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filingDate 2007-06-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2019-05-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2019-05-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-105669531-B
titleOfInvention The prodrug of non-steroidal anti-inflammatory drugs with fast skin and membranes penetration speed and its new medical usage
abstract " prodrug of the novel positively charged non-steroidal anti-inflammatory drugs of these in structural formula 1,2a, 2b, 2c or 2d " has been designed and has synthesized general formula (1,2a, 2b, 2c or 2d)." compound represented by structural formula 1,2a, 2b, 2c or 2d " can react preparation with halide appropriate by the metal salt, organic alkali salt or immobilization alkali salt of non-steroidal anti-inflammatory drugs to above-mentioned general formula (1,2a, 2b, 2c or 2d).Positively charged amino in the present invention in prodrug greatly increases the solubility of these drugs in water, but also can be in conjunction with the negative electrical charge on the phosphate end group of biomembrane.Thus, local concentration of the drug on the outside of biomembrane or skin very high can be diffused into low concentration region from high concentration region to be conducive to these prodrugs.This combination can upset biomembrane slightly to concede segment space for the fatty contents of prodrug.When the molecule of biomembrane is mobile, due to the combination of prodrug, the amino that biomembrane can slightly be squeezed when amino is not protonated, in prodrug can be separated with the phosphate end group of biomembrane, and prodrug will be completely into biomembrane.When the amino in prodrug is moved to the other side of biomembrane and is therefore protonated, prodrug can be drawn into cytoplasm, in a kind of aqueous solution or suspension of semi liquid state.These prodrugs can be used for treating and preventing diabetes (I- type and/or II-type), pathoglycemia and dyslipidemia, apoplexy, myocardial infarction and other hearts and cardiovascular disease, alzheimer's disease, Parkinson's disease and other neurodegenerative diseases, psoriasis, lupus erythematosus discoides, systemic loupus erythematosus (SLE), oneself immunity hepatitis, multiple sclerosis (MS), with other autoimmune diseases, amyotrophic lateral sclerosis (ALS), oculopharyngeal muscular dystrophy (OPMD), it is abnormal with other muscle, the hemorrhoid of inflammation, cryptitis, other anorectal inflammatory states, pruritus ani, prostatitis, prostatocystitis, varication, oneself immunity hepatitis, autoimmune nephritis, phlebitis and other inflammation, cutaneum carcinoma, breast cancer, colon-rectum, mouthful Chamber cancer and other cancers, scar, blood vessel cutaneous lesions exception, birthmark, black mole (pigment) these prodrugs can direct cutaneous penetrations without dermal osmosis accelerator.
priorityDate 2007-06-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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