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11. 发明授权

US06444668B1 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：US06444668B1
公开(公告)日：2002-09-03
申请号：US09552350
申请日：2000-04-19
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 to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 allyl C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alknyl, 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 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, 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 endometrium, ovary, breast, colon, prostate, or inmization 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环状组合疗法和方案：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烯丙基C 3至C 6烯基，取代的C 1至C 6烯基，炔基或取代的烷基，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; R 4是H，卤素，CN，NO 2，C 1至C 6烷基，取代的C 1至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。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，子宫内膜癌，卵巢癌，乳腺癌，结肠癌，前列腺癌，腺癌，副作用或周期性月经出血。本发明的额外用途包括刺激食物摄取。

12. 发明授权

US06399593B1 Cyclic regimens using cyclic urea and cyclic amide derivatives 失效
标题翻译：使用环状脲和环状酰胺衍生物的循环方案
公开(公告)号：US06399593B1
公开(公告)日：2002-06-04
申请号：US09552037
申请日：2000-04-19
申请人： Gary S. Grubb , Puwen Zhang , Arthur A. Santilli , Andrew Fensome , Eugene A. Terefenko , Andrew Q. Viet , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Arthur A. Santilli , Andrew Fensome , Eugene A. Terefenko , Andrew Q. Viet , 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 , A61K31/565 , A61K31/57 , A61K31/535 , A61K2300/00
摘要： This invention concerns cyclic combination therapies using progestational agents and indoline derivatives which are progesterone receptor antagonists of the general structure: 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 membered 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.
摘要翻译：本发明涉及使用孕激素和二氢吲哚衍生物的循环联合疗法，其为一般结构的孕酮受体拮抗剂：其中：A，B和D为N或CH，尽管不是全部可以是CH; R1和R2是H，CORA，NRBCORA或任选取代的烷基，烯基，炔基，环烷基或芳基; 或R 1和R 2形成螺环; RA为H或任选取代的烷基芳基，烷氧基或氨基烷基; RB是H，烷基烷基; R3是H，OH，NH2，烷基，烯基或CORC; RC是H，烷基，芳基，烷氧基或氨基烷基; R4是苯或5或6元杂芳环; RF是H，烷基，芳基，烷氧基或氨基烷基; RG为H或烷基; R5是H或烷基; W是O或化学键; 或其药学上可接受的盐。这些方法可用于避孕。

13. 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。

14. 发明授权

US06329416B1 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：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。

15. 发明授权

US06380235B1 Benzimidazolones and analogues 失效
标题翻译：苯并咪唑酮和类似物
公开(公告)号：US06380235B1
公开(公告)日：2002-04-30
申请号：US09552546
申请日：2000-04-19
申请人： Puwen Zhang , Reinhold H. W. Bender , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Puwen Zhang , Reinhold H. W. Bender , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31415
CPC分类号： C07D263/58 , C07C215/76 , C07C229/18 , C07D235/26 , C07D235/28 , C07D241/44 , C07D277/68 , C07D279/16 , C07D409/04 , C07D487/04
摘要： The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.
摘要翻译：本发明提供可用作孕酮受体激动剂和拮抗剂并具有以下通式的化合物和药物制剂：其中：A为O，S或NR4; B为A和C = Q之间的键，或部分CR5R6; R4， R5，R5独立地选自H或任选取代的C1至C6烷基，C2至C6烯基，C2至C6炔基，C3至C8环烷基，取代C3至C8环烷基，芳基或杂环基，或通过将R4 和R5至5至7元环; R1选自H，OH，NH2，C1至C6烷基，取代C1至C6烷基，C3至C6烯基，取代C1至C6烯基，炔基，取代的炔基，-COH或任选取代的-CO（C 1至C 3烷基），-CO（芳基），-CO（C 1〜C 3烷氧基）或-CO（C 1〜C 3氨基烷基） R 2选自H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，C 1至C 6烷氧基或C 1至C 6氨基烷基; R3选自三取代苯环; 或含有1或2个取代基的5或6元杂芳环; Q是O，S，NR8或CR9R10; 或其药学上可接受的盐。本发明还包括避孕方法和治疗或预防与孕酮受体相关的疾病的方法。

