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1. 发明授权

US4925968A N-acyl-N-naphthoylglycines as aldose reductase inhibitors 失效
标题翻译： N-酰基-N-萘甲酰甘氨酸作为醛糖还原酶抑制剂
公开(公告)号：US4925968A
公开(公告)日：1990-05-15
申请号：US294712
申请日：1989-01-09
申请人： Kazimir Sestanj , Jay E. Wrobel , Joseph M. Kelly
发明人： Kazimir Sestanj , Jay E. Wrobel , Joseph M. Kelly
IPC分类号： C07C235/88 , C07C271/64 , C07C275/54 , C07C327/48 , C07C327/52
CPC分类号： C07C275/54 , C07C235/88 , C07C271/64 , C07C327/48 , C07C327/52
摘要： Disclosed herein are N-acyl-N-naphthoylglycines and methods of their preparation. The N-acyl-N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
摘要翻译：本文公开了N-酰基-N-萘甲酰甘氨酸及其制备方法。 N-酰基-N-萘甲酰甘氨酸是可用于治疗或预防糖尿病并发症的新型醛糖还原酶抑制剂。

2. 发明授权

US4843062A N-acyl-N-napthoylglycines as aldose reductase inhibitors 失效
标题翻译： N-酰基-N-萘甲酰甘氨酸作为醛糖还原酶抑制剂
公开(公告)号：US4843062A
公开(公告)日：1989-06-27
申请号：US137479
申请日：1987-12-23
申请人： Kazimir Sestanj , Jay E. Wrobel , Joseph M. Kelly
发明人： Kazimir Sestanj , Jay E. Wrobel , Joseph M. Kelly
IPC分类号： C07C235/88 , C07C271/64 , C07C275/54 , C07C327/48 , C07C327/52
CPC分类号： C07C327/52 , C07C235/88 , C07C271/64 , C07C275/54 , C07C327/48
摘要： Disclosed herein are N-acyl-N-napthoylglycines and methods of their preparation. The N-acyl-N-napthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
摘要翻译：本文公开了N-酰基-N-萘甲酰甘氨酸及其制备方法。 N-酰基-N-萘甲酰甘氨酸是可用于治疗或预防糖尿病并发症的新型醛糖还原酶抑制剂。

3. 发明授权

US4820727A N-acyl-N-naphthoylglycines as aldose reductase inhibitors 失效
标题翻译： N-酰基-N-萘甲酰甘氨酸作为醛糖还原酶抑制剂
公开(公告)号：US4820727A
公开(公告)日：1989-04-11
申请号：US137406
申请日：1987-12-23
申请人： Jay E. Wrobel , Kazimir Sestanj
发明人： Jay E. Wrobel , Kazimir Sestanj
IPC分类号： A61K31/215 , A61K31/195 , A61P3/08 , A61P3/10 , A61P13/02 , A61P15/00 , A61P25/00 , A61P27/02 , A61P43/00 , C07C41/18 , C07C43/225 , C07C65/24 , C07C233/65 , C07C233/77 , C07C233/81 , C07C235/66 , C07C271/22 , C07C271/64 , C07C125/065 , A61K31/27
CPC分类号： C07C235/66 , C07C271/64 , C07C43/225
摘要： Disclosed herein are N-acyl-N-naphthoylglycines and methods of their preparation. The N-acyl-N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.

4. 发明授权

US4962224A N-naphthoylglycines as aldose reductase inhibitors 失效
标题翻译： N-萘甲酰甘氨酸作为醛糖还原酶抑制剂
公开(公告)号：US4962224A
公开(公告)日：1990-10-09
申请号：US397623
申请日：1989-08-22
申请人： Jay E. Wrobel , Kazimir Sestanj
发明人： Jay E. Wrobel , Kazimir Sestanj
IPC分类号： C07C43/225 , C07C43/23 , C07C65/24 , C07C235/66 , C07C237/22 , C07C271/64 , C07C327/48
CPC分类号： C07C43/23 , C07C235/66 , C07C237/22 , C07C271/64 , C07C327/48 , C07C43/225 , C07C65/24
摘要： Disclosed herein are N-naphthoylglycines and methods of their preparation. The N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
摘要翻译：本文公开了N-萘甲酰甘氨酸及其制备方法。 N-萘甲酰甘氨酸是可用于治疗或预防糖尿病并发症的新型醛糖还原酶抑制剂。

