Burroughs Wellcome Co.

Other

Anthony W Randall

Alan T Hudson

Victoria S Latter

William H Richards

Novel antiprotozoal naphthoquinones having the general formula ##STR1## (wherein either R.sup.1 is hydrogen and R.sup.2 is selected from C.sub.1-6 alkoxy, aralkoxy, C.sub.1-6 alkyl-C.sub.1-6 alkoxy, phenyl substituted by one or two groups selected from halogen and C.sub.1-6 alkyl, halogen and perhalo-C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1) and salt thereof. The compounds of formula (I) are useful for the treatment or prophylaxis of protozoal diseases including malaria, theileriosis and coccidiosis. Various processes for preparing compounds of formula (I) are described.

Naphthoquinone derivatives

Novel combinations of an antiprotozoal naphthoquinone and a 4-pyridinol or an alkanoic ester thereof wherein the antiprotozoal activity of the combination is potentiated with respect to the corresponding activity of the components of the combination. The combinations are especially useful for the treatment or porphylaxis of malaria.

Antiprotozoal agents

1,4-Naphthoquinones of formula (I), methods for their preparation, veterinary formulations thereof, and the use thereof in animal therapy are disclosed. ##STR1## Particularly preferred compounds of formula (I) are, 2-[trans-(4-t-butylcyclohexyl)methyl]-3-hydroxy-1,4-naphthoquinone, and 2-[trans-(4-t-pentyl cyclohexyl)methyl]3-hydroxy-1,4-naphthoquinone. The compounds are of value as anti-protozoal agents, in particular as anti-theilerial agents.

Antiprotozoal compounds

1,4-Naphthoquinones of formula (I), methods for their preparation, pharmaceutical and veterinary formulations thereof and the use thereof in human and animal therapy are disclosed. ##STR1## Particularly preferred compounds of formula (I) are 2-(4'-t-butylcyclohexyl)-3-hydroxy-1,4-naphthoquinone and 2-hydroxy-3-(4'-t-pentylcyclohexyl)-1,4-naphthoquinone. The compounds are of value as antiprotozoal agents, in particular antimalarial and anticoccidial agents.

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Hayes, United Kingdom

Anthony W Randall