Use of fluorine containing pyridone carboxylic acid derivatives for preparing a medicament for the treatment of HIV infections

Claim 2

An anti-human immunodeficiency virus composition which comprises a fluorine-containing pyridone­carboxylic acid derivative as an active ingredient and a pharmaceutically acceptable carrier therefor.

Claim 3

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridonecarboxylic acid derivative is a 1-­cyclopropyl or 1-halo-substituted-cyclopropyl-6-fluoro-­1,4-dihydro-4-oxo-7-nitrogen-containing heterocycle-­substituted-3-quinolinecarboxylic acid, which may optionally have a halogen atom, a lower alkyl group or a lower alkoxy group as a substituent at 8-position.

Claim 4

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridonecarboxylic acid derivative is a 1-lower alkyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl- or lower alkyl-substituted 1-piperazinyl)-1,8-naphthyridine-3-­carboxylic acid.

Claim 5

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridonecarboxylic acid derivative is an 1-ethyl-­6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl or lower alkyl-­substituted 1-piperazinyl)-3-quinolinecarboxylic acid, which may optionally have a halogen atom, a lower alkyl group or a lower alkoxy group as a substituent at 8-position.

Claim 6

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridonecarboxylic acid derivative is a 9-fluoro-­2,3-dihydro-3-methyl-10-(4-lower alkyl-1-piperazinyl)-7-­oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid, a salt thereof or a hydrate thereof.

Claim 7

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridonecarboxylic acid derivative is a 3S-9-­fluoro-2,3-dihydro-3-methyl-10-(4-lower alkyl-1-piperazin-­yl)-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid.

Claim 8

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridonecarboxylic acid derivative is represented by the general formula: wherein Q is =N-, =C(R⁸)- (R⁸ being H, F, Cl, an alkyl group having from one to four carbon atoms, an alkoxyl group having from one to four carbon atoms, or -OCH₂CH(R⁸¹)-, -SCH₂CH(R⁸¹)-, -OCH₂N(R⁸¹)- (R⁸¹ being H or an alkyl group having from one to four carbon atoms) the latter three groups being connected with the pyridone nitrogen atom to complete an additional ring, whereby R¹ is not present); R¹ is a lower alkyl group, a cyclopropyl group, a halocyclopropyl group, a haloethyl group, a vinyl group, a phenyl group or a halo­phenyl group; and R⁷ is a nitrogen-containing heterocyclic group, which may be substituted by one or more substituents.

Claim 9

An anti-human immunodeficiency virus composition as claimed in Claim 7, wherein said fluorine-­containing pyridonecarboxylic acid derivative is selected from the group consisting of ofloxacin, the 3S form thereof, ciprofloxacin hydrochloride, enoxacin, norfloxacin, lomefloxacin, fleroxacin, difloxacin, levofloxacin, T-3262, A-62254, AT-4140, WIN57273, CP-92121 and (S)-9-fluoro-2,3-­dihydro-3-methyl-10-(2,6-dimethyl-4-pyridyl)-7-oxo-7H-­pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid.

Claim 10

An anti-human immunodeficiency virus composition as claimed in Claim 1, wherein said fluorine-­containing pyridone carboxylic acid derivative is the group consisting of 1-epoxymethano-7-fluoro-8-(4-methyl-1-­piperazinyl)-5-oxo-5H-thiazolo[3,2-a]quinoline-4-carboxylic acid hydrochloride or 6-fluoro-1-methyl-7-(1-piperazinyl)-­4-oxo-4H-[1,3]thiazedo[3,2-a]quinoline-3-carboxylic acid.

Claim 11

A process for preparing the compositions of claims 1 to 9 which comprises incorporating the active ingredient into a pharmaceutically acceptable carrier.

Claim 12

The use of at least one compound as defined in anyone of claims 1 to 9 for preparing a pharmaceutical composition for inhibiting multiplication of human imunodeficiency virus or for treatment of human imuno­deficiency virus infection and diseases caused by human imunodeficiency virus.