1104381-01-2Relevant academic research and scientific papers
6-PHENYL-LH-IMIDAZO [4, 5-C] PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN S AND/OR CATHEPSIN K INHIBITORS
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Page/Page column 19, (2010/08/08)
The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I) to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors
Cai, Jiaqiang,Baugh, Mark,Black, Darcey,Long, Clive,Jonathan Bennett,Dempster, Maureen,Fradera, Xavier,Gillespie, Jonathan,Andrews, Fiona,Boucharens, Sylviane,Bruin, John,Cameron, Kenneth S.,Cumming, Iain,Hamilton, William,Jones, Philip S.,Kaptein, Allard,Kinghorn, Emma,Maidment, Maurice,Martin, Iain,Mitchell, Ann,Rankovic, Zoran,Robinson, John,Scullion, Paul,Uitdehaag, Joost C.M.,Vink, Paul,Westwood, Paul,Van Zeeland, Mario,Van Berkom, Leon,Bastiani, Martijn,Meulemans, Tommi
scheme or table, p. 4350 - 4354 (2010/09/11)
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stable thio-trapping nitrile war-head in comparison with the well reported pyrimidine-2-carbonitrile cysteine cathepsin inhibitors. Compound 47 is also very potent in in vivo mouse spleenic Lip10 accumulation assays.
6-PHENYL-1H-IMIDAZO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
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Page/Page column 9, (2010/08/07)
The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament f
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important
Cai, Jiaqiang,Fradera, Xavier,Van Zeeland, Mario,Dempster, Maureen,Cameron, Kenneth S.,Bennett, D. Jonathan,Robinson, John,Popplestone, Lucy,Baugh, Mark,Westwood, Paul,Bruin, John,Hamilton, William,Kinghorn, Emma,Long, Clive,Uitdehaag, Joost C.M.
scheme or table, p. 4507 - 4510 (2010/10/21)
Using computer aided modelling studies, a new extended P2/S2 interaction was identified. This extended region can accommodate a variety of functional groups, such as aryls and basic amines. It was discovered that the N3 nitrogen of the pyrimidine-2-carbonitrile is critical for its cathepsin cysteine protease inhibition. N1 nitrogen also contributes to the inhibitory activity, but to a very limited degree. An 'in situ double activation' mechanism was proposed to explain these results.
6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS
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Page/Page column 17, (2009/03/07)
The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such asatherosclerosis,obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer,and chronic pain, such as neuropathic pain.
6-PHENYL-1H-IMIDAZO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
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Page/Page column 9-10, (2009/04/24)
The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
