[EN] QUINOLINE DERIVATIVES AS PIK3 INHIBITORS<br/>[FR] DÉRIVÉS DE QUINOLÉINE EN TANT QU'INHIBITEURS DE PI3K
申请人:AMGEN INC
公开号:WO2012068343A1
公开(公告)日:2012-05-24
Substituted bicyclic heteroaryls having the general formula (I) and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p1 108 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML), Myelodysplastic syndrome (MDS), myeio-proiiferative diseases (MPD), Chronic Myeloid Leukemia (CML), T-cell Acute Lymphoblastic leukaemia (T-ALL), B-cell Acute Lymphoblastic leukaemia (B-ALL), Non Hodgkins Lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer.
具有通用公式(I)的取代的双环杂环芳基化合物及含有它们的组合物,用于治疗一般性炎症、关节炎、风湿性疾病、骨关节炎、炎症性肠道疾病、炎症性眼部疾病、炎症性或不稳定的膀胱疾病、牛皮癣、伴有炎症成分的皮肤问题、慢性炎症性疾病,包括但不限于自身免疫性疾病如系统性红斑狼疮(SLE)、重症肌无力、类风湿性关节炎、急性播散性脑脊髓炎、特发性血小板减少性紫癜、多发性硬化、干燥综合征和自身免疫性溶血性贫血,包括所有形式的过敏症状。本发明还提供了治疗通过或与p1108活性介导、依赖或相关联的癌症的方法,包括但不限于白血病,如急性髓系白血病(AML)、骨髓增生异常综合征(MDS)、骨髓增殖性疾病(MPD)、慢性髓系白血病(CML)、T细胞急性淋巴细胞白血病(T-ALL)、B细胞急性淋巴细胞白血病(B-ALL)、非霍奇金淋巴瘤(NHL)、B细胞淋巴瘤和固体肿瘤,如乳腺癌。