公开(公告)号：US10369138B2

公开(公告)日：2019-08-06

申请号：US14861797

申请日：2015-09-22

Applicant: Novartis AG

Inventor： Virender Singh Aulakh ,  Anthony Casarez ,  Xiaodong Lin ,  Mika Lindvall ,  Glenn McEnroe ,  Heinz Ernst Moser ,  Folkert Reck ,  Meiliana Tjandra ,  Robert Lowell Simmons ,  Aregahegn Yifru ,  Qingming Zhu

IPC: A61K31/427 ,  C07D417/14 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/496 ,  A61K31/4545 ,  C07D487/04 ,  A61K45/06

Abstract: This invention pertains generally to antibacterial compounds of Formula I, as further described herein, and pharmaceutically acceptable salts and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds to treat infections such as those caused by Gram-negative bacteria.

公开(公告)号：US10919887B2

公开(公告)日：2021-02-16

申请号：US15762724

申请日：2016-09-20

Applicant: Novartis AG

Inventor： Eric Aubin ,  Anthony Casarez ,  Andreas Fisch ,  Zaixing Li ,  Mika Lindvall ,  Heinz Ernst Moser ,  Michael Mutz ,  Folkert Reck ,  Bernd Ulrich Riebesehl ,  Marc Schoenhentz ,  Vijay Sethuraman ,  Robert Lowell Simmons

IPC: C07D417/14 ,  A61P31/04

Abstract: The invention provides new solid forms, salts and polymorphs of 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), pharmaceutical compositions containing them, and processes for their manufacture and use in therapy.

公开(公告)号：US10597396B2

公开(公告)日：2020-03-24

申请号：US16323668

申请日：2017-09-28

Applicant: Novartis AG

Inventor： Anthony Casarez ,  Markus Furegati ,  Guido Koch ,  Xiaodong Lin ,  Flavio Ossola ,  Folkert Reck ,  Robert Lowell Simmons ,  Qingming Zhu

IPC: C07D471/18 ,  A61K31/5025 ,  A61P31/04 ,  A61K31/551 ,  A61K45/06 ,  A61K31/407 ,  A61K31/427 ,  A61K31/431 ,  A61K31/439 ,  A61K31/496 ,  A61K31/546 ,  A61K31/535 ,  A61K31/4545

Abstract: This invention pertains generally to compounds of Formula (A), as further described herein, which act as beta-lactamase inhibitors, and salts, crystalline forms and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds in combination with a beta-lactam antibiotic to treat infections caused by Gram-negative bacteria, including drug-resistant strains.

公开(公告)号：US10160726B2

公开(公告)日：2018-12-25

申请号：US15500870

申请日：2015-08-03

Applicant: NOVARTIS AG

Inventor： Javier de Vicente Fidalgo ,  Haiying He ,  Cheng Hu ,  Zhigan Jiang ,  Xiaolin Li ,  Peichao Lu ,  Wosenu Mergo ,  Daniel Mutnick ,  Folkert Reck ,  Alexey Rivkin ,  Colin Keith Skepper ,  Xiaojing Michael Wang ,  Jianhua Xia ,  Yongjin Xu

IPC: C07D215/38 ,  C07D215/22 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10 ,  C07D498/10

Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.

公开(公告)号：US10065957B2

公开(公告)日：2018-09-04

申请号：US15718571

申请日：2017-09-28

Applicant: Novartis AG

Inventor： Anthony Casarez ,  Markus Furegati ,  Guido Koch ,  Xiaodong Lin ,  Flavio Ossola ,  Folkert Reck ,  Robert Lowell Simmons ,  Qingming Zhu

IPC: C07D471/18 ,  A61K31/439 ,  A61K31/5025 ,  A61K31/407 ,  A61K31/427 ,  A61K31/431 ,  A61K31/496 ,  A61K31/546 ,  A61K31/535 ,  A61P31/04

Abstract: This invention pertains generally to compounds of Formula (A), as further described herein, which act as beta-lactamase inhibitors, and salts, crystalline forms and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds in combination with a beta-lactam antibiotic to treat infections caused by Gram-negative bacteria, including drug-resistant strains.