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Substituted 3-piperazinylalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones and their use in therapy

  • US 5,308,844 A
  • Filed: 08/05/1992
  • Issued: 05/03/1994
  • Est. Priority Date: 08/05/1991
  • Status: Expired due to Fees
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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