1035040-49-3

Upstream product

• 1035040-47-1 (R)-N-(2-(2-((4-(4-chlorobenzyl)-1-oxophthalazin-2(1H)-yl)methyl)pyrrolidin-1-yl)ethyl)-2,2,2-trifluoroacetamide 
• 74-88-4 methyl iodide 
• 955359-79-2 4-[(4-chlorophenyl)methyl]-2-{[(2R)-2-pyrrolidinyl]methyl}-1(2H)-phthalazinone 

Downstream Products

• 1035040-52-8 (R)-N-(2-(2-((4-(4-chlorobenzyl)-1-oxophthalazin-2(1H)-yl)methyl)pyrrolidin-1-yl)ethyl)-4-methoxy-N-methylbutanamide trifluoroacetate salt 

Relevant academic research and scientific papers

Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis

The synthesis of potent amide-containing phthalazinone H1 histamine receptor antagonists is described. Three analogues 3e, 3g, and 9g were equipotent with azelastine and were longer-acting in vitro. Amide 3g had low oral bioavailability, low brain-penetration, high metabolic clearance, and long duration of action in vivo, and it was suitable for once-daily dosing intranasally, with a predicted dose for humans of approximately 0.5 mg per day.

4-BENZYL-1(2H)-PHTHALAZINONES AS H1 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula (I) and salts thereof, process for preparation thereof, to compositions containing the same and to the use of such a compound in the treatment of various diseases, such as allergic rhinitis.