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1. 发明授权

US07968577B2 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：US07968577B2
公开(公告)日：2011-06-28
申请号：US12513187
申请日：2007-10-31
申请人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T. G. Murali Dhar
发明人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T. G. Murali Dhar
IPC分类号： A61K31/5377 , A61K31/5375 , A61K31/505 , A61K31/50 , A61K31/4965 , A61K31/496 , A61K31/4709 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/421 , A61K31/4168 , A61K31/415 , A61K31/165 , C07D417/04 , C07D417/12 , C07D277/46 , C07D285/135 , C07D263/48 , C07D241/20 , C07D239/42 , C07D233/88 , C07D231/44
CPC分类号： C07D211/58 , C07C235/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D277/46 , C07D277/82 , C07D285/08 , C07D285/135 , C07D417/04 , C07D417/10 , C07D417/12
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, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM 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; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.
摘要翻译：提供了新的非甾体化合物，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，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病），对映体，非对映体，互变异构体，溶剂合物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，R 1，R 2，R 3，R 4，R 6，R 7和R 22如本文所定义。还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

2. 发明申请

US20100075961A1 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：US20100075961A1
公开(公告)日：2010-03-25
申请号：US12513232
申请日：2007-10-31
申请人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
发明人： James E. Sheppeck , John L. Gilmore , T. G. Murali Dhar , Hai-Yun Xiao , Jianmin Wang , Bingwei Vera Yang , Lidia M. Doweyko
IPC分类号： A61K31/416 , C07D231/56 , C07D413/12 , A61K31/5377 , A61P3/00 , A61P29/00 , A61P37/00
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D409/12
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, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, provided that the E-F-G containing heterocyclic ring formed does not contain a S—S or S—O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.
摘要翻译：提供了新的非甾体化合物，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，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病），其对映异构体，非对映异构体或其药学上可接受的盐或水合物，其中X为（Ia）; 或X为（Ib）; 或X为（Ic）; （Id）是杂环或杂芳基; E是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2-; F是-N-，-NR1 - ， - O - ， - S - ， - SO2-或-CR2a-; G是N，-NR1b - ， - O - ， - S - ， - SO2-或-CR2b-，条件是所形成的含有EFG的杂环不含S-S或S-O键， E，F和G是杂原子; J，Ja，M，Ma，Q，Rx，Ry，R1，R1a，R1b，R2，R2a，R2b和R3至R21，Z，Za，Zb和Zc如上所定义。

3. 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.

4. 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。

5. 发明申请

US20100063051A1 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：US20100063051A1
公开(公告)日：2010-03-11
申请号：US12513187
申请日：2007-10-31
申请人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T.G. Murali Dhar
发明人： Bingwei Vera Yang , Lidia M. Doweyko , Wayne Vaccaro , Tram N. Huynh , David R. Tortolani , T.G. Murali Dhar
IPC分类号： A61K31/5377 , C07D277/38 , C07D417/12 , A61K31/426 , A61P37/00 , A61P29/00
CPC分类号： C07D211/58 , C07C235/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/75 , C07D231/40 , C07D233/88 , C07D239/42 , C07D277/46 , C07D277/82 , C07D285/08 , C07D285/135 , C07D417/04 , C07D417/10 , C07D417/12
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, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM 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; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.
摘要翻译：提供了新的非甾体化合物，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，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病），对映体，非对映体，互变异构体，溶剂合物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，R 1，R 2，R 3，R 4，R 6，R 7和R 22如本文所定义。还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

6. 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。

7. 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。

8. 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。

9. 发明授权

US08222247B2 Modulators of glucocorticoid receptor, AP-1, and/or NF-kappabeta activity and use thereof 有权
公开(公告)号：US08222247B2
公开(公告)日：2012-07-17
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： A61K31/5377 , C07D265/30
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 M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; 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. Also provided are pharmaceutical compositions, combinations and methods of treating metabolic and inflammatory or immune associated diseases or disorders using said compounds.

10. 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。

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