Monomeric and Dimeric Arylisoquinoline Alkaloids and Derivatives Thereof

Type
Compound(s)

The technology describes an exceptionally broad universe of novel naphthylisoquinoline alkaloid compounds, and methods of total synthesis thereof. These compounds have been shown to have potent in vitro activity against malaria parasites, including parasites that are highly resistant to available antimalarial drugs. These compounds have also been shown to have potent in vivo activity against malaria parasites in animal models. Pharmaceutical compositions comprising these compounds, as well as methods of using the compounds to treat or prevent a malarial infection of a host, are claimed.
NIH Internal Reference no E-200-1994/0-US-01, US Patent Application no 08/279,291, US Patent no 5,552,550; E-200-1994/0-US-02, US Patent Application no 08/674,362, US Patent no 5,763,613; E-200-1994/2-US-01, US Patent Application no 09/001,801, US Patent no 6,140,339; E-200-1994/2-US-08, US Patent Application no 09/527,002, US Patent no 6,331,630; E-200-1994/2-AU-04, AU Patent Application no 24496/99; E-200-1994/2-BR-05, BR Patent Application no 9814575-4; E-200-1994/2-CA-06, CA Patent Application no 2313487; E-200-1994/2-EP-07, EP Patent Application no 98966748.0, EP Patent no 1045837; E-200-1994/2-IN-03, IN Patent Application no 2000/00143/CHE; E-200-1994/1-AU-02, AU Patent Application no 31969/95, AU Patent no 709428; E-200-1994/1-CA-03, CA Patent Application no 2195647; E-200-1994/1-JP-05, JP Patent Application no 505844/1996; E-200-1994/1-EP-06, EP Patent Application no 03005979.4; follwoing EP patents share same EP Patent Application no 95928091.8 and same EP Patent no 0772595: E-200-1994/1-EP-04, E-200-1994/1-AT-07, E-200-1994/1-DE-08, E-200-1994/1-BE-09, E-200-1994/1-DK-10, E-200-1994/1-ES-11, E-200-1994/1-GR-12, E-200-1994/1-IT-13, E-200-1994/1-LU-14, E-200-1994/1-MC-15, E-200-1994/1-NL-16, E-200-1994/1-PT-17, E-200-1994/1-SE-18, E-200-1994/1-FR-19. The technology describes an exceptionally broad universe of novel naphthylisoquinoline alkaloid compounds, and methods of total synthesis thereof. These compounds have been shown to have potent in vitro activity against malaria parasites, including parasites that are highly resistant to available antimalarial drugs. These compounds have also been shown to have potent in vivo activity against malaria parasites in animal models. Pharmaceutical compositions comprising these compounds, as well as methods of using the compounds to treat or prevent a malarial infection of a host, are claimed.

Disease
Malaria
Research areas
Basic research
Drug
Condition of use

n/a