Title:
ANTI-SARS-COV-2 DRUG
Document Type and Number:
WIPO Patent Application WO/2021/235390
Kind Code:
A1
Abstract:
The present invention pertains to an anti-SARS-CoV-2 drug containing a compound represented by formula (I): [in the formula, one of Ra and Rc is a substituted phenylamino group, the other of Ra and Rc is a hydrogen atom, a deuterium atom, or a C1-10-alkyl group, Rb, Rf, and Rg are the same or different and are hydrogen atoms or deuterium atoms, Rd is a hydrogen atom, a deuterium atom, or a chlorine atom, and Re is a hydrogen atom, a deuterium atom, or a halogen atom] or a salt thereof, or a solvate of these.
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Inventors:
BABA MASANORI (JP)
OKAMOTO MIKA (JP)
TOYAMA MASAAKI (JP)
AOKI SHIN (JP)
TANAKA TOMOHIRO (JP)
OKAMOTO MIKA (JP)
TOYAMA MASAAKI (JP)
AOKI SHIN (JP)
TANAKA TOMOHIRO (JP)
Application Number:
PCT/JP2021/018602
Publication Date:
November 25, 2021
Filing Date:
May 17, 2021
Export Citation:
Assignee:
UNIV KAGOSHIMA (JP)
UNIV TOKYO SCIENCE FOUND (JP)
UNIV TOKYO SCIENCE FOUND (JP)
International Classes:
A61K31/4706; A61K31/4709; A61K31/5377; A61K31/541; A61K31/554; A61P31/14; C07D215/38; C07D215/44; C07D215/46
Domestic Patent References:
| WO2018191642A1 | 2018-10-18 | |||
| WO2018135449A1 | 2018-07-26 |
Other References:
JEON, S ET AL.: "Identification of antiviral drug candidates against SARS- CoV-2 from FDA-approved drugs", BIORXIV, 28 March 2020 (2020-03-28), pages 1 - 9, XP055825491, DOI: https:// doi.org/10.1101/ 2020.03.20.999730
ARSHAD USMAN, PERTINEZ HENRY, BOX HELEN, TATHAM LEE, RAJOLI RAJITH KR, CURLEY PAUL, NEARY MEGAN, SHARP JOANNE, LIPTROTT NEILL J, V: "Prioritisation of potential anti-SARS-CoV-2 drug repurposing opportunities based on ability to achieve adequate plasma and target site concentrations derived from thier established human pharmacokinetics", MEDRXIV, 22 April 2020 (2020-04-22), pages 1 - 37, XP055875256, DOI: https:// doi.org/10.1101/ 2020.04.16.20068379
KO, M. ET AL.: "Comparative analysis of antiviral efficacy of FDA-approved drugs against SARS-CoV-2 in human lung cells: Nafamostat is the most potent antivral drug candidate", BIORXIV, 12 May 2020 (2020-05-12), pages 1 - 18, XP055832266, DOI: https:// doi. org/10.1101/ 2020.05.12.090035
DATABASE REGISTRY 2 February 2011 (2011-02-02), "CN -INDEX NAME NOT YET ASSIGNED MF -C20 H12 Cl D10 N3 O . 2 Cl H SR", XP055875281, retrieved from STN Database accession no. 1261394-79-9
DATABASE REGISTRY 22 October 2009 (2009-10-22), "CN -INDEX NAME NOT YET ASSIGNED OTHER NAMES: CN -2-[(Bis(1,1,2,2,2-pentadeuterioethyl)amino)methyl]-4-[(7-chloroquinolin-4- yl)amino]phenol", XP055875283, retrieved from STN Database accession no. 1189449-70-4
DATABASE REGISTRY 15 April 2009 (2009-04-15), "Phenol, 2-[[bis(2-chloroethyl)amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]-, hydrochloride (1:1) (CA INDEX NAME)", XP055875285, retrieved from STN Database accession no. 1135025-04-5
DATABASE REGISTRY 22 December 2008 (2008-12-22), "CN - Phenol, 2-[[bis(2-ethylhexyl)amino]methyl]-4-[(7-chloro-4-quinolinyl)amino]- (CA INDEX NAME)", XP055875287, retrieved from STN Database accession no. 1088233-44-6
DATABASE REGISTRY 22 December 2008 (2008-12-22), "CN - Phenol, 2-[[bis(phenylmethyl)amino]methyl]-4-[(7-chloro-4-quinolinyl)amino]- (CA INDEX NAME)", XP055875290, retrieved from STN Database accession no. 1088232-06-7
