盐，以及使用该化合物作为孕酮受体的拮抗剂的药物组合物和方法。

    Cyanopyrroles
    56.
    发明授权
    Cyanopyrroles 有权
    青色

    公开(公告)号：US06562857B2

    公开(公告)日：2003-05-13

    申请号：US10043513

    申请日：2002-01-09

    申请人： Mark A. Collins ,  Valerie A. Mackner ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    发明人： Mark A. Collins ,  Valerie A. Mackner ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    IPC分类号： C07D40310

    CPC分类号： C07D403/04 ,  A61K31/405 ,  A61K31/5415 ,  C07D413/04

    摘要： This invention provides a progesterone receptor agonist 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 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; R4 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 CORB, RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof

    摘要翻译： 本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体激动剂; R 1和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，并且一起含有-CH 2（CH 2）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R 3是氢，OH，NH 2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的 氨基烷基或取代的氨基烷基; R 5为氢，烷基或取代的烷基; R 6为氢，烷基，取代的烷基或CORB， RB是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R7是氢或烷基; 或其药学上可接受的盐

    Combination regimens using 3,3-substituted indoline derivatives
    58.
    发明授权
    Combination regimens using 3,3-substituted indoline derivatives 失效
    使用3,3-取代的二氢吲哚衍生物的组合方案

    公开(公告)号：US06503939B2

    公开(公告)日：2003-01-07

    申请号：US09977790

    申请日：2001-10-15

    申请人： Gary S. Grubb ,  John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    发明人： Gary S. Grubb ,  John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    IPC分类号： A61K31405

    CPC分类号： A61K45/06 ,  A61K31/57 ,  A61K31/565 ,  A61K31/40 ,  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 the structure: wherein: R1 and R2 are (i) H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and optionally substituted alkyl, O(alkyl), aryl, or heteroaryl; (ii) a ring or (iii) a double bond; R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is a benzene ring; heterocyclic ring; an indole or benzothiophene; or pharmaceutically acceptable salt. R6 and R7 are H, methyl, ethyl, propyl, butyl, iso-propyl, isobutyl, cyclohexyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl. These methods may be used for contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas, cyclic menstrual bleeding, or food intake.

    摘要翻译： 本发明涉及使用具有以下结构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：R1和R2是（i）H，OH，OAc，烷基芳基，烷基杂芳基，1-丙炔基， 丙炔基和任选取代的烷基，O（烷基），芳基或杂芳基; （ii）环或（iii）双键; R3是H，OH，NH2，CORA; 或任选取代的烯基或炔基; RA = H或任选取代的烷基，烷氧基或氨基烷基; R4 = H，卤素，CN，NH2或任选取代的烷基，烷氧基或氨基烷基; R5是苯环; 杂环 吲哚或苯并噻吩; 或药学上可接受的盐。 R 6和R 7是H，甲基，乙基，丙基，丁基，异丙基，异丁基，环己基，芳基，取代的芳基，杂芳基或取代的杂芳基。 这些方法可用于避孕，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，癌，腺癌，周期性月经出血或食物摄入。

    Combination regimens using 3,3-substituted indoline derivatives
    60.
    发明授权
    Combination regimens using 3,3-substituted indoline derivatives 失效
    使用3,3-取代的二氢吲哚衍生物的组合方案

    公开(公告)号：US06329416B1

    公开(公告)日：2001-12-11

    申请号：US09552631

    申请日：2000-04-19

    申请人： Gary S. Grubb ,  John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    发明人： Gary S. Grubb ,  John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    IPC分类号： A01N4338

    CPC分类号： A61K45/06 ,  A61K31/57 ,  A61K31/565 ,  A61K31/40 ,  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 the general structure: 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; R4=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.

    摘要翻译： 本发明涉及使用具有一般结构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：R1和R2彼此独立地选自H，OH; OAc; 烷基芳基 烷基杂芳基 1-丙炔基; 3-丙炔基; 和任选取代的烷基，O（烷基）; 芳基; 或杂芳基; 或R 1和R 2与FORM连接，所述环包含-CH 2（CH 2）n CH 2 - ，其中n = 0-5; -CH2CH2CMe2CH2CH2-; -O（CH 2）m CH 2 - ，其中m = 1-4; O（CH 2）p O-，其中p = 1-4; -CH2CH2OCH2CH2-; -CH 2 CH 2 N（H或烷基）CH 2 CH 2 - ;或R 1和R 2一起包含与CMe2的双键; C（环烷基），O或C（环醚）; R3是H，OH，NH2，CORA; 或任选取代的烯基或炔基; RA = H或任选取代的烷基，烷氧基或氨基烷基; R 4 = H，卤素，CN，NH 2或任选取代的烷基，烷氧基或氨基烷基; R 5选自任选取代的苯环 ; 五元或六元杂环; 4或7-取代的吲哚或取代的苯并噻吩; 或其药学上可接受的盐。 这些治疗方法可用于避孕。