474329-72-1

Usage

Chemical class

Piperazinecarboxylic acid derivative

Molecular weight

369.29 g/mol

Structure

Contains a piperazine ring, a benzene ring with nitro and trifluoromethyl substituents, and an ester group.

Usage

Building block in the synthesis of various drugs and active pharmaceutical ingredients.

Potential applications

Treatment of various diseases and health conditions due to its unique chemical structure and properties.

Mechanism of action

Targeting specific mechanisms within the human body.

Importance

Considered important in the field of medical research.

Pharmaceutical industry potential

Has potential for further development in the pharmaceutical industry.

Upstream product

• 367-86-2 1-fluoro-2-nitro-4-trifluoromethyl-benzene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 402-12-0 2-fluoro-1-nitro-4-(trifluoromethyl)benzene 
• 58315-38-1 1-(2-nitro-4-(trifluoromethyl)phenyl)piperazine 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 1253936-83-2 1-{4-[2-(2-methoxy-pyrimidin-5-yl)-4-trifluoromethyl-phenyl]piperazin-1-yl}-2-pyrrolo[2,3-b]pyridin-1-yl-ethanone 
• 1253936-66-1 1-[4-(2-bromo-4-trifluoromethyl-phenyl)-piperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-yl-ethanone 
• 1253936-64-9 4-(2-bromo-4-(trifluoromethyl)phenyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1253936-65-0 1-(2-bromo-4-(trifluoromethyl)phenyl)piperazine 
• 862874-74-6 tert-butyl 4-(2-amino-4-(trifluoromethyl)phenyl)piperazine-1-carboxylate 

Relevant academic research and scientific papers

Novel pyrazole amide compound and preparation thereof, and application of novel pyrazole amide compound in prevention and treatment of plant pathogenic diseases and pest killing

The invention relates to a novel pyrazole amide compound I and a preparation method thereof and application of the novel pyrazole amide compound I in prevention and treatment of plant pathogenic disease and pest killing. The novel pyrazole amide compound

Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity

Malaria is a devastating parasitic disease caused by parasites from the genus Plasmodium. Therapeutic resistance has been reported against all clinically available antimalarials, threatening our ability to control the disease and therefore there is an ongoing need for the development of novel antimalarials. Towards this goal, we identified the 2-(N-phenyl carboxamide) triazolopyrimidine class from a high throughput screen of the Janssen Jumpstarter library against the asexual stages of the P. falciparum parasite. Here we describe the structure activity relationship of the identified class and the optimisation of asexual stage activity while maintaining selectivity against the human HepG2 cell line. The most potent analogues from this study were shown to exhibit equipotent activity against P. falciparum multidrug resistant strains and P. knowlesi asexual parasites. Asexual stage phenotyping studies determined the triazolopyrimidine class arrests parasites at the trophozoite stage, but it is likely these parasites are still metabolically active until the second asexual cycle, and thus have a moderate to slow onset of action. Non-NADPH dependent degradation of the central carboxamide and low aqueous solubility was observed in in vitro ADME profiling. A significant challenge remains to correct these liabilities for further advancement of the 2-(N-phenyl carboxamide) triazolopyrimidine scaffold as a potential moderate to slow acting partner in a curative or prophylactic antimalarial treatment.

CXCR3 RECEPTOR ANTAGONISTS

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising the

PIM KINASE INHIBITORS AND METHODS OF THEIR USE

New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase- mediated disorder, such as cancer.

BISARYLUREA DERIVATIVES

The present invention relates to bisarylurea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

INHIBITORS OF BACE

The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer's Disease and other BACE-mediated diseases.