DATABASE REGISTRY 7 November 2008 (2008-11-07), "CN - Phenol, 2-[(butylethylamino)methyl]-4-[(7-chloro-4-quinolinyl)amino]- (CA INDEX NAME)", XP055875293, retrieved from STN Database accession no. 1071655-76-9
DATABASE REGISTRY 17 September 2008 (2008-09-17), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(dipentylamino)methyl]-, hydrochloride (1:1) (CA INDEX NAME)", XP055875297, retrieved from STN Database accession no. 1049789-20-9
DATABASE REGISTRY 2 April 2006 (2006-04-02), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(2-methyl-1- piperidinyl)methyl]- (CA INDEX NAME)", XP055875303, retrieved from STN Database accession no. 878902-87-5
DATABASE REGISTRY 27 December 2004 (2004-12-27), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[[2-[2-(diethylamino)ethyl]-1- piperidinyl]methyl]- (CA INDEX NAME)", XP055875306, retrieved from STN Database accession no. 803621-12-7
DATABASE REGISTRY 26 December 2004 (2004-12-26), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(decylmethylamino)methyl]- (CA INDEX NAME)", XP055875308, retrieved from STN Database accession no. 802595-07-9
DATABASE REGISTRY 23 December 2004 (2004-12-23), "CN - Phenol, 2-[[bis[2-(diethylamino)ethyl]amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]- (CA INDEX NAME)", XP055875310, retrieved from STN Database accession no. 802025-59-8
DATABASE REGISTRY 22 December 2004 (2004-12-22), "CN - Phenol, 2-[[bis[(tetrahydro-2-furanyl)methyl]amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]- (CA INDEX NAME)", XP055875311, retrieved from STN Database accession no. 801191-15-1
DATABASE REGISTRY 1 September 2004 (2004-09-01), "CN - Phenol, 2-(1-pyrrolidinylmethyl)-4-(4-quinolinylamino)- (CA INDEX NAME)", XP055875313, retrieved from STN Database accession no. 736877-77-3
DATABASE REGISTRY 16 November 1984 (1984-11-16), "CN - Phenol, 2-[[bis(2-methoxyethyl)amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]- (CA INDEX NAME)", XP055875315, retrieved from STN Database accession no. 23539-54-0
DATABASE REGISTRY 16 November 1984 (1984-11-16), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(4-ethyl-1-piperazinyl)methyl]-(CA INDEX NAME)", XP055875317, retrieved from STN Database accession no. 23539-53-9
DATABASE REGISTRY 16 November 1984 (1984-11-16), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[[(2- furanylmethyl)methylamino]methyl]- (CA INDEX NAME)", XP055875319, retrieved from STN Database accession no. 23539-34-6
ARSHAD USMAN, PERTINEZ HENRY, BOX HELEN, TATHAM LEE, RAJOLI RAJITH KR, CURLEY PAUL, NEARY MEGAN, SHARP JOANNE, LIPTROTT NEILL J, V: "Prioritisation of potential anti-SARS-CoV-2 drug repurposing opportunities based on ability to achieve adequate plasma and target site concentrations derived from thier established human pharmacokinetics", MEDRXIV, 22 April 2020 (2020-04-22), pages 1 - 37, XP055875256, DOI: https:// doi.org/10.1101/ 2020.04.16.20068379
KO, M. ET AL.: "Comparative analysis of antiviral efficacy of FDA-approved drugs against SARS-CoV-2 in human lung cells: Nafamostat is the most potent antivral drug candidate", BIORXIV, 12 May 2020 (2020-05-12), pages 1 - 18, XP055832266, DOI: https:// doi. org/10.1101/ 2020.05.12.090035
DATABASE REGISTRY 2 February 2011 (2011-02-02), "CN -INDEX NAME NOT YET ASSIGNED MF -C20 H12 Cl D10 N3 O . 2 Cl H SR", XP055875281, retrieved from STN Database accession no. 1261394-79-9
