1285513-38-3

Usage

Uses

Used in Pharmaceutical Industry:
2-(benzyloxy)-5-bromo-N-(pyridazin-4-yl)benzamide is used as a potential pharmaceutical agent for its structural features that may contribute to therapeutic effects. The presence of the benzyl ether, bromo substituent, and pyridazine-4-yl group could provide specific binding affinities or interactions with biological targets, making it a candidate for the development of new drugs.
The specific application reasons and types, such as its use as an anticancer agent, anti-inflammatory, or for other therapeutic purposes, would depend on the results of further research into its biological activity and pharmacological profile. As of the provided information, no specific uses have been detailed, but the compound's structural elements suggest it may be explored for various medicinal chemistry applications.

Upstream product

• 850350-09-3 phenylmethyl 5-bromo-2-[(phenylmethyl)oxy]benzoate 
• 20744-39-2 4-aminopyridazine 
• 62176-31-2 5-bromo-2-[(phenylmethyl)oxy]benzoic acid 
• 89-55-4 5-bromosalicyclic acid 

Downstream Products

• 1285514-64-8 2-[(phenylmethyl)oxy]-N-4-pyridazinyl-5-(4-pyridinyl)benzamide 
• 1285514-61-5 5-(1-methyl-1H-pyrazol-4-yl)-2-[(phenylmethyl)oxy]-N-4-pyridazinylbenzamide 

Relevant academic research and scientific papers

5-Substituted-N-pyridazinylbenzamides as potent and selective LRRK2 inhibitors: Improved brain unbound fraction enables efficacy

We describe the discovery and optimization of 5-substituted-N-pyridazinylbenzamide derivatives as potent and selective LRRK2 inhibitors. Extensive SAR studies led to the identification of compounds 18 and 23, which demonstrated good in vitro pharmacokinetic profile and excellent selectivity over 140 other kinases. Both compounds demonstrated high unbound fractions in both blood and brain. Compound 18 proved to be brain penetrant, and the high unbound fraction of compound 18 in brain enabled its in vivo efficacy in CNS, wherein a significant inhibition of LRRK2 Ser935 phosphorylation was observed in rat brain following intravenous infusion at 5 mg/kg/h.

Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors

Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson's disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.

NOVEL COMPOUNDS

The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.