Iron complexes and salts thereof as contrast agents for MRI
AssigneeBracco Imaging S.P.A.
InventorCamilla Cavallotti
Life of this patent
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Abstract
The present invention relates to an iron complex having the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition formulated for oral and/or parenteral administration, preferably intravenous, said pharmaceutical composition preferably being formulated as an aqueous solution comprising said complex or salt. The present invention further relates to said complex or a salt thereof or said pharmaceutical composition for use as a contrast agent for magnetic resonance imaging (MRI), as well as a method and a kit for in situ preparation of said complex or salt and said pharmaceutical composition.
Claims20
A pharmaceutical composition comprising a pharmaceutically acceptable salt of an iron complex having the general formula (I):
- wherein:
- R1 and R2 are both in position 3 or both in position 5 of the aromatic ring and, simultaneously with or independently of each other, they are selected from:
- H, halogen, C1-C5 alkyl, C1-C5 alkoxyl;
- and
- R3 is selected from:
- H, C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 carboxyalkyl, aryl possibly substituted with at least one group selected from:
- COOH, halogen, C1-C5alkyl, C1-C5 alkoxyl, OH, NZ2, CONZ2, wherein Z is simultaneously or independently selected from:
- H, C1-C5 alkyl;
- and one or more excipients, diluents and/or pharmaceutically acceptable media;
- wherein said pharmaceutically acceptable salt is with an inorganic or organic base selected from the group consisting of:
- a salt of an alkali metal or alkaline earth metal, an amine, and an amino alcohol;
- wherein the pharmaceutical composition is formulated for parenteral administration, said pharmaceutical composition being formulated as an aqueous solution.
A pharmaceutically acceptable salt of an iron complex having the general formula (I)
- wherein:
- R1 and R2 are both in position 3 or both in position 5 of the aromatic ring and, simultaneously with or independently of each other, they are selected from:
- H, halogen, C1-C5 alkyl, C1-C5 alkoxyl;
- and
- R3 is selected from:
- H, C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 carboxyalkyl, aryl possibly substituted with at least one group selected from:
- COOH, halogen, C1-C5alkyl, C1-C5 alkoxyl, OH, NZ2, CONZ2, wherein Z is simultaneously or independently selected from:
- H, C1-C5 alkyl;
- with meglumine.
A kit for in situ preparation of a pharmaceutically acceptable salt of an iron complex having the general formula (I):
- wherein:
- R1 and R2 are both in position 3 or both in position 5 of the aromatic ring and, simultaneously with or independently of each other, they are selected from:
- H, halogen, C1-C5 alkyl, C1-C5 alkoxyl;
- and
- R3 is selected from:
- H, C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 carboxyalkyl, aryl possibly substituted with at least one group selected from:
- COOH, halogen, C1-C5 alkyl, C1-C5 alkoxyl, OH, NZ2, CONZ2, wherein Z is simultaneously or independently selected from:
- H, C1-C5 alkyl, said kit comprising at least three separate containers, wherein;
- (i) a first container comprises a compound having the general formula (II):
- wherein:
- R1 and R2 are both in position 3 or both in position 5 of the aromatic ring and, simultaneously with or independently of each other, they are selected from:
- H, halogen, C1-C5 alkyl, C1-C5 alkoxyl;
- R3 is selected from:
- H, C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 carboxyalkyl, aryl possibly substituted with at least one group selected from:
- COOH, halogen, C1-C5 alkyl, C1-C5 alkoxyl, OH, NZ2, CONZ2, wherein Z is simultaneously or independently selected from:
- H, C1-C5 alkyl;
- R4 and R5, simultaneously with or independently of each other, are selected from:
- H, C1-C4 alkanoyl or aroyl possibly substituted with at least one group selected from:
- COOH, C1-C2 alkyl, C1-C2 alkoxyl, OH;
- (ii) a second container comprises an iron compound capable of providing Fe(III) ions;
- and
- (iii) a third container comprises an inorganic or organic base.
Dependencies are inferred from the claim text.