DATABASE REGISTRY 22 October 2009 (2009-10-22), "CN -INDEX NAME NOT YET ASSIGNED OTHER NAMES: CN -2-[(Bis(1,1,2,2,2-pentadeuterioethyl)amino)methyl]-4-[(7-chloroquinolin-4- yl)amino]phenol", XP055875283, retrieved from STN Database accession no. 1189449-70-4
DATABASE REGISTRY 15 April 2009 (2009-04-15), "Phenol, 2-[[bis(2-chloroethyl)amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]-, hydrochloride (1:1) (CA INDEX NAME)", XP055875285, retrieved from STN Database accession no. 1135025-04-5
DATABASE REGISTRY 22 December 2008 (2008-12-22), "CN - Phenol, 2-[[bis(2-ethylhexyl)amino]methyl]-4-[(7-chloro-4-quinolinyl)amino]- (CA INDEX NAME)", XP055875287, retrieved from STN Database accession no. 1088233-44-6
DATABASE REGISTRY 22 December 2008 (2008-12-22), "CN - Phenol, 2-[[bis(phenylmethyl)amino]methyl]-4-[(7-chloro-4-quinolinyl)amino]- (CA INDEX NAME)", XP055875290, retrieved from STN Database accession no. 1088232-06-7
DATABASE REGISTRY 7 November 2008 (2008-11-07), "CN - Phenol, 2-[(butylethylamino)methyl]-4-[(7-chloro-4-quinolinyl)amino]- (CA INDEX NAME)", XP055875293, retrieved from STN Database accession no. 1071655-76-9
DATABASE REGISTRY 17 September 2008 (2008-09-17), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(dipentylamino)methyl]-, hydrochloride (1:1) (CA INDEX NAME)", XP055875297, retrieved from STN Database accession no. 1049789-20-9
DATABASE REGISTRY 2 April 2006 (2006-04-02), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(2-methyl-1- piperidinyl)methyl]- (CA INDEX NAME)", XP055875303, retrieved from STN Database accession no. 878902-87-5
DATABASE REGISTRY 27 December 2004 (2004-12-27), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[[2-[2-(diethylamino)ethyl]-1- piperidinyl]methyl]- (CA INDEX NAME)", XP055875306, retrieved from STN Database accession no. 803621-12-7
DATABASE REGISTRY 26 December 2004 (2004-12-26), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(decylmethylamino)methyl]- (CA INDEX NAME)", XP055875308, retrieved from STN Database accession no. 802595-07-9
DATABASE REGISTRY 23 December 2004 (2004-12-23), "CN - Phenol, 2-[[bis[2-(diethylamino)ethyl]amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]- (CA INDEX NAME)", XP055875310, retrieved from STN Database accession no. 802025-59-8
DATABASE REGISTRY 22 December 2004 (2004-12-22), "CN - Phenol, 2-[[bis[(tetrahydro-2-furanyl)methyl]amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]- (CA INDEX NAME)", XP055875311, retrieved from STN Database accession no. 801191-15-1
DATABASE REGISTRY 1 September 2004 (2004-09-01), "CN - Phenol, 2-(1-pyrrolidinylmethyl)-4-(4-quinolinylamino)- (CA INDEX NAME)", XP055875313, retrieved from STN Database accession no. 736877-77-3
DATABASE REGISTRY 16 November 1984 (1984-11-16), "CN - Phenol, 2-[[bis(2-methoxyethyl)amino]methyl]-4-[(7-chloro-4- quinolinyl)amino]- (CA INDEX NAME)", XP055875315, retrieved from STN Database accession no. 23539-54-0
DATABASE REGISTRY 16 November 1984 (1984-11-16), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(4-ethyl-1-piperazinyl)methyl]-(CA INDEX NAME)", XP055875317, retrieved from STN Database accession no. 23539-53-9
DATABASE REGISTRY 16 November 1984 (1984-11-16), "CN - Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[[(2- furanylmethyl)methylamino]methyl]- (CA INDEX NAME)", XP055875319, retrieved from STN Database accession no. 23539-34-6
Attorney, Agent or Firm:
HIRAKI & ASSOCIATES (JP)
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