| 摘要 |
Ergolinyl compounds which are nitrogensubstituted in the 8-position and have Formula (I) (I) and physiologically compatible salts thereof, wherein (a) R1 is hydrogen and the 8-substituent can be in the .alpha.- or .beta.-position; (i) when represents a double bond, R2 is hydrogen, C1-4-alkyl or C1-7-acyl, R3 is hydrogen, chlorine or bromine, and R4 is C1-6-alkyl, C3-6-cycloalkyl-C1-3-alkyl, C3-6-alkenyl, or C3-6-alkynyl or (ii) when the bond represents a single bond R2 and R are as defined above, and R is C4 6-alkyl, C3 6 cycloalkyl-C1-3-alkyl, C3-6-alkenyl, or C3-6-alkynyl; or (b) R1 is -?-NR5R6, and the 8-substituent can be in the .alpha.or .beta.-position, represents a single or double bond, R2, R3 are as defined above, R4 is C2-6-alkyl, C3-6-cycloalkyl-C1-3-alkyl, C3-6-alkenyl, or C3-6-alkynyl; and R5 is hydrogen, C1-10 alkyl, C3-10-alkenyl, or C3-10-alkynyl, is C1-10 alkyl C3-10-alkenyl, C3-10-alkynyl, or aryl or R5 and R6 together with the connecting N-atom form a 5- to 10-membered heterocyclic ring, preferably 5- or 6-membered, which optionally can contain further heteroatoms. The compounds of this invention are distinguished, e.g., as shown in animal experiments, by higher efficacy, longer duration of activity, and lower acute toxicity. The compounds predominantly affect central dopamine receptors, on which they can act in an agonistic and/or antagonistic fashion. The direct dopaminergic effectiveness of the compounds shows them to be valuable compounds for the treatment of dopamine deficiency conditions of the central nervous system, for example, for treatment of parkinsonism, certain forms of dementia, and in hyperprolactinemia. Because of the preferential stimulation of certain dopamine receptor subpopulations, dopaminergic routes of the central nervious system can be influences selectively, thus lessening the risk of undasirable side effects. |
