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1. 发明申请

US20130079325A1 PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS 有权
标题翻译：吡啶和吡嗪衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：US20130079325A1
公开(公告)日：2013-03-28
申请号：US13676826
申请日：2012-11-14
申请人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
发明人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
IPC分类号： C07D413/14 , C07D401/14 , C07D401/12
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00
摘要： Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

2. 发明申请

US20100160280A1 AMINOPYRIDINE AND CARBOXYPYRIDINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS 有权
标题翻译：氨基吡啶和羧基吡啶化合物作为磷酸二酯酶10抑制剂
公开(公告)号：US20100160280A1
公开(公告)日：2010-06-24
申请号：US12639931
申请日：2009-12-16
申请人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael Frohn , Paul Harrington , Essa Hu , Matthew R. Kaller , Roxanne Kunz , Stephanie J. Mercede , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Christopher M. Tegley , Guomin Yao
发明人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael Frohn , Paul Harrington , Essa Hu , Matthew R. Kaller , Roxanne Kunz , Stephanie J. Mercede , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Christopher M. Tegley , Guomin Yao
IPC分类号： A61K31/397 , C07D213/22 , A61K31/444 , C07D213/62 , C07D413/14 , A61K31/5377 , C07D401/02 , A61K31/506 , C07D403/14 , A61K31/4545 , A61K31/496 , C07D267/10 , A61K31/553 , C07D243/08 , A61K31/551 , A61P25/00
CPC分类号： C07D401/04 , C07D213/74 , C07D213/84 , C07D401/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5，R6，R7，X1，X2，X3，X4，X5，X6，X7，X8和Y为如说明书中所定义; 或其药学上可接受的盐，其中环A，m，n，y，R2，R3，R4，R5，R6，R7，R8，R9，X1，X2和环A如说明书中所定义; 和其药学上可接受的盐，其中m，n，y，R2，R3，R4，R5，R6，R7，R9，X1，X2和环A如说明书中所定义; 含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖型糖尿病，精神分裂症，双相情感障碍，强迫症等。

3. 发明申请

US20080032973A1 2-Quinazolinone compounds and methods of use 失效
标题翻译： 2-喹唑啉酮化合物及其使用方法
公开(公告)号：US20080032973A1
公开(公告)日：2008-02-07
申请号：US11879243
申请日：2007-07-16
申请人： Fang-Tsao Hong , Kelvin Sham , Seifu Tadesse , Andrew Tasker
发明人： Fang-Tsao Hong , Kelvin Sham , Seifu Tadesse , Andrew Tasker
IPC分类号： C07D239/80 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P19/00 , C07D413/14 , C07D471/04 , C07D413/02 , A61P3/00 , A61P31/12 , A61P7/00
CPC分类号： C07D471/04 , C07D239/82
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, s, T, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of kinase mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式I，其中A 1，A 2，B，s，T，R 1，R 2， / SUP>，R 3和R 4在本文中定义。本发明还包括药物组合物，其包含一种或多种式I化合物，使用方法，例如通过施用式I化合物或包含式I化合物的组合物治疗激酶介导的疾病，以及可用于制备式Ⅰ的化合物。

