Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-09-25
1994-02-08
Dentz, Bernard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514314, 514320, 514337, 514394, 514443, 514444, 514455, 546167, 546196, 546269, 548525, 5483051, 549 51, 549 58, 549 60, 549389, C07D31192, A61K 3135
Patent
active
052848680
ABSTRACT:
A pharmaceutical compound of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 5, 6, 7, 8, 9 or 10, and each R.sup.1 is 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.5 where R.sup.5 is an ester group, --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, 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 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 R.sup.11 SO.sub.2 -- where R.sup.11 is C.sub.1-4 alkyl or optionally substituted phenyl; and R.sup.4 is --NR.sup.12 R.sup.13, --NHCOR.sup.12, --N(COR.sup.12).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.12 where R.sup.12 and R.sup.13 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.14 where R.sup.14 is C.sub.1-4 alkyl or optionally substituted phenyl; provided that when n is 0, R.sup.3 is nitrile and R.sup.4 is --NH.sub.2, R.sup.2 is not phenyl or phenyl substituted in the para-position with a single chloro, hydroxy or methoxy substituent; and salts thereof.
REFERENCES:
Elnagdi et. al., Naturforschung B, 47(4), pp. 572-578 (Apr. 1992).
Elagamey et. al., Indian J. of Chem., 29B, pp. 885-886 (1990).
Elagamey et. al., Collection of Czechoslovak Chem. Commun., 53, pp. 1534-1538 (1988).
Reaktionen, Monatshefte fur Chemie, 110, 115-119 and 249-256 (1979).
Otto, et al., Arch. Pharm., 312(6), 548-550 (1979).
Dell Colin P.
Singh Jai P.
Smith Colin W.
Caltrider Steven P.
Dentz Bernard
Eli Lilly and Company
Lilly Industries Limited
Whitaker Leroy
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