1016-36-0

Usage

Uses

Used in Pharmaceutical Research and Drug Development:
ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE is used as a key intermediate in the synthesis of potential therapeutic agents, particularly for the development of new chemical entities with pharmacological activity. Its unique structure and properties make it a valuable building block in the creation of novel drug candidates.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE is employed as a versatile intermediate for the preparation of various drug candidates. Its ethyl ester group enhances solubility and bioavailability, facilitating the development of more effective and safer medications.
Used in Chemical Synthesis:
ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE is utilized as a synthetic building block in the creation of new chemical entities with potential applications in various industries, including pharmaceuticals, agrochemicals, and materials science.
Used in Drug Design and Optimization:
In drug design and optimization processes, ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE is employed as a structural component to improve the pharmacokinetic and pharmacodynamic properties of drug candidates, enhancing their therapeutic potential and safety profiles.
Used in Biochemical Research:
ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE is also used in biochemical research to study the interactions between small molecules and biological targets, providing insights into the development of targeted therapies and understanding the molecular mechanisms of diseases.

Upstream product

• 443-69-6 5-fluoro-1H-indole-2,3-dione 
• 64-17-5 ethanol 
• 1077-96-9 5-fluoro-1H-indazole-3-carboxylic acid 

Downstream Products

• 1021390-29-3 1-(5-chloro-2-methoxy-benzyl)-5-fluoro-1H-indazole-3-carboxylic acid ethyl ester 
• 1448314-60-0 5-fluoro-1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase

Human neutrophil elastase (HNE) is an important therapeutic target for treatment of pulmonary diseases. Previously, we identified novel N-benzoylindazole derivatives as potent, competitive, and pseudoirreversible HNE inhibitors. Here, we report further development of these inhibitors with improved potency, protease selectivity, and stability compared to our previous leads. Introduction of a variety of substituents at position 5 of the indazole resulted in the potent inhibitor 20f (IC50 ～10 nM) and modifications at position 3 resulted the most potent compound in this series, the 3-CN derivative 5b (IC50 = 7 nM); both derivatives demonstrated good stability and specificity for HNE versus other serine proteases. Molecular docking of selected N-benzoylindazoles into the HNE binding domain suggested that inhibitory activity depended on geometry of the ligand-enzyme complexes. Indeed, the ability of a ligand to form a Michaelis complex and favorable conditions for proton transfer between Hys57, Asp102, and Ser195 both affected activity.

Aryl Substituted Indoles and Their Use as Blockers of Sodium Channels

The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

INDAZOLE DERIVATIVES

The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologic

INDAZOLECARBOXAMIDE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS

This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such