公开(公告)号：WO2010151740A2

公开(公告)日：2010-12-29

申请号：PCT/US2010/039942

申请日：2010-06-25

Applicant: AMGEN INC.

Inventor： BUI, Minna Hue Thanh ,  CHEN, Yi ,  CUSHING, Timothy D. ,  DUQUETTE, Jason A. ,  FISHER, Benjamin ,  GONZALEZ LOPEZ DE TURISO, Felix ,  HAO, Xiaolin ,  HE, Xiao ,  JOHNSON, Michael G. ,  LUCAS, Brian

IPC: C07D401/12

CPC classification number: C07D487/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D473/34

Abstract: 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.

Abstract translation: 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，具有炎症的皮肤病 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，过敏性病症包括所有 本发明还使得能够治疗依赖于或与p110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）慢性骨髓炎 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。

公开(公告)号：WO2008118468A1

公开(公告)日：2008-10-02

申请号：PCT/US2008/003962

申请日：2008-03-24

Applicant: AMGEN INC.

Inventor： CHEN, Yi ,  CUSHING, Timothy D. ,  DUQUETTE, Jason A. ,  GONZALEZ LOPEZ DE TURISO, Felix ,  HAO, Xiaolin ,  HE, Xiao ,  LUCAS, Brian ,  MCGEE, Lawrence R. ,  REICHELT, Andreas ,  RZASA, Robert M. ,  SEGANISH, Jennifer ,  SHIN, Youngsook ,  ZHANG, Dawei

IPC: C07D473/30 ,  C07D473/34 ,  C07D487/04 ,  A61K31/519 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D473/30 ,  C07D473/34

Abstract: 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.

Abstract translation: 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。 本发明还能够治疗与p110活性介导，依赖或相关的癌症的方法，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（myelo-dysplastic syndrome，MDS），骨髓增殖性疾病 （MPD），慢性骨髓性白血病（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。

公开(公告)号：WO2013049250A1

公开(公告)日：2013-04-04

申请号：PCT/US2012/057389

申请日：2012-09-26

Applicant: AMGEN INC. ,  BARTBERGER, Michael D. ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DUQUETTE, Jason A. ,  EKSTEROWICZ, John ,  FOX, Brian M. ,  FU, Jiasheng ,  GONZALEZ BUENROSTRO, Ana ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GUSTIN, Darin J. ,  HEATH, Julie A. ,  JOHNSON, Michael G. ,  KAYSER, Frank ,  KOPECKY, David J. ,  LI, Yihong ,  LI, Zhihong ,  MA, Zhihua ,  MCINTOSH, Joel ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  REW, Yosup ,  ROVETO, Philip M. ,  SCHMITT, Michael J. ,  SUN, Daqing ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  WEATHERS, Christine ,  YAN, Xuelei

Inventor： BARTBERGER, Michael D. ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DUQUETTE, Jason A. ,  EKSTEROWICZ, John ,  FOX, Brian M. ,  FU, Jiasheng ,  GONZALEZ BUENROSTRO, Ana ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GUSTIN, Darin J. ,  HEATH, Julie A. ,  JOHNSON, Michael G. ,  KAYSER, Frank ,  KOPECKY, David J. ,  LI, Yihong ,  LI, Zhihong ,  MA, Zhihua ,  MCINTOSH, Joel ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  REW, Yosup ,  ROVETO, Philip M. ,  SCHMITT, Michael J. ,  SUN, Daqing ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  WEATHERS, Christine ,  YAN, Xuelei

IPC: C07D265/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D413/12

CPC classification number: C07D413/04 ,  C07D265/06 ,  C07D265/32 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract translation: 本发明提供式I或II的MDM2抑制剂化合物或其药学上可接受的盐，其中变量如上所定义，哪些化合物可用作治疗剂，特别是用于治疗癌症。 本发明还涉及含有MDM2抑制剂的药物组合物。

公开(公告)号：WO2012003271A1

公开(公告)日：2012-01-05

申请号：PCT/US2011/042519

申请日：2011-06-30

Applicant: AMGEN INC. ,  DUQUETTE, Jason A. ,  LUCAS, Brian

Inventor： DUQUETTE, Jason A. ,  LUCAS, Brian

IPC: C07D401/12 ,  C07D487/04 ,  A61P29/00 ,  A61P35/00 ,  A61K31/4709

CPC classification number: C07D473/34 ,  C07D401/12 ,  C07D401/14 ,  C07D487/04

Abstract: 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) 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.

Abstract translation: 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，如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增殖性疾病（MPD）慢性骨髓性白血病（MPD）慢性骨髓性白血病 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。