Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1986-10-01
1988-04-12
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540492, 540555, A61K 3133, C07D48712
Patent
active
047374969
ABSTRACT:
The invention relates to 1,3,4,16b-tetrahydro-2H,10H-indolo[2,1-c]pyrazino[1,2-a][1,4]benzodiazepin e derivatives of the formula I, ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, C.sub.3-7 -alkenyl, C.sub.3-7 -alkynyl, 3 to 7 ring-membered cycloalkyl, C.sub.2-7 -alkyl substituted by a substituent selected from hydroxy, amino, N-mono-lower alkyl-amino and N,N-di-lower alkyl-amino; or R.sup.1 is lower alkyl substituted by a substituent selected from 3 to 7 ring-membered cycloalkyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl and lower alkanoyl; or R.sup.1 is lower alkyl substituted by either phenyl or benzoyl each of said phenyl or benzoyl radicals being unsubstituted or substituted by up to three members selected from lower alkyl, lower alkoxy, lower alkylthio, halogen and trifluoromethyl; R.sup.2 and R.sup.3 represent hydrogen, lower alkyl, hydroxy, lowr alkoxy, halogen or trifluoromethyl; and R.sup.4 represents hydrogen, lower alkyl, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono- or N,N-di-lower alkyl-carbamoyl, or formyl; salts and 2N-oxides; which are useful as serotonin-2 receptor antagonists.
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Ciba-Geigy Corporation
Daus Donald G.
Gruenfeld Norbert
Shen Cecilia
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