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1. 发明授权

US06566372B1 Bicyclic androgen and progesterone receptor modulator compounds and methods 有权
标题翻译：双环雄激素和孕激素受体调节剂的化合物和方法
公开(公告)号：US06566372B1
公开(公告)日：2003-05-20
申请号：US09649466
申请日：2000-08-24
申请人： Lin Zhi , Christopher Tegley , Barbara Pio , Cornelis Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Sarah West
发明人： Lin Zhi , Christopher Tegley , Barbara Pio , Cornelis Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Sarah West
IPC分类号： A61K3147
CPC分类号： C07D215/227 , C07D209/34 , C07D209/96 , C07D215/36 , C07D215/38 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要翻译：本发明涉及用于调节由AR和PR介导的过程的化合物，药物组合物和方法。更具体地，本发明涉及非甾类化合物和组合物，其是高亲和力，高特异性激动剂，部分激动剂（即部分激活剂和/或组织特异性激活剂）和AR和PR的拮抗剂。还提供制备这些化合物和药物组合物的方法，以及用于其合成的关键中间体。

2. 发明申请

US20110112084A9 Bicyclic androgen and progesterone receptor modulator compounds and methods 审中-公开
标题翻译：双环雄激素和孕激素受体调节剂的化合物和方法
公开(公告)号：US20110112084A9
公开(公告)日：2011-05-12
申请号：US12590805
申请日：2009-11-13
申请人： Lin Zhi , Christopher Tegley , Barbara Pio , Corneils Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Robert Higuchi , Lawrence G. Hamann
发明人： Lin Zhi , Christopher Tegley , Barbara Pio , Corneils Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Robert Higuchi , Lawrence G. Hamann
IPC分类号： A61K31/47 , C07D311/04 , C07D265/14 , C07D215/00 , A61K31/536 , A61K31/352 , A61P35/00 , A61P15/00
CPC分类号： C07D215/227 , C07D209/34 , C07D209/96 , C07D215/36 , C07D215/38 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要翻译：本发明涉及用于调节由AR和PR介导的过程的化合物，药物组合物和方法。更具体地，本发明涉及非甾类化合物和组合物，其是高亲和力，高特异性激动剂，部分激动剂（即部分激活剂和/或组织特异性激活剂）和AR和PR的拮抗剂。还提供制备这些化合物和药物组合物的方法，以及用于其合成的关键中间体。

3. 发明申请

US20100069379A1 Bicyclic androgen and progesterone receptor modulator compounds and methods 审中-公开
公开(公告)号：US20100069379A1
公开(公告)日：2010-03-18
申请号：US12590805
申请日：2009-11-13
申请人： Lin Zhi , Christopher Tegley , Barbara Pio , Corneils Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Robert Higuchi , Lawrence G. Hamann
发明人： Lin Zhi , Christopher Tegley , Barbara Pio , Corneils Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Robert Higuchi , Lawrence G. Hamann
IPC分类号： A61K31/47 , C07D311/04 , C07D265/14 , C07D215/00 , A61K31/536 , A61K31/352 , A61P35/00 , A61P15/00
CPC分类号： C07D215/227 , C07D209/34 , C07D209/96 , C07D215/36 , C07D215/38 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.

4. 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.

5. 发明申请

US20060160882A1 Indoline derivatives 失效
标题翻译：二氢吲哚衍生物
公开(公告)号：US20060160882A1
公开(公告)日：2006-07-20
申请号：US11378851
申请日：2006-03-17
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 , C07D409/02 , C07D405/02 , C07D403/02
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化合物，其制备方法和药物应用，特别是包括具有以下一般结构的良性或恶性肿瘤疾病的避孕和治疗：其中R 1和 R 2可以是单个取代基或稠合形成螺环。

6. 发明申请

US20050054711A1 Thio-oxindole derivatives 有权
标题翻译：硫氧吲哚衍生物
公开(公告)号：US20050054711A1
公开(公告)日：2005-03-10
申请号：US10969531
申请日：2004-10-20
申请人： Andrew Fensome , Puwen Zhang , Marci Koko , Lin Zhi , Todd Jones , Jay Wrobel , Christopher Tegley , James Edwards , Edward Melenski
发明人： Andrew Fensome , Puwen Zhang , Marci Koko , Lin Zhi , Todd Jones , Jay Wrobel , Christopher Tegley , James Edwards , Edward 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 , C07D209/36 , C07D43/02
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。

