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1. 发明授权

US06407101B1 Cyanopyrroles 有权
标题翻译：青色
公开(公告)号：US06407101B1
公开(公告)日：2002-06-18
申请号：US09552544
申请日：2000-04-19
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： C07D41310
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 alky, 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, allyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alko, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof
摘要翻译：本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体拮抗剂; R 1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）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 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CORA; RA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 R5是氢，烯丙基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; R是氢，烷基，取代的烷基，或烷氧基，取代的烷氧基， RB是氢，烷基，取代的烷基，烷基，取代的烷氧基，氨基烷基或取代的氨基烷基; R7是氢或烷基; 或其药学上可接受的盐

2. 发明授权

US08476262B2 Cyanopyrroles 失效
标题翻译：青色
公开(公告)号：US08476262B2
公开(公告)日：2013-07-02
申请号：US12915211
申请日：2010-10-29
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
IPC分类号： A61K31/535
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）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R3是氢，OH，NH2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA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; R4是氢，卤素，CN，NH2，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; R5是氢，烷基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; RB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; R7是氢或烷基; 或其药学上可接受的盐。

3. 发明申请

US20110039839A1 Cyanopyrroles 失效
标题翻译：青色
公开(公告)号：US20110039839A1
公开(公告)日：2011-02-17
申请号：US12915211
申请日：2010-10-29
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31/536 , A61K31/404 , A61P15/18 , A61P35/00
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）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R3是氢，OH，NH2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA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; R4是氢，卤素，CN，NH2，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; R5是氢，烷基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; RB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; R7是氢或烷基; 或其药学上可接受的盐。

4. 发明授权

US06339098B1 2,1-benzisothiazoline 2,2-dioxides 失效
标题翻译： 2,1-苯并异噻唑啉2,2-二氧化物
公开(公告)号：US06339098B1
公开(公告)日：2002-01-15
申请号：US09552630
申请日：2000-04-19
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K31428
CPC分类号： C07D275/06 , C07D413/04
摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, heteroarylalkyl, and alkynyl. R1 and R2 may be taken together to form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)PCH2—, O(CH2)qO—, —CH2CH2OCH2CH2—, —CH2CH2NR7CH2CH2—. R1 and R2 may be taken together to form a double bond, the double bond having two methyl groups bonded to the terminal end, having a cycloalkyl group bonded to the terminal end, having an oxygen bonded to the terminal end, or having a cycloether bonded to the terminal end; or a double bond. R3 is hydrogen, hydroxyl, NH2, alkyl, substituted alkyl, alkenyl, alkynyl, substituted or, CORA. R4 is hydrogen, halogen, —CN, —NH2, alkyl, substituted alkyl, alkoxy, alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is a trisubstituted phenyl ring having the structure, or is a five or six membered heteroaryl ring, containing 1, 2, or 3 heteroatoms selected from the group consisting of O, S, SO, SO2 and NR6, or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有其中R1的结构的式1的孕酮受体拮抗剂，R 2各自独立地为氢，烷基，取代的烷基，羟基，烷氧基，取代的烷氧基，芳基，取代的芳基，杂芳基，取代的杂芳基，芳基烷基，杂芳基烷基，和炔基。 R 1和R 2可以一起形成环，并且一起含有-CH 2（CH 2）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）PCH 2 - ，O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - ， - CH 2 CH 2 NR 7 CH 2 CH 2 - 。 R1和R2可以一起形成双键，该双键具有与末端键合的两个甲基，具有与末端键合的环烷基，具有与末端结合的氧，或具有环醚键合到终端; 或双键。 R3是氢，羟基，NH2，烷基，取代的烷基，烯基，炔基，取代的或CORA。 R4是氢，卤素，-CN，-NH2，烷基，取代的烷基，烷氧基，烷氧基，氨基烷基或取代的氨基烷基; R5是具有结构的三取代的苯环，或是含有1,2或3个选自O，S，SO，SO 2和NR 6的杂原子的五或六元杂芳基环，或其药学上可接受的盐。

5. 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。

6. 发明授权

US07846924B2 Cyanopyrroles 有权
标题翻译：青色
公开(公告)号：US07846924B2
公开(公告)日：2010-12-07
申请号：US11184313
申请日：2005-07-19
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
IPC分类号： A61K31/54
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）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R3是氢，OH，NH2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA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; R4是氢，卤素，CN，NH2，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; R5是氢，烷基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; RB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; R7为氢或烷基; 或其药学上可接受的盐。

7. 发明授权

US06982261B2 Cyanopyrroles 失效
标题翻译：青色
公开(公告)号：US06982261B2
公开(公告)日：2006-01-03
申请号：US10342719
申请日：2003-01-15
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31/54 , A01K31/535 , C07D279/16 , C07D498/00
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：本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体拮抗剂; 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. 发明授权

US06562857B2 Cyanopyrroles 有权
标题翻译：青色
公开(公告)号：US06562857B2
公开(公告)日：2003-05-13
申请号：US10043513
申请日：2002-01-09
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： C07D40310
CPC分类号： C07D403/04 , A61K31/405 , A61K31/5415 , C07D413/04
摘要： This invention provides a progesterone receptor agonist 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：本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体激动剂; R 1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）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 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CORA; RA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或取代的氨基烷基; R 5为氢，烷基或取代的烷基; R 6为氢，烷基，取代的烷基或CORB， RB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; R7是氢或烷基; 或其药学上可接受的盐

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