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。

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

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