公开(公告)号：US06329416B1

公开(公告)日：2001-12-11

申请号：US09552631

申请日：2000-04-19

申请人： Gary S. Grubb ,  John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

发明人： Gary S. Grubb ,  John W. Ullrich ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

IPC分类号： A01N4338

CPC分类号： A61K45/06 ,  A61K31/57 ,  A61K31/565 ,  A61K31/40 ,  A61K2300/00

摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the general structure: 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. These methods of treatment may be used for contraception.

摘要翻译： 本发明涉及使用具有一般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与FORM连接，所述环包含-CH 2（CH 2）n CH 2 - ，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）; R3是H，OH，NH2，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，卤素，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。 这些治疗方法可用于避孕。

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

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。

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。

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。

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。

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。

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。

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

公开(公告)号：US5696127A

公开(公告)日：1997-12-09

申请号：US465429

申请日：1995-06-05

申请人： Todd K. Jones ,  Lin Zhi ,  James P. Edwards ,  Christopher M. Tegley ,  Sarah J. West

发明人： Todd K. Jones ,  Lin Zhi ,  James P. Edwards ,  Christopher M. Tegley ,  Sarah J. West

IPC分类号： C07D215/06 ,  C07D221/18 ,  C07D311/80 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052 ,  A61K31/44 ,  A61K31/47 ,  C07D491/52

CPC分类号： C07D401/04 ,  C07D215/06 ,  C07D221/18 ,  C07D311/80 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04

摘要： Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.