Title:
EP300/CREBBP INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2018/235966
Kind Code:
A1
Abstract:
The present invention provides a compound which has an excellent inhibitory activity on histone acetyltransferase of EP300 and/or CREBBP, or a pharmacologically acceptable salt of the compound. A compound represented by formula (1) or a pharmacologically acceptable salt of the compound. (In formula (1), ring Q1, ring Q2, R1, R2, R3 and R4 are as defined in the description.)
Inventors:
NAITO HIROYUKI (JP)
KAGOSHIMA YOSHIKO (JP)
FUNAMI HIDEAKI (JP)
NAKAMURA AKIFUMI (JP)
ASANO MASAYOSHI (JP)
HARUTA MAKOTO (JP)
SUZUKI TAKASHI (JP)
WATANABE JUN (JP)
KANADA RYUTARO (JP)
HIGUCHI SAITO (JP)
ITO KENTARO (JP)
EGAMI AKIKO (JP)
KOBAYASHI KATSUHIRO (JP)
KAGOSHIMA YOSHIKO (JP)
FUNAMI HIDEAKI (JP)
NAKAMURA AKIFUMI (JP)
ASANO MASAYOSHI (JP)
HARUTA MAKOTO (JP)
SUZUKI TAKASHI (JP)
WATANABE JUN (JP)
KANADA RYUTARO (JP)
HIGUCHI SAITO (JP)
ITO KENTARO (JP)
EGAMI AKIKO (JP)
KOBAYASHI KATSUHIRO (JP)
Application Number:
PCT/JP2018/024476
Publication Date:
December 27, 2018
Filing Date:
June 21, 2018
Export Citation:
Assignee:
DAIICHI SANKYO CO LTD (JP)
International Classes:
C07D207/16; A61K31/401; A61K31/404; A61K31/4155; A61K31/416; A61K31/426; A61K31/427; A61K31/437; A61K31/4439; A61K31/444; A61K31/4709; A61K31/506; A61K31/5377; A61K31/5383; A61K31/55; A61P35/00; C07D223/06; C07D231/56; C07D277/06; C07D401/12; C07D401/14; C07D403/12; C07D405/14; C07D413/06; C07D417/12; C07D471/04; C07D498/04
Domestic Patent References:
| WO2007082666A1 | 2007-07-26 | |||
| WO1998022432A1 | 1998-05-28 | |||
| WO2016044777A1 | 2016-03-24 | |||
| WO2011085039A2 | 2011-07-14 | |||
| WO2015153410A1 | 2015-10-08 | |||
| WO2016086200A1 | 2016-06-02 | |||
| WO2012162635A1 | 2012-11-29 | |||
| WO2015118342A1 | 2015-08-13 | |||
| WO2015005901A1 | 2015-01-15 |
Foreign References:
| JP2006504796A | 2006-02-09 | |||
| US6124354A | 2000-09-26 | |||
| US6531511B1 | 2003-03-11 | |||
| US20030100772A1 | 2003-05-29 |
Other References:
DATABASE Database REGISTRY [o] 2011, retrieved from STN Database accession no. 1322342-67-5
DATABASE Database REGISTRY [o] 2015, retrieved from STN Database accession no. 1647998-04-6
DATABASE Database REGISTRY [o] 2011, retrieved from STN Database accession no. 1301318-39-7
DATABASE Database REGISTRY [o] 2011, retrieved from STN Database accession no. 1297934-08-7
DATABASE Database REGISTRY [o] 2012, retrieved from STN Database accession no. 1389629-55-3
DATABASE Database REGISTRY [o] 2010, retrieved from STN Database accession no. 1210032-09-9
DATABASE Database REGISTRY [o] 2012, retrieved from STN Database accession no. 1390335-19-9
