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US 5,514,699 AGranted
Pharmaceutical compounds
AssigneeLilly Industries Limited
InventorAndrew C. Williams
Life of this patent
Estimating the term…
Abstract
The invention provides pharmaceutical compounds of the formula: ##STR1## in which A - - - B is CH.sub.2 --CH.sub.2 or CH.dbd.CH; X is a pyridine or benzene ring; when X is pyridine n is 0; when X is benzene n is 0, 1 or 2 and when A - - - B is CH.sub.2 --CH.sub.2, R.sup.1 is attached at any of the positions 7 to 10, and when A - - - B is CH.dbd.CH, R.sup.1 is attached at any of the positions 5 to 10; and salts thereof.
Claims8
A compound of the formula:
- ##STR17## in which A - - - B is CH.sub.2 --CH.sub.2 or CH.dbd.CH;
- X is a benzene ring;
- n is 0, 1 or 2 and when A - - - B is CH.sub.2 --CH.sub.2, R.sup.1 is attached at any of the positions 7 to 10, and when A - - - B is CH.dbd.CH, R.sup.1 is attached at any of the positions 5 to 10;
- each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, 2-pyridyl, 3-pyridyl, 4-pyridyl, 1-piperidino, 1-pyrrolidino, and 4-morphholinyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester-forming group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;
- R.sup.2 is phenyl, naphthyl, or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted with one or two substituents each selected from halo, trifluoromethyl, C.sub.1-4 alkoxy, hydroxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, trifluoromethoxy, carboxy, --COOR.sup.12 where R.sup.12 is an ester-forming group, --CONR.sup.13 R.sup.14 or --NR.sup.13 R.sup.14 where R.sup.13 and R.sup.14 are each hydrogen or C.sub.1-4 alkyl, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;
- R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester-forming group, --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl, or --SO.sup.2 R.sup.11 where R.sup.11 is C.sub.1-4 alkyl, optionally substituted phenyl or phenyl or phenyl-C.sub.1-4 alkyl, said phenyl or phenyl-C.sub.1-4 alkyl being optionally substituted with one or two substituents each selected from halo, trifluoromethyl, C.sub.1-4 alkoxy, hydroxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, trifluoromethoxy, carboxy, --COOR.sup.12 where R.sup.12 is an ester-forming group, --CONR.sup.13 R.sup.14 or --NR.sup.13 R.sup.14 where R.sup.13 and R.sup.14 are each hydrogen or C.sub.1-4 alkyl;
- and
- R.sup.4 is 1-pyrrolyl, 1-imidazolyl or 1-pyrazolyl, said 1-pyrrolyl, 1-imidazolyl and 1-pyrazolyl being optionally substituted by one or two C.sub.1-4 alkyl, carboxyl, hydroxy-C.sub.1-4 alkyl or --CHO groups, or 1-(1,2,4-triazolyl), 1-(1,3,4-triazolyl) or 2-(1,2,3-triazolyl), said triazolyl groups being optionally substituted by a C.sub.1-4 alkyl or C.sub.1-4 perfluoroalkyl group, or 1-tetrazolyl optionally substituted by C.sub.1-4 alkyl;
- and salts thereof.
6 more elements
Dependencies are inferred from the claim text.