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1. 发明申请

US20200048265A1 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
公开(公告)号：US20200048265A1
公开(公告)日：2020-02-13
申请号：US16656328
申请日：2019-10-17
申请人： AMGEN INC.
发明人： Yi CHEN , Timothy D. CUSHING , Jason A. DUQUETTE , Felix GONZALEZ LOPEZ DE TURISO , Xiaolin HAO , Xiao HE , Brian S. LUCAS , Lawrence R. MCGEE , Andreas REICHELT , Robert M. RZASA , Jennifer L. SEGANISH , Youngsook SHIN , Dawei ZHANG
IPC分类号： C07D487/04 , C07D473/30 , C07D473/34 , C07D471/04
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 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.

2. 发明申请

US20180105532A1 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
公开(公告)号：US20180105532A1
公开(公告)日：2018-04-19
申请号：US15841153
申请日：2017-12-13
申请人： AMGEN INC.
发明人： Yi CHEN , Timothy D. CUSHING , Jason A. DUQUETTE , Felix GONZALEZ LOPEZ DE TURISO , Xiaolin HAO , Xiao HE , Brian S. LUCAS , Lawrence R. MCGEE , Andreas REICHELT , Robert M. RZASA , Jennifer L. SEGANISH , Youngsook SHIN , Dawei ZHANG
IPC分类号： C07D487/04 , C07D471/04 , C07D473/30 , C07D473/34
CPC分类号： C07D487/04 , C07D471/04 , C07D473/30 , 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 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. 发明申请

US20230052348A1 COMPOUNDS THAT INHIBIT MCL-1 PROTEIN 有权
公开(公告)号：US20230052348A1
公开(公告)日：2023-02-16
申请号：US17501075
申请日：2021-10-14
申请人： AMGEN INC.
发明人： Sean P BROWN , David Karl BEDKE , Michael R. DEGRAFFENREID , Jiasheng FU , Zhinghong LI , Felix GONZALEZ LOPEZ DE TURISO , Ana GONZALEZ BUENROSTRO , Michael W. GRIBBLE JR. , Michael G. JOHNSON , Todd J. KOHN , Kexue LI , Yunxiao LI , Mike Elias LIZARZABURU , Yosup REW , Joshua TAYGERLY , Yingcai WANG , Xuelei YAN , Ming YU , Jiang ZHU , Manuel ZANCANELLA , Xian Yun JIAO , Liusheng ZHU , Xianghong WANG , Julio C. MEDINA , Jason A. DUQUETTE , Jonathan B. HOUZE , Marc VIMOLRATANA , Mario G. CARDOZO , Alan C. CHENG
IPC分类号： C07D513/10 , C07D513/20 , C07D515/10
摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

4. 发明申请

US20150045361A1 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
标题翻译：杂环化合物及其用途
公开(公告)号：US20150045361A1
公开(公告)日：2015-02-12
申请号：US14520899
申请日：2014-10-22
申请人： AMGEN INC.
发明人： Yi CHEN , Timothy D. CUSHING , Jason A. DUQUETTE , Felix GONZALEZ LOPEZ DE TURISO , Xiaolin HAO , Xiao HE , Brian S. LUCAS , Lawrence R. MCGEE , Andreas REICHELT , Robert M. RZASA , Jennifer L. SEGANISH , Youngsook SHIN , Dawei ZHANG
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04 , C07D473/30 , 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 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.
摘要翻译：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）骨髓增生性疾病（MPD）慢性骨髓性白血病（MPD），介导，依赖或与p110δ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。

