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Details for Patent: 5,175,319

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Details for Patent: 5,175,319

Title: Naphthoquinone derivatives
Abstract: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.
Inventor(s): Hudson; Alan T. (Sevenoaks, GB2), Randall; Anthony W. (Hayes, GB2)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC)
Filing Date:Sep 12, 1991
Application Number:07/758,629
Claims:1. A compound of formula (I) ##STR14## 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.sub.1 and R.sub.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1 and X is halogen.

2. A compound as claimed in claim 1, wherein n is 0.

3. A compound as claimed in claim 1, wherein n is 1.

4. A compound as claimed in claim 1, wherein R.sup.1 is hydrogen and R.sup.2 is tertbutoxy or a phenyl group substituted by one or two groups selected from chlorine and methyl in a 3- and/or 4-position(s).

5. A compound of Formula (I) ##STR15## wherein R.sup.1 is hydrogen and R.sup.2 is a phenyl group substituted by C.sub.1-6 alkyl and optionally substituted by halogen or R.sup.2 is a phenyl group substituted by perhalo-C.sub.1-6 alkyl and optionally substituted by halogen; and n is 0 or 1 and X is halogen.
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