WO2018128664A3 - 18f-labeled compounds for pet imaging and uses thereof - Google Patents

18f-labeled compounds for pet imaging and uses thereof Download PDF

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Publication number
WO2018128664A3
WO2018128664A3 PCT/US2017/057595 US2017057595W WO2018128664A3 WO 2018128664 A3 WO2018128664 A3 WO 2018128664A3 US 2017057595 W US2017057595 W US 2017057595W WO 2018128664 A3 WO2018128664 A3 WO 2018128664A3
Authority
WO
WIPO (PCT)
Prior art keywords
labeled compounds
imaging
pet imaging
solid tumor
subject
Prior art date
Application number
PCT/US2017/057595
Other languages
French (fr)
Other versions
WO2018128664A2 (en
Inventor
Zibo Li
Zhanhong WU
Ben GIGLIO
Stergios MOSCHOS
Original Assignee
The University Of North Carolina At Chapel Hill
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to US201662410681P priority Critical
Priority to US62/410,681 priority
Application filed by The University Of North Carolina At Chapel Hill filed Critical The University Of North Carolina At Chapel Hill
Publication of WO2018128664A2 publication Critical patent/WO2018128664A2/en
Publication of WO2018128664A3 publication Critical patent/WO2018128664A3/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0404Lipids, e.g. triglycerides; Polycationic carriers
    • A61K51/0406Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K2123/00Preparations for testing in vivo
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Abstract

The present invention relates to 18F-labeled compounds suitable for positron emission tomography (PET) imaging. The invention further relates to the use of these compounds for carrying out PET scans, imaging the indoleamine 2,3-dioxygenase, pathway, predicting the responsiveness of a subject with a solid tumor to therapies including immunotherapy such as PD-1/PD-L1 inhibition, and determining whether a solid tumor in a subject contains tumor-infiltrating immune cells.
PCT/US2017/057595 2016-10-20 2017-10-20 18f-labeled compounds for pet imaging and uses thereof WO2018128664A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US201662410681P true 2016-10-20 2016-10-20
US62/410,681 2016-10-20

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16/343,267 US11103603B2 (en) 2016-10-20 2017-10-20 18F-labeled compounds for PET imaging and uses thereof

Publications (2)

Publication Number Publication Date
WO2018128664A2 WO2018128664A2 (en) 2018-07-12
WO2018128664A3 true WO2018128664A3 (en) 2018-12-13

Family

ID=62791367

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/057595 WO2018128664A2 (en) 2016-10-20 2017-10-20 18f-labeled compounds for pet imaging and uses thereof

Country Status (2)

Country Link
US (1) US11103603B2 (en)
WO (1) WO2018128664A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3045466A1 (en) 2016-12-01 2018-06-07 Regeneron Pharmaceuticals, Inc. Radiolabeled anti-pd-l1 antibodies for immuno-pet imaging
CA3053348A1 (en) 2017-02-10 2018-08-16 Regeneron Pharmaceuticals, Inc. Radiolabeled anti-lag3 antibodies for immuno-pet imaging
US10730944B2 (en) 2017-07-24 2020-08-04 Regeneron Pharmaceuticals, Inc. Anti-CD8 antibodies and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201517922A (en) * 2013-11-12 2015-05-16 Nat Defense Medical Ct Method for synthesizing fluorine-18 labeled serotonin transporter imaging agents
WO2016040458A2 (en) * 2014-09-09 2016-03-17 H. Lee Moffitt Cancer Center And Research Institute, Inc. Pet probes of radiofluorinated carboximidamides for ido-targeted imaging

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4695588A (en) * 1977-06-01 1987-09-22 Merck & Co., Inc. Fluorinated amino acids
US7220730B2 (en) * 2003-09-25 2007-05-22 Board Of Regents Of The University Of Nebraska Cancer specific radiolabeled conjugates regulated by the cell cycle for the treatment and diagnosis of cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201517922A (en) * 2013-11-12 2015-05-16 Nat Defense Medical Ct Method for synthesizing fluorine-18 labeled serotonin transporter imaging agents
WO2016040458A2 (en) * 2014-09-09 2016-03-17 H. Lee Moffitt Cancer Center And Research Institute, Inc. Pet probes of radiofluorinated carboximidamides for ido-targeted imaging

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
CHIOTELLIS A. ET AL.: "Synthesis, Radiolabeling, and Biological Evaluation of 5-Hydroxy-2-[18F]fluoroaIkyl-tryptophan Analogues as Potential PET Radiotracers for Tumor Imaging", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, no. 11, 19 May 2016 (2016-05-19), pages 5324 - 5340, XP055556993 *
CHUGANI D. ET AL.: "Alpha[C-11]methyl-L-tryptophan PET maps brain serotonin synthesis and kynurenine pathway metabolism", JOURNAL OF CEREBRAL BLOOD FLOW METABOLISM, vol. 20, no. X21, 2000, pages 2 - 9, XP055557822 *
HOU DE-YAN ET AL.: "Inhibition of indoleamine 2,3-dioxygenase in dendritic cells by stereoisomers of 1-methyl-tryptophan correlates with antitumor responses", CANCER RES, vol. 67, no. 2, 15 January 2007 (2007-01-15), pages 792 - 801, XP055557102 *
LIN XIE ET AL.: "Development of 1-N-1 1C-Methyl-1- and -d-Tryptophan for pharmacokinetic imaging of the immune checkpoint inhibitor 1 -Methyl-Tryptophan", SCIENTIFIC REPORTS, vol. 5, no. 1, 10 November 2015 (2015-11-10), pages 1 - 9, XP055557027 *
MULLER J. ALEXANDER: "Differential targeting of tryptophan catabolism in tumors and in tumor-draining lymph nodes by stereoisomers of the IDO inhibitor 1-methyl- tryptophan", INTERNATIONAL CONGRESS SERIES, vol. 1304, 2007, pages 250 - 261, XP022340189 *
RAMAN CHIRAKAL ET AL.: "Synthesis of f-18 labelled fluoro-melatonins and 5-hydroxy- fluoro-tryptophans", J. OF LABELED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. XXV, no. 1, 1988, pages 63 - 71, XP055557833 *

Also Published As

Publication number Publication date
WO2018128664A2 (en) 2018-07-12
US11103603B2 (en) 2021-08-31
US20190247527A1 (en) 2019-08-15

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