7. 发明申请

US20050256110A1 Cyanopyrroles 有权
标题翻译：青色
公开(公告)号：US20050256110A1
公开(公告)日：2005-11-17
申请号：US11184313
申请日：2005-07-19
申请人： Mark Collins , Valerie Mackner , Jay Wrobel , Lin Zhi , Todd Jones , James Edwards , Christopher Tegley
发明人： Mark Collins , Valerie Mackner , Jay Wrobel , Lin Zhi , Todd Jones , James Edwards , Christopher Tegley
IPC分类号： C07D403/04 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/536 , A61K31/5415 , A61P5/34 , A61P13/08 , A61P15/00 , A61P15/14 , A61P15/16 , A61P15/18 , A61P35/00 , A61P43/00 , C07D413/04
CPC分类号： C07D403/04 , A61K31/405 , A61K31/5415 , C07D413/04
摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有以下结构的式1的孕酮受体拮抗剂，其中T为O，S或不存在; R 1，R 2和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，并且一起含有-CH 2（CH 2）2 CH 2 CH 2 - ， - CH 2 CH 2 CH 2 CH 2 N 2 CH 2 2 CH 2 - ， - O（CH 2）2 CH 2 - ， - （CH 2 CH 2） O（CH 2 CH 2）q O - ， - CH 2 CH 2 OCH 2 - / SUB CH 2，或CH 2 CH 2，NR 7，CH 2，CH 2， CH 2 - ; n = 1-5; p = 1-4; q = 1-4; R 3是氢，OH，NH 2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或COR A。 R A是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 4是氢，卤素，CN，NH 2，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 5是氢，烷基或取代的烷基; R 6是氢，烷基，取代的烷基或COR B; R B是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 7是氢或烷基; 或其药学上可接受的盐。

8. 发明申请

US20060142280A1 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：US20060142280A1
公开(公告)日：2006-06-29
申请号：US11351002
申请日：2006-02-09
申请人： Puwen Zhang , Andrew Fensome , Eugene Terefenko , Lin Zhi , Todd Jones , James Edwards , Christopher Tegley , Jay Wrobel , Mark Collins
发明人： Puwen Zhang , Andrew Fensome , Eugene Terefenko , Lin Zhi , Todd Jones , James Edwards , Christopher Tegley , Jay Wrobel , Mark Collins
IPC分类号： A61K31/538
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, R2, R3, R4, R5, and Q1 are defined herein.
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，R 2，R 3，R 4，R SUP > 5 和Q 1是本文定义的。

9. 发明申请

US20050171186A1 Thio-oxindole derivatives 审中-公开
标题翻译：硫氧吲哚衍生物
公开(公告)号：US20050171186A1
公开(公告)日：2005-08-04
申请号：US11083011
申请日：2005-03-17
申请人： Andrew Fensome , Puwen Zhang , Marci Koko , Lin Zhi , Todd Jones , Jay Wrobel , Christopher Tegley , James Edwards , Edward Melenski
发明人： Andrew Fensome , Puwen Zhang , Marci Koko , Lin Zhi , Todd Jones , Jay Wrobel , Christopher Tegley , James Edwards , Edward 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
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 estrone, 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。

10. 发明申请

US20120010256A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 失效
标题翻译： 11-羟基甾体脱氢酶1型抑制剂
公开(公告)号：US20120010256A1
公开(公告)日：2012-01-12
申请号：US13233699
申请日：2011-09-15
申请人： Martin HENRIKSSON , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric A. Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J. St. Jean, JR. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
发明人： Martin HENRIKSSON , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric A. Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J. St. Jean, JR. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
IPC分类号： A61K31/426 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/12 , A61P17/06 , A61P25/28 , A61P25/24 , A61P31/12 , A61P29/00 , A61P17/02 , C07D277/54 , A61P19/10
CPC分类号： C07D277/54 , C07D263/34 , C07D275/03 , C07D277/60 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和Z如本文所定义，涉及包含该化合物的药物组合物，以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶相关的病症的用途和用于制备作用于人类11- 羟类固醇脱氢酶1型酶。

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