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81. 发明授权

US06759408B2 Combination regimens using progesterone receptor modulators 失效
标题翻译：使用孕酮受体调节剂的联合治疗方案
公开(公告)号：US06759408B2
公开(公告)日：2004-07-06
申请号：US10141792
申请日：2002-05-09
申请人： Gary S. Grubb , Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K31535
CPC分类号： A61K31/535 , A61K31/56 , Y10S514/843 , 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; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.
摘要翻译：本发明涉及使用具有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环状组合疗法和方案：其中R 1和R 2可以是单个取代基或稠合的; R 3是H，OH，NH 2，C 1 -C 6烷基，COR C或任选取代的C 1 -C 6烷基，C 3至C 6烯基或炔基; R C是H或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，炔基，C 1至C 6烷氧基，氨基或C 1至C 6氨基烷基; 和R 5为苯环，五或六元杂环; 或其药学上可接受的盐。治疗方法包括避孕，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，腺癌最小化副作用或食物摄取刺激。

82. 发明授权

US06579896B2 Method for treating allergies using substituted pyrazoles 有权
公开(公告)号：US06579896B2
公开(公告)日：2003-06-17
申请号：US09946713
申请日：2001-09-05
申请人： Hui Cai , James P. Edwards , Yin Gu , Lars Karlsson , Steven P. Meduna , Barbara A. Pio , Siquan Sun , Robin L. Thurmond , Jianmei Wei
发明人： Hui Cai , James P. Edwards , Yin Gu , Lars Karlsson , Steven P. Meduna , Barbara A. Pio , Siquan Sun , Robin L. Thurmond , Jianmei Wei
IPC分类号： A61K31415
CPC分类号： A61K31/4745 , A61K31/00 , A61K31/13 , A61K31/275 , A61K31/4155 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55
摘要： A method for the treatment of an allergic condition, including an an atopic allergic conditions, using substituted pyrazoles.

83. 发明授权

US06506766B1 Glucocortiocoid-selective antinflammatory agents 失效
标题翻译：糖皮质激素选择性抗炎药
公开(公告)号：US06506766B1
公开(公告)日：2003-01-14
申请号：US09610638
申请日：2000-07-05
申请人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
发明人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.
摘要翻译：具有式I的化合物可用于部分或完全拮抗，抑制，激动或调节糖皮质激素受体并在哺乳动物中治疗免疫，自身免疫和炎性疾病。还公开了包含式I化合物的药物组合物和在哺乳动物中抑制免疫或自身免疫性疾病的方法。

84. 发明授权

US06448405B1 Steroid receptor modulator compounds and methods 失效
标题翻译：类固醇受体调节剂化合物及方法
公开(公告)号：US06448405B1
公开(公告)日：2002-09-10
申请号：US08947428
申请日：1997-10-08
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： C07D491052
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.
摘要翻译：公开了用于类固醇受体的高亲和力，高选择性调节剂的非甾体化合物。还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物，可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。

85. 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。

86. 发明授权

US06369056B1 Cyclic urea and cyclic amide derivatives 失效
标题翻译：环状脲和环状酰胺衍生物
公开(公告)号：US06369056B1
公开(公告)日：2002-04-09
申请号：US09552356
申请日：2000-04-19
申请人： Puwen Zhang , Arthur A. Santilli , Andrew Fensome , Eugene A. Terefenko , Andrew Q. Viet , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Puwen Zhang , Arthur A. Santilli , Andrew Fensome , Eugene A. Terefenko , Andrew Q. Viet , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K31535
CPC分类号： C07D498/04
摘要： This invention provides compounds of the formula: wherein: A, B and D are N or CH, with the proviso that A, B and D can not all be CH; R1 and R2 are independent substituents selected from H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or groups; or R1 and R2 are fused to form an optionally substituted 3 to 8 membered spirocyclic or heterocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, or optionally substituted alkyl, or alkenyl, or CORC; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is a substituted benzene ring or a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR5; RF is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RG is H, alkyl, or substituted alkyl; R5 is H or alkyl; Q is O, S, NR6, or CR7R8; R6 is CN, SO2CF3, or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic ring; R7 and R8 are H, NO2, CN CO2R9, or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic; R9 is C1 to C3 alkyl; or CR7R8 form a six membered ring of the structure below: W is O or a chemical bond; or a pharmaceutically acceptable salt thereof, as well as their use and pharmaceutical compositions as agonists and antagonists of the progesterone receptor.
摘要翻译：本发明提供下式的化合物：其中：A，B和D为N或CH，条件是A，B和D不能全部为CH; R1和R2是选自H，CORA，NRBCORA或任选取代的烷基，烯基，炔基，环烷基，芳基或基团的独立取代基; 或R 1和R 2稠合形成任选取代的3至8元螺环或杂环; RA为H或任选取代的烷基，芳基，烷氧基或氨基烷基; RB是H，C 1至C 3烷基或取代的C 1至C 3烷基; R3是H，OH，NH2或任选取代的烷基或烯基或CORC; RC为H或任选取代的烷基，芳基，烷氧基或氨基烷基; R4是取代的苯环或具有1,2或3个杂原子的五或六元环，所述杂原子包括O，S，SO，SO 2或NR 5; RF是H或任选取代的烷基，芳基，烷氧基或氨基烷基; RG是H，烷基或取代的烷基; R5是H或烷基; Q是O，S，NR6或CR7R8; R6是CN，SO2CF3或任选取代的烷基，环烷基，芳基或杂环; R 7和R 8是H，NO 2，CN CO 2 R 9或任选取代的烷基，环烷基，芳基或杂环; R9为C1至C3烷基; 或CR7R8形成以下结构的六元环：W为O或化学键; 或其药学上可接受的盐，以及它们的用途和药物组合物作为孕激素受体的激动剂和拮抗剂。

