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US 6,387,903 B1Granted
Inhibitors of prenyl-protein transferase
AssigneeMerck & Co., Inc.
InventorsChristopher J Dinsmore, John H. Hutchinson, Theresa M. Williams
Life of this patent
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Abstract
The present invention is directed to compounds which inhibit prenyl-protein transferases, farnesyl-protein transferase and geranylgeranyl-protein transferase type I, and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I and the prenylation of the oncogene protein RAS.
Claims12
A compound which inhibits farnesyl-protein transferase which is:
- 1-(3 -Trifluoromethoxyphenyl)-4-[1-(4-cyanobenzyl)imidazolylmethyl]-2 -piperazinone
- 1-(2,5-Dimethylphenyl)-4-[1-(4-cyanobenzyl)imidazolylmethyl]-2-piperazinone
- 1-(3-Methylphenyl)-4-[1-(4-yanobenzyl)imidazolylmethyl]-2-piperazinone
- 1-(3-Iodophenyl)4-[1-(4-cyanobenzyl)imidazolylmethyl]-2-piperazinone
- 1-(3-Chlorophenyl)-4-[1-(3-methoxy-4-cyanobenzyl)imidazolylmethyl]-2-piperazinone
- 1-(3-Trifluoromethoxyphenyl)-4-[1-( 3-methoxy-4-cyanobenzyl)imidazolylmethyl]-2-piperazinone
- (R)-5-[(Benzyloxy)methyl]-1-(3-chlorophenyl)4-[1-(4-cyanobenzyl)-imidazolylmethyl]-2-piperazinone
- 1-(3-Chlorophenyl)-4-[1-(2-fluoro-4-cyanobenzyl)-1H-imidazol-5-ylmethyl]piperazin-2-one
- 4-[1-(4-Cyanobenzyl)-1H-imidazol-5-ylmethyl]-1-(3-methylthiophenyl)piperazin-2-one
- 4-[1-(4-Cyanobenzyl)-1H-imidazol-5-ylmethyl]-1-(3,5-dichlorophenyl)piperazin-2-one
- 1-(3-Chlorophenyl)-4-{[1-(4-cyanophenyl) 1-ethyl1-1H-imidazol-5-ylmethyl}piperazin-2-one
- 1-(3-Chloro-4-fluorophenyl)-4-[1-(4-cyanobenzyl)-1H-imidazol-5-ylmethyl]piperazin-2-one
- 4-[1-(4-Cyanobenzyl)-1H-imidazol-5-ylmethyl]-1-(3,5-dimethylphenyl)piperazin-2-one
- (S)-5-Benzyl-4-[3-(4-cyanobenzyl-1-imidazol-5-yl)prop-1-phenyl-2-piperazinone
- 1-(3-Chlorophenyl)4-[1-(4nitrobenzyl)-1H-imidazol-5-ylmethyl]piperazin-2-one
- 4-[1-(4-Cyanobenzyl)-1H-imidazol-5-ylmethyl]-1-(3,5-difluorophenyl)piperazin-2-one or
- 4-[1-(4-Cyanobenzyl)-1H-imidazol-5-ylmethyl]-1-(3,4-difluorophenyl)piperazin-2-one
- or a pharmaceutically acceptable salt or optical isomer thereof.
15 more elements
Dependencies are inferred from the claim text.