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US 9,315,506 B2Granted
18F-labelled folates
AssigneeMerck & Cie
InventorsSimon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Viola Groehn
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Abstract
The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
Claims26
A folate compound of formula I
- wherein
- A is an amino acid,
- X1 to X5 are each N,
- Z is an electron-withdrawing group,
- R1, R2 are independently of each other H, Hal, O, —OR″, —NHR″, C1-C12 alkyl, C1-C12 alkoxy, C1-C12 alkanoyl, C2-C12 alkenyl, C2-C12 alkynyl, (C1-C12 alkoxy)carbonyl, or (C1-C12 alkylamino)carbonyl,
- R″ is H or C1-C6 alkyl,
- R3, R4 are independently of each other H, formyl, iminomethyl, nitroso, C1-C12 alkyl, C1-C12 alkoxy, C1-C12 alkanoyl, or halosubstituted C1-C12 alkanoyl,
- m is 0, 1, 2 or 3,
- n is 1,
- p is 0, 1 or 2,
- q has a value of 1 to 7, and
- r is 0 or 1.
9 more elements
Dependencies are inferred from the claim text.