3-(alkylthio, alkylsulphinyl or alkylsulphonyl)-4- quinolones

C - Chemistry – Metallurgy – 07 – D

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C07D 215/36 (2006.01) A61K 31/47 (2006.01) C07D 265/26 (2006.01)

Patent

CA 1151652

Abstract Therapeutic Agents Compositions which contain a quinolone compound of the general formula Image wherein n is 0, 1 or 2; R1 is lower alkyl optionally substituted by hydroxy or C1-4 alkoxycarbonyl; allyl; propynyl or phenyl- lower alkyl in which the phenyl ring is optionally substituted by 1 or 2 C1-4 alkoxy groups; R2 is C1-4 alkyl with the proviso that when n is 0, R2 is methyl; and R3, R4 and R5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, halo, trifluorometnyl or lower alkylthio show antihypertensive activity. Compounds of general formula Image in which n, R1 R2, R3, R4 and R5 are as described above are novel subject to the following provisos (a) when R3, R4 and R4 and R5 are hydrogen R2 is methyl and R1 is lower alkyl, R1 contains more than one carbon atom, and (b) when R3 and R4 are hydrogen, R5 is hydrogen or 7- methyl, and R1 is ethyl, R2 contains more than one carbon atom. The specification describes and claims methods of making the compounds and novel intermediates used in such methods.

348520

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