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    5 -CYANO-4, 6 -DIAMINOPYRIMIDINE OR 6 -AMINOPURINE DERIVATIVES AS PI3K- DELTA INHIBITORS
    1.
    发明公开
    5 -CYANO-4, 6 -DIAMINOPYRIMIDINE OR 6 -AMINOPURINE DERIVATIVES AS PI3K- DELTA INHIBITORS 审中-公开
    作为PI3K-三角洲抑制剂的5-氰基-4,6-二氨基嘧啶或6-氨基嘌呤衍生物

    公开(公告)号：EP2635565A1

    公开(公告)日：2013-09-11

    申请号：EP11785857.1

    申请日：2011-11-04

    申请人： Amgen Inc.

    发明人： FISHER, Benjamin ,  JOHNSON, Michael G. ,  LUCAS, Brian ,  SHIN, Youngsook ,  KAIZERMAN, Jacob

    IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D473/34 ,  C07D239/48 ,  C07D403/12 ,  A61K31/506 ,  A61K31/52 ,  A61K31/505 ,  A61P29/00 ,  A61P19/02 ,  A61P35/00 ,  A61P37/00

    CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D473/34

    摘要： 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 pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic 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.

    摘要翻译： 取代的双环杂芳基及其组合物，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，炎性或不稳定性膀胱病，牛皮癣，具有炎性成分的皮肤病，慢性炎症，包括但不限于 不限于系统性红斑狼疮（SLE），重症肌炎，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，舍约格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性病症等自身免疫性疾病。 本发明还使得能够治疗依赖于或与p1105活性相关的癌症的方法，所述癌症包括但不限于白血病，例如急性髓细胞性白血病（AML）骨髓增生异常综合征（MDS）骨髓增生性疾病（MPD） ）慢性粒细胞白血病（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细胞淋巴瘤和实体瘤，如乳腺癌。

    3- SUBSTITUTED QUINOLINE OR QUINOXALINE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE (PI3K) INHIBITORS
    4.
    发明授权
    3- SUBSTITUTED QUINOLINE OR QUINOXALINE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE (PI3K) INHIBITORS 有权
    3-取代的喹啉或喹喔啉衍生物及其作为磷脂酰肌醇3-激酶（PI3K）抑制剂的

    公开(公告)号：EP2139882B1

    公开(公告)日：2013-12-25

    申请号：EP08742273.9

    申请日：2008-03-24

    申请人： Amgen Inc.

    发明人： CHEN, Yi ,  CUSHING, Timothy D. ,  HAO, Xiaolin ,  HE, Xiao ,  REICHELT, Andreas ,  RZASA, Robert M. ,  SEGANISH, Jennifer ,  SHIN, Youngsook ,  ZHANG, Dawei

    IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/4709 ,  A61K31/506

    CPC分类号： C07D401/12 ,  C07D401/14

    摘要： Substituted bicyclic heteroaryls having the general formula 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) Myelo-dysplastic 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.

    3- SUBSTITUTED QUINOLINE OR QUINOXALINE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE ( PI3K) INHIBITORS
    5.
    发明公开
    3- SUBSTITUTED QUINOLINE OR QUINOXALINE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE ( PI3K) INHIBITORS 有权
    3-取代的喹啉或喹喔啉衍生物及其作为磷脂酰肌醇3-激酶（PI3K）抑制剂的

    公开(公告)号：EP2139882A1

    公开(公告)日：2010-01-06

    申请号：EP08742273.9

    申请日：2008-03-24

    申请人： Amgen Inc.

    发明人： CHEN, Yi ,  CUSHING, Timothy D. ,  HAO, Xiaolin ,  HE, Xiao ,  REICHELT, Andreas ,  RZASA, Robert M. ,  SEGANISH, Jennifer ,  SHIN, Youngsook ,  ZHANG, Dawei

    IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/4709 ,  A61K31/506

    CPC分类号： C07D401/12 ,  C07D401/14

    摘要： Substituted bicyclic heteroaryls having the structure: (I) or any pharmaceutically-acceptable salt thereof, wherein: X1 is C(R9) or N; X2 is C(R10) or N; Y is N(R11), O or S; which are useful to inhibit the biological activity of human PI3Kδ 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) Myelo- dysplastic syndrome (MDS) myeloproliferative 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.

    QUINOLINE DERIVATIVES AS PIK3 INHIBITORS
    8.
    发明公开
    QUINOLINE DERIVATIVES AS PIK3 INHIBITORS 审中-公开
    ALS CHINOLINDERIVATE PIK3，缝边

    公开(公告)号：EP2640715A1

    公开(公告)日：2013-09-25

    申请号：EP11791704.7

    申请日：2011-11-17

    申请人： Amgen Inc.

    发明人： CUSHING, Timothy D. ,  LOHMAN, Julia Winslow ,  SHIN, Youngsook

    IPC分类号： C07D401/14 ,  C07D413/14 ,  A61K31/506 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

    CPC分类号： A61K31/506 ,  C07D239/42 ,  C07D401/14 ,  C07D413/14

    摘要： 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.

    HETEROCYCLIC COMPOUNDS AND THEIR USES
    9.
    发明公开
    HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
    杂环化合物和它们作为PI3K抑制剂

    公开(公告)号：EP2552908A2

    公开(公告)日：2013-02-06

    申请号：EP11713167.2

    申请日：2011-04-01

    申请人： Amgen Inc.

    发明人： CUSHING, Timothy, D. ,  DUQUETTE, Jason, A. ,  HE, Xiao ,  LOHMAN, Julia, Winslow ,  SHIN, Youngsook

    IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D409/12 ,  C07D473/34 ,  C07D487/04 ,  A61K31/506 ,  A61P29/00

    CPC分类号： C07D403/12 ,  C07D401/14 ,  C07D409/12 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04

    摘要： 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 p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic 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.