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1. 发明申请

US20090075995A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
标题翻译： GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途
公开(公告)号：US20090075995A1
公开(公告)日：2009-03-19
申请号：US11835438
申请日：2007-08-08
申请人： David S. Weinstein , Ping Chen , T.G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
发明人： David S. Weinstein , Ping Chen , T.G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
IPC分类号： A61K31/5377 , A61K31/436 , C07D491/052 , A61P31/12 , A61K31/427 , C07D417/12
CPC分类号： C07D417/12 , C07D277/46 , C07D405/12 , C07D417/14 , C07D491/04
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including inflammatory and immune diseases, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与式（I）结构的糖皮质激素受体，AP-1和/或NF-κB活性（包括炎症和免疫疾病）调节相关的疾病：对映异构体，非对映异构体或其互变异构体，或其前药酯或其药学上可接受的盐，其中：Z是杂环或杂芳基; A是5至8元碳环或5至8元杂环; B是环烷基，环烯基，芳基，杂环基或杂芳基环，其中每个环与相邻原子上的A环稠合并任选地被一至四个相同或不同的基团取代，并且独立地选自R5，R6， R7和R8; J1，J2和J3各自出现相同或不同，独立地为-A1QA2-; Q是键，O，S，S（O）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C2-4亚烯基和取代的C2-4亚烯基，条件是选择A1和A2使得环A为 5-至8-元碳环或杂环; R1至R11如本文所定义。还提供了使用所述化合物治疗炎性或免疫相关疾病和肥胖症和糖尿病的药物组合物和方法。

2. 发明授权

US08034940B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途
公开(公告)号：US08034940B2
公开(公告)日：2011-10-11
申请号：US11835438
申请日：2007-08-08
申请人： David S. Weinstein , Ping Chen , T. G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
发明人： David S. Weinstein , Ping Chen , T. G. Murali Dhar , Jingwu Duan , Hua Gong , Bin Jiang , Bingwei Vera Yang , Arthur M. Doweyko
IPC分类号： C07D491/052 , A61K31/436
CPC分类号： C07D417/12 , C07D277/46 , C07D405/12 , C07D417/14 , C07D491/04
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including inflammatory and immune diseases, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
摘要翻译：提供新的非甾体化合物，其可用于治疗与式（I）结构的糖皮质激素受体，AP-1和/或NF-κB活性（包括炎症和免疫疾病）的调节相关的疾病：其对映异构体，非对映体或其互变异构体或其前药酯或其药学上可接受的盐，其中：Z是杂环或杂芳基; A是5至8元碳环或5至8元杂环; B是环烷基，环烯基，芳基，杂环基或杂芳基环，其中每个环与相邻原子上的A环稠合并任选地被一至四个相同或不同的基团取代，并且独立地选自R5，R6， R7和R8; J1，J2和J3各自出现相同或不同，独立地为-A1QA2-; Q是键，O，S，S（O）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C2-4亚烯基和取代的C2-4亚烯基，条件是选择A1和A2使得环A为 5-至8-元碳环或杂环; R1至R11如本文所定义。还提供了使用所述化合物治疗炎性或免疫相关疾病和肥胖症和糖尿病的药物组合物和方法。

3. 发明授权

US07888381B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的调节剂及其用途
公开(公告)号：US07888381B2
公开(公告)日：2011-02-15
申请号：US11451660
申请日：2006-06-13
申请人： Jingwu Duan , Zhonghui Lu , David S. Weinstein , Bin Jiang
发明人： Jingwu Duan , Zhonghui Lu , David S. Weinstein , Bin Jiang
IPC分类号： C07D231/56 , A01N43/56
CPC分类号： C07D401/04 , C07D231/56 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/12
摘要： Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR1 or C(R4)(R4a); K is selected from NR2 or C(R5)(R5a); L is selected from NR3 or C(R6)(R6a); and A, X, Y, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R8, R10, R11, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式 I）或其对映异构体，非对映异构体，药学上可接受的盐或水合物，其中J选自NR 1或C（R 4）（R 4a）; K选自NR2或C（R5）（R5a）; L选自NR 3或C（R 6）（R 6a）; 并且A，X，Y，R 1，R 2，R 3，R 4，R 4a，R 5，R 5a，R 6，R 6a，R 8，R 10，R 11和n如本文所定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

