Title:
G9a INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2021/106988
Kind Code:
A1
Abstract:
It was found that a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof has potent G9a inhibitory activity. Because of the ability to inhibit G9a, the compound (I) or a pharmaceutically acceptable salt thereof is highly useful in treatment, prevention or suppression of a variety of diseases (including proliferative diseases such as cancer, β-globin abnormalities, fibrosis, pain, neurodegenerative diseases, Prader-Willi syndrome, malaria, viral infections, myopathy, and autism).
Inventors:
SUMIYA TATSUNOBU (JP)
NISHIGAYA YOSUKE (JP)
NAMIE RYOSUKE (JP)
HASHIMOTO NORIAKI (JP)
ITO AKIHIRO (JP)
SHIRAI FUMIYUKI (JP)
KIKUZATO KO (JP)
YOSHIDA MINORU (JP)
NISHIGAYA YOSUKE (JP)
NAMIE RYOSUKE (JP)
HASHIMOTO NORIAKI (JP)
ITO AKIHIRO (JP)
SHIRAI FUMIYUKI (JP)
KIKUZATO KO (JP)
YOSHIDA MINORU (JP)
Application Number:
PCT/JP2020/043966
Publication Date:
June 03, 2021
Filing Date:
November 26, 2020
Export Citation:
Assignee:
KYORIN SEIYAKU KK (JP)
RIKEN (JP)
TOKYO UNIV OF PHARMACY AND LIFE SCIENCE (JP)
MICROBIAL CHEM RES FOUND (JP)
RIKEN (JP)
TOKYO UNIV OF PHARMACY AND LIFE SCIENCE (JP)
MICROBIAL CHEM RES FOUND (JP)
International Classes:
A61P7/00; A61K31/404; A61K31/407; A61K31/4155; A61K31/416; A61K31/4184; A61K31/4427; A61K31/4439; A61K31/444; A61K31/454; A61K31/4545; A61K31/4709; A61K31/4725; A61K31/496; A61K31/5377; A61K31/551; A61P21/00; A61P25/00; A61P25/04; A61P29/00; A61P31/12; A61P33/06; A61P35/00; A61P35/02; A61P35/04; A61P43/00; C07D209/42; C07D209/96; C07D213/75; C07D401/12; C07D401/14; C07D403/12; C07D405/12; C07D405/14; C07D417/12; C07D417/14; C07D471/04; C07D487/10; C07D491/107
Domestic Patent References:
| WO2015130964A1 | 2015-09-03 | |||
| WO2008135526A1 | 2008-11-13 | |||
| WO2017176962A1 | 2017-10-12 | |||
| WO2012023285A1 | 2012-02-23 | |||
| WO2013140148A1 | 2013-09-26 | |||
| WO2012023285A1 | 2012-02-23 | |||
| WO2013140148A1 | 2013-09-26 |
Foreign References:
| US3255202A | 1966-06-07 | |||
| US20150274660A1 | 2015-10-01 | |||
| US20150274660A1 | 2015-10-01 | |||
| JP2019513778A | 2019-05-30 | |||
| JP2019511472A | 2019-04-25 |
Other References:
DATABASE Database RECISTRY [online] 2018, XP055833093, retrieved from STN Database accession no. 2195593-70-3
DATABASE Database RECISTRY [online] 2011, XP055833095, retrieved from STN Database accession no. 1277333-97-7
DATABASE Database RECISTRY [online] 2014, XP055833104, retrieved from STN Database accession no. 1385078-76-1
DATABASE Database RECISTRY [online] 2014, XP055833098, retrieved from STN Database accession no. 1581959-49-0
FOX, S. W. ET AL.: "Enzymic synthesis of peptide bonds. VI. The influence of residue type on papain-catalyzed reactions of some benzoylamino acids with some amino acid anilides", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 75, 1953, pages 5539 - 5542, XP055833108, DOI: 10.1021/ja01118a02 1
KRIVEGA I. ET AL., BLOOD, vol. 126, no. 5, 2015, pages 665 - 672
LIN X. ET AL., ONCOL. REP., vol. 35, no. 5, 2016, pages 3041 - 3049
QIN J ET AL., ONCOL LETT, vol. 15, no. 6, 2017, pages 9757 - 9765
LEHNERTZ B ET AL., GENES DEV, vol. 28, no. 4, 2014, pages 317 - 327
CHEN R.J. ET AL., ONCOTARGET, vol. 8, no. 37, 2017, pages 62081 - 62098
KE X.X. ET AL., ANTICANCER DRUGS, vol. 24, no. 5, 2013, pages 484 - 493
GUO A.S. ET AL., MOL. MED. REP., vol. 14, no. 5, 2016, pages 4613 - 4621
PAN M.R. ET AL., ONCOTARGET, vol. 7, no. 38, 2016, pages 61136 - 61151
ZHANG J ET AL., ONCOTARGET, vol. 6, no. 5, 2015, pages 2917 - 2927
LI K.C. ET AL., MOL. CANCER., vol. 13, no. 172, 2014
DONG C. ET AL., J. CLIN. INVEST., vol. 122, no. 4, 2012, pages 1469 - 1486
