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1. 发明授权

US07361654B2 Substituted heteroaryl amide 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活性的取代的杂芳基酰胺调节剂及其用途
公开(公告)号：US07361654B2
公开(公告)日：2008-04-22
申请号：US11330553
申请日：2006-01-12
申请人： James Sheppeck , T. G. Murali Dhar , Lidia Doweyko , John Gilmore , David Weinstein , Hai-Yun Xiao , Bingwei V. Yang , Arthur M. Doweyko
发明人： James Sheppeck , T. G. Murali Dhar , Lidia Doweyko , John Gilmore , David Weinstein , Hai-Yun Xiao , Bingwei V. Yang , Arthur M. Doweyko
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/496 , A61K31/4439 , A61K31/427 , A61K31/426 , A61K31/4196 , A61K31/4168
CPC分类号： C07D233/91 , C07D277/46 , C07D417/06
摘要： The present invention relates to new class of non-steroidal compounds 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-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.
摘要翻译：本发明涉及新类型的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性调节有关的疾病，包括肥胖，糖尿病，炎性和免疫相关疾病，并且具有包括其所有立体异构体，其互变异构体或其前药或其药学上可接受的盐的结构，其中X选自N，O和S; Y是N或CR 6; Z是一个戒指并且其中R，R a，R b，R b，R c，R d，R 1， R 2，R 3，R 4和R 5如本文所定义。还提供了治疗肥胖，糖尿病和包含这些化合物的炎性或免疫相关疾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

US07411071B2 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活性的调节剂及其用途
公开(公告)号：US07411071B2
公开(公告)日：2008-08-12
申请号：US11330748
申请日：2006-01-12
申请人： Bingwei V. Yang , Lidia M. Doweyko , Arthur M. Doweyko
发明人： Bingwei V. Yang , Lidia M. Doweyko , Arthur M. Doweyko
IPC分类号： A61K31/425 , C07D277/44
CPC分类号： C07D277/46 , C07D233/90 , C07D277/56
摘要： A class of 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): where X is S, O or N; Z is —T—COOR1 or —T—COR1; and T, R, R1, Ra, Rb, Rc, Rd, Z, A and B 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：提供了一类新型非甾体化合物，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，包括肥胖症，糖尿病，炎症和免疫疾病，并且具有式（I）：其中X为S，O或N; Z是-T-COOR 1或-T-COR 1; 和T，R，R 1，R 2，R 2，R b，R d，R d，本文定义了Z，A和B。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. 发明授权

US06995181B2 Modulators of the glucocorticoid receptor and method 有权
标题翻译：糖皮质激素受体的调节剂和方法
公开(公告)号：US06995181B2
公开(公告)日：2006-02-07
申请号：US10621909
申请日：2003-07-17
申请人： Wayne Vaccaro , Bingwei Vera Yang , Soong-Hoon Kim , Tram Huynh , David R. Tortolani , Kenneth J. Leavitt , Wenying Li , Arthur M. Doweyko , Xiao-Tao Chen , Lidia Doweyko
发明人： Wayne Vaccaro , Bingwei Vera Yang , Soong-Hoon Kim , Tram Huynh , David R. Tortolani , Kenneth J. Leavitt , Wenying Li , Arthur M. Doweyko , Xiao-Tao Chen , Lidia Doweyko
IPC分类号： A61K31/426 , C07D277/38
CPC分类号： C07D495/04 , A61K31/403 , A61K31/473 , A61K45/06 , C07D207/34 , C07D209/48 , C07D213/40 , C07D213/75 , C07D213/82 , C07D215/38 , C07D217/22 , C07D231/16 , C07D233/88 , C07D235/14 , C07D235/30 , C07D239/42 , C07D239/94 , C07D241/20 , C07D261/12 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/64 , C07D285/06 , C07D307/58 , C07D317/58 , C07D333/20 , C07D333/34 , C07D401/04 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , A61K2300/00
摘要： Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, Z, A and B are defined herein.
摘要翻译：提供了新型非甾体化合物，其是糖皮质激素受体调节剂，其可用于治疗需要糖皮质激素受体激动剂或拮抗剂治疗的疾病，例如肥胖症，糖尿病，炎症和免疫疾病，并且具有结构

5. 发明授权

US4394155A Substituted pyridine 1-oxide herbicides 失效
标题翻译：取代的吡啶1-氧化物除草剂
公开(公告)号：US4394155A
公开(公告)日：1983-07-19
申请号：US231813
申请日：1981-02-05
申请人： Howard L. Plant , Steven E. Cantor , Arthur M. Doweyko , Mark A. Dekeyser , Allyn R. Bell
发明人： Howard L. Plant , Steven E. Cantor , Arthur M. Doweyko , Mark A. Dekeyser , Allyn R. Bell
IPC分类号： C07D213/71 , A01N43/40 , C07D213/89 , C07D213/64
CPC分类号： C07D213/89 , A01N43/40
摘要： Compounds of the following formula are effective as premergence herbicides: ##STR1## wherein R and R.sup.1 may be the same or different and are C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, phenyl or halogen, provided that R or R.sup.1 is not halogen if attached in the 3- position of the pyridine ring, and R or R.sup.1 may further be hydrogen provided that one of them is one of the recited moieties other than hydrogen; R.sup.2 is hydrogen, halogen, methyl or ethyl; R.sup.3 is phenyl or phenyl substituted with halogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, or nitro; and n is 1 or 2.
摘要翻译：下式的化合物作为预浸除草剂是有效的：其中R和R 1可以相同或不同，为C 1至C 4烷基，C 1至C 4烷氧基，苯基或卤素，条件是R或R 1不是卤素，如果连接在吡啶环的3-位，R或R 1可以进一步为氢，条件是它们之一是氢以外的所述部分之一; R2是氢，卤素，甲基或乙基; R3是苯基或被卤素取代的苯基，C1至C4烷基，C1至C4烷氧基或硝基; n为1或2。

6. 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。

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