BOWERS, E. M. ET AL.: "Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor", CHEMISTRY & BIOLOGY, vol. 17, no. 5, 28 May 2010 (2010-05-28), pages 471 - 482, XP002697557, ISSN: 1074-5521
GENES DEV., vol. 16, no. 14, 2002, pages 1739 - 1742
MOL GENET METAB., vol. 119, no. 1-2, 2016, pages 37 - 43
VIROLOGY, vol. 147, no. 1, 1985, pages 142 - 153
MOL CELL BIOL., vol. 6, no. 5, 1986, pages 1579 - 1589
NATURE, vol. 365, no. 6449, 1993, pages 855 - 859
CELL, vol. 87, no. 5, 1996, pages 953 - 959
NATURE, vol. 384, no. 6610, 1996, pages 641 - 643
CELL, vol. 90, no. 4, 1997, pages 595 - 606
LAU OD ET AL., J. BIOL. CHEM., vol. 275, no. 27, 2000, pages 21953 - 21959
SCIENCE, vol. 307, no. 5707, 2005, pages 269 - 273
J. CELL SCI., vol. 114, 2001, pages 2363 - 2373
EPIGENETICS, vol. 6, no. 8, 2011, pages 957 - 961
ADV. EXP. MED. BIOL., vol. 617, 2008, pages 535 - 540
PROSTATE, vol. 68, no. 10, 2008, pages 1097 - 1104
CANCER LETT., vol. 310, no. 2, 2011, pages 140 - 147
J. TRANSL. MED., vol. 9, 2011, pages 5
INT. J. CLIN. EXP. PATHOL., vol. 7, no. 2, 2014, pages 760 - 767
NAT. GENET., vol. 44, no. 10, 2012, pages 1104 - 1110
CLIN. CANCER RES., vol. 11, no. 2, 2005, pages 512 - 519
GENES CANCER, vol. 7, no. 3-4, 2016, pages 98 - 109
ONCOGENE, vol. 12, no. 7, 1996, pages 1565 - 1569
PROC. NATL. ACAD. SCI. USA., vol. 94, no. 16, 1997, pages 8732 - 8737
BLOOD, vol. 120, no. 15, 2012, pages 3058 - 3068
NAT. GENET., vol. 24, no. 3, 2000, pages 300 - 303
NAT. GENET., vol. 43, no. 9, 2011, pages 875 - 878
ONCOL. REP., vol. 36, no. 5, 2016, pages 2763 - 2770
J. BIOL. CHEM., vol. 290, no. 5, 2015, pages 2744 - 2758
ONCOTARGET., vol. 7, no. 14, 2016, pages 17790 - 17804
NAT. CHEM. BIOL., vol. 4, no. 10, 2008, pages 590 - 597
CHEM. BIOL., vol. 17, no. 5, 2010, pages 471 - 482
"Comprehensive Organic Transformations", 1989, ACADEMIC PRESS, INC.
P. G. WUTS: "Protective Groups in Organic Synthesis", 2014
J. MED. CHEM., vol. 35, 1992, pages 2582 - 2591
J. ORG. CHEM., vol. 61, 1996, pages 566 - 572
J. MED. CHEM., vol. 46, 2003, pages 2057 - 2073
ADV. SYNTH. CATAL., vol. 354, 2012, pages 2635 - 2640
SYNLETT, vol. 11, 1998, pages 1279 - 1281
TETRAHEDRON, vol. 49, 1993, pages 4201 - 4210
J. ORG. CHEM., vol. 63, 1998, pages 2442 - 2450
J. ORG. CHEM., vol. 48, 1983, pages 77 - 81
AUST. J. CHEM., vol. 53, 2000, pages 425 - 433
TETRAHEDRON LETT., vol. 42, 2001, pages 3807 - 3809
J. MED. CHEM., vol. 37, 1994, pages 888 - 896
TETRAHEDRON, vol. 54, 1998, pages 981 - 996
TETRAHEDRON LETT., vol. 35, 1994, pages 4649 - 4652
J. ORG. CHEM., vol. 77, 2012, pages 7262 - 7281
