ASYMETRICALLY REPLACED MONOESTER AND DIESTER PROFARMS OF THE DOPAMINE D1 RECEIVER AGONISTS.

摘要

An asymmetrically substituted monoester or diester prodrug of a D 1 dopamine agonist selected from the following formulas: (See formulas) in which one of R1 and R2 is hydrogen or acetyl and the other is selected from the group consisting of alkanoyl (C3-) C20), halo-alkanoyl (C3-C20), alkanoyl (C3-C20), cycloalkanoyl (C4-C7), cycloalkyl (C3-C6) alkanoyl (C2-C16); aroyl that is unsubstituted or substituted with 1 to 3 substituents selected from the group consisting of halogen, cyano, trifluoromethanesulfonyloxy, (C 1 -C 3) alkyl and (C 1-C 3) alkoxy which can subsequently be substituted with from 1 to 3 halogen atoms; arylalkanoyl (C2-C16) which is unsubstituted or substituted in the aryl moiety with 1 to 3 substituents selected from the group consisting of halogen, (C1-C3) alkyl and (C1-C3) alkoxy which can subsequently be substituted with 1 to 3 halogen atoms; and heteroarylalkanoyl having one to three heteroatoms selected from oxygen, sulfur and nitrogen in the heteroaryl moiety and 2 to 10 carbon atoms in the alkanoyl moiety and which is unsubstituted or substituted in the heteroaryl moiety with 1 to 3 substituents selected between the group consisting of halogen, cyano, trifluoromethanesulfonyloxy, (C1-C3) alkyl and (C1-C3) alkoxy which can in turn be substituted with 1 to 3 halogen atoms and the physiologically acceptable salts thereof.