| 摘要 |
The present invention is concerned with the phosphonic acids of formula I <IMAGE> (I) wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di-esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl, 2-carboxyperhydroindolyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents B-X-D wherein B represents a direct bond, or straight chain or branched lower alkylene; X represents O, S, SO, SO2, CO-NRb, RbN-CO or N-Ra; Ra represents hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl; Rb represents hydrogen, lower alkyl or aryl-lower alkyl; D represents straight chain or branched lower alkylene; and pharmaceutically acceptable salts thereof; which are useful in mammals as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.
|
