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US 8,044,035 B2Granted
Pharmaceutical compositions of pyrimidine-2,4,6-triones
AssigneeUniversite De Liege
InventorsPierre Bartsch, Didier Cataldo, Richard Endele, Brigitte Evrard, Jean-Michel Foidart, Hans-Willi Krell, Gerd Zimmermann
Life of this patent
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Abstract
A trioxopyrimidine-cyclodextrin complex formed of a trioxopyrimidine derivative or a salt thereof and a water-soluble cyclodextrin derivative has improved solubility.
Claims9
A trioxopyrimidine-cyclodextrin complex formed of a trioxopyrimidine derivative or a salt thereof and a water-soluble cyclodextrin, wherein the trioxopyrimidine derivative is a compound by formula (I):
- wherein
- R1 is C3-C20 alkyl, which may optionally be interrupted once or several times by —S—, —O— or —NH—;
- or
- a group W-V, wherein
- W is a chemical bond or phenyl;
- and
- V is phenyl, phenyloxy, phenylthio, phenylsulfinyl, phenylsulfonyl or phenylamino, which phenyl moieties may be unsubstituted or substituted once or several times by halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6-alkylthio, C1-C6 alkylsulfinyl, C1-C6-alkylamino, cyano, nitro or C1-C6-alkylsulfonyl;
- and
- R2 is C1-C10 alkyl, which alkyl group is unsubstituted or substituted one or two times by hydroxy or amino and may optionally be interrupted once or several times by —S—, —O— or —NH—;
- a benzoyl group, which may be unsubstituted or substituted once or several times by halogen, hydroxy, nitro, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, amidosulfonyl, C1-C6-alkylamidosulfonyl, bis-C1-C6-alkylamidosulfonyl;
- a heteroaromatic acyl group;
- or
- a phenyl- or heteroaryl group, which are unsubstituted or substituted once or several times by halogen, hydroxyl, C1-C6-aloxy, C1-C6-alkylamino, C1-C6-dialkylamino, cyano, C1-C6-alkyl, C2-C6 alkinyl, C1-C6-acyl, C1-C6-alkylthio, C1-C6-alkylsulfonyl, C1-C6-alkylsulfinyl, C1-C6-alkyl-aminocarbonyl, aminocarbonyl, C1-C6-alkylamidosulfonyl, amidosulfonyl, bis-C1-C6-alkylamidosulfonyl, nitro, C1-C6-alkoxycarbonyl, carboxy;
- and
- wherein the trioxopyrimidine derivative is
- 5-Biphenyl-4-yl-5[4-(4-nitro-phenyl)-piperazin-1-yl]pyrimidine-2,4,6-trione;
- 5-(4-Phenoxy-phenyl)-5-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrimidine-2,4,6-trione;
- 5[4-(4-Chloro-phenoxy)-phenyl]-5-(4-pyrimidin-2-yl-piperazin- -1-yl)- pyrimidine-2,4,6-trione;
- 5-[4-(3,4-Dichloro-phenoxy)-phenyl]-5-(4-pyrimidin-2-yl-piperazin-1-yl)- pyrimidine-2,4,6-trione;
- 5-[4-(4-Bromo-phenoxy)-phenyl]-5-(4-pyrimidin-2-yl-piperazin-1-yl)- pyrimidine-2,4,6-trione
- or a salt thereof.
18 more elements
Dependencies are inferred from the claim text.