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Water-soluble prodrugs positively charged with n-arylanthranilic acids with very rapid penetration rate into the skin
专利权人:
Techfields Biochem Co. Ltd;Yu, Chongxi
发明人:
YU, Chongxi,XU, Lina,YU CHONGXI,XU LINA
申请号:
ES06795893
公开号:
ES2694685T3
申请日:
2006.09.03
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound having a general formula of Structure 1 ** Formula ** in which a) R1 represents H; R2 represents H, an alkyl, alkyloxy, alkenyl or alkynyl residue having 1 to 12 carbon atoms, or an aryl residue; R3 represents H, an alkyl, alkyloxy, alkenyl or alkynyl residue having 1 to 12 carbon atoms, or an aryl residue; X represents O, S, or NH; A- represents Cl-, Br-, F-, I-, AcO-, citrate, or a negative ion; Y1 represents H, Cl, F, CH3, C2H5, or CF3; Y2 represents H, Cl, F, CH3, C2H5, or CF3; Y3 represents H, Cl, F, CH3, C2H5, or CF3; Z represents CH; and n>; = 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 or a composition comprising at least one compound having the general formula of Structure 1 as an active ingredient for use in a method for treating a condition treatable with a nonsteroidal anti-inflammatory agent (NSAIA) in a subject, in which the subject is human or animal, the compound or composition is administered transdermally, and the condition treatable with a nonsteroidal anti-inflammatory agent (NSAIA) is selected from the group consisting of pain, toothache, headache, arthritis pain, inflammatory pain, fever, cancer, dysmenorrhea, radiation-induced vomiting, diabetic neuropathy, acute migraine, hemophilic arthropathy, bone loss, sunburn, inflammatory diseases of the eyes, eye pain after corneal surgery, glaucoma, inflammatory and painful conditions of the ear. (otitis) in a subject, rheumatoid arthritis, osteoarthritis psoriasis, acne, sunburn, and other skin disorders; or b) R1 represents H; R2 represents H, an alkyl, alkyloxy, alkenyl or alkynyl residue having 1 to 12 carbon atoms, or an aryl residue; R3 represents H, an alkyl, alkyloxy, alkenyl or alkynyl residue having 1 to 12 carbon atoms, or an aryl residue; X represents S or NH; A- represents Cl-, Br-, F-, I-, AcO-, citrate, or a negative ion; Y1 represents H, Cl, F, CH3, C2H5, or CF3; Y2 represents H, Cl, F, CH3, C2H5, or CF3; Y3 represents Cl, F, CH3, C2H5, or CF3; Z represents CH or N; and n>; = 0,
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