4. 发明申请

US20110002952A1 FUSED HETEROARYL MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kappaB ACTIVITY AND USE THEREOF 有权
标题翻译： GLUCOCORTICOID受体，AP-1和/或NF-κB活性的融合血管调节剂及其用途
公开(公告)号：US20110002952A1
公开(公告)日：2011-01-06
申请号：US12866270
申请日：2009-02-05
申请人： Jingwu Duan , David S. Weinstein , Bin Jiang
发明人： Jingwu Duan , David S. Weinstein , Bin Jiang
IPC分类号： A61K31/5377 , C07D491/147 , A61K31/4375 , A61K38/26 , A61K38/28 , A61K39/00 , A61P37/00 , A61P29/00 , A61P3/00 , A61P37/06 , A61P19/02 , A61P25/00 , A61P11/06 , A61P1/00 , A61P17/06
CPC分类号： C07D491/147
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; -A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B1 and B2 rings are pyridyl rings, wherein the B1 and B2 rings are each fused to the A ring and the B1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R1, R2, and R4, and the B2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R3, R7, and R3 71, J2, and J3 are at each occurrence the same or different and are independently -AIQA2-; Q is a bond, O, S, S(0), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3 alkylene, substituted C1-3 alkylene, C24 alkenylene, and substituted C24 alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 are as defined herein.
摘要翻译：提供新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病或病症，包括具有结构的代谢和炎症和免疫疾病或病症式（I）的化合物：其对映异构体，非对映异构体或其互变异构体或其前药酯或其药学上可接受的盐，其中：Z是杂环基或杂芳基; -A是5-至8-元碳环或5-至8-元杂环; B1和B2环是吡啶环，其中B1和B2环各自与A环稠合，B1环任选被一至三个相同或不同并且独立地选自R 1，R 2和R 4的基团取代并且B2环任选地被一至三个相同或不同并且独立地选自R3，R7和R371的基团取代，J2和J3在每次出现时相同或不同，并且独立地为-AIQA2- ; Q是键，O，S，S（0）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C24亚烯基和取代的C24亚烯基，条件是选择A1和A2，使得环A为 5-至8-元碳环或杂环; R1至R11如本文所定义。

5. 发明授权

US08304539B2 Fused heteroaryl modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的融合杂芳基调节剂及其用途
公开(公告)号：US08304539B2
公开(公告)日：2012-11-06
申请号：US12866270
申请日：2009-02-05
申请人： Jingwu Duan , David S. Weinstein , Bin Jiang
发明人： Jingwu Duan , David S. Weinstein , Bin Jiang
IPC分类号： C07D491/147 , C07D413/00
CPC分类号： C07D491/147
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or taυtomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; •A is a S- to 8-membered carbocyclic ring or a S- to 8-membered heterocyclic ring; B1 and B2 rings are pyridyl rings, wherein the B1 and B2 rings are each fused to the A ring and the B1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R1, R2, and R4, and the B2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R5, R7, and R3 J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3 alkylene, substituted C1-3 alkylene, C2-4 alkenylene, and substituted C2-4 alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 are as defined herein.
摘要翻译：提供新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病或病症，包括具有结构的代谢和炎症和免疫疾病或病症式（I）的化合物：其对映异构体，非对映异构体或其互变异构体或其前药酯或其药学上可接受的盐，其中：Z是杂环基或杂芳基; A是5至8元碳环或5至8元杂环; B1和B2环是吡啶环，其中B1和B2环各自与A环稠合，B1环任选被一至三个相同或不同并且独立地选自R 1，R 2和R 4的基团取代并且B2环任选被一至三个相同或不同并且独立地选自R5，R7和R8的基团取代，J1，J2和J3在每次出现时相同或不同，并且独立地为-A 1 QA 2 - ; Q是键，O，S，S（O）或S（O）2; A1和A2相同或不同，并且在每次出现时独立地选自键，C1-3亚烷基，取代的C1-3亚烷基，C2-4亚烯基和取代的C2-4亚烯基，条件是A1和A2被选择为该环A为5-至8-元碳环或杂环; R1至R11如本文所定义。

