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31. 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.

32. 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。

33. 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。

34. 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.

35. 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。

36. 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.

37. 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。

38. 发明授权

US06835744B2 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：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。

39. 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。

40. 发明申请

US20070259944A1 Indoline derivatives 失效
公开(公告)号：US20070259944A1
公开(公告)日：2007-11-08
申请号：US11821384
申请日：2007-06-22
申请人： Andrew Fensome , Lori Miller , John Ullrich , Reinhold Bender , Puwen Zhang , Jay Wrobel , Lin Zhi , Todd Jones , James Edwards , Christopher Tegley
发明人： Andrew Fensome , Lori Miller , John Ullrich , Reinhold Bender , Puwen Zhang , Jay Wrobel , Lin Zhi , Todd Jones , James Edwards , Christopher Tegley
IPC分类号： A61K31/404 , C07D209/04
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.

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