公开(公告)号：US20150045562A1

公开(公告)日：2015-02-12

申请号：US14384233

申请日：2013-03-22

Applicant: NOVARTIS AG

Inventor： Michael Crowe ,  Michael Foulkes ,  Giancarlo Francese ,  Dominique Grimler ,  Ernst Kuesters ,  Kurt Laumen ,  Yunzhong Li ,  Changxue Lin ,  Jovana Nazor ,  Thomas Ruch ,  Derek Smith ,  Shiwei Song ,  Shangjun Teng

IPC: C12P17/10 ,  C07D209/38 ,  C07D209/12 ,  C07D405/06

CPC classification number: C12P17/10 ,  C07D209/12 ,  C07D209/14 ,  C07D209/34 ,  C07D209/38 ,  C07D405/06 ,  C07D471/20 ,  C12N9/1096 ,  Y02P20/52

Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1′R,3′S)-5,7′-dichloro-6′-fluoro-3′-methyl-2′,3′,4′,9′-tetrahydrospiro[indoline-3,1′-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.

Abstract translation: 本发明涉及可用于制备螺旋体酮化合物的方法和中间体，例如（1'R，3'S）-5,7'-二氯-6'-氟-3'-甲基-2'，3'， 4'，9'-四氢螺[二氢吲哚-3,1'-吡啶并[3,4-b]吲哚] -2-酮及其盐和水合物和溶剂化物。

公开(公告)号：US11434192B2

公开(公告)日：2022-09-06

申请号：US16452452

申请日：2019-06-25

Applicant: Novartis AG

Inventor： Florian Karl Kleinbeck-Riniker ,  Benjamin Martin ,  Gerhard Penn ,  Francesco Venturoni ,  Thierry Schlama ,  Thomas Ruch ,  Thomas Allmendinger ,  Bernhard Wietfeld ,  Paolo Filipponi

IPC: C07C59/84 ,  C07C67/035 ,  C07C213/08 ,  C07C69/738 ,  C07C313/06 ,  C07C229/34 ,  C07D265/02 ,  C07D207/36 ,  C07C251/40 ,  C07C251/66 ,  C07C51/373

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

公开(公告)号：US11414411B2

公开(公告)日：2022-08-16

申请号：US16635596

申请日：2018-08-01

Applicant: Novartis AG

Inventor： Like Chen ,  Chi Ming Cheung ,  Zhongbo Fei ,  Qun Jiang ,  Lei Li ,  Bin Li ,  Thomas Ruch ,  Hao Wang ,  Quanbing Wu

IPC: C07D417/14

Abstract: The present invention provides a process of synthesizing 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (referred to herein as Compound X), or a salt thereof, or a solvate including hydrate thereof, and/or intermediates thereof, and the use of intermediates for preparing Compound X. In particular, the process relates to the preparation of Compound X using dynamic kinetic resolution (DKR) and asymmetric catalytic reduction, thereby providing an improved route to 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (Compound X) and compositions containing said compound, including the arginine salt, sodium salt and hydrated solid forms of Compound X.

公开(公告)号：US10774036B2

公开(公告)日：2020-09-15

申请号：US16472386

申请日：2017-12-20

Applicant: Novartis AG

Inventor： Florian Karl Kleinbeck-Riniker ,  Tobias Kapferer ,  Hongyong Kim ,  Jie Ku ,  Kurt Laumen ,  Yunzhong Li ,  Wei Peng ,  Thomas Ruch ,  Thierry Schlama ,  Yao Yang

IPC: C07C227/06 ,  C07C229/36 ,  C12P41/00

Abstract: The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone.

公开(公告)号：US10377697B2

公开(公告)日：2019-08-13

申请号：US15780957

申请日：2016-12-08

Applicant: Novartis AG

Inventor： Florian Karl Kleinbeck-Riniker ,  Benjamin Martin ,  Gerhard Penn ,  Francesco Venturoni ,  Thierry Schlama ,  Thomas Ruch ,  Thomas Allmendinger ,  Bernhard Wietfeld ,  Paolo Filipponi

IPC: C07C51/373 ,  C07C69/738 ,  C07C313/06 ,  C07C229/34 ,  C07D265/02 ,  C07D207/36 ,  C07C251/40 ,  C07C251/66 ,  C07C59/84 ,  C07C67/035

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.