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1. WO2008012605 - PROMÉDICAMENTS HYDROSOLUBLES À CHARGE POSITIVE DE KÉTOPROFÈNE ET COMPOSÉS ASSOCIÉS À VITESSE DE PÉNÉTRATION CUTANÉE TRÈS RAPIDE

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Claims
[1] The compounds of the general formula (1) 'Structure 1'


Structure 1
In structure 1, R represents H, one of any alkyl, alkyl, alkenyl or alkynyl
residues having 1 to 12 carbon atoms, or aryl residues; R represents H, one of
any alkyl, alkyloxy, alkenyl or alkynyl residues having 1 to 12 carbon atoms, or aryl residues; R represents H, one of any alkyl, alkyloxy, alkenyl or alkynyl
residues having 1 to 12 carbon atoms, or aryl residues; R 4 represents



, X represents O, S or NH; A" represents Cl", Br", F", I", AcO", citrate, or any
negative ions; and n=0,l,2,3,4,5,6,7,8,9,10 All R groups may include C, H,

O, S, N atoms and may have single, double, and treble bonds. Any CH groups may be replaced with O, S, or NH
[2] Process for the preparation of compounds of the general formula (1) 'Structure 1' according to Claim 1.
[3] Compounds of the general 'Structure 1' or a composition comprising of at least one compound of the general formula (1) 'Structure 1', as an active ingredient,
according to Claim 1, where they can be administered orally or transdermally,
for treating any ketoprofen and fenoprofen-treatable conditions in humans or
animals. The ketoprofen and fenoprofen-treatable conditions include, but are not limited to, pain from a toothache, headache, and arthritis and other inflammatory pain, fever, cancer, dysmenorrhea, radiation-induced vomiting, diabetic
neuropathy and acute migraine headache, hemophilic arthropathy, bone loss, and sunburn.
[4] Methods for treating any ketoprofen and fenoprofen-treatable conditions in humans or animals by administering transdermally to any part of body (in the
from of a solution, spray, lotion, ointment, emulsion or gel) to deliver therapeutically effective plasma levels of compounds of the general formula (1)
'Structure 1' according to Claim 1.
[5] Methods for topically treating pain such as a headache, toothache, and muscle
pain, and arthritis and other inflammatory pain in humans or animals by administering to the inflamed area a therapeutically effective amount of the
compounds of the general formula (1) 'Structure 1' or a composition comprising of at least one compound of the general formula (1) 'Structure 1', as an active
ingredient, according to Claim 1.
[6] Compounds of the general formula (1) 'Structure 1' or a composition comprising of at least one compound of the general formula (1) 'Structure 1', as an active
ingredient, according to Claim 1, may be administered transdermally, for treating acne, sunburn or other skin disorders in the from of a solution, spray, lotion, oin tment, emulsion or gel.
[7] Compounds of the general 'Structure 1' or a composition comprising of at least one compound of the general formula (1) 'Structure 1', as an active ingredient,
according to Claim 1, are administered by spraying to through the mouth or nose or other parts of body for treating asthma.
[8] Compounds of the general 'Structure 1' or a composition comprising of at least one compound of the general formula (1) 'Structure 1', as an active ingredient,
according to Claim 1, for treating any eye inflammatory diseases, for treating of ocular pain after corneal surgery, for treating glaucoma or for treating ear inflammatory and/or painful conditions (otitis) in humans or animals.
[9] Transdermal therapeutic application systems of Compounds of the general
formula (1) 'Structure 1' or a composition comprising of at least one compound of the general formula(l) 'Structure 1', as an active ingredient, according to claim 1, for treating any kenoprofen and fenoprofen-treatable conditions in humans or animals. These systems can be a bandage or a patch comprising of one active
substance-containing matrix layer and an impermeable backing layer. The most preferable system is an active substance reservoir, which has a permeable bottom facing the skin. By controlling the rate of release, this system enables the
ketoprofen and fenoprofen to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of ketoprofen and fenoprofen.