C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 217/24 (2006.01) A61K 31/47 (2006.01) C07D 491/052 (2006.01)
Patent
CA 2183155
The present invention provides antimalarial pharmaceutical compositions containing antimalarial naphthylisoquinoline alkaloids or antimalarial deriva- tives thereof, useful new antimalarial naphthylisoquino- line alkaloid derivatives, methods for obtaining such derivatives, and methods of using such antimalarial compounds for the prevention of malarial infections in mammals and for treating mammals with malarial infec- tions. The novel antimalarial compounds of the present invention are selected from the group consisting of a compound selected from the group consisting of derivatives of dioncophylline B, dioncolactone A, dioncopeltine A, dioncophylline A, dioncophylline C, ancistrobrevine D, ancistrocladine, N-methyl- dioncophylline A and atropisomer thereof, 5'-O-demethyl- 8-O-methyl-7-epi-dioncophylline A, 4'-O-demethyl-dionco- phylline A, dioncophylleine A, (~)-dioncophyllacine A, hamatine, ancistrobrevine B, ancistrobrevine A, 6-O- dimethyl-ancistrobrevine A, ancistrobarterine A, 7-epi- dioncophylline A, N-formyl-ancistrocladine, N-methyl- ancistrocladine, 6-deoxy-N-methyl-ancistrocladine, N- formyl-O,O-dimethyl-dioncophylline C, N-formyl-dionco- phylline C, N-formyl-8-O-benzyl-dioncophylline C, N- formyl-8-O-methyl-dioncophylline C, N-formyl-8-O-pival- oyl-dioncophylline C, N-formyl-8-O-acetyl-dioncophylline C, N-formyl-8-O-benzoyl-dioncophylline C, and 8-O-methyl- dioncophylline C, wherein at least one phenolic hydroxyl group is a sulfonate ester group; at least one methyl ether group is a phenolic hydroxyl group; at least one phenolic hydroxyl group is an aromatic hydrogen substituent; at least one secondary amine site is an amide, sulfonamide, tertiary amine or alkyl quaternary ammonium salt; at least one tertiary amine site is a secondary amine; or at least one aromatic hydrogen substituent is a halogen, nitro, amino hydroxyl, thiol or cyano substituent; and pharmaceutically acceptable salts of the aforesaid derivatives. They inhibit the reproduction and cytopathicity of Plasmodium sp. parasites in vitro and in vivo.
L'invention porte sur des préparations pharmaceutiques antiantipaludiques contenant des alcaloïdes du type naphthylisoquinoléine ou leurs dérivés, sur de nouveaux dérivés de la naphthylisoquinoléine et leurs procédés d'obtention, ainsi que leur mode d'utilisation en vue de la prévention et du traitement des affections malariques chez les mammifères. Ces composés antipaludiques inhibent la reproduction et la capacité cytopathogène in vitro et in vivo des parasites du type Plasmodium sp.
Assi Laurent Ake
Boyd Michael R.
Bringmann Gerhard
Francois Guido
Phillipson J. David
Department O. F. Health And Human Services The United States Of America Represented By The Secretary
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
The Secretary Department Of Health And Human Services
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