183499-57-2

Usage

Uses

Used in Pharmaceutical Industry:
L-778123 is used as a therapeutic agent for controlling symptoms of psychosis and addiction in patients with psychiatric disorders such as schizophrenia and alcohol dependence. Its ability to effectively block the effects of dopamine on the D4 receptor contributes to its potential therapeutic implications in managing these conditions.
Used in Research and Development:
L-778123 is used as a research tool for studying the role of dopamine D4 receptors in various neurological and psychiatric conditions. Its high selectivity for the D4 receptor makes it valuable in exploring the underlying mechanisms of these disorders and identifying potential targets for treatment.

Upstream product

• 107-10-8 propylamine 
• 183500-70-1 1-(3-chlorophenyl)-2-piperazinone 
• 183500-36-9 4-(5-hydroxymethyl-imidazol-1-ylmethyl)-benzonitrile 
• 253862-99-6 N¹-(3-chlorophenyl)-N²-{[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl}-N²-(2-hydroxyethyl)glycinamide 
• 183500-94-9 1-(3-chlorophenyl)-2-piperazinone hydrochloride 
• 215649-70-0 N¹-(3-chlorophenyl)-N²-(2-hydroxyethyl)glycinamide 
• 108-42-9 3-chloro-aniline 
• 2564-05-8 2-chloro-N-(3-chlorophenyl)acetamide 

Downstream Products

• 183499-56-1 1-(3-chlorophenyl)-4-[1-(4-cyanobenzyl)-5-imidazolylmethyl]-2-piperazinone dihydrochloride 

Relevant academic research and scientific papers

Method of treating cancer

The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either s

Preparation of a clinically investigated ras farnesyl transferase inhibitor

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.

Method of treating cancer

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.

Radiolabeled farnesyl-protein transferase inhibitors

The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.

INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation 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 the farnesylation of the oncogene protein Ras