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US 5,470,977 AGranted
Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes and 3-aminothiochromanes
AssigneeEli Lilly and Company
InventorsJohn M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, 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, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.
Claims6
A compound of the formula ##STR13## in which R is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, or cyclopropylmethyl;
- R.sub.3 is hydrogen;
- or
- R and R.sub.3 taken together are a divalent group of the formula --CH.sub.2 CH.sub.2 CH.sub.2 --;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, cyclopropylmethyl, aryl(C.sub.1 -C.sub.4 -alkyl), --COR.sub.4, --(CH.sub.2).sub.n S(C.sub.1 -C.sub.4 alkyl) or --(CH.sub.2).sub.n CONR.sub.5 R.sub.6 ;
- n is an integer from 1 to 4;
- R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, or phenyl;
- R.sub.5 and R.sub.6 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.3 -C.sub.7 cycloalkyl with the proviso that when one of R.sub.5 or R.sub.6 is cycloalkyl the other is hydrogen;
- S is --CH--, --O--, --S--, >SO, or >SO.sub.2 ;
- and R.sub.8 is hydrogen, C.sub.1 -C.sub.7 alkyl, substituted C.sub.1 -C.sub.7 alkyl, aryl, substituted aryl, aryl(C.sub.1 -C.sub.3 alkyl), or substituted aryl(C.sub.1 -C.sub.3 alkyl).
6 more elements
Dependencies are inferred from the claim text.