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1. 发明授权

US08987268B2 Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases 有权
标题翻译：吡咯并哒嗪JAK3抑制剂及其用于治疗炎症和自身免疫疾病的用途
公开(公告)号：US08987268B2
公开(公告)日：2015-03-24
申请号：US14005568
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Jagabandhu Das , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , William J. Pitts , Steven H. Spergel , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Jagabandhu Das , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , William J. Pitts , Steven H. Spergel , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07D471/04 , A01N43/58 , A61K31/50
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎症和自身免疫性疾病。

2. 发明申请

US20140011800A1 PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 有权
标题翻译：吡咯烷酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途
公开(公告)号：US20140011800A1
公开(公告)日：2014-01-09
申请号：US14005568
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Jagabandhu Das , JIngwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , William J. Pitts , Steven H. Spergel , Hong Hu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Jagabandhu Das , JIngwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , William J. Pitts , Steven H. Spergel , Hong Hu , Bingwei Vera Yang
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎症和自身免疫性疾病。

3. 发明授权

US08921368B2 Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases 有权
标题翻译：吡咯并哒嗪JAK3抑制剂及其用于治疗炎症和自身免疫疾病的用途
公开(公告)号：US08921368B2
公开(公告)日：2014-12-30
申请号：US14005570
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07D471/04 , A01N43/58 , A61K31/50
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐。式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。

4. 发明申请

US20140011795A1 PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 有权
标题翻译：吡咯烷酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途
公开(公告)号：US20140011795A1
公开(公告)日：2014-01-09
申请号：US14005570
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Gregory D. Brown , Lidia M. Doweyko , Jingwu Duan , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Zhonghui Lu , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐。式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。

5. 发明申请

US20140005146A1 PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES 有权
标题翻译：吡咯烷酮JAK3抑制剂及其用于治疗炎症和自发性疾病的用途
公开(公告)号：US20140005146A1
公开(公告)日：2014-01-02
申请号：US14005572
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Jagabandhu Das , Lidia M. Doweyko , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Jagabandhu Das , Lidia M. Doweyko , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐。式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。

6. 发明授权

US09221826B2 Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases 有权
标题翻译：吡咯并哒嗪JAK3抑制剂及其用于治疗炎症和自身免疫疾病的用途
公开(公告)号：US09221826B2
公开(公告)日：2015-12-29
申请号：US14005572
申请日：2012-03-16
申请人： Stephen T. Wrobleski , Jagabandhu Das , Lidia M. Doweyko , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
发明人： Stephen T. Wrobleski , Jagabandhu Das , Lidia M. Doweyko , Junqing Guo , John Hynes , Bin Jiang , James Kempson , Shuqun Lin , Steven H. Spergel , John S. Tokarski , Hong Wu , Bingwei Vera Yang
IPC分类号： A61K31/5025 , A61K31/675 , C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐。式（I）化合物抑制JAK3的酪氨酸激酶活性，从而使其可用于治疗炎性和自身免疫性疾病。

7. 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。

8. 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。

9. 发明授权

US08106046B2 Cyclopentathiophene 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活性的环戊噻吩调节剂及其用途
公开(公告)号：US08106046B2
公开(公告)日：2012-01-31
申请号：US12996806
申请日：2009-06-24
申请人： Bingwei Vera Yang
发明人： Bingwei Vera Yang
IPC分类号： C07D413/14 , C07D417/12 , A61K31/433 , A61K31/5377 , A61P19/02 , A61P29/00
CPC分类号： C07D417/12
摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
摘要翻译：式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。还公开了含有式I化合物的药物组合物和组合以及治疗包括代谢和炎症或免疫相关疾病或病症的疾病或病症的方法。

10. 发明申请

US20100004219A1 MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KAPPABETA ACTIVITY AND USE THEREOF 有权
公开(公告)号：US20100004219A1
公开(公告)日：2010-01-07
申请号：US12513229
申请日：2007-10-31
申请人： Bingwei Vera Yang , Lidia M. Doweyko
发明人： Bingwei Vera Yang , Lidia M. Doweyko
IPC分类号： A61K31/397 , A61K31/433 , A61K31/426 , C07D277/02 , A61K31/444 , A61K31/4439 , C07D417/02 , A61K31/5377 , C07D413/14 , A61K31/454 , C07D417/14 , A61P29/00 , A61P3/00 , A61P37/00
CPC分类号： C07D417/12 , C07D417/14
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 metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and M are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; and Z is selected from alkyl, CF3, OH, cycloalkyl, heterocyclo, aryl, heteroaryl, —C(═O)NR8R9, —C(═O)R8, —C(NCN)NR8R9, —C(═O)OR8, —SO2R8, and —SO2NR8R9. Ma, Za, R1, R2, R3, R5a, R6, R7, R8, R9 and R22 are as defined herein. Also provided are pharmaceutical compositions, combinations and methods of treating metabolic and inflammatory or immune associated diseases or disorders using said compounds.

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