Medicines for Malaria Venture (mmv)

Hoffmann-la Roche Inc.

Medicines for Malaria Venture Mmv International Centre Cointrin

Mmv Medicines for Malaria Venture

Jacques Chollet

Hugues Matile

Jonathan L Vennerstrom

Yuxiang Dong

William Charman

Maniyan Padmanilayam

Kamaraj Spiraghavan

Christian N Hubschwerlen

Susan A Charman

Lin Zhou

William N Chapman

Yuangqing Tang

Yuanqing Tang

Robert George Ridley

Jawad Alzeer

Darren J Creek

Sergio Wittlin

William N Charman

Kamaraj Sriraghavan

A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.

Dispiro 1,2,4-trioxolane antimalarials

A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Spiro and dispiro 1,2,4-trioxolane antimalarials

Spiro and dispiro 1,2,4-trixolane antimalarials

A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.

.beta.-Alkoxyacrylates against malaria

Growing community of inventors

Basel, Switzerland

Jacques Chollet