Ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes
AssigneeEli Lilly and Company
InventorsJohn M. Schaus, Robert D. Titus
Life of this patent
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Abstract
The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.
Claims12
A compound of the formula ##STR13## in which R is C.sub.1 -C.sub.4 alkyl, allyl, or cyclopropylmethyl;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, allyl, or cyclopropylmethyl;
- R.sub.2 is hydrogen or methyl;
- X is --CH.sub.2 --;
- R.sub.3 is C.sub.1 -C.sub.8 alkyl, phenyl, phenyl substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl, pyridyl, pyridyl substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl, phenyl C.sub.1 -C.sub.4 alkyl, phenyl C.sub.1 -C.sub.4 alkyl substituted on the phenyl ring with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl;
- n is 0, 1 or 2;
- and pharmaceutically acceptable acid addition salts thereof.
A pharmaceutical formulation which comprises, in association with a pharmaceutically acceptable carrier, diluent, or excipient, an effective amount of a compound of the formula ##STR14## in which R is C.sub.1 -C.sub.4 alkyl, allyl, or cyclopropylmethyl;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, allyl, or cyclopropylmethyl;
- R.sub.2 is hydrogen or methyl;
- X is --CH.sub.2 --;
- R.sub.3 is C.sub.1 -C.sub.8 alkyl, phenyl, phenyl substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl, pyridyl, pyridyl substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio, or trifluoromethyl, phenyl C.sub.1 -C.sub.4 alkyl, phenyl C.sub.1 -C.sub.4 alkyl substituted on the phenyl ring with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl;
- n is 0, 1 or 2;
- and pharmaceutically acceptable acid addition salts thereof.
A compound of the formula ##STR15## in which R is C.sub.1 -C.sub.4 alkyl, allyl, or cyclopropylmethyl;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, allyl, or cyclopropylmethyl;
- R.sub.2 is hydrogen or methyl;
- X is --O--;
- R.sub.3 is C.sub.1 -C.sub.8 alkyl, phenyl, phenyl substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl, pyridyl, pyridyl substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio, or trifluoromethyl, phenyl C.sub.1 -C.sub.4 alkyl, phenyl C.sub.1 -C.sub.4 alkyl substituted on the phenyl ring with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo, hydroxy, C.sub.1 -C.sub.3 alkylthio or trifluoromethyl;
- n is 0, 1 or 2;
- and pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.