Patent search ap:("Amgen Inc.") AND inv:"Albert AMEGADZIE" Page 1

1.

发明公开
KRAS G12C INHIBITORS AND METHODS OF USING THE SAME 审中-公开

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.

2.

发明申请
SOLID STATE FORMS 审中-公开

公开(公告)号：US20200369662A1

公开(公告)日：2020-11-26

申请号：US16878824

申请日：2020-05-20

Applicant: AMGEN INC.

Inventor： Mary CHAVES , Patricia LOPEZ , Prashant AGARWAL , Albert AMEGADZIE , Stephanie AZALI , Roman SHIMANOVICH , Ron C. KELLY , Darren Leonard REID

IPC: C07D471/04

Abstract: The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

3.

发明申请
CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开

公开(公告)号：US20170267673A1

公开(公告)日：2017-09-21

申请号：US15354877

申请日：2016-11-17

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN , Albert AMEGADZIE , Matthew P. BOURBEAU , James A. BROWN , Jian J. CHEN , Yuan CHENG , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Longbin LIU , Qingyian LIU , Jonathan D. LOW , Vu Van MA , James R. MANNING , Ana Elena MINATTI , Thomas T. NGUYEN , Nobuko NISHIMURA , Mark H. NORMAN , Liping H. PETTUS , Alexander J. PICKRELL , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Aaron C. SIEGMUND , Markian M. STEC , Ryan D. WHITE , Qiufen XUE

IPC: C07D417/12 , C07D417/14 , C07D471/04 , C07D279/08 , C07D417/04 , C07D513/10

CPC classification number: C07D417/12 , C07D279/08 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/10

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, and 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.

4.

发明申请
Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use 有权
Title translation: 环丙基稠合噻嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法

公开(公告)号：US20160046618A1

公开(公告)日：2016-02-18

申请号：US14819256

申请日：2015-08-05

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN , Albert AMEGADZIE , Matthew P. BOURBEAU , James A. BROWN , Jian J. CHEN , Yuan CHENG , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Longbin LIU , Qingyian LIU , Jonathan D. LOW , Vu Van MA , James MANNING , Ana Elena MINATTI , Thomas T. NGUYEN , Nobuko NISHIMURA , Mark H. NORMAN , Liping H. PETTUS , Alexander J. PICKRELL , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Aaron C. SIEGMUND , Markian M. STEC , Ryan D. WHITE , Qiufen XUE

IPC: C07D417/12 , C07D471/04 , C07D513/10 , C07D417/14

CPC classification number: C07D417/12 , C07D279/08 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/10

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, and 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: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。所述化合物具有通式I：其中式I中的变量A4，A5，A6，A8以及R 1，R b，R 1，R 2，R 3和R 7各自独立地定义。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。

5.

发明申请
HETEROCYCLIC COMPOUNDS AS DELTA-5 DESATURASE INHIBITORS AND METHODS OF USE 有权

公开(公告)号：US20210171529A1

公开(公告)日：2021-06-10

申请号：US17103350

申请日：2020-11-24

Applicant: Amgen Inc.

Inventor： Jennifer R. ALLEN , Albert AMEGADZIE , Matthew P. BOURBEAU , Ning CHEN , Clifford GOODMAN , Giulia LATTANZI , Iain LINGARD , Qingyian LIU , Jonathan D. LOW , Vu Van MA , Ana E. MINATTI , Alfonso POZZAN , Corey REEVES , Aaron C. SIEGMUND , Sabrina TASSINI , Federica TONELLI , Mary WALTON

IPC: C07D487/04 , A61P3/04 , C07D471/04 , C07D498/04

Abstract: The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5D”). The compounds have a general Formula 1: wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

6.

发明申请
CYCLOPROPYL FUSED THIAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开

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.

7.

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
Title translation: 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。