Title:
NOVEL COMPOUND BINDING TO DESIGNER RECEPTOR, IMAGING METHOD FOR DESIGNER RECEPTOR, AGONIST OR ANTAGONIST, THERAPEUTIC AGENT, COMPANION DIAGNOSTIC AGENT, AND IMAGING METHOD FOR NERVE CELL
Document Type and Number:
WIPO Patent Application WO/2019/245047
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide a technique for imaging the brain of a living animal and application of the technique. A radiolabeled dibenzoazepine derivative, which shows excellent brain transferability, high receptor selectivity and high quantitativity, is used for imaging a living animal body. A dibenzoazepine derivative is used for treating a disease in which hM4D receptor or hM3D receptor participates. Further, a radiolabeled dibenzoazepine derivative is used for imaging an axonal end which is innervated by a nerve cell.
Inventors:
MINAMIMOTO TAKAFUMI (JP)
NAGAI YUJI (JP)
JI BIN (JP)
MIYAKAWA NAOHISA (JP)
HIGUCHI MAKOTO (JP)
SUHARA TETSUYA (JP)
NAGAI YUJI (JP)
JI BIN (JP)
MIYAKAWA NAOHISA (JP)
HIGUCHI MAKOTO (JP)
SUHARA TETSUYA (JP)
Application Number:
PCT/JP2019/024834
Publication Date:
December 26, 2019
Filing Date:
June 21, 2019
Export Citation:
Assignee:
NATIONAL INSTITUTES FOR QUANTUM AND RADIOLOGICAL SCIENCE AND TECH (JP)
International Classes:
C07D243/38; A61K31/5513; A61K51/00; A61P25/18; A61P25/20; A61P25/28; A61P43/00; C07K14/705
Domestic Patent References:
| WO2019157083A1 | 2019-08-15 | |||
| WO2017049252A1 | 2017-03-23 |
Foreign References:
| JP2015071560A | 2015-04-16 | |||
| JP2017509625A | 2017-04-06 |
Other References:
NAGAI, YUJI: "PET imaging-guided chemogenetic silencing reveals a critical role of primate rostromedial caudate in reward evaluation", NATURE COMMUNICATIONS, vol. 7, no. 13605, 6 December 2016 (2016-12-06), pages 1 - 8, XP002790276, ISSN: 2041-1723, DOI: 10.1038/ncomms13605
CHEN, XIN: "The First Structure-Activity Relationship Studies for Designer Receptors Exclusively Activated by Designer Drugs", ACS CHEMICAL NEUROSCIENCE, vol. 6, no. 3, 2015, pages 476 - 484, XP002790277, DOI: 10.1021/cn500325v
BURKI, H. R.: "EFFECTS OF CLOZAPINE AND OTHER DIBENZO-EPINES ON CENTRAL DOPAMINERGIC AND CHOLINERGIC SYSTEMS STRUCTURE-ACTIVITY RELATIONSHIPS", ARZNEIMITTEL-FORSCHUNG, vol. 27, 1977, pages 1561 - 1565, XP009037300, ISSN: 0004-4172
HARRIS, TERRY W.: "Affinity of 10-(4-Methylpiperazino)dibenz[b,f]oxepins for Clozapine and Spiroperidol Binding Sites in Rat Brain", JOURNAL OF THE MEDICINAL CHEMISTRY, vol. 25, no. 7, 1 January 1982 (1982-01-01), pages 855 - 858, XP055665900
ARMBRUSTER, B ,N: "Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 104, 20 March 2007 (2007-03-20), pages 5163 - 5168, XP055185711, ISSN: 0027-8424, DOI: 10.1073/pnas.0700293104
See also references of EP 3812373A4
ARMBRUSTER BN ET AL.: "Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand", PROC NATL ACAD SCI USA., vol. 104, no. 12, 2007, pages 5163 - 5168, XP055185711, DOI: 10.1073/pnas.0700293104
JI ET AL.: "Multimodal Imaging for DREADD-Expressing Neurons in Living Brain and Their Application to Implantation of iPSC-Derived Neural Progenitors", JOURNAL NEUROSCI, vol. 36, no. 45, 2016, pages 11544 - 11558
NAGAI ET AL.: "PET imaging-guided chemogenetic silencing reveals a critical role of primate rostromedial caudate in reward evaluation", NATURE COMMUNICATIONS, vol. 7, 2016, pages 13605
GOMEZ J ET AL.: "Chemogenetics revealed: DREADD occupancy and activation via converted clozapine", SCIENCE, vol. 357, no. 6350, 2017, pages 503 - 507
CHEN, XIN: "The First Structure-Activity Relationship Studies for Designer Receptors Exclusively Activated by Designer Drugs", ACS CHEMICAL NEUROSCIENCE, vol. 6, no. 3, 2015, pages 476 - 484, XP002790277, DOI: 10.1021/cn500325v
BURKI, H. R.: "EFFECTS OF CLOZAPINE AND OTHER DIBENZO-EPINES ON CENTRAL DOPAMINERGIC AND CHOLINERGIC SYSTEMS STRUCTURE-ACTIVITY RELATIONSHIPS", ARZNEIMITTEL-FORSCHUNG, vol. 27, 1977, pages 1561 - 1565, XP009037300, ISSN: 0004-4172
HARRIS, TERRY W.: "Affinity of 10-(4-Methylpiperazino)dibenz[b,f]oxepins for Clozapine and Spiroperidol Binding Sites in Rat Brain", JOURNAL OF THE MEDICINAL CHEMISTRY, vol. 25, no. 7, 1 January 1982 (1982-01-01), pages 855 - 858, XP055665900
ARMBRUSTER, B ,N: "Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 104, 20 March 2007 (2007-03-20), pages 5163 - 5168, XP055185711, ISSN: 0027-8424, DOI: 10.1073/pnas.0700293104
See also references of EP 3812373A4
ARMBRUSTER BN ET AL.: "Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand", PROC NATL ACAD SCI USA., vol. 104, no. 12, 2007, pages 5163 - 5168, XP055185711, DOI: 10.1073/pnas.0700293104
JI ET AL.: "Multimodal Imaging for DREADD-Expressing Neurons in Living Brain and Their Application to Implantation of iPSC-Derived Neural Progenitors", JOURNAL NEUROSCI, vol. 36, no. 45, 2016, pages 11544 - 11558
NAGAI ET AL.: "PET imaging-guided chemogenetic silencing reveals a critical role of primate rostromedial caudate in reward evaluation", NATURE COMMUNICATIONS, vol. 7, 2016, pages 13605
GOMEZ J ET AL.: "Chemogenetics revealed: DREADD occupancy and activation via converted clozapine", SCIENCE, vol. 357, no. 6350, 2017, pages 503 - 507
Attorney, Agent or Firm:
NIIYAMA Yuichi et al. (JP)
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