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1. 发明授权

US07192956B2 Methods of treating hormone-related conditions using cyclothiocarbamate derivatives 有权
标题翻译：使用环硫代氨基甲酸酯衍生物治疗激素相关病症的方法
公开(公告)号：US07192956B2
公开(公告)日：2007-03-20
申请号：US10601481
申请日：2003-06-23
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker , Puwen Zhang , Jeffrey Curtis Kern , Eugene Anthony Terefenko
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker , Puwen Zhang , Jeffrey Curtis Kern , Eugene Anthony Terefenko
IPC分类号： A61K31/535 , A61K31/445 , A61K31/135
CPC分类号： A61K31/426 , A61K31/536 , A61K31/54 , A61K31/554 , A61K31/565 , A61K2300/00
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1–R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供诱导避孕的方法，其包括递送给女性含有式I或式II化合物或其互变异构体的组合物，其方案包括递送一种或多种选择性雌激素受体调节剂，其中式I为：其中R 1〜Z 5和Q 1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

2. 发明申请

US20090099223A1 METHODS OF TREATING HORMONE-RELATED CONDITIONS USING THIO-OXINDOLE DERIVATIVES 失效
标题翻译：使用氧代衍生物处理与HORMONE相关的条件的方法
公开(公告)号：US20090099223A1
公开(公告)日：2009-04-16
申请号：US12336588
申请日：2008-12-17
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
IPC分类号： A61K31/438 , A61K31/403
CPC分类号： A61K31/404 , A61K45/06
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供了诱导避孕的方法，其包括将包含式I化合物或其互变异构体的组合物递送给女性，该方案涉及递送一种或多种选择性雌激素受体调节剂，其中式I是：并且其中 R1-R5和Q1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

3. 发明申请

US20120220558A1 Methods of Treating Hormone-Related Conditions Using Thio-Oxindole Derivatives 审中-公开
标题翻译：使用硫氧吲哚衍生物治疗激素相关病症的方法
公开(公告)号：US20120220558A1
公开(公告)日：2012-08-30
申请号：US13466375
申请日：2012-05-08
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
IPC分类号： A61K31/404 , A61K31/454 , A61P15/18 , A61K31/55 , A61P35/00 , A61P15/00 , A61K31/4535 , A61K31/567
CPC分类号： A61K31/404 , A61K45/06
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供了诱导避孕的方法，其包括将包含式I化合物或其互变异构体的组合物递送给女性，该方案涉及递送一种或多种选择性雌激素受体调节剂，其中式I是：并且其中 R1-R5和Q1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

4. 发明授权

US07488734B2 Methods of treating hormone-related conditions using thio-oxindole derivatives 失效
标题翻译：使用硫代羟吲哚衍生物治疗激素相关病症的方法
公开(公告)号：US07488734B2
公开(公告)日：2009-02-10
申请号：US10601438
申请日：2003-06-23
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
IPC分类号： A61K31/505 , A61K31/35
CPC分类号： A61K31/404 , A61K45/06
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供了诱导避孕的方法，其包括将包含式I化合物或其互变异构体的组合物递送给女性，该方案涉及递送一种或多种选择性雌激素受体调节剂，其中式I是：并且其中 R1-R5和Q1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

5. 发明授权

US08242098B2 Methods of treating hormone-related conditions using thio-oxindole derivatives 失效
标题翻译：使用硫代羟吲哚衍生物治疗激素相关病症的方法
公开(公告)号：US08242098B2
公开(公告)日：2012-08-14
申请号：US12336588
申请日：2008-12-17
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
IPC分类号： A61K31/56
CPC分类号： A61K31/404 , A61K45/06
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供了诱导避孕的方法，其包括将包含式I化合物或其互变异构体的组合物递送给女性，该方案涉及递送一种或多种选择性雌激素受体调节剂，其中式I是：并且其中 R1-R5和Q1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

6. 发明授权

US06759408B2 Combination regimens using progesterone receptor modulators 失效
标题翻译：使用孕酮受体调节剂的联合治疗方案
公开(公告)号：US06759408B2
公开(公告)日：2004-07-06
申请号：US10141792
申请日：2002-05-09
申请人： Gary S. Grubb , Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K31535
CPC分类号： A61K31/535 , A61K31/56 , Y10S514/843 , 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 the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.
摘要翻译：本发明涉及使用具有通式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R 1和R 2可以是单个取代基或稠合的; R 3是H，OH，NH 2，C 1 -C 6烷基，COR C或任选取代的C 1 -C 6烷基，C 3至C 6烯基或炔基; R C是H或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，炔基，C 1至C 6烷氧基，氨基或C 1至C 6氨基烷基; 和R 5为苯环，五或六元杂环; 或其药学上可接受的盐。治疗方法包括避孕，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，腺癌最小化副作用或食物摄取刺激。

