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Title:
OPIOID RECEPTOR ANTAGONIST AND PHARMACEUTICAL COMPOSITION
Document Type and Number:
WIPO Patent Application WO/2023/054006
Kind Code:
A1
Abstract:
Provided are an opioid receptor antagonist, which contains, as an active ingredient, one atropisomer between a pair of atropisomers of a compound represented by formula (1), said atropisomer having an opioid receptor antagonistic action, or a pharmacologically acceptable salt thereof, and a pharmaceutical composition. In formula (1), R1 represents a heteroaryl group, etc. and R2 and R3 independently represent an alkyl group, etc.

Inventors:
TAKAHASHI HIDEYO (JP)
MAKINO KOSHO (JP)
ARITA HIRONOBU (JP)
KIKUKAWA SHUNTARO (JP)
TOMIZAWA TSUKASA (JP)
FUNADA MASAHIKO (JP)
TOMIYAMA KENICHI (JP)
Application Number:
PCT/JP2022/034681
Publication Date:
April 06, 2023
Filing Date:
September 16, 2022
Export Citation:
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Assignee:
UNIV TOKYO SCIENCE FOUND (JP)
NAT CENTER NEUROLOGY & PSYCHIATRY (JP)
International Classes:
A61K31/4468; A61K31/4525; A61P43/00; C07D405/12
Domestic Patent References:
WO2006101245A12006-09-28
Foreign References:
JPS60248670A1985-12-09
US20210396706A12021-12-23
Other References:
SINGH P., PAI U. B.: "EFFECT OF MOLECULAR SIZE ON OPIATE RECEPTOR AFFINITY OF FENTANYL DERIVATIVES & ALPHA1-AGONIST POTENCY OF 2-AMINOTETRALINS.", INDIAN JOURNAL OF CHEMISTRY, COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH (C S I R), IN, vol. 22B., no. 10., 1 October 1983 (1983-10-01), IN , pages 1076 - 1078., XP000853930, ISSN: 0019-5103
DUFFY JONATHAN, URBAS AARON, NIEMITZ MATTHIAS, LIPPA KATRICE, MARGINEAN IOAN: "Differentiation of fentanyl analogues by low-field NMR spectroscopy", ANALYTICA CHIMICA ACTA, vol. 1049, 1 February 2019 (2019-02-01), AMSTERDAM, NL , pages 161 - 169, XP093054470, ISSN: 0003-2670, DOI: 10.1016/j.aca.2018.12.014
LAMY FRANCOIS R.; DANIULAITYTE RAMINTA; BARRATT MONICA J.; LOKALA USHA; SHETH AMIT; CARLSON ROBERT G.: "Listed for sale: Analyzing data on fentanyl, fentanyl analogs and other novel synthetic opioids on one cryptomarket", DRUG AND ALCOHOL DEPENDENCE, vol. 213, 12 June 2020 (2020-06-12), IR , XP086215752, ISSN: 0376-8716, DOI: 10.1016/j.drugalcdep.2020.108115
LURIE, I.S. ; IIO, R.: "Use of multiple-reaction monitoring ratios for identifying incompletely resolved fentanyl homologs and analogs via ultra-high-pressure liquid chromatography-tandem mass spectrometry", JOURNAL OF CHROMATOGRAPHY A, vol. 1216, no. 9, 27 February 2009 (2009-02-27), AMSTERDAM, NL, pages 1515 - 1519, XP025909474, ISSN: 0021-9673, DOI: 10.1016/j.chroma.2008.12.097
Attorney, Agent or Firm:
SHOBAYASHI Masayuki et al. (JP)
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