261956-65-4

Upstream product

• 52334-81-3 2-chloro-5-trifluoromethylpyridine 
• 144-55-8 sodium hydrogencarbonate 

Downstream Products

• 52334-81-3 2-chloro-5-trifluoromethylpyridine 
• 1076234-45-1 3,4-dimethyl-1-{[6-phenyl-5-(trifluoromethyl)(2-pyridyl)]amino}azoline-2,5-dione 
• 1076234-34-8 1-{[6-chloro-5-(trifluoromethyl)(2-pyridyl)]amino}-3,4-di-methylazoline-2,5-dione 
• 55304-75-1 2,6-dichloro-3-(trifluoromethyl)pyridine 

Relevant academic research and scientific papers

SUBSTITUTED AZOLE DIONE COMPOUNDS WITH ANTIVIRAL ACTIVITY

Provided herein are methods of using substituted azole dione compounds for treatment of viral infections.

New 2-Thiopyridines as potential candidates for killing both actively growing and dormant mycobacterium tuberculosis cells

From in vivo observations, a majority of M. tuberculosis cells in latently infected individuals are in a dormant and probably nonculturable state, display little metabolic activity, and are phenotypically resistant to antibiotics. Despite many attempts, no specific antimicrobials effective against latent tuberculosis have yet been found, partly because of a lack of reliable and adequate in vitro models for screening of drug candidates. We propose here a novel in vitro model of M. tuberculosis dormancy that meets the important criteria of latency, namely, nonculturability of cells, considerable reduction of metabolic activity, and significant phenotypic resistance to the first-line antibiotics rifampin and isoniazid. Using this model, we found a new group of 2-thiopyridine derivatives that had potent antibacterial activity against both actively growing and dormant M. tuberculosis cells. By means of the model of M. tuberculosis nonculturability, several new 2-thiopyridine derivatives were found to have potent antitubercular activity. The compounds are effective against both active and dormant M. tuberculosis cells. The bactericidal effects of compounds against dormant M. tuberculosis was confirmed by using three different in vitro models of tuberculosis dormancy. The model of nonculturability could be used as a reliable tool for screening drug candidates, and 2-thiopyridine derivatives may be regarded as prominent compounds for further development of new drugs for curing latent M. tuberculosis infection.

Fluorescence polarization for the evaluation of small-molecule inhibitors of PCAF BRD/Tat-AcK50 association

A fluorescence polarization competitive assay was developed to efficiently screen and evaluate inhibitors of PCAF bromodomain/Tat-AcK50 protein-peptide interaction. A series of pyridine 1-oxide derivatives were synthesized and evaluated. Some of the novel

A novel reagent combination for the oxidation of highly electron deficient pyridines to N-oxides: trifluoromethanesulfonic anhydride/sodium percarbonate

A novel reagent combination, Tf2O/Na2CO3·1.5H2O2, has been developed for the oxidation of highly electron deficient pyridines to their corresponding N-oxides. The N-oxidation reaction, utilizing the in situ generated peracid, proceeds under mild conditions that allow for a number of functional groups and substitution patterns on the pyridine ring.

Compounds with anti-cancer activity

Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.

SUBSTITUTED BIARYL QUINOLIN-4-YLAMINE ANALOGUES

Substituted biaryl quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Fluorinated pyridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls

The present invention describes compounds of Formula I or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.

PROLINE DERIVATIVES AND USE THEREOF AS DRUGS

The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

A practical, efficient, and rapid method for the oxidation of electron deficient pyridines using trifluoroacetic anhydride and hydrogen peroxide- urea complex

A general method for the oxidation of electron-poor pyridines to their N-oxides using UHP and TFAA in either CH2Cl2 or CH3CN was developed. The methodology proved to tolerate a number of functional groups and substitution

Herbicidal heterocyclic N-oxides compounds

This invention relates to novel optionally substituted heterocyclic N-oxide compounds of formula (I): wherein: R, R1, R2, R3, R4, R5, R6, R7, A, X, Z and m are defined herein. In other aspects, this invention relates to herbicidal compositions containing a optionally substituted heterocyclic N-oxide compound or derivative thereof and an agriculturally acceptable carrier and to a method of controlling undesirable vegetation by applying to an area where control is desired an herbicidally effective amount of an optionally substituted heterocyclic N-oxide compound or derivative thereof.