- PAPAIN FAMILY CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES
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The invention relates to the treatment of parasitic disease with inhibitors of the papain family cysteine proteases The parasitic diseases include toxoplasmosis, malaria, African trypanosomiasis, Changas disease, leishmanasis and schistosomiasis The inven
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Page/Page column 24
(2008/06/13)
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- Primary amides as selective inhibitors of cathepsin K
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The nitrile warhead used in a series of cathepsin K inhibitors can be replaced by a less electrophilic primary amide. The accompanying loss of potency can be partially recovered by introducing a substituent α to the amide. The potency gain resulting from this addition is not achieved with the nitrile derivatives due to a different geometry of the cysteine adduct in the enzyme active site. This study led to the identification of the primary amide 2g, which is an inhibitory substrate, with an IC50 of 10 nM against cathepsin K and excellent selectivity versus the other cathepsins.
- Leger, Serge,Bayly, Christopher I.,Black, W. Cameron,Desmarais, Sylvie,Falgueyret, Jean-Pierre,Masse, Frederic,Percival, M. David,Truchon, Jean-Francois
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p. 4328 - 4332
(2008/02/10)
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- Diastereoselective arylithium addition to an α-trifluoromethyl imine. Practical synthesis of a potent cathepsin K inhibitor
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A practical, chromatography-free synthesis of potent cathepsin K inhibitor 1 is described. The addition of 4-bromophenyllithium to an α- trifluoromethylimine derived from commercially available (S)-leucinol was accomplished in a highly diastereoselective
- Roy, Amelie,Gosselin, Francis,O'Shea, Paul D.,Chen, Cheng-Y
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p. 4320 - 4323
(2007/10/03)
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- Identification of a potent and selective non-basic cathepsin K inhibitor
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Based on our previous study with trifluoroethylamine as a P2-P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound showed e
- Li, Chun Sing,Deschenes, Denis,Desmarais, Sylvie,Falgueyret, Jean-Pierre,Gauthier, Jacques Yves,Kimmel, Donald B.,Leger, Serge,Masse, Frederic,McGrath, Mary E.,McKay, Daniel J.,Percival, M. David,Riendeau, Denis,Rodan, Sevgi B.,Therien, Michel,Truong, Vouy-Linh,Wesolowski, Gregg,Zamboni, Robert,Black, W. Cameron
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p. 1985 - 1989
(2007/10/03)
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- CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of G, E, E, n, R1, R2, R3 et R4 are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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Page/Page column 45
(2010/02/11)
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- CATHEPSIN INHIBITORS
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This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3 and R4 are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritis.
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Page/Page column 49-50
(2010/02/11)
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- Cathepsin cysteine protease inhibitors
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This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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