C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/38 (2006.01) A01N 57/22 (2006.01) A61K 31/662 (2006.01) A61P 31/00 (2006.01) A61P 33/00 (2006.01) C07F 9/40 (2006.01) C07F 9/6553 (2006.01)
Patent
CA 2634362
The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1- 4 alkoxy, C1-4 alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R1 is selected from the group consisting of hydrogen, C1-7 alkyl, C3-10 cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R2 is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents.
L'invention concerne de nouveaux composés d'acide phosphonique de formule (I). Dans cette formule, (a) R désigne un groupe de 1 à 5 substituants indépendamment sélectionnés dans le groupe comprenant: fluor, chlore, brome, alkoxy C1-4, alkyle C1-4, hydroxy, formyle, trifluorométhoxy, phényle, hétérocycle, méthyle hétérocyclique substitué, aminométhyle, hydroxyméthyle, bromométhyle, chlorure de sulfonyle, chlorure d'acétyle, composé nitreux et cyano, (b) R1 est sélectionné dans le groupe comprenant: hydrogène, alkyle C1-7, cycloalkyle C3-10, aryle, arylalkyle et hétérocycle, et (c) R2 est sélectionné dans le groupe comprenant: hydroxy et des groupes de protection hydroxy, et des stéréoisomères, des solvates et des sels de ceux-ci. Ces composés servent d'agents anti-infectieux et d'agents antiparasitaires, en particulier d'agents anti-malaria.
Devreux Vincent
Haemers Timothy
Jomaa Hassan
Van Calenbergh Serge
Wiesner Jochen
Smart & Biggar
Universiteit Gent
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