Generated: April 25, 2017
|Abstract:||Novel 2-aminoalkyl-7-substituted-1,2,3,4-tetrahydroquinoline compounds, useful as effective anti-schistosomal agents, are disclosed and suitable modes of preparation are described. These compounds all possess either nitro, cyano or halogen substituted at the 7-position of the molecule, in addition to having a methyl, hydroxymethyl, alkoxymethyl or formyl group located at the adjacent 6-position.|
|Inventor(s):||Richards; Hugh Colin (Canterbury, EN)|
|Assignee:||Pfizer Inc. (New York, NY)|
1. A compound of the formula: ##SPC5##
and the pharmaceutically acceptable mono-acid addition salts thereof, wherein R.sup.1 and R.sup.2, when taken separately, are each selected from the group consisting of hydrogen, alkyl having from 1 to 5 carbon atoms, .beta.-hydroxyethyl and cycloalkyl having from 3 to 6 carbon atoms; R.sup.1 and R.sup.2, when taken together, complete a ring selected from the group consisting of pyrrolidino, piperidino and morpholino; R.sup.3 is selected from the group consisting of hydrogen, methyl and ethyl; R.sup.4 is methyl; R.sup.5 is selected from the group consisting of nitro, cyano, fluorine, chlorine and bromine, R.sup.6 is hydrogen or methyl; R.sup.8 is hydrogen or methyl, and n is 1 or 2, and the N-oxides of said base compounds wherein R.sup.1 and R.sup.2, when taken separately, are each other than hydrogen.
2. A compound as claimed in claim 1 wherein R.sup.3 is hydrogen, R.sup.5 is nitro, R.sup.6 is hydrogen, R.sup.8 is hydrogen, and n is 1.
3. A compound as claimed in claim 2 wherein R.sup.1 and R.sup.2 are each ethyl.
4. A compound as claimed in claim 2 wherein R.sup.1 is ethyl and R.sup.2 is hydrogen.
5. A compound as claimed in claim 2 wherein R.sup.1 is isopropyl and R.sup.2 is hydrogen.
6. A compound as claimed in claim 2 wherein R.sup.1 is tertiary-butyl and R.sup.2 is hydrogen.
7. A compound as claimed in claim 2 wherein R.sup.1 is secondary-butyl and R.sup.2 is hydrogen.
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