专利检索 ap:("Amgen Inc.") AND inv:"Lawrence R. McGee" 第 1 页

1.

发明公开
Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer 审中-公开

公开(公告)号：US20240300892A1

公开(公告)日：2024-09-12

申请号：US18484675

申请日：2023-10-11

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, I , John Eksterowicz , Benjamin Fisher , Brian M. Fox , Jiasheng Fu , Zice Fu , Felix Gonzalez Lopez De Turiso , Michael W. Gribble , 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 , Yossup Rew , Philip M. Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu

IPC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

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.

2.

发明授权
Methods for preparing triazole agonists of the APJ receptor 有权

公开(公告)号：US09751864B2

公开(公告)日：2017-09-05

申请号：US15298434

申请日：2016-10-20

申请人： AMGEN INC.

发明人： Ning Chen , Xiaoqi Chen , Richard V. Connors , Jeffrey Deignan , Paul John Dransfield , Xiaohui Du , Zice Fu , Julie Anne Heath , Daniel B. Horne , Jonathan Houze , Matthew R. Kaller , David John Kopecky , Su-Jen Lai , Zhihua Ma , Lawrence R. McGee , Julio C. Medina , Jeffrey T. Mihalic , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Xiaodong Wang , Kevin Yang , Mikkel V. DeBenedetto , Robert P. Farrell , Simon J. Hedley , Ted C. Judd

IPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , C07D413/14 , C07D413/04 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D241/12 , C07D241/24 , C07D249/08 , C07D405/14 , C07D401/12 , A61K31/695 , C07F7/08 , A61K31/437 , C07C311/13 , C07D213/61 , C07D239/34 , C07D241/18 , C07D295/16

CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08

摘要： Methods of preparing compounds of Formula VI, salts thereof, tautomers thereof, or salts of the tautomers include cyclizing compounds of Formula V, salts thereof, tautomers thereof, or salts of the tautomers. Compounds of Formula VI and Formula V have the following structures: where the definitions of the variables are provided herein.

3.

发明申请
Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer 有权

公开(公告)号：US20210179560A1

公开(公告)日：2021-06-17

申请号：US16983027

申请日：2020-08-03

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, I , John Eksterowicz , Benjamin Fisher , Brian M. Fox , Jiasheng Fu , Zice Fu , Felix Gonzalez Lopez De Turiso , Michael W. Gribble , 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 , Yossup Rew , Philip M. Roveto , Daqing Sun , Xiaodong Wang , Yingcai Wang , Xuelei Yan , Ming Yu , Jiang Zhu

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

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.

4.

发明授权
Processes of making and crystalline forms of a MDM2 inhibitor 有权

公开(公告)号：US09801867B2

公开(公告)日：2017-10-31

申请号：US15175824

申请日：2016-06-07

申请人： AMGEN INC.

发明人： Matthew Bio , Sebastien Caille , Brian Cochran , Yuanqing Fang , Brian M. Fox , Brian S. Lucas , Lawrence R. McGee , Filisaty Vounatsos , Sean H. Wiedemann , Sarah Wortman

IPC分类号： C07D211/76 , A61K31/451 , C07D211/94 , C07D491/048 , C07C309/25 , C07C309/04 , C07C313/02 , C07D498/04 , C07C309/35

CPC分类号： A61K31/451 , C07B2200/13 , C07C309/04 , C07C309/25 , C07C309/35 , C07C313/02 , C07D211/76 , C07D211/94 , C07D491/048 , C07D498/04

摘要： The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

5.

发明授权
Intermediates for preparing triazole agonists of the APJ receptor 有权

公开(公告)号：US09656998B2

公开(公告)日：2017-05-23

申请号：US15298686

申请日：2016-10-20

申请人： AMGEN INC.

