Title:
NEAR-INFRARED FLUORESCENT PROBE FOR DETECTION OF PEPTIDASE ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2018/159631
Kind Code:
A1
Abstract:
[Problem] To provide a novel fluorescent probe that has superior tissue permeability and is capable of detecting the activity of peptidase highly expressed in cancer cells using a fluorescent response having a longer wavelength. [Solution] This fluorescent probe for detecting peptidase activity includes a compound represented by formula (I) or a salt thereof [in the formula: X represents Si(Ra)(Rb) (where Ra and Rb each independently represent a hydrogen atom or an alkyl group); Y represents a C0-C3 alkylene group, and the alkylene group may be substituted with a halogen atom or haloalkyl; R1 represents 1-4 substituents, which are the same or different from each other, and which are independently selected from the group consisting of a hydrogen atom, a cyano group, and optionally substituted alkyl group, carboxyl group, ester group, alkoxy group, amide group, and azide group; R2 forms, together with R3, a 5- to 8-membered heterocyclic structure containing a nitrogen atom and a carbon atom to which R2 and R3 are bound; R4 forms, together with R5, a 5- to 8-membered heterocyclic structure containing a nitrogen atom and a carbon atom to which R4 and R5 are bound; R6, R7, R8, and R9 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group, a sulfo group, a carboxyl group, an ester group, an amide group, or an azide group; and R10 represents an amino acid-derived acyl residue].
Inventors:
URANO YASUTERU (JP)
KAMIYA MAKO (JP)
IWATATE RYU (JP)
KAMIYA MAKO (JP)
IWATATE RYU (JP)
Application Number:
PCT/JP2018/007327
Publication Date:
September 07, 2018
Filing Date:
February 27, 2018
Export Citation:
Assignee:
UNIV TOKYO (JP)
International Classes:
A61K49/00; C12Q1/37; C07F7/10; G01N21/64
Domestic Patent References:
| WO2014106957A1 | 2014-07-10 | |||
| WO2010095450A1 | 2010-08-26 |
Other References:
"IVIS Lumina Series III", PERKINELMER, 28 May 2016 (2016-05-28), Retrieved from the Internet [retrieved on 20180518]
IWATATE R.J. ET AL.: "Asymmetric rhodamine-based fluorescent probe for multicolour in vivo imaging", CHEM. EUR. J., vol. 22, 2016, pages 1696 - 1703, XP055538415
FU M. ET AL.: "A design concept of long-wavelength fluorescent analogs of rhodamine dyes: replacement of oxygen with silicor atom", CHEM. COMMUN., 2008, pages 1780 - 1782, XP055538418
IWATATE R.J. ET AL.: "Silicon rhodamine-based near-infrared fluorescent probe for y-glutamyltransferase", BIOCONJUGATE CHEM., vol. 29, 2018, pages 241 - 244, XP055538421
IWATATE R.J. ET AL.: "Asymmetric rhodamine-based fluorescent probe for multicolour in vivo imaging", CHEM. EUR. J., vol. 22, 2016, pages 1696 - 1703, XP055538415
FU M. ET AL.: "A design concept of long-wavelength fluorescent analogs of rhodamine dyes: replacement of oxygen with silicor atom", CHEM. COMMUN., 2008, pages 1780 - 1782, XP055538418
IWATATE R.J. ET AL.: "Silicon rhodamine-based near-infrared fluorescent probe for y-glutamyltransferase", BIOCONJUGATE CHEM., vol. 29, 2018, pages 241 - 244, XP055538421
Attorney, Agent or Firm:
ONO Makoto et al. (JP)
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