BIOORG. MED. CHEM. LETT., vol. 16, 2006, pages 2270 - 2273
J. MED. CHEM., vol. 47, 2004, pages 530 - 549
J. ORG. CHEM., vol. 50, 1985, pages 1356 - 1359
J. MED. CHEM., vol. 49, 2006, pages 3520 - 3535
"ORGANIC FUNCTIONAL GROUP PREPARATIONS'' and ''Comprehensive Organic Transformations", ORG. LETT., vol. 3, 2001, pages 3417 - 3419
ORG. LETT., vol. 3, 2001, pages 2729 - 2732
ORG. LETT., vol. 12, 2010, pages 3748 - 3751
TETRAHEDRON LETT., vol. 49, 2008, pages 7213 - 7216
J. MED. CHEM., vol. 58, 2015, pages 7341 - 7348
J. ORG. CHEM., vol. 59, 1994, pages 6464 - 6469
BIOORG. MED. CHEM. LETT., vol. 21, 2011, pages 1438 - 1441
BIOORG. MED. CHEM. LETT., vol. 12, 2002, pages 2141 - 2144
CHEM. PHARM. BULL., vol. 53, 2005, pages 965 - 973
CHEM. PHARM. BULL., vol. 59, 2011, pages 1376 - 1385
ORG. PROC. RES. DEV., vol. 16, 2012, pages 1069 - 1081
ORG. LETT., vol. 10, 2008, pages 1549 - 1552
CHEM. EUR. J., vol. 18, 2012, pages 4375 - 4379
J. AM. CHEM. SOC., vol. 124, 2002, pages 12557 - 12565
J. ORG. CHEM., vol. 78, 2013, pages 8250 - 8266
GAO T ET AL., METHODS MOL BIOL., vol. 981, 2013, pages 229 - 38
BERNDSEN CE, DENU JM. METHODS, vol. 36, 2005, pages 321 - 33
DATABASE Database REGISTRY [o] 2015, retrieved from STN Database accession no. 1647998-04-6
DATABASE Database REGISTRY [o] 2011, retrieved from STN Database accession no. 1301318-39-7
DATABASE Database REGISTRY [o] 2011, retrieved from STN Database accession no. 1297934-08-7
DATABASE Database REGISTRY [o] 2012, retrieved from STN Database accession no. 1389629-55-3
DATABASE Database REGISTRY [o] 2010, retrieved from STN Database accession no. 1210032-09-9
DATABASE Database REGISTRY [o] 2012, retrieved from STN Database accession no. 1390335-19-9
BOWERS, E. M. ET AL.: "Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor", CHEMISTRY & BIOLOGY, vol. 17, no. 5, 28 May 2010 (2010-05-28), pages 471 - 482, XP002697557, ISSN: 1074-5521
GENES DEV., vol. 16, no. 14, 2002, pages 1739 - 1742
MOL GENET METAB., vol. 119, no. 1-2, 2016, pages 37 - 43
VIROLOGY, vol. 147, no. 1, 1985, pages 142 - 153
MOL CELL BIOL., vol. 6, no. 5, 1986, pages 1579 - 1589
NATURE, vol. 365, no. 6449, 1993, pages 855 - 859
CELL, vol. 87, no. 5, 1996, pages 953 - 959
NATURE, vol. 384, no. 6610, 1996, pages 641 - 643
CELL, vol. 90, no. 4, 1997, pages 595 - 606
LAU OD ET AL., J. BIOL. CHEM., vol. 275, no. 27, 2000, pages 21953 - 21959
SCIENCE, vol. 307, no. 5707, 2005, pages 269 - 273
J. CELL SCI., vol. 114, 2001, pages 2363 - 2373
EPIGENETICS, vol. 6, no. 8, 2011, pages 957 - 961
ADV. EXP. MED. BIOL., vol. 617, 2008, pages 535 - 540
PROSTATE, vol. 68, no. 10, 2008, pages 1097 - 1104