16. 发明授权

US06794373B2 Contraceptive methods using benzimidazolones 失效
标题翻译：使用苯并咪唑酮的避孕方法
公开(公告)号：US06794373B2
公开(公告)日：2004-09-21
申请号：US10091222
申请日：2002-03-01
申请人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , 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 , A61K31/415 , A61K31/535 , A61K31/54 , A61K31/56 , A61K31/57 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing indoline compounds which are antagonists of the progesterone receptor and having the general structure: A is O, S, or NR4; B is a bond or CR5R6; R4, to R6 are H, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, aryl, or heterocyclic, or R4 and R5 are fused to form a ring; R1 is H, OH, NH2, C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, or CORA; RA is as defined; R2 is H, halogen, CN, NO2, C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl; R3 is a substituted benzene ring, or heteroaromatic ring, in combination with a progestational agent and/or an estrogen to treat or prevent secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas, and contraception, among others.
摘要翻译：本发明涉及使用作为孕酮受体的拮抗剂并具有以下一般结构的二氢吲哚化合物的环组合疗法和方案：A是O，S或NR 4; B是键或CR 5 R 6; R 4至R 6是H，C 1至C 6烷基，C 2至C 6烯基，C 2至C 6炔基，C 3至C 8环烷基，芳基或杂环或R 4和R 5稠合形成环; R 1是H，OH，NH 2，C 1至C 6烷基，C 3至C 6烯基，炔基或COR 3; R 如定义; R 2是H，卤素，CN，NO 2，C 1至C 6烷基，C 1至C 6烷氧基或C 1至C 6氨基烷基; R 3是与促孕剂和/或雌激素组合的取代苯环或杂芳环，用于治疗或预防继发性闭经，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，癌和腺癌，以及避孕等等。

17. 发明授权

US06423699B1 Combination therapies using benzimidazolones 失效
标题翻译：联合治疗使用苯并咪唑酮
公开(公告)号：US06423699B1
公开(公告)日：2002-07-23
申请号：US09552355
申请日：2000-04-19
申请人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , 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 , A61K31/415 , A61K31/535 , A61K31/54 , A61K31/56 , A61K31/57 , 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: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R6 are independently selected from H or optionally substituted C1 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 R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, 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; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromnatic 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 to in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.
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组合疗法和方案：其中：A是O，S或NR4; B是A和C = Q之间的键，或 CR5R6部分; R4，R5，R6独立地选自H或任选取代的C1至C6烷基，C2至C6烯基，C2至C6炔基，C3至C8环烷基，取代C3至C8环烷基，芳基或杂环基，或由将R4和R5与5至7元环融合; R1选自H，OH，NH2，C1至C6烷基，取代C1至C6烷基，C3至C6烯基，取代C1至C6烯基，炔基，取代炔基，-COH或任选取代的-CO（C 1至C 3烷基），-CO（芳基），-CO（C 1〜C 3烷氧基）或-CO（C 1〜C 3氨基烷基） R2选自H，卤素，CN，NO2或任选取代的C1至C6烷基C1至C6烷氧基或C1至C6氨基烷基; R3选自三取代苯环; 或含有1或2个取代基的5-或6-元杂芳族环; 或其药学上可接受的盐与促孕剂，雌激素或两者组合，或用于治疗和/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，前列腺癌和腺癌。这些组合也可用于避孕方法，刺激食物摄取或最小化副作用或周期性月经出血。

