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11.发明申请公开(公告)号：US20150376221A1
公开(公告)日：2015-12-31
申请号：US14767737
申请日：2014-02-20
Applicant: AMGEN INC.
Inventor： John Gordon Allen , Christopher H. FOTSCH , Michael J. FROHN , John Douglas MCCARTER , Mirna MUJACIC , Alexander J. PICKRELL
CPC classification number: C07H7/02 , C07D309/10 , C07D309/14 , C07K16/2875 , C07K2317/14 , C07K2317/41 , C12N5/0603 , C12N2501/999 , C12N2510/00
Abstract: Compounds of Formula (I) are useful as modulators of glycosylation. Compounds of Formula (I) have the following structure: (I) and the definitions of the other variables are provided herein.
Abstract translation: 式（I）的化合物可用作糖基化的调节剂。 式（I）的化合物具有以下结构：（I），本文提供其它变量的定义。
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12.发明申请公开(公告)号：US20200231585A1
公开(公告)日：2020-07-23
申请号：US16466199
申请日：2017-12-13
Applicant: AMGEN INC.
Inventor： Jennifer R. ALLEN , Albert AMEGADZIE , Matthew P. BOURBEAU , Jian J. CHEN , Michael J. FROHN , Paul E. HARRINGTON , Jonathan D. LOW , Vu V. MA , Thomas T. NGUYEN , Alexander PICKRELL , Corey REEVES
IPC: C07D417/14 , C07D417/10
Abstract: The present disclosure 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 A, R1, R2, R2′, R3, R4, and R5 of Formula (I) are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.
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公开(公告)号：US20170107255A1
公开(公告)日：2017-04-20
申请号：US15317911
申请日：2015-06-10
Applicant: AMGEN INC.
Inventor： Jerry Ryan HOLDER , Gayathri SWAMINATH , Michael J. FROHN , Brian Alan LANMAN , Anthony B. REED , Leslie P. Miranda , John G. Allen , Alexander J. Pickrell , Aaron C. Siegmund , Lewis D. Pennington , Bryant Yang
CPC classification number: C07K7/08 , A61K38/00 , A61K38/10 , A61K47/542 , A61K47/60 , C07K14/47 , C07K2319/30
Abstract: The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.
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14.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：US20160176874A1
公开(公告)日：2016-06-23
申请号：US15058023
申请日：2016-03-01
Applicant: AMGEN INC.
Inventor： Jennifer R. ALLEN , Jian J. CHEN , Michael J. FROHN , Matthew R. KALLER , Qingyian LIU , Thomas T. NGUYEN , Alexander J. PICKRELL , Wenyuan QIAN , Robert M. RZASA , Wenge ZHONG
IPC: C07D471/04 , C07D403/14 , C07D401/14
CPC classification number: C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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Patent Agency Ranking
公开(公告)号：US20240327461A1
公开(公告)日：2024-10-03
申请号：US18497081
申请日：2024-06-11
Applicant: AMGEN INC.
Inventor： Jerry Ryan HOLDER , Gayathri SWAMINATH , Michael J. FROHN , Brian Alan LANMAN , Anthony B. REED , Leslie P. MIRANDA , John Gordon ALLEN , Alexander J. PICKRELL , Aaron C. SIEGMUND , Lewis D. PENNINGTON , Bryant YANG
CPC classification number: C07K7/08 , A61K38/10 , A61K47/542 , A61K47/60 , C07K14/47 , A61K38/00 , C07K2319/30
Abstract: The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.
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公开(公告)号：US20230159510A1
公开(公告)日：2023-05-25
申请号：US17799077
申请日：2021-02-11
Applicant: AMGEN INC.
Inventor： Jennifer Rebecca ALLEN , Albert AMEGADZIE , Diane Jennifer BEYLKIN , Shon BOOKER , Matthew Paul BOURBEAU , John R. BUTLER , Michael J. FROHN , Sanne Ormholt Schroder GLAD , Birgitte Weinreich HUSEMOEN , Matthew R. KALLER , Todd J. KOHN , Brian Alan LANMAN , Kexue LI , Qingyian LIU , Patricia LOPEZ , Vu Van MA , Francesco MANONI , Jose MEDINA , Ana Elena MINATTI , Jorge PEIRO CADAHIA , Liping PETTUS , Alexander J. PICKRELL , Ian SARVARY , Nuria A. TAMAYO , Mikkel VESTERGAARD
IPC: C07D413/14 , C07D471/04 , C07D401/14 , C07D401/12 , C07D405/14
CPC classification number: C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/04
Abstract: Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: (I)
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公开(公告)号：US20220395504A1
公开(公告)日：2022-12-15
申请号：US17363878
申请日：2021-06-30
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
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：US20210261619A1
公开(公告)日：2021-08-26
申请号：US17160819
申请日：2021-01-28
Applicant: AMGEN INC.
Inventor： Jerry Ryan HOLDER , Gayathri SWAMINATH , Michael J. FROHN , Brian Alan LANMAN , Anthony B. REED , Leslie P. MIRANDA , John Gordon ALLEN , Alexander J. PICKRELL , Aaron C. SIEGMUND , Lewis D. PENNINGTON , Bryant YANG
Abstract: The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.
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20.发明申请公开(公告)号：US20200231601A1
公开(公告)日：2020-07-23
申请号：US16466207
申请日：2017-12-13
Applicant: AMGEN INC.
Inventor： Jennifer R. ALLEN , Matthew P. BOURBEAU , James A. BROWN , Ning CHEN , Michael J. FROHN , Zice FU , Longbin LIU , Qingyian LIU , Liping H. PETTUS , Wenyuan QIAN , Corey REEVES , Aaron C. SIEGMUND
IPC: C07D513/08 , C07D417/10 , A61P25/28
Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2′, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.
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