4. 发明申请

US20050182072A1 Substituted heterocyclic compounds and methods of use 有权
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050182072A1
公开(公告)日：2005-08-18
申请号：US11034042
申请日：2005-01-11
申请人： Guo-Qiang Cao , Jian Chen , Celia Dominguez , Anthony Reed , Kelvin Sham , Maya Thaman , Dawei Zhang , Bradley Herberich
发明人： Guo-Qiang Cao , Jian Chen , Celia Dominguez , Anthony Reed , Kelvin Sham , Maya Thaman , Dawei Zhang , Bradley Herberich
IPC分类号： C07D213/56 , C07D239/95 , C07D401/04 , C07D401/14 , C07D417/14 , C07D487/06 , C07D487/08 , C07D519/00 , A61K31/519 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/513 , A61K31/517 , C07D487/02
CPC分类号： C07D487/06 , C07D213/56 , C07D239/95 , C07D401/04 , C07D401/14 , C07D417/14
摘要： The present invention relates to therapeutic diazobicyclo pyridines and their use in the treatment of arthritis, rheumatoid arthritis, psoriatic arthritis or osteoarthritis, organ transplant, acute transplant or heterograft and homograft rejection, ischemic and reperfusion injury, transplantation tolerance induction, multiple sclerosis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, lupus, graft vs. host diseases, T -cell mediated hypersensitivity diseases, contact hypersensitivity, delayed-type hypersensitivity, gluten-sensitive enteropathy, Type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Graves' Disease, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, autoimmune diseases, glomerulonephritis, serum sickness, uticaria, respiratory allergies, asthma, hayfever, allergic rhinitis, skin allergies, scleracielma, mycosis flugoides, acute inflammatory responses, acute respiratory distress syndrome, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, Type II diabetes and cancers where PKC theta or other PKC-family kinases are activated, overexpressed or facilitate tumor growth or survival of tumor cells, T cell leukemia, thymoma, T and B cell lymphoma, colon carcinoma, breast carcinoma and lung carcinoma or provides resistance to chemotherapeutic drugs.
摘要翻译：本发明涉及治疗性重氮二环吡啶及其在治疗关节炎，类风湿性关节炎，银屑病关节炎或骨关节炎，器官移植，急性移植或异种移植和同种异体移植排斥，缺血和再灌注损伤，移植耐受诱导，多发性硬化，炎性肠中的用途疾病，溃疡性结肠炎，克罗恩病，狼疮，移植物抗宿主病，T细胞介导的超敏反应性疾病，接触性超敏反应，延迟型超敏反应，麸质敏感性肠病，1型糖尿病，牛皮癣，接触性皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进症，格雷夫斯病，艾迪生病，自身免疫性多腺病，自身免疫性脱发，恶性贫血，白癜风，自身免疫性低分化症，吉兰巴利综合征，自身免疫性疾病，肾小球肾炎，血清病，荨麻疹，呼吸道过敏，哮喘，过敏性鼻炎，过敏性鼻炎，皮肤过敏 es，scleracielma，真菌性感冒，急性炎症反应，急性呼吸窘迫综合征，皮肌炎，斑秃，慢性光化性皮炎，湿疹，Behcet氏病，脓疱疮，新生皮炎，Sezary综合征，特应性皮炎，全身性硬化症，morphea，II型糖尿病和PKCθ或其他PKC家族激酶被激活，过度表达或促进肿瘤细胞，T细胞白血病，胸腺瘤，T细胞和B细胞淋巴瘤，结肠癌，乳腺癌和肺癌的肿瘤生长或存活的癌症，或提供对化学治疗的抗性药物

5. 发明授权

US08637500B2 Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors 有权
标题翻译：氨基吡啶和羧基吡啶化合物作为磷酸二酯酶10抑制剂
公开(公告)号：US08637500B2
公开(公告)日：2014-01-28
申请号：US12639931
申请日：2009-12-16
申请人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Essa Hu Harrington , Matthew R. Kaller , Roxanne K. Kunz , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Guomin Yao
发明人： Jennifer R. Allen , Ning Chen , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Essa Hu Harrington , Matthew R. Kaller , Roxanne K. Kunz , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Aaron C. Siegmund , Guomin Yao
IPC分类号： A61K31/551 , A61K31/553 , A61K31/5377 , A61K31/497 , C07D243/08 , C07D267/10 , C07D401/12 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , C07D213/74 , C07D213/84 , C07D401/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5，R6，R7，X1，X2，X3，X4，X5，X6，X7，X8和Y为如说明书中所定义; 或其药学上可接受的盐，其中环A，m，n，y，R2，R3，R4，R5，R6，R7，R8，R9，X1，X2和环A如说明书中所定义; 和其药学上可接受的盐，其中m，n，y，R2，R3，R4，R5，R6，R7，R9，X1，X2和环A如说明书中所定义; 含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

6. 发明申请

US20100125062A1 PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS 有权
标题翻译：吡啶和吡嗪衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：US20100125062A1
公开(公告)日：2010-05-20
申请号：US12619573
申请日：2009-11-16
申请人： Jennifer R. Allen , Kaustav Biswas , Frank Chavez, Jr. , Ning Chen , Frenel Fils Demorin , James R. Falsey , Mike Frohn , Paul Harrington , Dan Horne , Essa Hu , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Tom Nguyen , Alex Pickrell , Andreas Reichelt , Shannon Rumfelt , Rob Rzasa , Kelvin Sham , Guomin Yao
发明人： Jennifer R. Allen , Kaustav Biswas , Frank Chavez, Jr. , Ning Chen , Frenel Fils Demorin , James R. Falsey , Mike Frohn , Paul Harrington , Dan Horne , Essa Hu , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Tom Nguyen , Alex Pickrell , Andreas Reichelt , Shannon Rumfelt , Rob Rzasa , Kelvin Sham , Guomin Yao
IPC分类号： A61K31/4439 , C07D401/12 , C07D471/04 , C07D473/00 , C07D413/14 , C07D401/14 , A61K31/437 , A61K31/52 , A61K31/5377 , A61K31/55 , A61K31/397 , A61P25/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00
摘要： Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖型糖尿病，精神分裂症，双相情感障碍，强迫症等。

