Radiolabeled compounds and their use as radiotracers for quantitative imaging of phosphodiesterase (pde10a) in mammals
AssigneeTakeda Pharmaceutical Company Limited
InventorsTakahiko Taniguchi, Shotaro Miura, Tomoaki Hasui, Christer Halldin, Vladimir Stepanov, Akihiro Takano
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Abstract
The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.
Claims22
A compound represented by the formula (I):
- wherein:
- ring A is selected from the group consisting of
- (1) a benzene,
- (2) a pyrazole,
- (3) a thiazole,
- (4) a piperidine, and
- (5) a tetrahydropyridine,
- wherein said ring A may optionally be substituted by 1 to 4 substituents selected from the group consisting of halogens, an optionally substituted C1-4 alkyl, an optionally substituted C1-4 alkoxy, an optionally substituted C7-14 aralkyl, an optionally substituted C2-4 alkenyl, an optionally substituted C2-4 alkynyl and a cyclic group which may optionally be substituted (provided that a cyclic group represented by the formula
- (wherein p is 1 to 4) which may optionally be substituted, is excluded),
- R1 is an optionally substituted C1-4 alkoxy, wherein the optionally substituted C1-4 alkoxy is radiolabeled,
- R2 and R3 are each substituent,
- m is 0 to 2,
- n is 0 to 5;
- provided that
- 1-(2-fluorophenyl)-5-[11C]methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one,
- 1-[4-(3,5-dimethylisoxazol-4-yl)-2-fluorophenyl]-5-11C-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one and
- 1-(2 fluoro-4-(morpholin-4-yl)phenyl)-5-11C-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-pyridazin-4(1H)-one
- are excluded;
- or a salt thereof.
1-[2-Fluoro-4-(tetrahydro-2H-pyran-4-yl)phenyl]-5-11C-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one or a salt thereof.
1-[4-(3,3-Difluoroazetidin-1-yl)-2-fluorophenyl]-5-11C-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one or a salt thereof.
5-([18F]Fluoro-methyloxy-d2)-1-(2-fluoro-4-(tetrahydro-2H-pyran-4-yl)phenyl)-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one or a salt thereof.
5-(2-[18F]Fluoro-ethyloxy-d4)-1-(2-fluoro-4-(tetrahydro-2H-pyran-4-yl)phenyl)-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one or a salt thereof.
Dependencies are inferred from the claim text.