Claims for Patent: 3,903,283

Summary for Patent: 3,903,283

Title:	2-Aminoalkyl tetrahydroquinolines as anti-schistosomal agents
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)
Application Number:	05/462,211
Patent Claims:	1. A method for the treatment of schistosomiasis which comprises orally or parenterally administering to a host infected with schistosomes an effective anti-schistosomicidal amount of a compound selected from the group consisting of substituted 2-aminoalkyl-1,2,3,4-tetrahydroquinoline bases of the formula ##SPC8## and the pharmaceutically acceptable monoacid 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 selected from the group consisting of methyl, hydroxymethyl and alkoxymethyl having from 1 to 6 carbon atoms in the alkoxy moiety; 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, 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. The method as claimed in claim 1 wherein the compound administered is 2-(N,N-diethylaminomethyl)-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline. 3. The method as claimed in claim 1 wherein the compound administered is 2-(N-ethylaminomethyl)-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline. 4. The method as claimed in claim 1 wherein the compound administered is 2-isopropylaminomethyl-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline. 5. The method as claimed in claim 1 wherein the compound administered is 2-(N-methyl-N-isopropylaminomethyl)-6-methyl-7-nitro-1,2,3,4-tetrahydroqui noline. 6. The method as claimed in claim 1 wherein the compound administered is 2-(N-sec.-butylaminomethyl)-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline. 7. The method as claimed in claim 1 wherein the compound administered is 2-(N-tert.-butylaminomethyl)-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline. 8. The method as claimed in claim 1 where the compound administered is 2-(N-cyclopropylaminomethyl)-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline. 9. The method as claimed in claim 1 wherein the compound administered is 6-hydroxymethyl-2-isopropylaminomethyl-7-nitro-1,2,3,4-tetrahydroquinoline 10. The method as claimed in claim 1 wherein the compound administered is 6-ethoxymethyl-2-iso-propylaminomethyl-7-nitro-1,2,3,4-tetrahydroquinoline .