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filingDate 2007-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2016-06-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2016-06-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-101595217-B
titleOfInvention There is positively charged water miscible 1H-imidazo [4,5-c] the quinolin-4-amines class of rapid skin penetration speed and the prodrug of related compound thereof
abstract Novel be designed with 1H-imidazo [4,5-c] the quinolin-4-amines class of positive charge and the prodrug of related compound thereof and synthesized in formula (1) " structural formula 1 " or formula (2) " structural formula 2 ". Compound represented by above-mentioned formula (1) " structural formula 1 " or formula (2) " structural formula 2 ", it is possible to by 1H-imidazo [4,5-c] quinolin-4-amines class and related compound thereof, prepares with suitable acetic anhydride or excess acetyl chloride. Amino positively charged in prodrugs not only substantially increases medicine dissolubility in water, and can be combined with the negative charge of biomembranous phosphate head. This bonding action can change biomembrane slightly, concedes a part of space to the fatty contents of prodrug. When biomembrane molecule moves, the reason combined because of prodrug can make biomembrane slight " splitting ". This can make prodrug insert biomembrane. When pH value 7.4, only the amino of about 99% can be protonated. When amino is not protonated, the amino in prodrug can separate with the combination of biomembranous phosphate head structure, so that prodrug is completely in biomembrane. When the amino of these prodrugs penetrate biomembranous opposite side and therefore and protonate after, prodrug can be drawn into Cytoplasm, the concentrated aqueous solution of a kind of semi liquid state or suspension. Experimental result display prodrug passes through the speed of human body skin than 1H-imidazo [4,5-c] quinolin-4-amines class and fast about 25 times of related compound thereof. In blood plasma, these prodrugs more than 90% can return to female medicine structure within a few minutes. These prodrugs can be used for treating the state of any 1H-imidazo [4,5-c] quinolin-4-amines class of human or animal and related compounds-treatable thereof. In the treatment, these prodrugs can pass through transdermal administration, thus avoiding most of side effect produced by 1H-imidazo [4,5-c] quinolin-4-amines class and related compound thereof. The 1H-imidazo [4 in blood can be made by the controlled release transdermal drug-supplying system of prodrug, 5-c] concentration of quinolin-4-amines class and related compound thereof is stable in best treatment concentration, promote curative effect and reduce 1H-imidazo [4,5-c] quinolin-4-amines class and the side effect of related compound generation thereof.
priorityDate 2007-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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