2-substituted ergolines useful as neuroleptics and antidepressants
AssigneeSchering Corporation
InventorsGerhard Sauer, Andreas Huth, Helmut Wachtel, Herbert H. Schneider
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AssigneeSchering Corporation
InventorsGerhard Sauer, Andreas Huth, Helmut Wachtel, Herbert H. Schneider
Estimating the term…
Novel ergoline derivatives, substituted in the 2-position, of the formula ##STR1## wherein C.sub.8 -C.sub.9 and C.sub.9 -C.sub.10 each independently is a CC-single or a C.dbd.C-double bond, but not together a cumulated double bond, and the substituent in the 8-position is in the .alpha.- or .beta.-configuration where C.sub.8 -C.sub.9 is a CC-single bond, R.sup.2 is CN, SR, SOR, ##STR2## wherein n is 2 or 3, ##STR3## and --CH(OH)R, wherein R has the meaning of H or C.sub.1-4 -alkyl, the grouping COR' and CSR' wherein R'.dbd.OH, OC.sub.1-4 -alkyl, benzyl, NH.sub.2 or NHR", the grouping CH.dbd.CH--CO.sub.2 R" and CH.sub.2 --CH.sub.2 --CO.sub.2 R" wherein R".dbd.C.sub.1-4 -alkyl, the grouping C.vertline.C-R'" and HC.dbd.CH--R'" wherein R'".dbd. hydrogen, C.sub.1-4 -alkyl, phenyl, CH.sub.2 OH, CR".sub.2 OH, ##STR4## CO.sub.2 R", CH.sub.2 NR".sub.2 or SiMe.sub.2 R"; C.sub.1-3 -alkyl, or C.sub.1-3 -alkyl substituted by OH or phenyl; or ##STR5## wherein R" is C.sub.1-4 alkyl, R.sup.6 is C.sub.1-4 -alkyl and R.sup.8 is methyl, NH--CO--NEt.sub.2 or NH--CS--NEt.sub.2, and the physiologically acceptable acid addition salt thereof, possess biological efficacy in the region of the central nervous system, e.g., as neuroleptics and anti-depressants.
An ergoline substituted in the 2-position of the formula ##STR20## wherein C.sub.8 - - - C.sub.9 and C.sub.9 - - - C.sub.10 each independently is a CC-single or a C.dbd.C-bond, but not a cumulated double bond, and the substituent in the 8-position is in the .alpha.- or .beta.-configuration where C.sub.8 - - - C.sub.9 is a CC-single bond,
Dependencies are inferred from the claim text.