349125-08-2

Usage

Uses

Used in Medicinal Chemistry:
N-(5-Chloropyridin-2-yl)oxalamic acid ethyl ester is utilized as a chemical intermediate in the synthesis of various pharmaceutical agents. Its chloropyridine moiety and ester functionality can be leveraged to create novel compounds with potential therapeutic applications.
Used in Drug Discovery:
In the realm of drug discovery, N-(5-Chloropyridin-2-yl)oxalamic acid ethyl ester serves as a key building block for the development of new drugs. Its structural features may contribute to the design of molecules with specific biological activities, making it a valuable asset in the search for innovative therapeutic agents.
Used in Chemical Research:
N-(5-Chloropyridin-2-yl)oxalamic acid ethyl ester is employed as a research tool in chemical investigations. Its reactivity and functional groups can be explored to understand the underlying mechanisms of various chemical reactions and to develop new synthetic methodologies.
Used in Pharmaceutical Industry:
Within the pharmaceutical industry, N-(5-Chloropyridin-2-yl)oxalamic acid ethyl ester is used as a precursor for the production of active pharmaceutical ingredients. Its unique structure may be incorporated into drug molecules to enhance their efficacy, selectivity, or pharmacokinetic properties.
Used in Biochemical Studies:
N-(5-Chloropyridin-2-yl)oxalamic acid ethyl ester can be applied in biochemical research to probe the interactions between small molecules and biological targets. Its chloropyridine group may facilitate binding to specific enzymes or receptors, providing insights into the molecular basis of various diseases and potential therapeutic interventions.

Upstream product

• 1072-98-6 5-chloro-2-pyridylamine 
• 4755-77-5 Ethyl oxalyl chloride 

Downstream Products

• 552850-73-4 2-((5-chloropyridin-2-yl)amino)-2-oxoacetic acid 
• 480449-70-5 edoxaban 
• 480452-36-6 carbamic acid, N-[(1R,2S,5S)-2-[[2-[(5-chloro-2-pyridinyl)amino]-2-oxoacetyl]amino]-5-[(dimethylamino)carbonyl]cyclohexyl]-1,1-dimethylethyl ester 
• 480449-71-6 [14C]-Edoxaban tosylate 

Relevant academic research and scientific papers

Exploratory studies on soluble small molecule CD4 mimics as HIV entry inhibitors

Several small molecule CD4 mimics, which inhibit the interaction of gp120 with CD4, have been developed. Original CD4 mimics such as NBD-556, which has an aromatic ring, an oxalamide linker and a piperidine moiety, possess significant anti-HIV activity bu

Soluble-type small-molecule CD4 mimics as HIV entry inhibitors

Several small molecule CD4 mimics have been reported previously as HIV-1 entry inhibitors, which block the interaction between the Phe43 cavity of HIV-1 gp120 and the host CD4. Known CD4 mimics such as NBD-556 possess significant anti-HIV activity but are less soluble in water, perhaps due to their hydrophobic aromatic ring-containing structures. Compounds with a pyridinyl group in place of the phenyl group in these molecules have been designed and synthesized in an attempt to increase the hydrophilicity. Some of these new CD4 mimics, containing a tetramethylpiperidine ring show significantly higher water solubility than NBD-556 and have high anti-HIV activity and synergistic anti-HIV activity with a neutralizing antibody. The CD4 mimic that has a cyclohexylpiperidine ring and a 6-fluoropyridin-3-yl ring has high anti-HIV activity and no significant cytotoxicity. The present results will be useful in the future design and development of novel soluble-type molecule CD4 mimics.

Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase

Stearoyl-CoA desaturase (SCD) catalyzes the first step in the conversion of saturated fatty acids to unsaturated fatty acids. Unsaturated fatty acids are required for membrane integrity and for cell proliferation. For these reasons, inhibitors of SCD represent potential treatments for cancer. However, systemically active SCD inhibitors result in skin toxicity, which presents an obstacle to their development. We recently described a series of oxalic acid diamides that are converted into active SCD inhibitors within a subset of cancers by CYP4F11-mediated metabolism. Herein, we describe the optimization of the oxalic acid diamides and related N-acyl ureas and an analysis of the structure-activity relationships related to metabolic activation and SCD inhibition.

PROCESS FOR PRODUCING DIAMINE DERIVATIVE

The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a process for industrially producing a compound (1) represented by the following formula (1): wherein Boc represents a tert-butoxycarbonyl group.

LACTAM-CONTAINING CYCLIC DIAMINES AND DERIVATIVES AS FACTOR XA INHIBITORS

The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trysin-like serine proteases, specifically factor Xa.