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公开(公告)号：WO2021226168A1
公开(公告)日：2021-11-11
申请号：PCT/US2021/030780
申请日：2021-05-05
Applicant: AMGEN INC.
Inventor： SMITH, Austin G. , TEDROW, Jason S. , ST-PIERRE, Gabrielle , THIEL, Oliver Ralf , HUANG, Liang , ROOSEN, Philipp C. , COLYER, John T. , BAUCOM, Kyle D. , ERICSON, Ari , BEAVER, Matthew G. , SANGODKAR, Rahul P. , LOVETTE, Michael A. , MILBURN, Robert Ronald , CHERNEY, Alan H. , CUI, Sheng
IPC: C07D267/16 , C07D281/00 , C07D513/08 , A61P35/00 , A61K31/553
Abstract: Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.
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公开(公告)号：WO2021202452A1
公开(公告)日：2021-10-07
申请号：PCT/US2021/024779
申请日：2021-03-30
Applicant: AMGEN INC.
Inventor： ACHMATOWICZ, Michael , CUI, Sheng , HWANG, Tsang-Lin , LANGILLE, Neil Fred , TOM, Janine K. , HUCKLE, James E. , STEC, Markian , WU, Tian , BROWN, Sean P.
IPC: C07D519/00 , A61P35/00 , A61K31/553
Abstract: Disclosed herein is an improved process for the synthesis of compound (A): (A), or a salt or solvate thereof via methylation of compound (B): (B), or a salt or solvate thereof, a crystalline hydrate of compound A, and pharmaceutical formulations comprising a crystalline hydrate of compound (A).
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公开(公告)号：WO2020037164A1
公开(公告)日：2020-02-20
申请号：PCT/US2019/046726
申请日：2019-08-16
Applicant: AMGEN INC. , CYTOKINETICS, INC.
Inventor： MORRISON, Henry , CUI, Sheng , QUASDORF, Kyle , YANEZ, Evelyn , QUAN, Bin, Peter , KELLY, Ron, C. , CAILLE, Sebastien , XIAO, Lingyun , PEARSON, David , RAEBURN, Jaclyn , GOLIGHTLY, Ailsa , MORGAN, Bradley , PETERSON, Matthew , EBERLIN, Alex , OBLEZOV, Alexander
IPC: A61P9/00 , C07D213/75 , A61K31/496 , C07C55/06 , C07C55/08 , C07C55/10 , C07C57/145 , C07C57/15 , C07C59/255 , C07C309/04 , C07C309/08 , C07C309/35
Abstract: Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.
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公开(公告)号：WO2016154580A1
公开(公告)日：2016-09-29
申请号：PCT/US2016/024308
申请日：2016-03-25
Applicant: AMGEN INC.
Inventor： CUI, Sheng , RANGANATHAN, Krishnakumar , CROCKETT, Richard , CHEN, Ying , SWIETLOW, Aleksander , CROSSLEY, Kevin , SHI, Yun , DECROOS, Karel , MONIOTTE, Etienne
CPC classification number: C07K1/026 , C07K1/18 , C07K5/081 , C07K5/1019 , C07K7/06
Abstract: The instant disclosure is directed to solution phase fragment coupling methods for preparing etelcalcetide and its pharmaceutically acceptable salts.
Abstract translation: 本公开涉及用于制备西替卡肽及其药学上可接受的盐的溶液相片段偶联方法。
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公开(公告)号：WO2021226009A1
公开(公告)日：2021-11-11
申请号：PCT/US2021/030548
申请日：2021-05-04
Applicant: AMGEN INC.
Inventor： SMITH, Austin G. , CORBETT, Michael T. , LANGILLE, Neil Fred , BAUCOM, Kyle D. , DORNAN, Peter K. , ST-PIERRE, Gabrielle , ROOSEN, Philipp C. , CUI, Sheng , PROFETA, Roberto
IPC: C07D249/18 , C07C69/16 , C07C69/78 , C07C309/23 , C07D513/08 , C07D513/10
Abstract: Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound F, or a salt thereof, wherein R1 and OPG2 are described herein. Compound F can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.
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Patent Agency Ranking
公开(公告)号：WO2015154031A1
公开(公告)日：2015-10-08
申请号：PCT/US2015/024347
申请日：2015-04-03
Applicant: AMGEN INC.
