公开(公告)号：EP1896452B1

公开(公告)日：2011-11-16

申请号：EP06770806.5

申请日：2006-05-22

申请人： Novartis AG ,  Vicuron Pharmaceuticals, Inc.

发明人： BRACKEN, Kathryn Rene ,  BUSHELL, Simon ,  DEAN, Karl ,  FRANCAVILLA, Charles ,  JAIN, Rakesh K. ,  LEE, Kwangho ,  SEEPERSAUD, Mohindra ,  SHU, Lei ,  SUNDARAM, Arathia ,  YUAN, Zhengyu

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61P31/04

CPC分类号： C07D401/12 ,  C07D403/12

摘要： Novel N-formyl hydroxylamine compounds (I) and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes . The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed. wherein R1 is hydrogen, alkyl, heteroalkyi, heterocycloalkyl, aryl or heteroaryl.; R3 is hydrogen, halogen, or alkoxy; R4 is aryl, or heteroaryl; or n is 0 to 3 and provided that R1 is cycloalkyl and/or R4 is an optionally substituted 6 membered, monocyclic heteroaryl ring having 2, 3 or 4 nitrogen heteroatoms in the ring wherein one or more of the ring nitrogen heteroatoms is optionally oxidized.

公开(公告)号：EP1896452A2

公开(公告)日：2008-03-12

申请号：EP06770806.5

申请日：2006-05-22

申请人： Novartis Pharma AG ,  NOVARTIS-PHARMA GMBH ,  Vicuron Pharmaceuticals, Inc.

发明人： BRACKEN, Kathryn Rene ,  BUSHELL, Simon ,  DEAN, Karl ,  FRANCAVILLA, Charles ,  JAIN, Rakesh K. ,  LEE, Kwangho ,  SEEPERSAUD, Mohindra ,  SHU, Lei ,  SUNDARAM, Arathia ,  YUAN, Zhengyu

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61P31/04

CPC分类号： C07D401/12 ,  C07D403/12

摘要： Novel N-formyl hydroxylamine compounds (I) and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes . The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed. wherein R1 is hydrogen, alkyl, heteroalkyi, heterocycloalkyl, aryl or heteroaryl.; R3 is hydrogen, halogen, or alkoxy; R4 is aryl, or heteroaryl; or n is 0 to 3 and provided that R1 is cycloalkyl and/or R4 is an optionally substituted 6 membered, monocyclic heteroaryl ring having 2, 3 or 4 nitrogen heteroatoms in the ring wherein one or more of the ring nitrogen heteroatoms is optionally oxidized.

公开(公告)号：EP2595983A1

公开(公告)日：2013-05-29

申请号：EP11743481.1

申请日：2011-07-21

申请人： Novartis AG

发明人： BARNES, David ,  COHEN, Scott Louis ,  FU, Jiping ,  SHU, Lei ,  ZHENG, Rui

IPC分类号： C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04 ,  A61K31/381 ,  A61P31/12

CPC分类号： A61K31/541 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/422 ,  A61K31/4535 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/553 ,  A61K45/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04

摘要： The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：EP3681883A1

公开(公告)日：2020-07-22

申请号：EP18769353.6

申请日：2018-09-12

申请人： Novartis AG

发明人： DALES, Natalie ,  GORMISKY, Paul ,  KERRIGAN, John Ryan ,  SHU, Lei

IPC分类号： C07D405/14 ,  C07D333/20 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D413/10 ,  C07D417/10 ,  C07D249/10 ,  C07D487/04 ,  C07D491/04 ,  C07D498/04 ,  A61P25/28 ,  A61K31/4196 ,  A61K31/4439

公开(公告)号：EP4101849A1

公开(公告)日：2022-12-14

申请号：EP21194692.6

申请日：2013-08-13

申请人： Novartis AG

发明人： CHEUNG, Atwood ,  CHIN, Donovan Noel ,  DALES, Natalie ,  FAZAL, Aleem ,  HURLEY, Timothy Brian ,  KERRIGAN, John ,  O'BRIEN, Gary ,  SHU, Lei ,  SUN, Robert ,  SUNG, Moo

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  A61K31/501 ,  A61P21/00

摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof;

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：EP3564233A1

公开(公告)日：2019-11-06

申请号：EP18209821.0

申请日：2013-08-13

申请人： Novartis AG

发明人： CHEUNG, Atwood ,  CHIN, Donovan Noel ,  DALES, Natalie ,  FAZAL, Aleem ,  HURLEY, Timothy Brian ,  KERRIGAN, John ,  O'BRIEN, Gary ,  SHU, Lei ,  SUN, Robert ,  SUNG, Moo

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  A61K31/501 ,  A61P21/00

摘要： The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof;

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：EP2885288A1

公开(公告)日：2015-06-24

申请号：EP13752768.5

申请日：2013-08-13

申请人： Novartis AG

发明人： CHEUNG, Atwood ,  CHIN, Donovan Noel ,  DALES, Natalie ,  FAZAL, Aleem ,  HURLEY, Timothy Brian ,  KERRIGAN, John ,  O'BRIEN, Gary ,  SHU, Lei ,  SUN, Robert ,  SUNG, Moo

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  A61K31/501 ,  A61P21/00

CPC分类号： A61K31/501 ,  A61K31/41 ,  A61K31/427 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D237/06 ,  C07D237/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

摘要： The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

摘要翻译： 本发明提供了式I或其药学上可接受的盐的化合物; 用于制造本发明的化合物的方法，它的治疗用途。 本发明还提供了药理学活性剂和药物组合物的组合。