Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1995-03-27
1997-11-04
Clark, W. Robinson H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514646, 514299, 514613, 514617, 514619, 514620, 514623, 546153, 564 74, 564123, A61K 3116, A61K 31165, A61K 3118
Patent
active
056840497
ABSTRACT:
A compound for use as a medicine having the formula ##STR1## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cyclo-alkyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom bearing said R.sup.1 and R.sup.2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C.sub.1-4 alkylpiperazinyl group; X is O or S; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl-carbonyl, aminocarbonyl, or hydroxy; R.sup.7 is hydrogen or halo; and R.sup.8, R.sup.9 and R.sup.10 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, hydroxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, (trifluoromethyl)carbonyl, aminocarbonyl, (cyclopropyl)carbonyl or a radical C.sub.1-6 alkyl-(C.dbd.Y)- wherein .dbd.Y represents .dbd.O, .dbd.N--OH, .dbd.N--OCH.sub.3, .dbd.N--NH.sub.2 or .dbd.N--N(CH.sub.3).sub.2 ; provided that (1) R.sup.1 is other than n-propyl when R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 represent hydrogen, R.sup.8 represents 4-ethoxy and X represents oxygen, and (2) X is other than sulfur, when R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 represent hydrogen and R.sup.4 and R.sup.5 represent 3,4-dimethoxy. Novel compounds, pharmaceutical compositions containing said compounds of formula (I), and processes for preparing compositions.
REFERENCES:
patent: 5407961 (1995-04-01), Janssen et al.
patent: 5480912 (1996-01-01), Janssen et al.
Bosmans Jean-Paul Rene
Janssen Paul Adriaan
Van Daele Georges Henri
Verdonck Marc Gustaaf
Clark W. Robinson H.
Janssen Pharmaceutica N.V.
Metz Charles J.
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