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31. 发明授权

US06391907B1 Indoline derivatives 失效
标题翻译：二氢吲哚衍生物
公开(公告)号：US06391907B1
公开(公告)日：2002-05-21
申请号：US09552632
申请日：2000-04-19
申请人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K314015
CPC分类号： C07D209/34 , C07D209/96 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D491/10
摘要： This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.
摘要翻译：本发明涉及作为孕酮受体拮抗剂的取代二氢吲哚衍生物，其制备和药物应用，特别是包括具有以下通式结构的良性或恶性肿瘤性疾病的避孕和治疗：其中R1和R2可以是单取代基或与形成螺环。

32. 发明授权

US06841568B2 Thio-oxindole derivatives 失效
标题翻译：硫氧吲哚衍生物
公开(公告)号：US06841568B2
公开(公告)日：2005-01-11
申请号：US10420276
申请日：2003-04-22
申请人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Jay E. Wrobel , Edward G. Melenski , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
发明人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Jay E. Wrobel , Edward G. Melenski , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
IPC分类号： C07D409/10 , A61K31/404 , A61P1/00 , A61P5/34 , A61P5/36 , A61P7/00 , A61P7/04 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/30 , C07D209/40 , C07D209/96 , A61K31/405 , C07D209/04
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激动剂的化合物，其具有以下通式：其中：R 1，R 2，R 3，R 4，R 5和Q 1如本文所定义，或其药学上可接受的盐，以及方法使用这些化合物诱导避孕或治疗孕酮相关的癌和腺癌。

33. 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。

34. 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.

35. 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。

36. 发明授权

US07084168B2 Indoline derivatives 失效
公开(公告)号：US07084168B2
公开(公告)日：2006-08-01
申请号：US10456892
申请日：2003-06-06
申请人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H.W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H.W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31/404 , C07D209/34
CPC分类号： C07D209/34 , C07D209/96 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D491/10
摘要： This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

37. 发明授权

US06946454B2 Thio-oxindole derivatives 失效
标题翻译：硫氧吲哚衍生物
公开(公告)号：US06946454B2
公开(公告)日：2005-09-20
申请号：US10117156
申请日：2002-04-05
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： C07D409/10 , A61K31/404 , A61P1/00 , A61P5/34 , A61P5/36 , A61P7/00 , A61P7/04 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/30 , C07D209/40 , C07D209/96 , A61K31/56 , A61K31/40 , A61K31/44
CPC分类号： C07D209/40 , C07D209/08 , C07D209/30
摘要： This invention relates to methods of co-administering compounds of formula 1 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, with estrogen, an estrogen, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.
摘要翻译：本发明涉及共同施用式1化合物的方法，其为具有以下通式结构的孕酮受体的激动剂：其中：R 1，R 2，R 2， R 3，R 4，R 5和Q 1如本文所定义，或其药学上可接受的盐，与雌激素，雌激素或雌激素受体激动剂用于避孕，激素替代治疗或治疗孕激素相关的癌和腺癌。

38. 发明授权

US06608068B2 Indoline derivatives 失效
公开(公告)号：US06608068B2
公开(公告)日：2003-08-19
申请号：US10014173
申请日：2001-12-11
申请人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31404
CPC分类号： C07D209/34 , C07D209/96 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D491/10
摘要： This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

39. 发明授权

US06319912B1 Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides 失效
标题翻译：使用2,1-苯并异噻唑啉二氧化物的环状方案
公开(公告)号：US06319912B1
公开(公告)日：2001-11-20
申请号：US09552038
申请日：2000-04-19
申请人： Gary S. Grubb , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel
发明人： Gary S. Grubb , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel
IPC分类号： A61K3156
CPC分类号： A61K31/565 , A61K31/425 , A61K31/535 , A61K31/56 , A61K31/57 , A61K45/06 , A61K31/428 , A61K2300/00
摘要： This invention relates to cyclic combination therapies utilizing, in combination with a progestin, an estrogen, or both, progesterone receptor antagonists of the general structure: wherein the substituents are as defined herein, or pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及利用与孕激素，雌激素或两者一起使用的一般结构的孕酮受体拮抗剂的环状组合疗法：其中取代基如本文所定义，或其药学上可接受的盐。

40. 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。

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