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US 5,916,916 AGranted
1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods
AssigneeEli Lilly and Company
InventorsKenneth Lee Hauser, Alan David Palkowitz
Life of this patent
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Abstract
The instant invention provides a series of naphthyl compounds having an oxygen linker at the 1-position which are useful as selective estrogen receptor modulators.
Claims14
A compound of formula 1 ##STR11## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is selected from the group consisting of
- hydrogen,
- hydroxy,
- alkoxy of one to four carbon atoms,
- alkoxycarbonyl of two to seven carbon atoms,
- alkoxycarbonyloxy of two to seven carbon atoms,
- alkylsulfonyloxy,
- phenoxycarbonyloxy, and
- aryloxycarbonyl where the aryl portion is selected from the group consisting of
- unsubstituted phenyl, and
- phenyl substituted with one or more substituents independently selected from the group consisting of
- halo,
- methyl,
- methoxy,
- nitro, and
- trifluoromethyl;
- R.sup.2 and R.sup.3 are, independently selected from the group consisting of
- hydrogen,
- chloro,
- fluoro,
- hydroxy,
- alkoxy of one to four carbon atoms,
- alkoxycarbonyl of two to seven carbon atoms,
- alkoxycarbonyloxy of two to seven carbon atoms,
- alkylsulfonyloxy,
- phenoxycarbonyloxy, and
- aryloxycarbonyl where the aryl portion is selected from the group consisting of
- unsubstituted phenyl, and
- phenyl substituted with one or more substituents independently selected from the group consisting of
- halo,
- methyl,
- methoxy,
- nitro, and
- trifluoromethyl;
- R.sup.4 is selected from the group consisting of
- hydroxy,
- alkoxy of one to six carbon atoms,
- cycloalkoxy of four to six carbon atoms,
- 1-piperidinyl,
- 1-pyrrolidinyl,
- methyl-1-pyrrolidinyl,
- dimethyl-1-pyrrolidino,
- 4-morpholino,
- dimethylamino,
- diethylamino,
- diisopropylamino,
- 1-hexamethyleneimino, and
- aryloxy where wherein the aryl portion is selected from the group consisting of
- unsubstituted phenyl, and
- phenyl substituted with one or more substituents independently selected from the group consisting of
- halo,
- methyl,
- methoxy,
- nitro, and
- trifluoromethyl;
- X is selected from the group consisting of
- alkylene of two to four carbon atoms,
- --CH.dbd.CH--,
- --CH.sub.2 CH.dbd.CH--, and
- --CH.sub.2 CH.sub.2 CH.dbd.CH--;
- and
- Y is absent or is carbonyl, with the proviso that when
- Y is absent, R.sup.4 may not be hydroxy, --O(C.sub.1 -C.sub.6 alkyl), --O(C.sub.4 -C.sub.6 cycloalkyl), or --OAr.
59 more elements
Dependencies are inferred from the claim text.