Ring substituted pyrazino-isoquinoline derivatives and their preparation
AssigneeMerck Patent GmbH
InventorsJurgen Seubert, Rolf Pohlke, Herbert Thomas, Peter Andrews
Life of this patent
Estimating the term…
Abstract
Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is 0; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.
Claims22
A compound of the formula ##STR7## wherein R.sup.1 is a hydrogen atom, hydroxy or alkyl;
- R.sup.2 is ##STR8## R.sup.3 is a hydrogen atom, alkyl or hydroxyalkyl;
- R.sup.4 is a hydrogen atom, alkyl or phenyl;
- R.sup.5 is an oxygen atom, two hydrogen atoms, or a hydrogen atom and one of alkyl, phenyl, halogen atoms, or hydroxy;
- R.sup.6 and R.sup.7, which can be alike or different, each are a hydrogen atom, a halogen atom, hydroxy, amino, nitro, cyano, alkyl, alkoxy, alkanoyl, monoalkylamino, dialkylamino, alkanoylamino, or benzoyloxy;
- R.sup.8 is a hydrogen atom or alkyl;
- R.sup.9 is cycloalkyl or cycloalkenyl of 5 to 7 carbon atoms which is unsubstituted or, substituted by a carbonyl oxygen atom X and Y, which can be the same or different, each is an oxygen or sulfur atom;
- with the proviso that R.sup.2 is ##STR9## when R.sup.1 and R.sup.3 to R.sup.8, inclusive, each are hydrogen atoms and X is an oxygen atom alkyl, hydroxyalkyl, alkoxy and alkanoyl being up to 4 carbon atoms.
The compound of claim 1, 2-cyclohexylcarbonyl-4-oxo-6-trans-methyl-1,2,3,6,7,11b-hexahydro-4H-pyraz ino[2,1-a]isoquinoline.
Dependencies are inferred from the claim text.