18. 发明授权

US07081457B2 Cyclothiocarbamate derivatives as progesterone receptor modulators 失效
标题翻译：环硫代氨基甲酸酯衍生物作为孕酮受体调节剂
公开(公告)号：US07081457B2
公开(公告)日：2006-07-25
申请号：US10140034
申请日：2002-05-06
申请人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Jay E. Wrobel , Mark A. Collins
发明人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Jay E. Wrobel , Mark A. Collins
IPC分类号： A61K31/535 , C07D295/00 , C07D265/12
CPC分类号： A61K31/536 , A61K31/538 , C07D265/18 , C07D413/04
摘要： Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.
摘要翻译：提供使用孕酮受体激动剂用于避孕的化合物和单独或与雌激素受体激动剂或孕酮受体拮抗剂联合治疗孕激素相关性疾病的方法。这些化合物具有以下结构：其中R 1和R 2选自H，任选取代的C 1至C 1 - C 6烷基，链烯基，炔基或炔基C 3至C 8环烷基，芳基，取代的芳基或杂环基，或COR A 或或 B 或R 1和R 2 2稠合形成如本文所定义的任选取代的环结构; R＆lt; A＆gt;和＆lt; B＆gt; B＆gt;如本文所定义; R 3是H，OH，NH 2，COR C或任选取代的C 1至C

19. 发明授权

US06693103B2 1,2,3,4-tetrahydro-2-thioxo-quinolinyl and 1,2,3,4-tetrahydro-2-oxo-quinolinyl derivatives as progesterone receptor modulators 失效
标题翻译： 1,2,3,4-四氢-2-硫代 - 喹啉基和1,2,3,4-四氢-2-氧代喹啉基衍生物作为孕酮受体调节剂
公开(公告)号：US06693103B2
公开(公告)日：2004-02-17
申请号：US10023063
申请日：2001-12-17
申请人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： C07D215227
CPC分类号： C07D215/227 , A61K31/4704 , A61K31/517 , A61K31/536 , C07D215/38 , C07D239/80 , C07D265/16 , C07D413/04
摘要： This invention provides compounds which are agonists and antagonists of the progesterone receptor having the general structure: wherein: R1 and R2 are independently selected from H, CORA, or NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic moieties; or R1 and R2 are fused 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, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, CORC or optionally substituted alkyl, alkenyl, or alkynyl; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted alkyl alkynyl, alkoxy, amino or aminoalkyl; R5 is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR6; R6 is H or C1 to C3 alkyl; G1 is O, NR7, or CR7R8; G2 is CO, CS, 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, and methods using these compounds in mammals as agonists or antagonists of the progesterone receptor.
摘要翻译：本发明提供作为孕酮受体的激动剂和拮抗剂的化合物，其具有以下通式结构：其中：R 1和R 2独立地选自H，COR A或NR C COR 3，或任选取代的烷基，烯基，炔基，环烷基，芳基或杂环部分;或R 1和R 2稠合形成：3至8元螺环烷基，烯基或杂环; R A是H或任选取代的烷基，芳基，烷氧基或氨基烷基; R B是H，C 1至C 3烷基或取代的C 1至C 3烷基; R 3是H，OH，NH 2，COR C或任选取代的烷基，烯基或炔基; R C是H或任选取代的烷基，芳基，烷氧基或氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的烷基炔基，烷氧基，氨基或氨基烷基; R 5是任选取代的苯或具有1,2或3个选自O，S，SO，SO 2或NR 6的杂原子的五或六元环; R 6是H或C 1至C 3烷基; G1是O，NR7或CR7R8; G2是CO，CS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，以及在哺乳动物中使用这些化合物作为孕酮受体的激动剂或拮抗剂的方法。

20. 发明授权

US06358947B1 Tetracyclic progesterone receptor modulator compounds and methods 失效
标题翻译：四环孕酮受体调节剂的化合物及方法
公开(公告)号：US06358947B1
公开(公告)日：2002-03-19
申请号：US09552353
申请日：2000-04-19
申请人： Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , Andrew Fensome , Puwen Zhang , James P. Edwards
发明人： Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , Andrew Fensome , Puwen Zhang , James P. Edwards
IPC分类号： C07D49802
CPC分类号： C07D498/04
摘要： Nonsteroidal compounds that are high affinity, high selectivity modulators for progesterone receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring progesterone receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the progesterone receptor modulator compounds.
摘要翻译：公开了用于孕酮受体的高亲和力，高选择性调节剂的非甾体化合物。还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要孕酮受体激动剂，部分激动剂或拮抗剂治疗的患者的组合物，可用于制备化合物的中间体和用于制备孕酮受体调节剂化合物的方法。

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