公开(公告)号：US20230374029A1

公开(公告)日：2023-11-23

申请号：US18004313

申请日：2021-07-06

Applicant: Novartis AG

Inventor： Zhongbo FEI ,  Huanqing JIA ,  Wei LI ,  Jianhua WANG ,  Huangchao YU

IPC: C07D491/107

CPC classification number: C07D491/107

Abstract: The present invention relates to a method for the manufacture of a compound of Formula I or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein LG, A, n, m and p are as defined in the Summary of the Invention, said manufacture including the manufacture and use of a compound of the formula VI; wherein R1 is a secondary amino protecting group and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl or unsubstituted or substituted aryl.

公开(公告)号：US20200239461A1

公开(公告)日：2020-07-30

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：US20210299100A1

公开(公告)日：2021-09-30

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Cara BROCKLEHURST ,  Patrick CHENE ,  Zhongbo FEI ,  Pascal FURET ,  Vito GUAGNANO ,  Patricia IMBACH-WEESE ,  Joerg KALLEN ,  Mickael LE DOUGET ,  Jialiang LI ,  Wei LI ,  Edwige Liliane Jeanne LORTHIOIS ,  Joseph McKENNA ,  Bahaa SALEM ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

IPC: A61K31/4155 ,  C07D307/81 ,  C07D405/12 ,  A61K31/343 ,  A61K31/443 ,  A61K31/426 ,  C07D417/04 ,  C07D407/04 ,  A61K31/357 ,  C07D405/04 ,  A61K31/403 ,  A61K31/4525 ,  A61K31/351 ,  C07D407/12 ,  A61K31/506 ,  A61K31/41 ,  A61K31/4025 ,  A61K31/4439 ,  C07D405/14 ,  A61P35/00

Abstract: The present invention provides a compound of formula (1) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.