6. 发明授权

US07317032B2 Imidazolyl inhibitors of 15-lipoxygenase 有权
标题翻译： 15-脂氧合酶的咪唑基抑制剂
公开(公告)号：US07317032B2
公开(公告)日：2008-01-08
申请号：US10932594
申请日：2004-09-01
申请人： David S. Weinstein , Khehyong Ngu , Jeffrey A. Robl
发明人： David S. Weinstein , Khehyong Ngu , Jeffrey A. Robl
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： C04B35/632 , C07D233/64 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D417/04 , C07D471/10 , C07D487/08
摘要： The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
摘要翻译：本发明提供15-LO的咪唑基抑制剂，含有这种抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联有关的疾病的方法。

7. 发明授权

US06887870B1 Heterocyclic sodium/proton exchange inhibitors and method 有权
标题翻译：杂环钠/质子交换抑制剂及方法
公开(公告)号：US06887870B1
公开(公告)日：2005-05-03
申请号：US09669298
申请日：2000-09-25
申请人： Saleem Ahmad , Shung C. Wu , Steven V. O'Neil , Khehyong Ngu , Karnail S. Atwal , David S. Weinstein
发明人： Saleem Ahmad , Shung C. Wu , Steven V. O'Neil , Khehyong Ngu , Karnail S. Atwal , David S. Weinstein
IPC分类号： C07D233/64 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/4172 , A61K31/4178 , A61K31/4196 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K45/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/10 , A61P25/28 , A61P29/00 , A61P43/00 , C07D231/38 , C07D233/54 , C07D233/84 , C07D233/88 , C07D239/48 , C07D277/20 , C07D277/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D405/08 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/08 , C07D417/04 , C07D417/08 , C07D417/14 , C07D471/02 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
CPC分类号： C07D233/56 , C07D233/64 , C07D233/88 , C07D239/49 , C07D277/20 , C07D277/40 , C07D401/04 , C07D401/14 , C07D403/08 , C07D405/08 , C07D409/14 , C07D417/08 , C07D471/04 , C07D487/04
摘要： Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.
摘要翻译：提供了具有其中n为1至5的结构的钠/质子交换（NHE）抑制剂的杂环; X是N或C-R 5，其中R 5是H，卤素，烯基，炔基，烷氧基，烷基，芳基或杂芳基; Z是杂芳基，R 1，R 2，R 3和R 4如本文所定义，并且其中X为N.R 1优选为芳基或杂芳基，并且可用作抗心绞痛和心脏保护剂。此外，提供了使用上述杂环衍生物预防或治疗心绞痛，心脏功能障碍，心肌坏死和心律失常的方法。

8. 发明授权

US07351727B2 Inhibitors of 15-lipoxygenase 有权
标题翻译： 15-脂肪氧化酶抑制剂
公开(公告)号：US07351727B2
公开(公告)日：2008-04-01
申请号：US10932457
申请日：2004-09-01
申请人： David S. Weinstein
发明人： David S. Weinstein
IPC分类号： A61K31/425 , C07D327/04
CPC分类号： C07D277/46 , C07D263/28 , C07D277/40
摘要： The present invention provides oxazolyl and thiazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
摘要翻译：本发明提供15-LO的恶唑基和噻唑基抑制剂，含有这些抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联相关的疾病的方法。

9. 发明授权

US07534804B2 Benzoxazole inhibitors of 15-lipoxygenase 有权
标题翻译：苯并恶唑抑制剂15-脂肪氧合酶
公开(公告)号：US07534804B2
公开(公告)日：2009-05-19
申请号：US11509373
申请日：2006-08-24
申请人： David S. Weinstein
发明人： David S. Weinstein
IPC分类号： A61K31/423 , C07D263/54
CPC分类号： C07D263/56 , C07D413/12 , C07D413/14
摘要： The present application provides benzoxazole inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
摘要翻译：本申请提供15-LO的苯并恶唑抑制剂，含有这些抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联有关的疾病的方法。

10. 发明授权

US07253283B2 Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的三环调节剂及其用途
公开(公告)号：US07253283B2
公开(公告)日：2007-08-07
申请号：US11035176
申请日：2005-01-13
申请人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
发明人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
IPC分类号： C07D417/02 , C07D413/02 , A61K31/473
CPC分类号： C07D417/12 , A23K20/168 , A23K50/40 , C07D233/88 , C07D277/46 , C07D405/12 , C07D453/06
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并且具有式（I ）或其立体异构体或前药或其药学上可接受的盐，其中B，J，K，Z，R，R a，R b，R b， >，R“，R”，“O”，m和n如本文所定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

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