876919-10-7

Usage

Uses

Used in Pharmaceutical Industry:
2-CHLORO-5-FLUOROISONICOTINIC ACID METHYL ESTER is used as a key intermediate in the synthesis of various pharmaceuticals for its potential to contribute to the development of new drugs. Its unique chemical structure and reactivity allow for the creation of compounds with specific therapeutic properties, enhancing the range of treatments available for various medical conditions.
Used in Agrochemical Industry:
In the agrochemical sector, 2-CHLORO-5-FLUOROISONICOTINIC ACID METHYL ESTER is utilized as a building block in the formulation of pesticides. Its incorporation into these products helps in the development of effective and targeted pest control solutions, contributing to improved crop protection and agricultural yield.
Used in Medicinal Chemistry Research:
2-CHLORO-5-FLUOROISONICOTINIC ACID METHYL ESTER is employed as a research compound in medicinal chemistry. Its unique properties make it a valuable tool for exploring new drug candidates and understanding the mechanisms of action for potential therapeutic agents.
Used in Agricultural Chemistry Research:
Similarly, in agricultural chemistry, 2-CHLORO-5-FLUOROISONICOTINIC ACID METHYL ESTER is used for research purposes. It aids in the investigation of new pesticide formulations and the optimization of existing ones, ensuring the development of more effective and environmentally friendly agrochemicals.

InChI:InChI=1/C7H5ClFNO2/c1-12-7(11)4-2-6(8)10-3-5(4)9/h2-3H,1H3

Upstream product

• 876919-08-3 methyl 3-fluoropyridine-4-carboxylate 
• 67-56-1 methanol 
• 884494-74-0 2-chloro-5-fluoro-pyridine-4-carboxylic acid 

Relevant academic research and scientific papers

Fluorinated derivatives of pyridine-2,4-dicarboxylate are potent inhibitors of human 2-oxoglutarate dependent oxygenases

2-Oxoglutarate (2OG) oxygenases have important roles in human biology and are validated medicinal chemistry targets. Improving the selectivity profile of broad-spectrum 2OG oxygenase inhibitors may help enable the identification of selective inhibitors for use in functional assignment work. We report the synthesis of F- and CF3-substituted derivatives of the broad-spectrum 2OG oxygenase inhibitor pyridine-2,4-dicarboxylate (2,4-PDCA). Their inhibition selectivity profile against selected functionally distinct human 2OG oxygenases was determined using mass spectrometry-based assays. F-substituted 2,4-PDCA derivatives efficiently inhibit the 2OG oxygenases aspartate/asparagine-β-hydroxylase (AspH) and the JmjC lysine-specific Nε-demethylase 4E (KDM4E); The F- and CF3-substituted 2,4-PDCA derivatives were all less efficient inhibitors of the tested 2OG oxygenases than 2,4-PDCA itself, except for the C5 F-substituted 2,4-PDCA derivative which inhibited AspH with a similar efficiency as 2,4-PDCA. Notably, the introduction of a F- or CF3-substituent at the C5 position of 2,4-PDCA results in a substantial increase in selectivity for AspH over KDM4E compared to 2,4-PDCA. Crystallographic studies inform on the structural basis of our observations, which exemplifies how a small change on a 2OG analogue can make a substantial difference in the potency of 2OG oxygenase inhibition.

REMEDY OR PREVENTIVE FOR DIGESTIVE ULCER

An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety. The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric/duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.

2-PHENYLPYRIDINE DERIVATIVE

The present invention relates to a novel 2-phenylpyridine derivative or a salt thereof, wherein the pyridine ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.

2-PHENYLPYRIDINE DERIVATIVE

A 2-phenylpyridine derivative represented by the following general formula (I) or a salt thereof. The compounds have satisfactory xanthine oxidase inhibitory activity and uric acid-lowering activity and are useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory intestinal diseases, diabetic nephropathy, diabetic retinopathy, etc. [The symbols in the formula have the following meanings: R1: H, etc.; R2: -CO2H, etc.; R3 and R4: H, etc.; R5: -CN, etc.; R6: H, etc.; X: -O-, -N(R8)-, or -S-; (provided that the groups represented by R5 and -X-R7 are bonded in a meta position or the para position to the pyridyl group) R8: H, etc.; R7: C1-8 linear or branched alkyl, etc.; Y: a bond, etc.; and R9, R10, and R11: H, etc. (provided that when X is -N(R8)-, then R8 may be bonded to R7 to form a nitrogenous saturated heterocycle in cooperation with the adjacent nitrogen atom).]