- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
-
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
- -
-
Page/Page column 45-46
(2008/06/13)
-
- PROCESSES AND INTERMEDIATES FOR PREPARING CYSTEINE PROTEASE INHIBITORS
-
The present invention is directed to a novel process for preparing certain cysteine protease inhibitors.
- -
-
Page/Page column 57
(2010/10/20)
-
- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
-
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
- -
-
Page/Page column 56
(2008/06/13)
-
- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
-
The application is directed to haloalkyl-substituted compounds of Formula (I), wherein R1, R1a, R2, R3, R4’ and E are as defined in the claims. The compounds are inhibitors of cysteine proteases, in p
- -
-
Page/Page column 43-44
(2010/02/11)
-
- AMIDINO COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
-
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceu
- -
-
Page/Page column 40
(2010/02/09)
-
- CYSTEINE PROTEASE INHIBITORS
-
The present invention is directed to compounds that are inhibitors of cysteine protease, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceut
- -
-
Page/Page column 53
(2010/02/07)
-
- PEPTIDIC COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
-
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
- -
-
-
- Phenylalanine ammonia-lyase: The use of its broad substrate specificity for mechanistic investigations and biocatalysis - Synthesis of L-arylalanines
-
Several fluoro-and chlorophenylalanines were found to be good substrates of phenylalanine ammonialyase (PAL/EC 4.3.1.5) from parsley. The enantiomerically pure L-amino acids were obtained in good yields by reaction of the corresponding cinnamic acids with 5M ammonia solution (buffered to pH 10) in the presence of PAL. The kinetic constants for nine different fluoro-and chlorophenylalanines do not provide a rigorous proof for but are consistent with the previously proposed mechanism comprising an electrophilic attack of the methylidene-imidazolone cofactor of PAL at the aromatic nucleus as a first chemical step. In the resulting Friedel-Crafts-type σ complex the β-protons are activated for abstraction and consequently the pro-S is abstracted by an enzymic base. Results from semi-empirical calculations combined with a proposed partial active site model showed a correlation between the experimental kinetic constants and the change in polarization of the pro-S Cβ-H bond and heat of formation of the σ complexes, thus making the electrophilic attack at the neutral aromatic ring plausible. Furthermore, while 5-pyrimidinylalanine was found to be a moderately good substrate of PAL, 2-pyrimidinylalanine was an inhibitor.
- Gloge, Andreas,Zon, Jerzy,Koevari, Agnes,Poppe, Laszlo,Retey, Janos
-
p. 3386 - 3390
(2007/10/03)
-
- Synthesis of a complete set of L-difluorophenylalanines, L-(F2)Phe, as molecular explorers for the CH/π interaction between peptide ligand and receptor
-
A complete set of difluorophenylalanines in the L-configuration [L- (F2)Phe] (namely, L-(2,3-F2)Phe, L-(2,4-F2)Phe, L-(2,5-F2)Phe, L-(2,6- F2)Phe, L-(3,4-F2)Phe, L-(3,5-F2)Phe) w
- Fujita, Tsugumi,Nose, Takeru,Matsushima, Ayami,Okada, Kazushi,Asai, Daisuke,Yamauchi, Yasuko,Shirasu, Naoto,Honda, Takeshi,Shigehiro, Daiki,Shimohigashi, Yasuyuki
-
p. 923 - 927
(2007/10/03)
-
