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    • 5. 发明申请
    • SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
    • 取代的杂环化合物及其使用方法
    • WO2003099808A1
    • 2003-12-04
    • PCT/US2003/015473
    • 2003-05-15
    • AMGEN INC.DOMINGUEZ, CeliaZHANG, DaweiCAO, Guo-QiangGOLDBERG, Martin, H.HONG, Fang-TsaoSHAM, Kelvin, K., C.TADESSE, SeifuTAMAYO, Nuria, A.WEILER, Kurt, E.LIAO, Hongyu
    • DOMINGUEZ, CeliaZHANG, DaweiCAO, Guo-QiangGOLDBERG, Martin, H.HONG, Fang-TsaoSHAM, Kelvin, K., C.TADESSE, SeifuTAMAYO, Nuria, A.WEILER, Kurt, E.LIAO, Hongyu
    • C07D401/04
    • C07D401/04
    • The present invention relates to compounds having the general formula (I) or a pharmaceutically acceptable salt thereof, wherein R l 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 R 1 is additionally substituted; and R 2 is a substituted C 1 -6 balkyl. 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 HIV­1, 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.
    • 本发明涉及具有通式(I)的化合物或其药学上可接受的盐,其中R 1是含有0,1,2或3个原子的饱和或不饱和的5-,6-或7-元环 选自N,O和S,其中所述环可以与苯并稠合,并且被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,HIV1,HIV-2,HIV-3,巨细胞病毒 ),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 如上所述。