5. 发明申请

US20220281850A1 BISAMIDE SARCOMERE ACTIVATING COMPOUNDS AND USES THEREOF 有权
公开(公告)号：US20220281850A1
公开(公告)日：2022-09-08
申请号：US17672594
申请日：2022-02-15
申请人： Amgen Inc. , Cytokinetics, Inc.
发明人： Luke ASHCRAFT , Alessandro BOEZIO , John BUTLER , Aroop CHANDRA , Chihyuan CHUANG , Scott E. COLLIBEE , Mikkel DEBENEDETTO , Vincent DIMASSA , Russell GRACEFFA , Justin MALINOWSKI , David MOEBIUS , Bradley P. MORGAN , Joshua PAYETTE , Antonio ROMERO , David ST. JEAN, JR. , Richard VARGAS , John YEOMAN , Hanmo ZHANG , Alan CHENG , Felix GONZALEZ LOPEZ DE TURISO , Michael Garrett JOHNSON
IPC分类号： C07D403/12 , C07D401/14 , C07D401/12 , A61P9/00 , C07D413/14 , C07D207/16 , C07D209/52 , C07D405/12 , C07D417/14 , C07D401/06 , C07D403/14 , C07D209/02 , C07D413/12
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

6. 发明申请

US20160333017A1 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
公开(公告)号：US20160333017A1
公开(公告)日：2016-11-17
申请号：US15219624
申请日：2016-07-26
申请人： Amgen Inc.
发明人： 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分类号： C07D487/04 , C07D401/12 , C07D471/04 , C07D473/34 , C07D401/14
CPC分类号： C07D487/04 , C07D401/12 , C07D401/14 , C07D471/04 , 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 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.

7. 发明申请

US20180354918A1 CIS-MORPHOLINONE AND OTHER COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：US20180354918A1
公开(公告)日：2018-12-13
申请号：US16048677
申请日：2018-07-30
申请人： AMGEN INC.
发明人： Michael D. BARTBERGER , Hilary Plake BECK , Michael R. DEGRAFFENREID , Brian M. FOX , Felix GONZALEZ LOPEZ DE TURISO , Lisa D. JULIAN , Frank KAYSER , Julio C. MEDINA , Steven H. OLSON , Yosup REW , Philip M. ROVETO , Daqing SUN , Xuelei YAN
IPC分类号： C07D265/32 , C07D413/06 , C07D413/04 , C07D279/12 , C07D487/04
CPC分类号： C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D487/04
摘要： The present invention provides MDM2 inhibitor compounds of Formula I, 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.

8. 发明申请

US20160002185A1 CIS-MORPHOLINONE AND OTHER COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译： CIS-MORPHOLINONE和其他化合物作为MDM2抑制剂治疗癌症
公开(公告)号：US20160002185A1
公开(公告)日：2016-01-07
申请号：US14768529
申请日：2014-02-18
申请人： AMGEN INC.
发明人： Michael D. BARTBERGER , Hilary Plake BECK , Michael R. DEGRAFFENREID , Brian M. FOX , Felix GONZALEZ LOPEZ DE TURISO , Lisa D. JULIAN , Frank KAYSER , Julio C. MEDINA , Steven H. OLSON , Yosup REW , Philip M. ROVETO , Daqing SUN , Xuelei YAN
IPC分类号： C07D265/32 , C07D413/04 , C07D413/06 , C07D487/04 , C07D279/12
CPC分类号： C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D487/04
摘要： The present invention provides MDM2 inhibitor compounds of Formula (I), 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.
摘要翻译：本发明提供式（I）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。

9. 发明申请

US20170144971A1 Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer 审中-公开
公开(公告)号：US20170144971A1
公开(公告)日：2017-05-25
申请号：US15412804
申请日：2017-01-23
申请人： AMGEN INC.
发明人： 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分类号： 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分类号： 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
摘要： 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.

10. 发明申请

US20160137667A1 Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer 审中-公开
标题翻译：哌啶酮衍生物作为治疗癌症的MDM2抑制剂
公开(公告)号：US20160137667A1
公开(公告)日：2016-05-19
申请号：US15008342
申请日：2016-01-27
申请人： AMGEN INC.
发明人： 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分类号： C07D498/14 , C07D221/20 , C07D471/10
CPC分类号： 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
摘要： 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.
摘要翻译：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。

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