Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights
摘要:
Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause stroke or septic shock. Several classes of potent NOS inhibitors have been reported, most of them targeting the arginine binding site of the oxygenase domain. Here we disclose the SAR and the rational design of potent and selective iNOS inhibitors which may be useful as anti-inflammatory drugs. (C) 2011 Elsevier Ltd. All rights reserved.
[EN] IMIDAZO[4,5-B]QUINOLINE-DERIVATIVES AND THEIR USE AS NO-SYNTHASE INHIBITORS<br/>[FR] DERIVES DE IMIDAZO[4,5-B]QUINOLINE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE NO-SYNTHASE
申请人:ALTANA PHARMA AG
公开号:WO2004076451A1
公开(公告)日:2004-09-10
The compounds of formula I In which R1, R2, R3 and A have the meanings as given In the description are novel effective INOS Inhibitors.
式I中的化合物,其中R1、R2、R3和A的含义如描述中所述,是新颖有效的iNOS抑制剂。
[EN] PYRIMIDINE DERIVATIVES AND THEIR USE AS MODULATORS OF FGFR ACTIVITY<br/>[FR] DÉRIVÉS DE PYRIMIDINE ET LEUR UTILISATION EN TANT QUE MODULATEURS DE L'ACTIVITÉ DU FGFR
申请人:ASTRAZENECA AB
公开号:WO2009056886A1
公开(公告)日:2009-05-07
There is provided pyrimidine compounds of formula 1: or pharmaceutical salts thereof. There is al so provided processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, for exampl e in the treatment of proliferative disease such as cancer and particular ly in disease mediated by a FGFR inhibitory effect.
[EN] IMIDAZOPYRIDINE-DERIVATIVES AS INDUCIBLE NO-SYNTHASE INHIBITORS<br/>[FR] DERIVES D'IMIDAZOPYRIDINE UTILISES COMME INHIBITEURS INDUCTIBLES DE LA NO SYNTHASE
申请人:ALTANA PHARMA AG
公开号:WO2005030769A1
公开(公告)日:2005-04-07
The compounds of formula (I) in which R1, R2, Het1 and A have the meanings as given in the description are novel effective iNOS inhibitors.
公式(I)中R1,R2,Het1和A具有所述描述中给出的含义的化合物是新颖有效的iNOS抑制剂。
[EN] IMIDAZOPYRIDINE-DERIVATIVES AS INDUCTIBLE NO-SYNTHASE INHIBITORS<br/>[FR] DERIVES IMIDAZOPYRIDINE SERVANT D'INHIBITEURS DE NO-SYNTHASE INDUCTIBLE
申请人:ALTANA PHARMA AG
公开号:WO2005030771A1
公开(公告)日:2005-04-07
The compounds of formula (I) in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors.