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公开(公告)号：US20240254100A1
公开(公告)日：2024-08-01
申请号：US17632333
申请日：2020-08-03
Applicant: AMGEN INC.
Inventor： Nuria A. TAMAYO , Matthew Richard KALLER , Thomas T. NGUYEN , Nobuko NISHIMURA , Qiufen May XUE , John Gordon ALLEN
IPC: C07D401/04 , A61K31/497 , A61K31/5377 , A61K31/541 , C07D241/20 , C07D417/14
CPC classification number: C07D401/04 , A61K31/497 , A61K31/5377 , A61K31/541 , C07D241/20 , C07D417/14
Abstract: Compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
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公开(公告)号：US20200055845A1
公开(公告)日：2020-02-20
申请号：US16661907
申请日：2019-10-23
Applicant: Amgen Inc.
Inventor： Brian Alan LANMAN , Jian CHEN , Anthony B. REED , Victor J. CEE , Longbin LIU , David John KOPECKY , Patricia LOPEZ , Ryan Paul WURZ , Thomas T. NGUYEN , Shon BOOKER , Nobuko NISHIMURA , Youngsook SHIN , Nuria A. TAMAYO , John Gordon ALLEN , Jennifer Rebecca ALLEN
IPC: C07D417/04 , C07D475/00 , C07D275/04 , A61K31/7068 , A61P35/00 , A61K31/5025 , A61K31/502 , A61K31/519 , A61K31/517 , A61K31/454 , A61K31/55 , A61K31/416 , A61K31/496 , C07D403/04 , C07D237/34 , C07D401/14 , C07D239/80 , C07D401/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D513/04 , C07D417/12 , C07D487/08 , A61K38/07
Abstract: Provided herein are methods of using KRAS G12C inhibitors and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号：US20170320860A1
公开(公告)日：2017-11-09
申请号：US15584109
申请日：2017-05-02
Applicant: AMGEN INC.
Inventor： Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Mikkel V. DEBENEDETTO , Paul John DRANSFIELD , Zice FU , James S. HARVEY , Julie Anne HEATH , Simon J. HEDLEY , Jonathan HOUZE , Ted C. JUDD , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Wen-Chen YEH
IPC: C07D405/14 , C07D471/04 , C07D405/04 , A61K31/5383 , A61K31/437 , A61K31/506 , A61K31/497 , A61K31/4439 , C07D498/04 , A61K45/06
CPC classification number: C07D405/14 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D409/14 , C07D471/04 , C07D498/04
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may 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.
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公开(公告)号：US20170042872A1
公开(公告)日：2017-02-16
申请号：US15297940
申请日：2016-10-19
Applicant: AMGEN INC.
Inventor： 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: A61K31/4439 , A61K31/695 , A61K31/501 , A61K31/497 , A61K31/444 , A61K45/06 , A61K31/506
CPC classification number: 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
Abstract: 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.
Abstract translation: 其中在这里提供变量的定义。
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公开(公告)号：US20170042871A1
公开(公告)日：2017-02-16
申请号：US15297487
申请日：2016-10-19
Applicant: AMGEN INC.
Inventor： 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: A61K31/4439 , A61K31/501 , A61K31/444 , A61K31/506 , A61K31/497
CPC classification number: 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
Abstract: 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.
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Patent Agency Ranking
公开(公告)号：US20170037026A1
公开(公告)日：2017-02-09
申请号：US15297272
申请日：2016-10-19
Applicant: AMGEN INC.
Inventor： 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: C07D401/04 , A61K31/4439 , C07F7/08 , A61K31/695 , C07D401/14 , C07D405/14 , C07B59/00 , C07D471/04 , A61K31/444 , C07D417/14 , A61K31/497 , A61K45/06 , A61K31/506
CPC classification number: 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
Abstract: 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.
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17.发明申请PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开作为β-分泌酶抑制剂的全氟化环丙氯联-1,3-氧化物-2-胺化合物及其使用方法公开(公告)号：US20160280695A1
公开(公告)日：2016-09-29
申请号：US14932787
申请日：2015-11-04
Applicant: AMGEN INC.
Inventor： Ana Elena MINATTI , Jonathan D. LOW , Jennifer R. ALLEN , Albert AMEGADZIE , James BROWN , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Patricia LOPEZ , Vu Van MA , Nobuko NISHIMURA , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Kelvin SHAM , Adrian L. SMITH , Ryan WHITE , Qiufen XUE
IPC: C07D413/12
CPC classification number: C07D413/12 , C07D265/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 其中式I的Ra，Rb，R1，R2，R3和R7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
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公开(公告)号：US20240174660A1
公开(公告)日：2024-05-30
申请号：US18543498
申请日：2023-12-18
Applicant: Amgen Inc.
Inventor： Brian Alan LANMAN , Jian CHEN , Anthony B. REED , Victor J. CEE , Longbin LIU , David John KOPECKY , Patricia LOPEZ , Ryan Paul WURZ , Thomas T. NGUYEN , Shon BOOKER , Nobuko NISHIMURA , Youngsook SHIN , Nuria A. TAMAYO , John Gordon ALLEN , Jennifer Rebecca ALLEN
IPC: C07D417/04 , A61K31/416 , A61K31/454 , A61K31/496 , A61K31/502 , A61K31/5025 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/7068 , A61K38/07 , A61P35/00 , C07D237/34 , C07D239/80 , C07D275/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/12 , C07D471/04 , C07D475/00 , C07D487/04 , C07D487/08 , C07D487/10 , C07D513/04
CPC classification number: C07D417/04 , A61K31/416 , A61K31/454 , A61K31/496 , A61K31/502 , A61K31/5025 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/7068 , A61K38/07 , A61P35/00 , C07D237/34 , C07D239/80 , C07D275/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/12 , C07D471/04 , C07D475/00 , C07D487/04 , C07D487/08 , C07D487/10 , C07D513/04
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号：US20240050430A1
公开(公告)日：2024-02-15
申请号：US18213464
申请日：2023-06-23
Applicant: Amgen Inc.
Inventor： John Gordon ALLEN , Jennifer Rebecca ALLEN , Ana Elena MINATTI , Qiufen XUE , Ryan Paul WURZ , Christopher M. TEGLEY , Alexander J. PICKRELL , Thomas T. NGUYEN , Vu Van MA , Patricia LOPEZ , Longbin LIU , David John KOPECKY , Michael J. FROHN , Ning CHEN , Jian Jeffrey CHEN , Aaron C. SIEGMUND , Albert AMEGADZIE , Nuria A. TAMAYO , Shon BOOKER , Clifford GOODMAN , Mary WALTON , Nobuko NISHIMURA , Youngsook SHIN , Jonathan D. LOW , Victor J. CEE , Anthony B. REED , Hui-Ling WANG , Brian Alan LANMAN
IPC: A61K31/517 , A61P35/00 , A61K31/4985 , A61K39/395 , C07D403/04 , C07D471/04
CPC classification number: A61K31/517 , A61P35/00 , C07D471/04 , A61K39/39558 , C07D403/04 , A61K31/4985
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号：US20220372018A1
公开(公告)日：2022-11-24
申请号：US17632334
申请日：2020-08-03
Applicant: AMGEN INC.
Inventor： Nuria A. TAMAYO , Abhisek BANERJEE , Jian Jeffrey CHEN , Matthew Richard KALLER , Thomas T. NGUYEN , Nobuko NISHIMURA , Qiufen May XUE , John Gordon ALLEN , Michael J. FROHN
IPC: C07D401/14 , C07D401/04 , C07D405/14 , C07D413/14
Abstract: Amide compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
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