发明名称 COMPOUNDS CONTAINING LACTIC ACID ELEMENTS, METHOD FOR THE PRODUCTION AND USE THEREOF AS PHARMACEUTICALLY ACTIVE SUBSTANCES
摘要 The invention relates to compounds that contain lactic acid elements and that have the general formula (I), wherein is 1 to 16, and * means the chiral center of the lactic acid elements. The lactic acid elements are present on the chiral center either in a uniform or different configuration, optionally in the form of diastereomeric mixtures, wherein R1 represents either the acyl group of an active substance that is reactive under acidic conditions, and then X represents oxygen and R2 represents hydrogen or a straight-chain or branched alkyl group having 1 to 8 carbon atoms, or wherein R1 represents hydrogen, if X represents oxygen or NR', and R2 represents an active substance having a hydroxyl group (X represents oxygen) esterified with the lactic acid element or an active substance having an amine group (X represents NR') amidified with the lactic acid elements, wherein R' represents hydrogen for active substances of the primary amine type and for substances of the secondary amine type, and, if the secondary amine is not cyclic, represents the group on the amine group of the active substance, and, if the secondary amine is cyclic, represents the covalent bond of nitrogen to R2, in which case the general formula (I) defines a cyclic secondary amine. The compounds of general formula (I) can be produced from lactic acid oligomers or dimers in a simple manner. The invention further relates to drugs, especially prodrugs, that contain at least one compound of the general formula (I) together with a pharmaceutically acceptable excipient.
申请公布号 WO03016259(A3) 申请公布日期 2003.09.12
申请号 WO2002AT00247 申请日期 2002.08.16
申请人 PHARMACON-FORSCHUNG UND BERATUNG GMBH;NOE, CHRISTIAN, R.;KRUSE, JENS;LACHMANN, BODO;LAUER, REGINA 发明人 NOE, CHRISTIAN, R.;KRUSE, JENS;LACHMANN, BODO;LAUER, REGINA
分类号 C07C69/612;C07C69/67;C07C69/68;C07C233/25;C07D209/18 主分类号 C07C69/612
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