发明人： Ning Chen , Xiaoqi Chen , Richard V. Connors , Jeffrey Deignan , Paul John Dransfield , Xiaohui Du , Zice Fu , Julie Anne Heath , Daniel B. Horne , Jonathan Houze , Matthew R. Kaller , David John Kopecky , Su-Jen Lai , Zhihua Ma , Lawrence R. McGee , Julio C. Medina , Jeffrey T. Mihalic , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Xiaodong Wang , Kevin Yang , Mikkel V. Debenedetto , Robert P. Farrell , Simon J. Hedley , Ted C. Judd

IPC分类号： C07D213/82 , C07D241/24 , C07D401/12 , C07D401/14 , C07D401/04 , C07D413/04 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D239/26 , C07D239/30 , C07D241/12 , C07D249/08 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , A61K31/695

CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08

摘要： Compounds of Formula V, salts thereof, tautomers thereof, and salts of the tautomers are useful intermediates in the synthesis of agonists of the APJ Receptor. Compounds of Formula V have the following structure: where the definitions of the variables are provided herein.

6.

发明授权
Processes of making and crystalline forms of a MDM2 inhibitor 有权

公开(公告)号：US09623018B2

公开(公告)日：2017-04-18

申请号：US15175805

申请日：2016-06-07

申请人： AMGEN INC.

发明人： Matthew Bio , Sebastien Caille , Yuanqing Fang , Brian M. Fox , Brian S. Lucas , Lawrence R. McGee , Sean H. Wiedemann

IPC分类号： C07D498/04 , A61K31/451 , C07D211/94 , C07D491/048 , C07C309/25 , C07C309/04 , C07D211/76 , C07C309/35

CPC分类号： A61K31/451 , C07B2200/13 , C07C309/04 , C07C309/25 , C07C309/35 , C07C313/02 , C07D211/76 , C07D211/94 , C07D491/048 , C07D498/04

摘要： The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

7.

发明申请
FUSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3 审中-公开
标题翻译： CDK 4/6和FLT3的熔融TRICYCLIC双重抑制剂

公开(公告)号：US20140163052A1

公开(公告)日：2014-06-12

申请号：US14088796

申请日：2013-11-25

申请人： AMGEN INC.

发明人： Xiaoqi Chen , Kang Dai , Jason Duquette , Michael W. Gribble, JR. , Justin N. Huard , Kathleen S. Keegan , Zhihong Li , Sarah E. Lively , Lawrence R. McGee , Mark L. Ragains , Xianghong Wang , Margaret F. Weidner , Jian Zhang

IPC分类号： C07D471/14

CPC分类号： C07D519/00 , C07D471/14

摘要： Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.

摘要翻译： 式I化合物是CDK 4，CDK 6和FLT 3的有用抑制剂。这些化合物可用于治疗癌症和各种其他疾病状况。式I的化合物具有以下结构：其中R1是式IA，式IB，式IC或式ID的基团，并且本文提供了其它变量的定义。

8.

发明授权
Triazole agonists of the APJ receptor 有权

公开(公告)号：US10221162B2

公开(公告)日：2019-03-05

申请号：US16033632

申请日：2018-07-12

申请人： AMGEN INC.

发明人： Ning Chen , Xiaoqi Chen , Yinhong Chen , Alan C. Cheng , Richard V. Connors , Jeffrey Deignan , Paul John Dransfield , Xiaohui Du , Zice Fu , Julie Anne Heath , Daniel B. Horne , Jonathan Houze , Matthew R. Kaller , Aarif Yusuf Khakoo , David John Kopecky , Su-Jen Lai , Zhihua Ma , Lawrence R. McGee , Julio C. Medina , Jeffrey T. Mihalic , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Gayathri Swaminath , Xiaodong Wang , Kevin Yang , Wen-Chen Yeh , Mikkel V. Debenedetto , Robert P. Farrell , Simon J. Hedley , Ted C. Judd , Frank Kayser

IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D417/14 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D241/12 , C07D241/24 , C07D249/08 , C07D471/04 , C07D413/14 , C07D413/04 , C07D401/04 , C07D213/61 , C07D239/34 , C07D241/18 , C07F7/08 , C07D295/16 , C07C311/13 , A61K31/695 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/437

摘要： Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

9.

发明授权
Heterocyclic compounds and their uses 有权

公开(公告)号：US09873701B2

公开(公告)日：2018-01-23

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 , C07D473/30 , C07D473/34 , 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.