252882-62-5Relevant academic research and scientific papers
Method of treating cancer
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, (2008/06/13)
The present invention relates to methods of treating cancer using a combination of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase. The invention also relates to methods of preparing such compositions.
Preparation of a clinically investigated ras farnesyl transferase inhibitor
Maligres, Peter E.,Waters, Marjorie S.,Weissman, Steven A.,McWilliams, J. Christopher,Lewis, Stephanie,Cowen, Jennifer,Reamer, Robert A.,Volante,Reider, Paul J.,Askin, David
, p. 229 - 241 (2007/10/03)
The synthesis of ras farnesyl-protein transferase inhibitor 1 is described on a multi-kilogram scale. Retrosynthetic analysis reveals chloromethylimidazole 2 and a piperazinone 3 as viable precursors. The 1,5-disubstituted imidazole system was regioselectively assembled via an improved Marckwald imidazole synthesis. A new imidazole dethionation procedure has been developed to convert the Marckwald mercaptoimidazole product to the desired imidazole. This methodology was found to be tolerant of a variety of functional groups providing good to excellent yields of 1,5-disubstituted imidazoles. A new Mitsunobu cyclization strategy was developed to prepare the arylpiperazinone fragment 3.
INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
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Page column 60, (2010/01/21)
The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer
Geranylgeranyl transferase inhibitor screening assay
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, (2008/06/13)
The present invention is directed toward a GGTase-I competitive binding assay which can be used to determine the relative GGTase-I inhibitory potency of test compounds. The present invention is also directed toward radiolabeled geranylgeranyl-protein transferase type-I inhibitor compounds which are useful to label GGTase-I in assays, whether cell-based, tissue-based or in whole animal.
Sustained release drug dispersion delivery device
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, (2008/06/13)
The present invention is related to a drug delivery device, that is pH insensitive, for the sustained in situ production and release of a dispersion, in an environment of use, which comprises a) a compressed core prepared from an admixture comprising i) a
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention is directed to conformationally constrained compounds which inhibit prenyl-protein transferase 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 prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Process for making 1,5-disubstituted imidazoles
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, (2008/06/13)
The present invention is directed to a process for synthesizing 1,5-disubstituted imidazoles, which are useful in the preparation of farnesyl-protein transferase inhibitors.
