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US 6,649,638 B1Granted
Prenylation inhibitors and methods of their synthesis and use
AssigneePPD Discovery, Inc.
InventorsBradley B. Brown, Kenneth S. Rehder
Life of this patent
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Abstract
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.
Claims15
A compound of the following formula:
- wherein
- R1 is a halogenated phenyl;
- R2 is nitrogen, phenyl, pyrazole, methylpyrazole, dimethylpyrazole, pyridine, thiophene, dimethylcyclobutyl, dimethylcyclopropyl or cyclopropyl;
- R3 is benzyl, isopropyl, chlorobenzyl, methyl thiophene, trifluoro methyl benzyl, 3,5-trifluoromtethyl benzyl, ethylthiomethylene or
- R4 is NH2 or OH.
2 more elements
A method for inhibiting protein prenylation in an organism comprising contacting an isoprenoid transferase with a protein prenylation inhibitory effective amount of a compound of the formula:
- or a pharmaceutically-acceptable salt thereof, wherein
- R1 is a halogenated phenyl;
- R2 is nitrogen, phenyl, pyrazole, methylpyrazole, dimethylpyrazole, pyridine, thiophene, dimethylcyclobutyl, dimethylcyclopropyl or cyclopropyl;
- R3 is benzyl, isopropyl, chlorobenzyl, methyl thiophene, trifluoro methyl benzyl, 3,5-trifluoromethyl benzyl, ethylthiomethylene or
- R4 is NH2 or OH.
2 more elements
Dependencies are inferred from the claim text.