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    • 4. 发明申请
    • CONDENSED TRIAZOLES AND INDAZOLES USEFUL IN TREATING CITOKINES MEDIATED DISEASES AND OTHER DISEASES
    • 浓缩的三唑和吲哚有用的治疗介质性疾病和其他疾病
    • WO2006004702A1
    • 2006-01-12
    • PCT/US2005/022835
    • 2005-06-24
    • AMGEN INC.
    • ANDERSON, Denise, LynFROHN, Michael, J.HONG, Fang-TsaoLIU, LonginLOPEZ, Patricia
    • C07D487/04
    • C07D471/04C07D487/04
    • The present invention relates to triazolopyrimidines, imidazolopyrimidines and derivatives thereof of Formula (I), and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß 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 shack syndrome, fever, myalgias due to HIV-l, 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.
    • 本发明涉及式(I)的三唑并嘧啶,咪唑并嘧啶及其衍生物及其药学上可接受的盐。 还包括治疗炎症,类风湿性关节炎,佩吉特病,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,脓毒性休克,毒性综合症,发热,HIV-1,HIV-3,巨细胞病毒(CMV) ),流感病毒,腺病毒,哺乳动物中的疱疹病毒或带状疱疹感染,包括给予有效量的如上所述的化合物。
    • 6. 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
    • WO2006037117A1
    • 2006-04-06
    • PCT/US2005/035134
    • 2005-09-27
    • AMGEN INC.
    • ANDERSEN, Denise, LynCHANG, Catherine, M.FALSEY, James, R.FROHN, Michael, J.HONG, Fang-TsaoLIAO, HongyuLIU, LongbinLOPEZ, PatriciaRETZ, Daniel, MartinRISHTON, Gilbert, M.RZASA, Robert, M.SIEGMUND, Aaron, C.TADESSE, SeifuTAMAYO, NuriaTEGLEY, Christopher, M.
    • C07D239/48A61K31/506C07D401/12C07D401/14C07D403/12C07D403/14C07D405/14C07D409/14
    • C07D239/48C07D401/12C07D401/14C07D403/12C07D403/14C07D405/14C07D409/14
    • The present invention relates to pyridines, pyrimidines and derivatives thereof, (I) or a pharmaceutically acceptable salts thereof, wherein X 1 is N or CR 3 ; X 2 is N or CR 4 ; or -X 1 =X 2 - is -C(=O)-N(R a )- or -N(R a )-C(=O)-; X 3 is N or CR 4 ; X 4 is N or CR 4 ; X 5 is N or CR 6 ; X 6 is N or CR 6 ; wherein only 1, 2 or 3 of X 1 , X 2 , X 3 and X 4 are N; R 1 is a saturated partially 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 is substituted by 0, 1, 2 or 3 substituents. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß 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.
    • 本发明涉及吡啶,嘧啶及其衍生物,(I)或其药学上可接受的盐,其中X 1是N或CR 3; X 2是N或CR 4; 或-X 1 = X 2 - 是-C(= O)-N(R a) - 或-N(R 0) >一) - C(= O) - ; X 3是N或CR 4; X 4是N或CR 4; X 5是N或CR 6; X 6是N或CR 6; 其中X 1,X 2,X 3和X 4中仅有1,2或3是N; R 1是饱和的部分饱和或不饱和的含有0,1,2或3个选自N,O和S的原子的5-,6-或7-元环,其中环被 0,1,2或3个取代基。 还包括治疗炎症,类风湿性关节炎,佩吉特病,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,心肌梗塞,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 ),流感病毒,腺病毒,哺乳动物中的疱疹病毒或带状疱疹感染,包括给予有效量的如上所述的化合物。