US Government As Represented by the Secretary of the Army

Edgar A Steck

Carl R Alving

Leslie M Werbel

The subject 8-[6-(N-heterocyclic-substituted)hexylamino]-6-methoxy lepidine erivatives have the formula: ##STR1## wherein Z represents methyl or, together with the two contiguous carbon atoms, the benzo moiety of a benzopiperazinyl derivative when Y is --N(R')--, n is an integer from 0 to 2; Y represents --O--, --S--, --S(O)--, --S(O).sub.2 --, and --N(R')--; R' represents hydrogen, alkyl, lower alkyl, R' substituted lower alkyl, cycloalkyl, aryl, sulfonyl, saturated 1,4-diazepinyl, lower alkyl N-cyanocarboximidothioate, or --C(O)R''; R' represents at least one of hydroxy, alkoxy, aralkoxy, amino, lower alkyl substituted amino, phenyl, halogenated phenyl, or sufonyl; and R'' represents lower alkyl, alkoxy, aralkoxy, amino, lower alkyl substituted amino or aryl substituted amino; and pharmaceutically acceptable salts thereof. These derivatives afford improvement in means for the chemotherapy of leishmaniasis when administered parenterally or orally to infected animals.

Anti-leishmanial lepidine derivatives

A novel treatment has been discovered for interrupting the life cycle of malaria parasite during its development in the liver of the vertebrate host. The subject invention involves a method of chemotherapy against sporozoite-induced malaria by administering an 8-aminoquinoline drug, such as primaquine, encapsulated within liposomes containing glycoconjugates, to a vertebrate host which has been infected with sporozoites of the parasites. Preferred species of glycoconjugates have a terminal glucose or galactose moiety, such as present in glycosyl ceramide, galactosyl ceramide, lactosyl ceramide, or in glycoproteins.

Treatment of malaria with liposomes containing 8-aminoquinoline

An improved method is provided for the chemotherapy of leishmanial infects. An 8-aminoquinoline anti-leishmanial agent is encapsulated within liposomes and the liposome-encapsulated drug is injected into the body. Subject use of a liposome carrier has produced marked enhancement of the effectiveness of the drug against leishmanial parasites in the liver (such as characteristic of infections which are difficult to treat).

Liposome carriers in leishmaniasis chemotherapy with 8-aminoquinoline

An improved method is provided for the prevention of schistosomiasis in her animals. The topical application of a composition containing a dehydroabietylamine or a derivative thereof provides a coating of perdurable anti-penetrant through which the infective cercariae of the parasitic worm do not pass readily.

Topical prophylaxis against schistosomiasis

An improved method is provided for the chemotherapy of leishmanial infections. The anti-leishmanial agent is encapsulated within liposomes and the liposome-encapsulated drug is injected into the body. Subject use of a liposome carrier has produced marked enhancement of the effectiveness and duration of anti-leishmanial action of meglumine antimoniate, and of sodium stibogluconate, drugs which are recommended widely for therapy of leishmaniasis.

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Silver Spring, MD, United States of America

Edgar A Steck