5. 发明授权

US4906766A N-(6-methoxy-5-(trifluoromethyl)-1-naphthalenyl)-substituted imino)methyl)-N-methylglycines 失效
标题翻译： N-（6-甲氧基-5-（三氟甲基）-1-萘基） - 取代的亚氨基）甲基）-N-甲基甘氨酸
公开(公告)号：US4906766A
公开(公告)日：1990-03-06
申请号：US325609
申请日：1989-03-20
申请人： Jay E. Wrobel , Kazimir Sestanj
发明人： Jay E. Wrobel , Kazimir Sestanj
IPC分类号： C07C261/04 , C07C311/55
CPC分类号： C07C261/04 , C07C311/55
摘要： Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl][substituted imino]methyl]-N-methylglycines and methods for their preparation. The N-methylglycines are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
摘要翻译：本文公开了N - [[6-甲氧基-5-（三氟甲基）-1-萘基] [取代的亚氨基]甲基] -N-甲基甘氨酸及其制备方法。 N-甲基甘氨酸是用于治疗或预防糖尿病并发症的新的醛糖还原酶抑制剂。

6. 发明授权

US4853412A N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-[substituted imino]methyl]-n-methylglycines 失效
标题翻译： N - [[6-甲氧基-5-（三氟甲基）-1-萘基] - [取代的亚氨基]甲基] -N-甲基甘氨酸
公开(公告)号：US4853412A
公开(公告)日：1989-08-01
申请号：US137381
申请日：1987-12-23
申请人： Jay E. Wrobel , Kazimir Sestanj
发明人： Jay E. Wrobel , Kazimir Sestanj
IPC分类号： C07C261/04 , C07C311/55
CPC分类号： C07C261/04 , C07C311/55
摘要： Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl][substituted imino]methyl]-N-methylglycines and methods for their preparation. The N-methylglycines are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
摘要翻译：本文公开了N - [[6-甲氧基-5-（三氟甲基）-1-萘基] [取代的亚氨基]甲基] -N-甲基甘氨酸及其制备方法。 N-甲基甘氨酸是用于治疗或预防糖尿病并发症的新型醛糖还原酶抑制剂。

7. 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。

8. 发明授权

US07488822B2 Cyclocarbamate derivatives as progesterone receptor modulators 失效
标题翻译：环丙氨酸衍生物作为孕酮受体调节剂
公开(公告)号：US07488822B2
公开(公告)日：2009-02-10
申请号：US10767813
申请日：2004-01-29
申请人： Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： C07D265/12
CPC分类号： C07D265/18 , C07D413/04 , C07D413/10 , C07D417/04
摘要： This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.
摘要翻译：本发明提供式（I）的化合物：其中R 1和R 2是独立的取代基或稠合形成螺环; R3，RC和R4如本文所定义; 并且R5是取代的苯环或其主链1,2或3个杂原子包括O，S，SO，SO 2或NR 6的取代的五元或六元杂环; 或其药学上可接受的盐，以及使用该化合物作为孕酮受体的拮抗剂的药物组合物和方法。

9. 发明授权

US06794373B2 Contraceptive methods using benzimidazolones 失效
标题翻译：使用苯并咪唑酮的避孕方法
公开(公告)号：US06794373B2
公开(公告)日：2004-09-21
申请号：US10091222
申请日：2002-03-01
申请人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K3156
CPC分类号： A61K45/06 , A61K31/415 , A61K31/535 , A61K31/54 , A61K31/56 , A61K31/57 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing indoline compounds which are antagonists of the progesterone receptor and having the general structure: A is O, S, or NR4; B is a bond or CR5R6; R4, to R6 are H, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, aryl, or heterocyclic, or R4 and R5 are fused to form a ring; R1 is H, OH, NH2, C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, or CORA; RA is as defined; R2 is H, halogen, CN, NO2, C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl; R3 is a substituted benzene ring, or heteroaromatic ring, in combination with a progestational agent and/or an estrogen to treat or prevent secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas, and contraception, among others.
摘要翻译：本发明涉及使用作为孕酮受体的拮抗剂并具有以下一般结构的二氢吲哚化合物的环组合疗法和方案：A是O，S或NR 4; B是键或CR 5 R 6; R 4至R 6是H，C 1至C 6烷基，C 2至C 6烯基，C 2至C 6炔基，C 3至C 8环烷基，芳基或杂环或R 4和R 5稠合形成环; R 1是H，OH，NH 2，C 1至C 6烷基，C 3至C 6烯基，炔基或COR 3; R 如定义; R 2是H，卤素，CN，NO 2，C 1至C 6烷基，C 1至C 6烷氧基或C 1至C 6氨基烷基; R 3是与促孕剂和/或雌激素组合的取代苯环或杂芳环，用于治疗或预防继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症，多囊卵巢综合征，癌和腺癌，以及避孕等等。

10. 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

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