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1. 发明授权

US07576215B2 Quinolines and pharmaceutical compositions thereof 失效
标题翻译：喹啉及其药物组合物
公开(公告)号：US07576215B2
公开(公告)日：2009-08-18
申请号：US11010236
申请日：2004-12-10
申请人： Michael D. Collini , Robert R. Singhaus, Jr. , Baihua Hu , James W. Jetter , Robert L. Morris , David H. Kaufman , Christopher P. Miller , John W. Ullrich , Rayomand J. Unwalla , Jay E. Wrobel , Elaine Quinet , Ponnal Nambi , Ronald C. Bernotas , Merle Elloso
发明人： Michael D. Collini , Robert R. Singhaus, Jr. , Baihua Hu , James W. Jetter , Robert L. Morris , David H. Kaufman , Christopher P. Miller , John W. Ullrich , Rayomand J. Unwalla , Jay E. Wrobel , Elaine Quinet , Ponnal Nambi , Ronald C. Bernotas , Merle Elloso
IPC分类号： C07D215/38
CPC分类号： C07D401/04 , C07D215/14 , C07D215/54 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/06 , C07D417/12
摘要： This invention provides compounds of formula I that are useful in the treatment or inhibition of LXR mediated diseases.
摘要翻译：本发明提供可用于治疗或抑制LXR介导的疾病的式I化合物。

2. 发明授权

US07022733B2 Substituted 2-phenyl benzofurans as estrogenic agents 失效
公开(公告)号：US07022733B2
公开(公告)日：2006-04-04
申请号：US10828970
申请日：2004-04-21
申请人： Christopher P. Miller , Michael D. Collini , David H. Kaufman , Robert L. Morris , Robert R. Singhaus, Jr. , John W. Ullrich , Heather A. Harris , James C. Keith, Jr. , Leo M. Albert , Rayomand J. Unwalla
发明人： Christopher P. Miller , Michael D. Collini , David H. Kaufman , Robert L. Morris , Robert R. Singhaus, Jr. , John W. Ullrich , Heather A. Harris , James C. Keith, Jr. , Leo M. Albert , Rayomand J. Unwalla
IPC分类号： A61K31/343
CPC分类号： C07D307/80 , C07D405/06 , C07D413/04
摘要： This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.

3. 发明授权

US06774248B2 Substituted 2-phenyl benzofurans as estrogenic agents 失效
标题翻译：取代的2-苯基苯并呋喃酮作为雌激素剂
公开(公告)号：US06774248B2
公开(公告)日：2004-08-10
申请号：US10320207
申请日：2002-12-16
申请人： Christopher P. Miller , Michael D. Collini , David H. Kaufman , Robert L. Morris , Robert R. Singhaus, Jr. , John W. Ullrich , Heather A. Harris , James C. Keith, Jr. , Leo M. Albert , Rayomand J. Unwalla
发明人： Christopher P. Miller , Michael D. Collini , David H. Kaufman , Robert L. Morris , Robert R. Singhaus, Jr. , John W. Ullrich , Heather A. Harris , James C. Keith, Jr. , Leo M. Albert , Rayomand J. Unwalla
IPC分类号： A61K3134
CPC分类号： C07D307/80 , C07D405/06 , C07D413/04
摘要： This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式I的雌激素受体调节剂，其具有其中R，R'，A，A'，X，Y和Y如说明书中所定义的结构，或其药学上可接受的盐。

4. 发明授权

US07592363B2 Indazoles 失效
公开(公告)号：US07592363B2
公开(公告)日：2009-09-22
申请号：US11194263
申请日：2005-08-01
申请人： Robert J. Steffan , Edward M. Matelan , Stephen M. Bowen , John W. Ullrich , Jay E. Wrobel , Edouard Zamaratski , Lars Kruger , Annabel L. Olsen Hedemyr , Aiping Cheng , Tomas Hansson , Rayomand J. Unwalla , Christopher P. Miller , Patrik P. Rhönnstad
发明人： Robert J. Steffan , Edward M. Matelan , Stephen M. Bowen , John W. Ullrich , Jay E. Wrobel , Edouard Zamaratski , Lars Kruger , Annabel L. Olsen Hedemyr , Aiping Cheng , Tomas Hansson , Rayomand J. Unwalla , Christopher P. Miller , Patrik P. Rhönnstad
IPC分类号： A61K31/4162 , C07D231/56
CPC分类号： C07D403/04 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/04 , C07D409/04 , C07D491/10
摘要： This invention provides compounds of Formula (I) or (Ia): that are useful in the treatment or inhibition of LXR mediated diseases.
摘要翻译：本发明提供式（I）或（Ia）化合物：其可用于治疗或抑制LXR介导的疾病。

5. 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。

6. 发明授权

US07645761B2 Indoline derivatives 失效
标题翻译：二氢吲哚衍生物
公开(公告)号：US07645761B2
公开(公告)日：2010-01-12
申请号：US11821384
申请日：2007-06-22
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 , A61K31/4439 , C07D401/02 , 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，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。

7. 发明授权

US07253203B2 Indoline derivatives 失效
标题翻译：二氢吲哚衍生物
公开(公告)号：US07253203B2
公开(公告)日：2007-08-07
申请号：US11378851
申请日：2006-03-17
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： C07D401/02 , C07D403/02 , A61K31/404 , A61K31/4439
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。

8. 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。

9. 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.

10. 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。

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