1044136-99-3

Upstream product

• 923288-55-5 3,4-bis(benzyloxy)-5-nitrobenzoic acid 
• 1229803-77-3 C₂₉H₂₄Cl₂N₄O₆ 
• 923288-59-9 2,5-dichloro-N'-hydroxy-4,6-dimethylnicotinimidamide 

Downstream Products

• 1044137-00-9 3-(5-(3,4-bis(benzyloxy)-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-2,5-dichloro-4,6-dimethylpyridine 1-oxide 

Relevant academic research and scientific papers

Administration regime for nitrocatechols

A compound of formula (I) where R1, R2, X, Y, n, m, R3, R4, R5, R6 and R7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.

Discovery of a long-acting, peripherally selective inhibitor of catechol- O -methyltransferase

Novel nitrocatechol-substituted heterocycles were designed and evaluated for their ability to inhibit catechol-O-methyltransferase (COMT). Replacement of the pyrazole core of the initial hit 4 with a 1,2,4-oxadiazole ring resulted in a series of compounds endowed with longer duration of COMT inhibition. Incorporation of a pyridine N-oxide residue at position 3 of the 1,2,4-oxadiazole ring led to analogue 37f, which was found to possess activity comparable to entacapone and lower toxicity in comparison to tolcapone. Lead structure 37f was systematically modified in order to improve selectivity and duration of COMT inhibition as well as to minimize toxicity. Oxadiazole 37d (2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4, 6-dimethylpyridine 1-oxide (BIA 9-1067)) was identified as a long-acting, purely peripheral inhibitor, which is currently under clinical evaluation as an adjunct to l-Dopa therapy of Parkinson's disease.

DOSAGE REGIMEN FOR COMT INHIBITORS

The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.