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Claims for Patent: 5,053,432

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Claims for Patent: 5,053,432

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, GB), Randall; Anthony W. (Hayes, GB)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC)
Application Number:07/456,052
Patent Claims: 1. The trans compound of the formula (I): ##STR14##

2. A physiologically acceptable salt of the trans compound of the formula (I): ##STR15##

3. A method of treating malaria in a human having malaria comprising administering an effective malaria treatment amount of the trans compound of the formula (I): ##STR16##

4. The method of claim 3, in which said compound or salt is administered in a capsule or in a tablet.

5. The method of claim 3, in which said compound or salt is administered by injection.

6. A tablet or capsule containing the trans compound of the formula (I): ##STR17## or a physiologically acceptable salt thereof, said tablet or capsule containing 10 mg to 1 gram of said compound or salt thereof.

7. A parenterial injectable preparation comprising the trans compound of the formula (I): ##STR18## or a physiologically acceptable salt thereof and a pharmaceutically acceptable liquid carrier therefore.

8. A pharmaceutical preparation comprising the trans compound of the formula (I): ##STR19## or a pharmacologically acceptable salt thereof together with a pharmaceutically acceptable carrier therefore.
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