发明名称 PRODRUG-DERIVATER AF CARBOXYLSYRE-LAEGEMIDLER
摘要 <IMAGE> Previously unknown ester derivatives of carboxylic acid medicaments of the formula (I) where R-COO- denotes the acyloxy radical of a carboxylic acid medicament, n is an integer from 1 to 3, and R1 and R2 are identical or different and are selected from the class consisting of alkyl, alkenyl, aryl, aralkyl and cycloalkyl, which group can be unsubstituted or substituted, or R1 and R2, together with the N atom, form a 4-, 5-, 6- or 7-membered heterocyclic ring which, in addition to the nitrogen atom, can contain 1 or 2 further heteroatoms selected from a class consisting of nitrogen, oxygen and sulphur, which heterocyclic group can be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and have a strong tendency to undergo enzymic hydrolysis in vivo, while at the same time being very stable in aqueous solution. The previously unknown derivatives are less irritating for the mucous membranes than are the original carboxylic acids and can provide the medicaments with improved bioavailability. <IMAGE>
申请公布号 DK227088(A) 申请公布日期 1988.06.15
申请号 DK19880002270 申请日期 1988.04.26
申请人 BUNDGAARD, HANS;NIELSEN, NIELS MOERK 发明人 BUNDGAARD, HANS;NIELSEN, NIELS MOERK
分类号 C07C235/06;C07C235/08;C07C235/10;C07C235/12;C07D205/04;C07D207/08;C07D207/12;C07D207/16;C07D207/24;C07D209/26;C07D209/42;C07D211/16;C07D211/46;C07D295/10;C07D295/18;C07D295/185;C07D499/22;C07D499/32;(IPC1-7):C07C103/34;C07C103/38;C07C103/44;C07C103/48;C07C103/49 主分类号 C07C235/06
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