Prodrugs of non-steroidal anti-inflammatory agents (NSAIDs)

摘要

Compound of formula (I): ** Formula ** in which: R1 represents a unit that promotes the selected immobility of an organic moiety with a molecular weight of less than 1000 g / mol comprising one or more nitrogen-containing moieties each with a pKa between 4 and 7.6 at 37 ° C; and R1 is phenylamino, imidazolyl, isoquinolinyl, quinolinyl, benzimidazolyl, substituted or unsubstituted acridinyl according to the following structures: ** Formula ** wherein R3 is linear or branched C1-8 alkyl, or alkoxyalkyl, R4 and R5 are each and independently from each other hydrogen, linear or branched C1-8 alkyl, alkoxyalkyl or phenyl; and R3, which is located between the core of IPU and the NSAID, can be attached at any point to the core of IPU, either in a carbon atom or nitrogen in the ring; -O- (C = O) -R2 represents an acyloxy residue of a carboxylic acid group contained within a non-steroidal anti-inflammatory agent (NSAID) selected from the list consisting of: ketorolac, ketoprofen, fenoprofen, oxaprofen, diclofenac, tolmetin, tolfenamic acid, mefenamic acid, sulindac, indomethacin, acetylsalicylic acid, deflunisal, loxoprofen, indoprofen, priprofeno, clidanac, fenclorac, meclofenamate, benoxaprofen, carprofen, isofezolac, aceclofenac, fenbufen, etodólico acid, fleclózico acid, amfenac, mácido efenámico, Bromfenac, flenclofenac, alcofenac, orpanoxin, zomopyraco, flufenamic acid, niflumic acid, pranoprofen, zaltoprofen and suprofen, x is an integer selected from 1, 2, 3 or 4; wherein R1 contains an R3-OH group, which together with the NSAID carboxylic function forms the ester bond, and in which R3 is different from -CH2-OH when R3 binds to the nitrogen of R1; and salts, solvates and hydrates thereof.