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US 5,308,844 AGranted
Substituted 3-piperazinylalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones and their use in therapy
AssigneePierre Fabre Medicament
InventorsJean-Pierre Rieu, Dennis Bigg
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Abstract
The invention relates to novel substituted 3-piperazinylalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones of formula I ##STR1## their pharmaceutically acceptable inorganic or organic salts, optionally in their hydrated form, the racemates, the enantismers or their mixtures, their preparation and their use as medicaments as well as all the pharmaceutical compositions of I which are or are not combined with another active principle.
Claims11
A derivative of 2,3-dihydro-4-(piperazinylalkyl)-4H-1,3-benzoxazin-4-one of formula I ##STR23## in which the substituents are defined as follows:
- R.sub.1 and R.sub.2, which are identical or different, represent a hydrogen, a lower alkyl group containing 1 to 6 carbons, which is branched or unbranched;
- a lower alkyloxy group containing 1 to 4 carbons;
- a hydroxyl;
- a nitro;
- an amino which is unsubstituted or substituted by an acyl group or one or two alkyls, each independently containing 1 to 4 carbons;
- a sulfonylamino group;
- a halogen;
- R.sub.3 represents a hydrogen, an aliphatic group which is branched or unbranched and saturated or unsaturated, containing 1 to 5 carbons;
- R.sub.4 represents either:
- a phenyl group which can be unsubstituted or substituted by one or more identical or different radicals, chosen from amongst the following:
- a lower alkyl group containing 1 to 6 carbons, which is linear or branched,
- an alkyloxy group containing 1 to 6 carbons, which is linear or branched,
- a halogen,
- a trifluoromethyl,
- a nitro group,
- a hydroxy group,
- an amino which is unsubstituted or substituted by one or more alkyl groups, an acyl or a carboxylate, all three containing 1 to 4 carbons;
- a sulfonylamino group,
- a monocyclic heteroaryl group containing one or two nitrogen atoms selected from the class consisting of pyrridyl and pyrimidinyl groups;
- n can assume the values 2 to 6;
- as well as the therapeutically acceptable inorganic or organic salts of I;
- and also the racemates and the various enantiomers, or their mixtures when the compounds of the formula I contain an asymmetric carbon.
19 more elements
Dependencies are inferred from the claim text.