Title:
NUCLEOSIDE DERIVATIVE HAVING PHYSICAL ACTIVITIES INCLUDING ANTI-VIRAL ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2018/092728
Kind Code:
A1
Abstract:
It is found that a nucleoside derivative represented by general formula (1) has an anti-viral activity and is less toxic to host cells.
[In the formula, R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom or a halogen atom; R3 represents a cyano group, an alkyl group which may have a substituent, an alkenyl group which may have a substituent, an alkynyl group which may have a substituent, a halogen atom or an azide group; R4 represents an amino group, a hydrogen atom, a halogen atom or a hydroxy group; R5 represents a methine group or a nitrogen atom; R6 represents a hydrogen atom or a hydroxy group; and R7 represents a hydrogen atom or a hydroxy group.]
Inventors:
MITSUYA HIROAKI (JP)
KUMAMOTO HIROKI (JP)
KUMAMOTO HIROKI (JP)
Application Number:
PCT/JP2017/040790
Publication Date:
May 24, 2018
Filing Date:
November 13, 2017
Export Citation:
Assignee:
NAT CENTER FOR GLOBAL HEALTH AND MEDICINE (JP)
International Classes:
C07D487/04; A61K31/522; A61P31/12; A61P31/18; A61P31/20
Domestic Patent References:
| WO2016134054A1 | 2016-08-25 | |||
| WO2003068796A1 | 2003-08-21 | |||
| WO2005090349A1 | 2005-09-29 |
Foreign References:
| JP2013510904A | 2013-03-28 | |||
| JPH0680688A | 1994-03-22 | |||
| JPH04282373A | 1992-10-07 | |||
| JP2011503234A | 2011-01-27 | |||
| JP2004244422A | 2004-09-02 | |||
| JP2008273960A | 2008-11-13 | |||
| JP2001335592A | 2001-12-04 | |||
| JP2001335593A | 2001-12-04 | |||
| JP2004107329A | 2004-04-08 |
Other References:
OHRUI, HIROSHI: "Creation of low-toxic high-activity reverse transcriptase-inhibiting nucleosides that do not express resistant HIV. Could it be a magic bullet for AIDS and hepatitis B dreams?]", KAGAKU TO SEIBUTSU, vol. 44, no. 10, 2006, pages 660 - 662, XP009514931
TAKAMATSU, Y. ET AL.: "4′-modified nucleoside analogs: Potent inhibitors active against entecavir-resistant hepatitis B virus", HEPATOLOGY, vol. 62, no. 4, 2015, pages 1024 - 1036, XP055605356, ISSN: 0270-9139, DOI: 10.1002/hep.27962
KODAMA, E.: "4'-Ethynyl Nucleoside Analogs: Potent Inhibitors of Multidrug-Resistant Human Immunodeficiency Virus Variants In Vitro", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, vol. 45, no. 5, 2001, pages 1539 - 1546, XP001127402, ISSN: 0066-4804, DOI: 10.1128/AAC.45.5.1539-1546.2001
KUMAMOTO, H . ET AL.: "Diastereoselective Synthesis of 6″-( Z )- and 6″-( E )-Fluoro Analogues of Anti-hepatitis B Virus Agent Entecavir and Its Evaluation of the Activity and Toxicity Profile of the Diastereomers", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 81, no. 7, 24 March 2016 (2016-03-24), pages 2827 - 2836, XP055605358, ISSN: 0022-3263, DOI: 10.1021/acs.joc.6b00105
J. ORG. CHEM., vol. 69, 2004, pages 2634
J. ORG. CHEM., vol. 65, 2000, pages 7697
See also references of EP 3543238A4
TAKAMATSU, Y. ET AL.: "4′-modified nucleoside analogs: Potent inhibitors active against entecavir-resistant hepatitis B virus", HEPATOLOGY, vol. 62, no. 4, 2015, pages 1024 - 1036, XP055605356, ISSN: 0270-9139, DOI: 10.1002/hep.27962
KODAMA, E.: "4'-Ethynyl Nucleoside Analogs: Potent Inhibitors of Multidrug-Resistant Human Immunodeficiency Virus Variants In Vitro", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, vol. 45, no. 5, 2001, pages 1539 - 1546, XP001127402, ISSN: 0066-4804, DOI: 10.1128/AAC.45.5.1539-1546.2001
KUMAMOTO, H . ET AL.: "Diastereoselective Synthesis of 6″-( Z )- and 6″-( E )-Fluoro Analogues of Anti-hepatitis B Virus Agent Entecavir and Its Evaluation of the Activity and Toxicity Profile of the Diastereomers", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 81, no. 7, 24 March 2016 (2016-03-24), pages 2827 - 2836, XP055605358, ISSN: 0022-3263, DOI: 10.1021/acs.joc.6b00105
J. ORG. CHEM., vol. 69, 2004, pages 2634
J. ORG. CHEM., vol. 65, 2000, pages 7697
See also references of EP 3543238A4
Attorney, Agent or Firm:
CENTCREST IP ATTORNEYS (JP)
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