公开(公告)号：US20060040961A1

公开(公告)日：2006-02-23

申请号：US11169312

申请日：2005-06-29

申请人： John Buchanan ,  William Buckner ,  Simon Burkitt ,  Erin DiMauro ,  Christopher Farthing ,  Alexander Frenkel ,  Martin Harrison ,  Frank Kayser ,  Jinqian Liu ,  Sarah Lively ,  Teresa Marshall ,  David McGowan ,  Rajiv Sharma ,  Stephen Shuttleworth ,  Xiaotian Zhu

发明人： John Buchanan ,  William Buckner ,  Simon Burkitt ,  Erin DiMauro ,  Christopher Farthing ,  Alexander Frenkel ,  Martin Harrison ,  Frank Kayser ,  Jinqian Liu ,  Sarah Lively ,  Teresa Marshall ,  David McGowan ,  Rajiv Sharma ,  Stephen Shuttleworth ,  Xiaotian Zhu

IPC分类号： A61K31/519 ,  C07D491/02

CPC分类号： C07D491/04 ,  C07D495/04

摘要： The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I. The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula I.

摘要翻译： 本发明涉及具有通式I的呋喃并嘧啶化合物及其立体异构体，互变异构体，溶剂合物，药用盐和衍生物及其前药。 本发明还包括药物组合物，其包含式I化合物，治疗哺乳动物各种疾病和病症的方法，包括炎症，抑制T细胞活化，增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗塞，中风， 多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，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，艾迪生病，自身免疫性疾病，肾小球性肾炎，过敏性疾病，哮喘，干草病，湿疹， 结肠癌和胸腺瘤，包括向哺乳动物施用治疗有效量的式I化合物。本发明还涉及制备药物的方法，其包含一种或多种式I化合物。

公开(公告)号：US20070155777A1

公开(公告)日：2007-07-05

申请号：US11709895

申请日：2007-02-21

申请人： Simon Burkitt ,  Mario Cardozo ,  Timothy Cushing ,  Michael DeGraffeneid ,  Christopher Farthing ,  Xiaolin Hao ,  Juan Jaen ,  Xian Jiao ,  David Kopecky ,  Marc Labelle ,  Sarah Lively ,  Dustin McMinn ,  Sven Rasmussen ,  Youngsook Shin ,  Andrew Smith ,  Marie-Louise Smith

发明人： Simon Burkitt ,  Mario Cardozo ,  Timothy Cushing ,  Michael DeGraffeneid ,  Christopher Farthing ,  Xiaolin Hao ,  Juan Jaen ,  Xian Jiao ,  David Kopecky ,  Marc Labelle ,  Sarah Lively ,  Dustin McMinn ,  Sven Rasmussen ,  Youngsook Shin ,  Andrew Smith ,  Marie-Louise Smith

IPC分类号： A61K31/4743 ,  C07D498/02

CPC分类号： C07D231/56 ,  C07D239/74 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D495/14 ,  C07D513/04

摘要： Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism, infection and cell proliferation. The subject compounds contain a fused heterobicyclic ring.

摘要翻译： 本文提供了可用于治疗炎症，免疫调节，代谢，感染和细胞增殖性疾病或病症的化合物，组合物和方法。 特别地，本发明提供调节参与炎症，代谢，感染和细胞增殖的蛋白质的表达和/或功能的化合物。 主题化合物含有稠合的杂双环。