Lin Zhou

US Patent:

8067620, Nov 29, 2011

Filed:

Oct 31, 2007

Appl. No.:

11/930606

Inventors:

Jonathan L. Vennerstrom - Omaha NE, US
Yuxiang Dong - Omaha NE, US
Susan A. Charman - Parkville, AU
Sergio Wittlin - Basel, CH
Jacques Chollet - Basel, CH
Darren J. Creek - Parkville, AU
Xiaofang Wang - Omaha NE, US
Lin Zhou - Omaha NE, US
Hugues Matile - Basel, CH
William N. Charman - Parkville, AU

Assignee:

Medicines for Malaria Venture MMV - Geneva

International Classification:

A61K 31/357
C07D 323/02

US Classification:

549336, 514462, 549337, 544 6, 544148, 544374, 540543, 546 15

Abstract:

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.

US Patent:

20080125441, May 29, 2008

Filed:

Oct 31, 2007

Appl. No.:

11/930582

Inventors:

JONATHAN L. VENNERSTROM - Omaha NE, US
YUXIANG DONG - Omaha NE, US
SUSAN A. CHARMAN - Parkville, AU
SERGIO WITTLIN - Basel, CH
JACQUES CHOLLET - Basel, CH
XIAOFANG WANG - Omaha NE, US
KAMARAJ SRIRAGHAVAN - Omaha NE, US
LIN ZHOU - Omaha NE, US
HUGUES MATILE - Basel, CH
WILLIAM N. CHARMAN - Parkville, AU

Assignee:

MEDICINES FOR MALARIA VENTURE MMV - Geneva

International Classification:

A61K 31/496
C07D 323/02
C07D 405/12
A61K 31/343

US Classification:

51425411, 549339, 514462, 544230

Abstract:

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.