公开(公告)号：US20160333017A1

公开(公告)日：2016-11-17

申请号：US15219624

申请日：2016-07-26

Applicant: Amgen Inc.

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

IPC: C07D487/04 ,  C07D401/12 ,  C07D471/04 ,  C07D473/34 ,  C07D401/14

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 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.

公开(公告)号：US20170144971A1

公开(公告)日：2017-05-25

申请号：US15412804

申请日：2017-01-23

Applicant: AMGEN INC.

Inventor： Michael D. BARTBERGER ,  Ana GONZALEZ BUENROSTRO ,  Hilary Plake BECK ,  Xiaoqi CHEN ,  Richard Victor CONNORS ,  Jeffrey DEIGNAN ,  Jason A. DUQUETTE ,  John EKSTEROWICZ ,  Benjamin FISHER ,  Brian M. FOX ,  Jiasheng FU ,  Zice FU ,  Felix GONZALEZ LOPEZ DE TURISO ,  Michael W. GRIBBLE, Jr. ,  Darin J. GUSTIN ,  Julie A. HEATH ,  Xin HUANG ,  XianYun JIAO ,  Michael G. JOHNSON ,  Frank KAYSER ,  David John KOPECKY ,  SuJen LAI ,  Yihong LI ,  Zhihong LI ,  Jiwen LIU ,  Jonathan D. LOW ,  Brian S. LUCAS ,  Zhihua MA ,  Lawrence R. MCGEE ,  Joel MCINTOSH ,  Dustin L. MCMINN ,  Julio C. MEDINA ,  Jeffrey Thomas MIHALIC ,  Steven H. OLSON ,  Yosup REW ,  Phillip M. ROVETO ,  Daqing SUN ,  Xiaodong WANG ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU

IPC: C07D211/76 ,  C07D417/12 ,  C07D413/06 ,  C07D471/10 ,  C07D409/04 ,  C07D417/06 ,  C07D405/04 ,  C07D401/04 ,  C07D279/02 ,  C07D401/12 ,  C07D491/08 ,  C07D498/08 ,  C07D409/12 ,  C07D405/12 ,  C07D417/14 ,  C07D498/20 ,  C07D401/06

CPC classification number: C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, 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.

公开(公告)号：US20160137667A1

公开(公告)日：2016-05-19

申请号：US15008342

申请日：2016-01-27

Applicant: AMGEN INC.

Inventor： Michael D. BARTBERGER ,  Ana GONZALEZ BUENROSTRO ,  Hilary Plake BECK ,  Xiaoqi CHEN ,  Richard Victor CONNORS ,  Jeffrey DEIGNAN ,  Jason A. DUQUETTE ,  John EKSTEROWICZ ,  Benjamin FISHER ,  Brian M. FOX ,  Jiasheng FU ,  Zice FU ,  Felix GONZALEZ LOPEZ DE TURISO ,  Michael W. GRIBBLE, JR. ,  Darin J. GUSTIN ,  Julie A. HEATH ,  Xin HUANG ,  XianYun JIAO ,  Michael G. JOHNSON ,  Frank KAYSER ,  David John KOPECKY ,  SuJen LAI ,  Yihong LI ,  Zhihong LI ,  Jiwen LIU ,  Jonathan D. LOW ,  Brian S. LUCAS ,  Zhihua MA ,  Lawrence R. MCGEE ,  Joel MCINTOSH ,  Dustin L. MCMINN ,  Julio C. MEDINA ,  Jeffrey Thomas MIHALIC ,  Steven H. OLSON ,  Yosup REW ,  Phillip M. ROVETO ,  Daqing SUN ,  Xiaodong WANG ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU

IPC: C07D498/14 ,  C07D221/20 ,  C07D471/10

CPC classification number: C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, 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: 本发明提供了式I的MDM2抑制剂化合物，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：US20140350244A1

公开(公告)日：2014-11-27

申请号：US14453842

申请日：2014-08-07

Applicant: AMGEN INC.

Inventor： Richard V. Connors ,  Kang DAI ,  John EKSTEROWICZ ,  Pingchen FAN ,  Benjamin FISHER ,  Jiasheng FU ,  Kexue LI ,  Zhihong LI ,  Lawrence R. MCGEE ,  Rajiv SHARMA ,  Xiaodong WANG ,  Dustin L. MCMINN ,  Jeffrey T. MIHALIC ,  Jeffrey DEIGNAN

IPC: C07D471/14 ,  C07D498/10 ,  C07D491/107 ,  C07D471/04 ,  C07D487/14

CPC classification number: C07D471/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D491/107 ,  C07D491/147 ,  C07D498/04 ,  C07D498/10 ,  C07D513/14

Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.

Abstract translation: 提供了可用于治疗CDK4介导的疾病如癌症的化合物，药物组合物和方法。 本发明化合物是吡啶，吡嗪酰亚胺和三嗪衍生物。