Substituted 3-piperazinylalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones and their use in therapy
First Claim
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1. 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:
- R1 and R2, 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;
R3 represents a hydrogen, an aliphatic group which is branched or unbranched and saturated or unsaturated, containing 1 to 5 carbons;
R4 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.
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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.
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Citations
11 Claims
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1. 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:
- R1 and R2, 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;R3 represents a hydrogen, an aliphatic group which is branched or unbranched and saturated or unsaturated, containing 1 to 5 carbons; R4 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
- R1 and R2, which are identical or different, represent a hydrogen, a lower alkyl group containing 1 to 6 carbons, which is branched or unbranched;
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Current AssigneePierre Fabre Medicament (Fondation Pierre Fabre)
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Original AssigneePierre Fabre Medicament (Fondation Pierre Fabre)
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InventorsBigg, Dennis, Rieu, Jean-Pierre
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Primary Examiner(s)Shah, Mukund J.
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Assistant Examiner(s)Grumbling, Matthew V.
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Application NumberUS07/925,493Time in Patent Office636 DaysField of Search544/92, 514/230.5US Class Current514/230.5CPC Class CodesA61P 25/04 Centrally acting analgesics...A61P 25/06 Antimigraine agentsA61P 25/20 Hypnotics; SedativesA61P 25/24 AntidepressantsA61P 25/26 Psychostimulants, e.g. nico...A61P 3/04 Anorexiants; Antiobesity ag...A61P 9/12 AntihypertensivesC07D 265/22 Oxygen atomsC07D 413/10 linked by a carbon chain co...