7. 发明申请

US20070054916A1 Aryl nitrogen-containing bicyclic compounds and methods of use 审中-公开
标题翻译：芳基含氮双环化合物及其使用方法
公开(公告)号：US20070054916A1
公开(公告)日：2007-03-08
申请号：US11240590
申请日：2005-09-30
申请人： Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
发明人： Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
IPC分类号： A61K31/525 , A61K31/519 , A61K31/517
CPC分类号： C07D215/38 , C07C205/37 , C07D215/12 , C07D217/12 , C07D217/22 , C07D217/26 , C07D239/26 , C07D239/84 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症，癌症和相关病症的化合物。化合物具有通式I，其中A 1，A 2，A 3，B，R 1， R 2，R 3和R 4在本文中定义。因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

8. 发明授权

US08318718B2 Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors 有权
标题翻译：吡啶和嘧啶衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：US08318718B2
公开(公告)日：2012-11-27
申请号：US12619573
申请日：2009-11-16
申请人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
发明人： Jennifer R. Allen , Biswas Kaustav , Frank Chavez , Ning Chen , Frenel Fils De Morin , James R. Falsey , Michael J. Frohn , Paul E. Harrington , Daniel B. Horne , Essa Hu Harrington , Matthew R. Kaller , Roxanne Kunz , Holger Monenschein , Thomas T. Nguyen , Alexander J. Pickrell , Andreas Reichelt , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Guomin Yao
IPC分类号： A61K31/4439 , A61K31/437 , A61K31/52 , A61K31/5377 , A61K31/55 , A61K31/397 , C07D401/12 , C07D471/04 , C07D473/00 , C07D413/14 , C07D401/14 , A61P25/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00
摘要： Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

9. 发明申请

US20060199817A1 Phthalazine, aza- and diaza-phthalazine compounds and methods of use 有权
标题翻译：酞嗪，氮杂和二氮杂 - 酞嗪化合物及其使用方法
公开(公告)号：US20060199817A1
公开(公告)日：2006-09-07
申请号：US11367123
申请日：2006-03-02
申请人： Andrew Tasker , Dawei Zhang , Guo-Qiang Cao , Partha Chakrabarti , James Falsey , Bradley Herberich , Randall Hungate , Liping Pettus , Anthony Reed , Robert Rzasa , Kelvin Sham , Maya Thaman , Shimin Xu
发明人： Andrew Tasker , Dawei Zhang , Guo-Qiang Cao , Partha Chakrabarti , James Falsey , Bradley Herberich , Randall Hungate , Liping Pettus , Anthony Reed , Robert Rzasa , Kelvin Sham , Maya Thaman , Shimin Xu
IPC分类号： A61K31/5377 , A61K31/503 , A61K31/53 , C07D487/02
CPC分类号： C07D409/04 , C07D237/30 , C07D237/32 , C07D237/34 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/10
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。化合物具有通式I，其中A 1，A 2，B，R 1，R 2， R 3和R 4在本文中定义。本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗激酶介导的疾病包括类风湿性关节炎，牛皮癣和其它炎症疾病的用途，以及可用于制备一级方程式

10. 发明申请

US20050038010A1 Substituted heterocyclic compounds and methods of use 有权
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050038010A1
公开(公告)日：2005-02-17
申请号：US10438553
申请日：2003-05-13
申请人： Guo-Qiang Cao , Celia Dominguez , Martin Goldberg , Fang-Tsao Hong , Kelvin Sham , Seifu Tadesse , Nuria Tamayo , Kurt Weiler , Dawei Zhang , Hongyu Liao
发明人： Guo-Qiang Cao , Celia Dominguez , Martin Goldberg , Fang-Tsao Hong , Kelvin Sham , Seifu Tadesse , Nuria Tamayo , Kurt Weiler , Dawei Zhang , Hongyu Liao
IPC分类号： A61K31/444 , A61K31/4545 , A61K31/501 , A61K31/506 , A61P1/04 , A61P1/18 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/16 , A61P31/18 , A61P31/20 , A61P31/22 , A61P33/06 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P39/02 , C07D401/04 , C07D401/14 , A61K31/553 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/55
CPC分类号： C07D401/04
摘要： The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
摘要翻译：本发明涉及具有通式的化合物或其药学上可接受的盐，其中R 1是饱和或不饱和的含有0,1,2或3个选自N，，O和S，其中所述环可以与苯并稠合，并被0,1或2个氧代基取代，并且其中R 1另外被取代; R 2是取代的C 1-6烷基。还包括预防或治疗炎症，类风湿性关节炎，斑节病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征（ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病，中风，心肌梗死，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒引起的肌痛（CMV），流感，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的化合物d 以上所述。

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