87. 发明授权

US06306851B1 Cyclocarbamate and cyclic amide derivatives 失效
标题翻译：环氨基甲酸酯和环酰胺衍生物
公开(公告)号：US06306851B1
公开(公告)日：2001-10-23
申请号：US09552036
申请日：2000-04-19
申请人： Arthur A. Santilli , Andrew Q. Viet , Puwen Zhang , Andrew Fensome , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Arthur A. Santilli , Andrew Q. Viet , Puwen Zhang , Andrew Fensome , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： C07D49804
CPC分类号： C07D498/04 , A61K31/5365
摘要： This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. The compounds of this invention are useful as agonists and antagonists of the progesterone receptor and in methods of inducing contraception and in the treatment or prevention of benign or malignant neoplastic diseases.
摘要翻译：本发明提供下式的化合物：其中A和B是选自S，CH或N的独立取代基; 条件是当A为S时，B为CH或N; 当B为S时，A为CH或N; A和B不能同时为CH; 并且当A和B均等于N时，一个N可以任选地被C 1至C 6烷基取代; R1和R2是选自H，C1至C6烷基，取代C1至C6烷基，C2至C6烯基，取代C2至C6烯基，C2至C6炔基，取代C2至C6炔基，C3至C8环烷基的独立取代基取代的C 3至C 8环烷基，芳基，取代的芳基，杂环，取代的杂环，CORA或NRBCORA; 或R 1和R 2稠合形成任选取代的3至8元螺环烷基，烯基或杂环，所述杂环含有一至三个选自O，S和N的杂原子; 或其药学上有用的盐。本发明的化合物可用作孕激素受体的激动剂和拮抗剂以及诱导避孕和治疗或预防良性或恶性肿瘤疾病的方法。

88. 发明授权

US6093821A Process for preparing steroid receptor modulator compounds 失效
标题翻译：制备类固醇受体调节剂化合物的方法
公开(公告)号：US6093821A
公开(公告)日：2000-07-25
申请号：US943853
申请日：1997-10-08
申请人： Todd K. Jones , Mark E. Goldman , Charlotte L. F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
发明人： Todd K. Jones , Mark E. Goldman , Charlotte L. F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
IPC分类号： C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D215/12 , C07D215/18 , C07D215/38
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.
摘要翻译：公开了用于类固醇受体的高亲和力，高选择性调节剂的非甾体化合物。还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物，可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。

89. 发明授权

US6001846A Process for the preparation of 1,2-dihydroquinolines 失效
标题翻译： 1,2-二氢喹啉的制备方法
公开(公告)号：US6001846A
公开(公告)日：1999-12-14
申请号：US24986
申请日：1998-02-17
申请人： James P. Edwards , Todd K. Jones , Josef D. Riggenberg , Erick M. Carreira
发明人： James P. Edwards , Todd K. Jones , Josef D. Riggenberg , Erick M. Carreira
IPC分类号： C07D491/04 , A61K31/47 , C07D471/02
CPC分类号： C07D491/04
摘要： A method for preparing 1,2-dihydroquinolines that is more flexible than the Skraup reaction is provided. The method comprises treating an ortho-alkenyl aniline with a ketone in the presence of a Lewis acid. Novel intermediates and products of this method useful as steroid receptor modulators, as well as pharmaceutical compositions and methods of use thereof are also claimed.
摘要翻译：提供了一种制备比Skraup反应更灵活的1,2-二氢喹啉的方法。该方法包括在路易斯酸存在下用酮处理邻 - 烯基苯胺。还要求保护这种新型中间体和用于类固醇受体调节剂的该方法的产物，以及药物组合物及其使用方法。

90. 发明授权

US5696133A Steroid receptor modulator compounds and methods 失效
标题翻译：类固醇受体调节剂化合物及方法
公开(公告)号：US5696133A
公开(公告)日：1997-12-09
申请号：US465556
申请日：1995-06-05
申请人： Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi , Lawrence G. Hamann , Luc J. Farmer , Robert L. Davis
发明人： Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi , Lawrence G. Hamann , Luc J. Farmer , Robert L. Davis
IPC分类号： C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/47
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 requiting 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.
摘要翻译：公开了用于类固醇受体的高亲和力，高选择性调节剂的非甾体化合物。还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物，可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。

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