Title:
11C-LABELLED CATECHOL DERIVATIVE, POSITRON EMISSION TOMOGRAPHY (PET) PROBE FOR PHOSPHORYLATED TAU AGGREGATION INHIBITOR USING SAME, AND PRODUCTION METHODS THEREFOR
Document Type and Number:
WIPO Patent Application WO/2018/008552
Kind Code:
A1
Abstract:
[Problem] The purpose of the present invention is to provide: an 11C-labelled catechol derivative exhibiting sufficient radioactivity for obtaining imaging images using a PET device; a PET probe for a phosphorylated tau aggregation inhibitor using same; and production methods therefor. [Solution] This 11C-labelled catechol derivative is represented by general formula (a) (with the caveat that R represents a substituent having an isopropylamino group, and the carbon in position 2 of the isopropylamino group is labelled with 11C). In particular, the 11C-labelled isoproterenol represented by structural formula (b) (in the formula, the carbon indicated by * is labelled with 11C) can be used as a PET probe for examining in vivo kinetics of isoproterenol which has the effect of inhibiting aggregation of tau proteins, and thus is very useful for researching dementia.
Inventors:
SUZUKI MASAAKI (JP)
ITO KENGO (JP)
KATO TAKASHI (JP)
IKENUMA HIROSHI (JP)
KOYAMA HIROKO (JP)
ITO KENGO (JP)
KATO TAKASHI (JP)
IKENUMA HIROSHI (JP)
KOYAMA HIROKO (JP)
Application Number:
PCT/JP2017/024166
Publication Date:
January 11, 2018
Filing Date:
June 30, 2017
Export Citation:
Assignee:
NAT CT GERIATRICS & GERONTOLOGY (JP)
International Classes:
A61K49/00; A61K51/04; A61P25/00; A61P25/28
Other References:
MUNCH,G. ET AL.: "Evaluation of sympathetic nerve terminals with [11C]epinephrine and [11C]hydroxyephedrine and positron emission tomography", CIRCULATION, vol. 101, no. 5, 8 February 2000 (2000-02-08), pages 516 - 523, XP055452368, ISSN: 1524-4539
SOEDA,Y. ET AL.: "Toxic tau oligomer formation blocked by capping of cysteine residues with 1,2-dihydroxybenzene groups", NAT. COMMUN., vol. 6, 16 December 2015 (2015-12-16), pages 1 - 12, XP055452371, ISSN: 2041-1723
VAN DER MEIJ,M. ET AL.: "Reductive N-alkylation of secondary amines with [2-11C]acetone", J. LABEL. COMPD. RADIOPHARM., vol. 46, no. 11, 15 October 2003 (2003-10-15), pages 1075 - 1085, XP055452375, ISSN: 1099-1344
See also references of EP 3482775A4
SOEDA,Y. ET AL.: "Toxic tau oligomer formation blocked by capping of cysteine residues with 1,2-dihydroxybenzene groups", NAT. COMMUN., vol. 6, 16 December 2015 (2015-12-16), pages 1 - 12, XP055452371, ISSN: 2041-1723
VAN DER MEIJ,M. ET AL.: "Reductive N-alkylation of secondary amines with [2-11C]acetone", J. LABEL. COMPD. RADIOPHARM., vol. 46, no. 11, 15 October 2003 (2003-10-15), pages 1075 - 1085, XP055452375, ISSN: 1099-1344
See also references of EP 3482775A4
Attorney, Agent or Firm:
AOYAMA Yo (JP)
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