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    SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
    3.
    发明申请
    SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
    取代的杂环化合物及其使用方法

    公开(公告)号：WO2005021551A1

    公开(公告)日：2005-03-10

    申请号：PCT/US2004/029246

    申请日：2004-08-23

    Applicant: AMGEN INC. ,  NUNES, Joseph J. ,  ZHU, Xiaotian ,  ERMANN, Monika ,  GHIRON, Chiara ,  JOHNSTON, David N. ,  SALUSTE, Carl-Gustaf Pierre

    Inventor： NUNES, Joseph J. ,  ZHU, Xiaotian ,  ERMANN, Monika ,  GHIRON, Chiara ,  JOHNSTON, David N. ,  SALUSTE, Carl-Gustaf Pierre

    IPC: C07D487/14

    CPC classification number: C07D487/14

    Abstract: The present invention relates to tetracyclic pyrimidines or pyridines or pharmaceutically-acceptable salts or derivatives thereof. Also included are methods of use of the tetracyclic pyrimidines or pyridines including use related to treating inflammation, inhibiting T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease and many other related disorders in a subject, the methods comprising administering a therapeutically-effective amount a compound as described above to the subject.

    Abstract translation: 本发明涉及四环嘧啶或吡啶或其药学上可接受的盐或衍生物。 还包括使用四环嘧啶或吡啶的方法，包括与治疗炎症有关的用途，抑制T细胞活化和增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗死，中风，多发性硬化，炎性肠病等许多方法 所述方法包括向受试者施用治疗有效量的如上所述的化合物。

    CRYSTAL OF A LYMPHOCYTE KINASE-LIGAND COMPLEX AND METHODS OF USE
    5.
    发明申请
    CRYSTAL OF A LYMPHOCYTE KINASE-LIGAND COMPLEX AND METHODS OF USE 审中-公开
    LYMPHOCYTE KINASE-LIGAND复合物的晶体和使用方法

    公开(公告)号：WO2000070030A1

    公开(公告)日：2000-11-23

    申请号：PCT/US2000/013881

    申请日：2000-05-19

    Applicant: AMGEN INC. ,  ZHU, Xiaotian

    Inventor： ZHU, Xiaotian

    IPC: C12N9/12

    CPC classification number: C12N9/1205 ,  Y02A90/26

    Abstract: The invention relates to the three-dimensional structure of a crystal of a kinase enzyme complexed with a ligand. The three-dimensional structure of a protein kinase-ligand complex is disclosed. The invention also relates to methods of preparing such crystals. Kinase-ligand crystal structures wherein the ligand is an inhibitor molecule are useful for providing structure information that may be integrated into drug screening and drug design processes. Thus, the invention also relates to methods of using the crystal structure of kinase enzyme-ligand complexes for identifying, designing, selecting, or testing inhibitors of kinase enzymes, such inhibitors being useful as therapeutics for the treatment or modulation of (i) diseases; (ii) disease symptoms; or (iii) the effect of other physiological events mediated by kinases; having one or more kinase enzymes involved in their pathology.

    Abstract translation: 本发明涉及与配体络合的激酶的晶体的三维结构。 公开了蛋白激酶 - 配体复合物的三维结构。 本发明还涉及制备这种晶体的方法。 其中配体是抑制剂分子的激酶配体晶体结构可用于提供可以整合到药物筛选和药物设计过程中的结构信息。 因此，本发明还涉及使用激酶 - 配体配合物的晶体结构鉴定，设计，选择或测试激酶的抑制剂的方法，所述抑制剂可用作治疗或调节（i）疾病的治疗剂; （ii）疾病症状; 或（iii）由激酶介导的其他生理事件的作用; 具有参与其病理学的一种或多种激酶。

    2-AMINO-4-HYDROXY-5-PYRIMIDINECARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF T CELL ACTIVATION FOR THE TREATMENT OF INFLAMMATORY DISEASES
    6.
    发明申请
    2-AMINO-4-HYDROXY-5-PYRIMIDINECARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF T CELL ACTIVATION FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
    2-氨基-4-羟基-5-嘧啶甲酰胺衍生物及相关化合物作为T细胞活化的抑制剂治疗炎症性疾病

    公开(公告)号：WO2005009443A1

    公开(公告)日：2005-02-03

    申请号：PCT/US2004/020243

    申请日：2004-06-24

    Applicant: AMGEN INC. ,  NUNES, Joseph J. ,  ZHU, Xiaotian ,  AMOUZEGH, Patricia ,  GHIRON, Chiara ,  JOHNSTON, David N. ,  POWER, Eoin, Christopher

    Inventor： NUNES, Joseph J. ,  ZHU, Xiaotian ,  AMOUZEGH, Patricia ,  GHIRON, Chiara ,  JOHNSTON, David N. ,  POWER, Eoin, Christopher

    IPC: A61K31/506

    CPC classification number: C07D213/82 ,  C07D239/47 ,  C07D239/48

    Abstract: The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.

    Abstract translation: 本发明涉及嘧啶或吡啶甲酰胺或其药学上可接受的盐。 还包括治疗炎症，抑制T细胞活化和增殖，关节炎，类风湿性关节炎，银屑病关节炎，骨关节炎，器官移植，急性移植或异种移植或同种移植物排斥，移植耐受性诱导，缺血或再灌注损伤，心肌梗死的方法 ，中风，多发性硬化，炎症性肠病，包括溃疡性结肠炎，克罗恩病，狼疮，接触性超敏反应，迟发型超敏反应和麸质敏感性肠病，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 ，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，自身免疫性低位症，吉兰巴利综合征，肾小球性肾炎，血清病，荨麻疹，过敏性疾病，哮喘，高粱，过敏性鼻炎，巩膜瘤，蕈样真菌病，皮肌炎，秃头症 ，慢性交感 包括给予治疗有效量的如上所述的化合物，包括给予治疗有效量的上述化合物，其中，所述治疗有效量的治疗有效量的药物组合物包含给药治疗有效量的化合物。

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