Inventor： BEZEMER, Jeroen , CHEN, Ying , CROCKETT, Richard , CROSSLEY, Kevin , CUI, Sheng , HUANG, Liang , JONES, Sian , LOWER, Asher , RANGANATHAN, Krishnakumar
CPC classification number: C07K7/06 , A61K38/00 , C07K1/1075
Abstract: A method for preparing AMG 416, or a pharmaceutically acceptable salt thereof, is provided. AMG 416 is a synthetic, eight amino-acid selective peptide agonist of the calcium sensing receptor. It is being developed as an intravenous treatment of secondary hyperparathyroidism (SHPT) in hemodialysis patients with chronic kidney disease - mineral and bone disorder (CKD-MBD).
Abstract translation: 提供了制备AMG 416或其药学上可接受的盐的方法。 AMG 416是钙感应受体的合成的8个氨基酸选择性肽激动剂。 正在研制慢性肾脏疾病 - 矿物质和骨骼疾病（CKD-MBD）的血液透析患者的继发性甲状旁腺功能亢进症（SHPT）的静脉注射治疗。
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公开(公告)号：WO2014152270A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/027146
申请日：2014-03-14
Applicant: AMGEN INC. , CYTOKINETICS, INC.
Inventor： CUI, Sheng , MORRISON, Henry , NAGAPUDI, Karthik , WALKER, Shawn , BERNARD, Charles , HANSEN, Karl, Bennett , LANGILLE, Neil, Fred , ALLGEIER, Alan, Martin , MENNEN, Steven , WOO, Jacqueline , MORGAN, Bradley, Paul , MUCI, Alex
IPC: C07D213/75 , A61K31/444 , A61P9/00
CPC classification number: C07D213/75 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K31/496 , A61K47/38
Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use. Omecamtiv mecarbil (AMG 423, CK-1827452), having the structure:
Abstract translation: 本发明提供了奥美康米卡非二盐酸盐形式，其组合物和药物制剂及其制备和使用方法。 Omecamtiv mecarbil（AMG 423，CK-1827452），具有以下结构：
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公开(公告)号：EP3274360B1
公开(公告)日：2020-05-06
申请号：EP16720588.9
申请日：2016-03-25
Applicant: Amgen Inc.
Inventor： CUI, Sheng , RANGANATHAN, Krishnakumar , CROCKETT, Richard , CHEN, Ying , SWIETLOW, Aleksander , CROSSLEY, Kevin , SHI, Yun , DECROOS, Karel , MONIOTTE, Etienne
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公开(公告)号：WO2022115400A1
公开(公告)日：2022-06-02
申请号：PCT/US2021/060447
申请日：2021-11-23
Applicant: AMGEN INC.
Inventor： BAUCOM, Kyle D. , CORBETT, Michael T. , CUI, Sheng , LANGILLE, Neil F. , ROTHELI, Andreas Rene , PROFETA, Roberto , SMITH, Austin G.
IPC: C07C67/14 , C07C67/293 , C07C69/16 , C07C69/78 , C07D513/10 , B01J31/28
Abstract: Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound IA, wherein R1 is described herein. Compound IA can be useful in synthesizing compound A1, or a salt or solvate thereof, and compound A2, or a salt of solvate thereof.
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10.发明申请SYNTHESIS OF (S)-2-AMINO-4-METHYL-1-((R)-2-METHYLOXIRANE-2-YL)-PENTAN-1-ONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开（S）-2-氨基-4-甲基-1 - （（R）-2-甲基氧杂环戊烷-2-基） - 戊-1-酮的合成及其药用可接受的盐
公开(公告)号：WO2018027021A1
公开(公告)日：2018-02-08
申请号：PCT/US2017/045274
申请日：2017-08-03
Applicant: AMGEN INC.
Inventor： BEAVER, Matt , CUI, Sheng , SHI, Xianqing
IPC: C07D303/36 , C01G45/00
Abstract: The present invention provides new methods for preparing compound (5), and pharmaceutically acceptable salts thereof, of structure. Compound (5), or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.
Abstract translation: 本发明提供了用于制备具有结构的化合物（5）及其药学上可接受的盐的新方法。 化合物（5）或其药学上可接受的盐是卡非佐米合成中的重要中间体。 本发明还提供了制备可用于本发明的环氧化步骤的有用的锰催化剂的方法。
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