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81. 发明授权

US06583145B1 Thio-oxindole derivatives 有权
标题翻译：硫氧吲哚衍生物
公开(公告)号：US06583145B1
公开(公告)日：2003-06-24
申请号：US10253380
申请日：2002-09-24
申请人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
发明人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
IPC分类号： A61K31404
CPC分类号： C07D209/40 , C07D209/08 , C07D209/30
摘要： This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
摘要翻译：本发明涉及作为孕酮受体的激动剂的具有以下通式结构的化合物：其中：R1，R2，R3，R4，R5和Q1如本文所定义，或其药学上可接受的盐，以及使用它们的方法化合物诱导避孕或治疗孕激素相关的癌和腺癌。

82. 发明授权

US06521657B2 Thio-oxindole derivatives 有权
公开(公告)号：US06521657B2
公开(公告)日：2003-02-18
申请号：US10022467
申请日：2001-10-30
申请人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
发明人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
IPC分类号： A61K31404
CPC分类号： C07D209/40 , C07D209/08 , C07D209/30
摘要： This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.

83. 发明授权

US06509334B1 Cyclocarbamate derivatives as progesterone receptor modulators 失效
标题翻译：环丙氨酸衍生物作为孕酮受体调节剂
公开(公告)号：US06509334B1
公开(公告)日：2003-01-21
申请号：US09552633
申请日：2000-04-19
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： C07D26518
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, N02, amino, and C1 to C3 alkyl, 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; 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。

84. 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。

85. 发明授权

US06441019B2 Cyclocarbamate and cyclic amide derivatives 失效
标题翻译：环氨基甲酸酯和环酰胺衍生物
公开(公告)号：US06441019B2
公开(公告)日：2002-08-27
申请号：US09906875
申请日：2001-07-17
申请人： 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： 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： A61K31535
CPC分类号： C07D498/04 , A61K31/5365
摘要： This invention provides compounds of the formula: 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 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. The compounds of this invention are useful as agonists and antagonists of the progesterone receptor and in methods of inducing contraception and in the treatment or prevention of benign or malignant neoplastic diseases.
摘要翻译：本发明提供下式的化合物：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。本发明的化合物可用作孕激素受体的激动剂和拮抗剂以及诱导避孕和治疗或预防良性或恶性肿瘤疾病的方法。

86. 发明授权

US06436929B1 Cyclothiocarbamate derivatives as progesterone receptor modulators 有权
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：US06436929B1
公开(公告)日：2002-08-20
申请号：US09552354
申请日：2000-04-19
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： A61K31535
CPC分类号： A61K31/536 , A61K31/538 , C07D265/18 , C07D413/04
摘要： The present invention provides compounds which are agonists of the progesterone receptor and have the structures: wherein R1 and R2 are independent substituents 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 3 to 8 membered Spiro cyclic alkyl or alkenyl ring or a Spiro cyclic ring containing one to three heteroatoms selected from O, S and N; RA is selected from H, amino, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is selected from H or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring with 1, 2, or 3 ring heteroatoms selected from the group of O, S, SO, SO2 or NR6; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds for contraception and the treatment of progesterone-related maladies.
摘要翻译：本发明提供作为孕酮受体的激动剂并具有以下结构的化合物：其中R 1和R 2是选自H，任选取代的C 1至C 6烷基，烯基，炔基或炔基的独立取代基C 3至C 8环烷基，芳基，取代的芳基或杂环基，或CORA或NRBCORA; 或R 1和R 2稠合形成任选取代的3至8元螺环烷基或烯基环或含有一至三个选自O，S和N的杂原子的螺环; RA选自H，氨基或任选取代的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; RB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，CORC或任选取代的C 1至C 6烷基，C 3至C 6烯基或炔基; RC选自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; Q1是S，NR7或CR8R9; R5是任选的三取代的苯环或具有1,2或3个选自O，S，SO，SO 2或NR 6的环杂原子的任选取代的五元或六元杂环; 或其药学上可接受的盐，以及使用这些化合物用于避孕和治疗孕酮相关性疾病的方法。

87. 发明授权

US06417214B1 3,3-substituted indoline derivatives 失效
标题翻译： 3,3-取代的二氢吲哚衍生物
公开(公告)号：US06417214B1
公开(公告)日：2002-07-09
申请号：US09552352
申请日：2000-04-19
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： A61K3142
CPC分类号： C07D209/08
摘要： This invention provides compounds of the formula 1: 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, 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1化合物：其中：R 1和R 2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连接形成包含-CH 2（CH 2）n CH 2 - 的环，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）; R 3是H，OH，NH 2，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，，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，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。

88. 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。

89. 发明授权

US06355648B1 Thio-oxindole derivatives 有权
标题翻译：硫氧吲哚衍生物
公开(公告)号：US06355648B1
公开(公告)日：2002-03-12
申请号：US09552033
申请日：2000-04-19
申请人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
发明人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
IPC分类号： A61K31505
CPC分类号： C07D209/40 , C07D209/08 , C07D209/30
摘要： This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl; 1-propynyl; or 3-propynyl; or R1 and R2 are joined to form an alkyl, alkenyl or heterocyclic ring; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, substituted alkynyl, or CORA; RA is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NH2, NO2, C1 to C6 alkyl, or substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; R5 is optionally substituted and selected from a benzene ring, a five or six membered heterocyclic ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR6; or an indol-4-yl, indol-7-yl or benzo-2-thiophene moiety; Q1 is S, NR7, CR8R9; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
摘要翻译：本发明涉及作为孕酮受体激动剂的化合物，其具有以下通式结构：其中：R 1和R 2为H，烷基，取代的烷基; 哦; O（烷基）; O（取代的烷基）; OAc; 芳基; 取代芳基; 杂芳基; 取代的杂芳基; 烷基芳基烷基杂芳基 1-丙炔基; 或3-丙炔基; 或R 1和R 2连接形成烷基，链烯基或杂环; 或R1和R2一起包含与CMe2的双键; C（环烷基），O或C（环醚）; 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，炔基，取代的炔基或CORA; RA为H，C1至C3烷基，取代C1至C3烷基，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，NH 2，NO 2，C 1至C 6烷基或取代的C 1 -C 6烷基，C 1至C 6烷氧基，取代的C 1至C 6烷氧基，C 1至C 6氨基烷基或取代的C 1至C 6氨基烷基; R5任选被取代并选自苯环，具有1,2或3个选自O，S，SO，SO 2或NR 6的杂原子的五元或六元杂环; 或吲哚基-4-基，吲哚-7-基或苯并-2-噻吩部分; Q1是S，NR7，CR8R9; 或其药学上可接受的盐，以及使用这些化合物诱导避孕或治疗孕酮相关的癌和腺癌的方法。

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