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    • 7. 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
    • US20090149468A1
    • 2009-06-11
    • US12322671
    • 2009-02-04
    • Guo-Qiang CaoJian J. ChenCelia DominguezAnthony ReedKelvin K.C. ShamMaya C. ThamanDawei ZhangBradley J. Herberich
    • Guo-Qiang CaoJian J. ChenCelia DominguezAnthony ReedKelvin K.C. ShamMaya C. ThamanDawei ZhangBradley J. Herberich
    • A61K31/497C07D401/14A61K31/496
    • C07D487/06C07D213/56C07D239/95C07D401/04C07D401/14C07D417/14
    • 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 fungoides, 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.
    • 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 s,scleracielma,蕈样真菌病,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,白塞病,脓疱疮,疱疹性坏疽,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
    • 10. 发明申请
    • Heterocyclic compounds and their uses
    • 杂环化合物及其用途
    • US20090030002A1
    • 2009-01-29
    • US12079281
    • 2008-03-24
    • Yi ChenTimothy D. CushingXiaolin HaoXiao HeAndreas ReicheltRobert M. RzasaJennifer SeganishYoungsook ShinDawei Zhang
    • Yi ChenTimothy D. CushingXiaolin HaoXiao HeAndreas ReicheltRobert M. RzasaJennifer SeganishYoungsook ShinDawei Zhang
    • A61K31/498C07D473/34A61K31/52C07D471/02A61P29/00A61P19/02A61P37/02A61P35/00A61K31/519C07D487/02
    • C07D487/04C07D471/04C07D519/00
    • Substituted bicyclic heteroaryls 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 p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelodysplastic syndrome (MDS) myelo-proliferative 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.
    • 取代的双环杂芳基和含有它们的组合物,用于治疗一般炎症,关节炎,风湿性疾病,骨关节炎,炎性肠病,炎症性眼病,炎症性或不稳定性膀胱病,牛皮癣,皮肤炎症成分的投诉,慢性炎性病症 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,多发性硬化症,Sjoegren综合征和自身免疫性溶血性贫血,包括所有形式的超敏反应的过敏症状 包括但不限于白血病,例如急性骨髓性白血病(AML)骨髓增生异常综合征(MDS)骨髓增生性疾病(MPD)慢性骨髓性白血病(Myeloid Leukemi)的介导,依赖或与p110delta活性相关的癌症的方法 (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细胞淋巴瘤和实体瘤如乳腺癌。