CHEN M.W. ET AL., CANCER RES., vol. 70, no. 20, 2010, pages 7830 - 7840
HUA K.T. ET AL., MOL CANCER, vol. 13, no. 189, 2014
LOH S.W. ET AL., PLOS ONE, vol. 9, no. 7, 2014, pages e103915
LIGRESTI G ET AL., JCI INSIGHT, vol. 5, 2019, pages 127111
IRIFUKU T. ET AL., KIDNEY INT, vol. 89, no. 1, 2016, pages 147 - 157
SHARMA M. ET AL., AGING CELL, vol. 16, no. 5, 2017, pages 1062 - 1072
LAUMET G. ET AL., NEUROSCI, vol. 18, no. 12, 2015, pages 1746 - 1755
KIM Y. ET AL., NAT. MED., vol. 23, no. 2, 2017, pages 213 - 222
SINGH N. ET AL., J. INTERFERON CYTOKINE RES., vol. 36, no. 1, 2016, pages 37 - 47
OW J.R. ET AL., SCI. REP., vol. 6, 2016, pages 34163
WANG Z.J. ET AL., MOL. PSYCHIATRY, 2019
MIURA S ET AL., AM. J. DERMATOPATHOL, vol. 36, no. 3, 2014, pages 211 - 216
KUROKI S ET AL., PLOS GENET, vol. 13, no. 9, 2017, pages e1007034
J. PHARM. SCI., vol. 66, 1977, pages 1 - 19
STAHLWERMUTH: "Handbook of Pharmaceutical Salts: Properties, Selection, and Use", 2002, WILEY-VCH
THEODORA W. GREENEPETER G. M. WUTS: "Greene's Protective Groups in Organic Synthesis", 2006, WILEY-INTERSCIENCE
See also references of EP 4066896A4
DATABASE Database RECISTRY [online] 2011, XP055833095, retrieved from STN Database accession no. 1277333-97-7
DATABASE Database RECISTRY [online] 2014, XP055833104, retrieved from STN Database accession no. 1385078-76-1
DATABASE Database RECISTRY [online] 2014, XP055833098, retrieved from STN Database accession no. 1581959-49-0
FOX, S. W. ET AL.: "Enzymic synthesis of peptide bonds. VI. The influence of residue type on papain-catalyzed reactions of some benzoylamino acids with some amino acid anilides", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 75, 1953, pages 5539 - 5542, XP055833108, DOI: 10.1021/ja01118a02 1
KRIVEGA I. ET AL., BLOOD, vol. 126, no. 5, 2015, pages 665 - 672
LIN X. ET AL., ONCOL. REP., vol. 35, no. 5, 2016, pages 3041 - 3049
QIN J ET AL., ONCOL LETT, vol. 15, no. 6, 2017, pages 9757 - 9765
LEHNERTZ B ET AL., GENES DEV, vol. 28, no. 4, 2014, pages 317 - 327
CHEN R.J. ET AL., ONCOTARGET, vol. 8, no. 37, 2017, pages 62081 - 62098
KE X.X. ET AL., ANTICANCER DRUGS, vol. 24, no. 5, 2013, pages 484 - 493
GUO A.S. ET AL., MOL. MED. REP., vol. 14, no. 5, 2016, pages 4613 - 4621
PAN M.R. ET AL., ONCOTARGET, vol. 7, no. 38, 2016, pages 61136 - 61151
ZHANG J ET AL., ONCOTARGET, vol. 6, no. 5, 2015, pages 2917 - 2927
LI K.C. ET AL., MOL. CANCER., vol. 13, no. 172, 2014
DONG C. ET AL., J. CLIN. INVEST., vol. 122, no. 4, 2012, pages 1469 - 1486
CHEN M.W. ET AL., CANCER RES., vol. 70, no. 20, 2010, pages 7830 - 7840
HUA K.T. ET AL., MOL CANCER, vol. 13, no. 189, 2014
LOH S.W. ET AL., PLOS ONE, vol. 9, no. 7, 2014, pages e103915
LIGRESTI G ET AL., JCI INSIGHT, vol. 5, 2019, pages 127111
IRIFUKU T. ET AL., KIDNEY INT, vol. 89, no. 1, 2016, pages 147 - 157
SHARMA M. ET AL., AGING CELL, vol. 16, no. 5, 2017, pages 1062 - 1072
LAUMET G. ET AL., NEUROSCI, vol. 18, no. 12, 2015, pages 1746 - 1755
KIM Y. ET AL., NAT. MED., vol. 23, no. 2, 2017, pages 213 - 222
SINGH N. ET AL., J. INTERFERON CYTOKINE RES., vol. 36, no. 1, 2016, pages 37 - 47
OW J.R. ET AL., SCI. REP., vol. 6, 2016, pages 34163
WANG Z.J. ET AL., MOL. PSYCHIATRY, 2019
MIURA S ET AL., AM. J. DERMATOPATHOL, vol. 36, no. 3, 2014, pages 211 - 216
KUROKI S ET AL., PLOS GENET, vol. 13, no. 9, 2017, pages e1007034
J. PHARM. SCI., vol. 66, 1977, pages 1 - 19
STAHLWERMUTH: "Handbook of Pharmaceutical Salts: Properties, Selection, and Use", 2002, WILEY-VCH
THEODORA W. GREENEPETER G. M. WUTS: "Greene's Protective Groups in Organic Synthesis", 2006, WILEY-INTERSCIENCE
See also references of EP 4066896A4
Attorney, Agent or Firm:
HIRAKI & ASSOCIATES (JP)
Download PDF: