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31. 发明授权

US06608068B2 Indoline derivatives 失效
公开(公告)号：US06608068B2
公开(公告)日：2003-08-19
申请号：US10014173
申请日：2001-12-11
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： A61K31404
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.

32. 发明授权

US06566358B2 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：US06566358B2
公开(公告)日：2003-05-20
申请号：US09948309
申请日：2001-09-06
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： A61K31536
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 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alky, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; 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）化合物：其中R 1和R 2可以是单个取代基或稠合形成螺环或杂 - 六环环; R 3是H，OH，NH 2，C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3至C 6烯基，取代的C 1至C 6烯基，炔基或取代的炔基，CORC; RC为H，C1至C3烷基，取代C1至C3烷基，芳基，取代芳基，C1至C3烷氧基，取代C1至C3烷氧基，C1至C3氨基烷基或取代C1至C3氨基烷基; R4为H，卤素，CN 取代的C 1至C 6烷氧基，取代的C 1至C 6烷氧基，氨基，C 1至C 6氨基烷基或取代的C 1至C 6氨基烷基; 并且R 5选自具有1,2或3个杂原子的五元或六元环的三取代苯环，所述杂原子包括O，S，SO，SO 2或NR 6，并且包含一个或两个独立的取代基，包括H，卤素，CN，NO 2，氨基和C 1至C 3烷基，C 1至C 3烷氧基，C 1至C 3氨基烷基，CORF或NRGCORF; 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。

33. 发明授权

US06544970B2 Cyclic regimens utilizing indoline derivatives 失效
标题翻译：利用二氢吲哚衍生物的循环方案
公开(公告)号：US06544970B2
公开(公告)日：2003-04-08
申请号：US10153393
申请日：2002-05-22
申请人： Gary S. Grubb , Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , 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 , A61K31/535 , A61K31/56 , A61K31/57 , A61K31/565 , A61K31/40 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception, for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, or prostate, minimization of side effects, cyclic menstrual bleeding, or stimulation of food intake.
摘要翻译：本发明涉及使用具有以下通式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循环联合疗法和方案：其中R1和R2可以是单取代基或稠合形成螺环，与孕激素，雌激素或两者兼有。这些治疗方法可用于避孕，治疗和/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，子宫内膜，卵巢，乳腺，结肠或前列腺的癌和腺癌，最小化副作用，周期性月经出血或刺激食物摄入。

34. 发明授权

US06462032B1 Cyclic regimens utilizing indoline derivatives 失效
标题翻译：利用二氢吲哚衍生物的循环方案
公开(公告)号：US06462032B1
公开(公告)日：2002-10-08
申请号：US09552358
申请日：2000-04-19
申请人： Gary S. Grubb , Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H. W. Bender , Puwen Zhang , 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 , A61K31/535 , A61K31/56 , A61K31/57 , A61K31/565 , A61K31/40 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
摘要翻译：本发明涉及使用具有以下通式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循环联合疗法和方案：其中R1和R2可以是单取代基或稠合形成螺环，与孕激素，雌激素或两者兼有。这些治疗方法可用于避孕或治疗和/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，子宫内膜，卵巢，乳腺，结肠，前列腺的癌和腺癌，或副作用最小化或周期性月经出血。本发明的额外用途包括刺激食物摄取。

35. 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。

36. 发明授权

US06380235B1 Benzimidazolones and analogues 失效
标题翻译：苯并咪唑酮和类似物
公开(公告)号：US06380235B1
公开(公告)日：2002-04-30
申请号：US09552546
申请日：2000-04-19
申请人： Puwen Zhang , Reinhold H. W. Bender , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Puwen Zhang , Reinhold H. W. Bender , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31415
CPC分类号： C07D263/58 , C07C215/76 , C07C229/18 , C07D235/26 , C07D235/28 , C07D241/44 , C07D277/68 , C07D279/16 , C07D409/04 , C07D487/04
摘要： The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.
摘要翻译：本发明提供可用作孕酮受体激动剂和拮抗剂并具有以下通式的化合物和药物制剂：其中：A为O，S或NR4; B为A和C = Q之间的键，或部分CR5R6; R4， R5，R5独立地选自H或任选取代的C1至C6烷基，C2至C6烯基，C2至C6炔基，C3至C8环烷基，取代C3至C8环烷基，芳基或杂环基，或通过将R4 和R5至5至7元环; R1选自H，OH，NH2，C1至C6烷基，取代C1至C6烷基，C3至C6烯基，取代C1至C6烯基，炔基，取代的炔基，-COH或任选取代的-CO（C 1至C 3烷基），-CO（芳基），-CO（C 1〜C 3烷氧基）或-CO（C 1〜C 3氨基烷基） R 2选自H，卤素，CN，NO 2或任选取代的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; R3选自三取代苯环; 或含有1或2个取代基的5或6元杂芳环; Q是O，S，NR8或CR9R10; 或其药学上可接受的盐。本发明还包括避孕方法和治疗或预防与孕酮受体相关的疾病的方法。

37. 发明授权

US06423699B1 Combination therapies using benzimidazolones 失效
标题翻译：联合治疗使用苯并咪唑酮
公开(公告)号：US06423699B1
公开(公告)日：2002-07-23
申请号：US09552355
申请日：2000-04-19
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 substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R6 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alkynyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromnatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate. These combinations may also be used to in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.
摘要翻译：本发明涉及使用具有以下通式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循环组合疗法和方案：其中：A是O，S或NR4; B是A和C = Q之间的键，或 CR5R6部分; R4，R5，R6独立地选自H或任选取代的C1至C6烷基，C2至C6烯基，C2至C6炔基，C3至C8环烷基，取代C3至C8环烷基，芳基或杂环基，或由将R4和R5与5至7元环融合; R1选自H，OH，NH2，C1至C6烷基，取代C1至C6烷基，C3至C6烯基，取代C1至C6烯基，炔基，取代炔基，-COH或任选取代的-CO（C 1至C 3烷基），-CO（芳基），-CO（C 1〜C 3烷氧基）或-CO（C 1〜C 3氨基烷基） R2选自H，卤素，CN，NO2或任选取代的C1至C6烷基C1至C6烷氧基或C1至C6氨基烷基; R3选自三取代苯环; 或含有1或2个取代基的5-或6-元杂芳族环; 或其药学上可接受的盐与促孕剂，雌激素或两者组合，或用于治疗和/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，子宫内膜，卵巢，乳腺，结肠，前列腺癌和腺癌。这些组合也可用于避孕方法，刺激食物摄取或最小化副作用或周期性月经出血。

38. 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。

39. 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。

40. 发明授权

US06503939B2 Combination regimens using 3,3-substituted indoline derivatives 失效
标题翻译：使用3,3-取代的二氢吲哚衍生物的组合方案
公开(公告)号：US06503939B2
公开(公告)日：2003-01-07
申请号：US09977790
申请日：2001-10-15
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： A61K31405
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 structure: wherein: R1 and R2 are (i) H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and optionally substituted alkyl, O(alkyl), aryl, or heteroaryl; (ii) a ring or (iii) a double bond; R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is a benzene ring; heterocyclic ring; an indole or benzothiophene; or pharmaceutically acceptable salt. R6 and R7 are H, methyl, ethyl, propyl, butyl, iso-propyl, isobutyl, cyclohexyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl. These methods may be used for contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas, cyclic menstrual bleeding, or food intake.
摘要翻译：本发明涉及使用具有以下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是（i）H，OH，OAc，烷基芳基，烷基杂芳基，1-丙炔基，丙炔基和任选取代的烷基，O（烷基），芳基或杂芳基; （ii）环或（iii）双键; 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; R4 = H，卤素，CN，NH2或任选取代的烷基，烷氧基或氨基烷基; R5是苯环; 杂环吲哚或苯并噻吩; 或药学上可接受的盐。 R 6和R 7是H，甲基，乙基，丙基，丁基，异丙基，异丁基，环己基，芳基，取代的芳基，杂芳基或取代的杂芳基。这些方法可用于避孕，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，腺癌，周期性月经出血或食物摄入。

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