7. 发明授权

US06498154B1 Cyclic regimens using quinazolinone and benzoxazine derivatives 失效
标题翻译：使用喹唑啉酮和苯并恶嗪衍生物的循环方案
公开(公告)号：US06498154B1
公开(公告)日：2002-12-24
申请号：US09552357
申请日：2000-04-19
申请人： Gary S. Grubb , Lin Zhi , Todd K. Jones , Puwen Zhang , James P. Edwards , Andrew Fensome , Eugene A. Terefenko , Jay E. Wrobel , Christopher M. Tegley
发明人： Gary S. Grubb , Lin Zhi , Todd K. Jones , Puwen Zhang , James P. Edwards , Andrew Fensome , Eugene A. Terefenko , Jay E. Wrobel , Christopher M. Tegley
IPC分类号： A61K3156
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 the general structure: wherein: R1 and R2 are H, CORA, or NRBCORA, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic; or R1 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, NH2, CORC or alkyl, alkenyl, or alkynyl; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO2, alkyl, alkynyl, alkoxy, amino or aminoalkyl; R5 is benzene or 5- or 6-membered heterocyclic ring; R6 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.
摘要翻译：本发明涉及利用与孕激素，雌激素或两者作为一般结构的孕酮受体拮抗剂的化合物的环状组合疗法：其中：R1和R2是H，CORA或NRBCORA，烷基，烯基，炔基，环烷基，芳基或杂环基; 或R1和R2融合形成3至8元螺环烷基，烯基或杂环; RA为H或任选取代的烷基，芳基，烷氧基或氨基烷基; RB是H或烷基; R3是H，OH，NH2，CORC或烷基，烯基或炔基; RC是H，烷基，芳基，烷氧基或氨基烷基; R4是H，卤素，CN，NO2，烷基，炔基，烷氧基，氨基或氨基烷基; R5是苯或5-或6-元杂环; R6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。

8. 发明授权

US06380178B1 Cyclic regimens using cyclocarbamate and cyclic amide derivatives 失效
标题翻译：使用环状氨基甲酸酯和环状酰胺衍生物的循环方案
公开(公告)号：US06380178B1
公开(公告)日：2002-04-30
申请号：US09552545
申请日：2000-04-19
申请人： Gary S. Grubb , Arthur A. Santilli , Andrew Q. Viet , Puwen Zhang , Andrew Fensome , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Arthur A. Santilli , Andrew Q. Viet , Puwen Zhang , Andrew Fensome , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K3156
CPC分类号： A61K31/56 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: where 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 an 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, CORA, or NRBCORA; or R1 and R2 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.
摘要翻译：本发明涉及利用与孕激素组合的取代二氢吲哚衍生物化合物的循环组合疗法和方案，所述二氢吲哚衍生化合物是具有以下通式结构的孕酮受体的拮抗剂：其中A和B是选自S，CH或N的独立取代基; 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，取代的杂环，CORA或NRBCORA; 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。

9. 发明授权

US06544970B2 Cyclic regimens utilizing indoline derivatives 失效
标题翻译：利用二氢吲哚衍生物的循环方案
公开(公告)号：US06544970B2
公开(公告)日：2003-04-08
申请号：US10153393
申请日：2002-05-22
申请人： Gary S. Grubb , Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K3156
CPC分类号： A61K45/06 , A61K31/535 , A61K31/56 , A61K31/57 , A61K31/565 , A61K31/40 , 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 the general structure: 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, 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, or prostate, minimization of side effects, cyclic menstrual bleeding, or stimulation of food intake.
摘要翻译：本发明涉及使用具有以下通式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循环联合疗法和方案：其中R1和R2可以是单取代基或稠合形成螺环，与孕激素，雌激素或两者兼有。这些治疗方法可用于避孕，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，结肠或前列腺的癌和腺癌，最小化副作用，周期性月经出血或刺激食物摄入。

10. 发明授权

US06503939B2 Combination regimens using 3,3-substituted indoline derivatives 失效
标题翻译：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。

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