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US 5,494,910 AGranted
Benzofuran derivatives as 5-HT.sub.1 -like receptor antagonists
AssigneeGlaxo Group Limited
InventorsPeter C. North, Sjoerd N. Wadman
Life of this patent
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Abstract
This invention relates to benzofuran derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their medical use, in particular to compounds and compositions useful in the treatment of migraine. The compounds have the following general formula (I). ##STR1##
Claims19
A compound of formula (I) ##STR13## wherein R.sup.1 is --CH.sub.2 CONR.sup.3 R.sup.4 ;
- R.sup.2 is --CH.sub.2 CH.sub.2 NR.sup.5 R.sup.6 ;
- R.sup.3 and R.sup.4, together with the N-atom to which they are attached form a saturated 4- to 7-membered ring of formula ##STR14## where Z is a group of formula --CR.sup.7 R.sup.8 --, --O-- or --NR.sup.9 --;
- R.sup.5 and R.sup.6, which may be the same or different, are hydrogen or C.sub.1-3 alkyl;
- R.sup.7 and R.sup.8, which may be the same or different, are hydrogen, hydroxy or C.sub.1-3 alkoxy;
- R.sup.9 is --SO.sub.2 R.sup.10, --COR.sup.10 or --COOR.sup.10 ;
- R.sup.10 is C.sub.1-3 alkyl;
- and pharmaceutically acceptable salts 2nd solvates thereof.
4 more elements
A compound selected from:
- 1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]piper idine;
- 1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]pyrro lidine;
- 4-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]morph oline;
- 1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]-4-pi peridinol;
- 1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]-4-me thoxypiperidine;
- 1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]-4met hylsulphonyl)piperazine;
- 1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]-azet idine;
- 4-[[5-[3-[2-(Methylamino)ethyl]-5-benzofuranyl]-3-pyridinyl]acetyl]-acetyl ]morpholine;
- and pharmaceutically acceptable salts and solvates thereof.
6 more elements
1-[[5-[3-[2-(Dimethylamino)ethyl]-5-benzofuranyl]-3-pyri dinyl]acetyl]piperidine and pharmaceutically acceptable salts and solvates thereof.
Dependencies are inferred from the claim text.