CANCER LETT., vol. 310, no. 2, 2011, pages 140 - 147
J. TRANSL. MED., vol. 9, 2011, pages 5
INT. J. CLIN. EXP. PATHOL., vol. 7, no. 2, 2014, pages 760 - 767
NAT. GENET., vol. 44, no. 10, 2012, pages 1104 - 1110
CLIN. CANCER RES., vol. 11, no. 2, 2005, pages 512 - 519
GENES CANCER, vol. 7, no. 3-4, 2016, pages 98 - 109
ONCOGENE, vol. 12, no. 7, 1996, pages 1565 - 1569
PROC. NATL. ACAD. SCI. USA., vol. 94, no. 16, 1997, pages 8732 - 8737
BLOOD, vol. 120, no. 15, 2012, pages 3058 - 3068
NAT. GENET., vol. 24, no. 3, 2000, pages 300 - 303
NAT. GENET., vol. 43, no. 9, 2011, pages 875 - 878
ONCOL. REP., vol. 36, no. 5, 2016, pages 2763 - 2770
J. BIOL. CHEM., vol. 290, no. 5, 2015, pages 2744 - 2758
ONCOTARGET., vol. 7, no. 14, 2016, pages 17790 - 17804
NAT. CHEM. BIOL., vol. 4, no. 10, 2008, pages 590 - 597
CHEM. BIOL., vol. 17, no. 5, 2010, pages 471 - 482
"Comprehensive Organic Transformations", 1989, ACADEMIC PRESS, INC.
P. G. WUTS: "Protective Groups in Organic Synthesis", 2014
J. MED. CHEM., vol. 35, 1992, pages 2582 - 2591
J. ORG. CHEM., vol. 61, 1996, pages 566 - 572
J. MED. CHEM., vol. 46, 2003, pages 2057 - 2073
ADV. SYNTH. CATAL., vol. 354, 2012, pages 2635 - 2640
SYNLETT, vol. 11, 1998, pages 1279 - 1281
TETRAHEDRON, vol. 49, 1993, pages 4201 - 4210
J. ORG. CHEM., vol. 63, 1998, pages 2442 - 2450
J. ORG. CHEM., vol. 48, 1983, pages 77 - 81
AUST. J. CHEM., vol. 53, 2000, pages 425 - 433
TETRAHEDRON LETT., vol. 42, 2001, pages 3807 - 3809
J. MED. CHEM., vol. 37, 1994, pages 888 - 896
TETRAHEDRON, vol. 54, 1998, pages 981 - 996
TETRAHEDRON LETT., vol. 35, 1994, pages 4649 - 4652
J. ORG. CHEM., vol. 77, 2012, pages 7262 - 7281
BIOORG. MED. CHEM. LETT., vol. 16, 2006, pages 2270 - 2273
J. MED. CHEM., vol. 47, 2004, pages 530 - 549
J. ORG. CHEM., vol. 50, 1985, pages 1356 - 1359
J. MED. CHEM., vol. 49, 2006, pages 3520 - 3535
"ORGANIC FUNCTIONAL GROUP PREPARATIONS'' and ''Comprehensive Organic Transformations", ORG. LETT., vol. 3, 2001, pages 3417 - 3419
ORG. LETT., vol. 3, 2001, pages 2729 - 2732
ORG. LETT., vol. 12, 2010, pages 3748 - 3751
TETRAHEDRON LETT., vol. 49, 2008, pages 7213 - 7216
J. MED. CHEM., vol. 58, 2015, pages 7341 - 7348
J. ORG. CHEM., vol. 59, 1994, pages 6464 - 6469
BIOORG. MED. CHEM. LETT., vol. 21, 2011, pages 1438 - 1441
BIOORG. MED. CHEM. LETT., vol. 12, 2002, pages 2141 - 2144
CHEM. PHARM. BULL., vol. 53, 2005, pages 965 - 973
CHEM. PHARM. BULL., vol. 59, 2011, pages 1376 - 1385
ORG. PROC. RES. DEV., vol. 16, 2012, pages 1069 - 1081
ORG. LETT., vol. 10, 2008, pages 1549 - 1552
CHEM. EUR. J., vol. 18, 2012, pages 4375 - 4379
J. AM. CHEM. SOC., vol. 124, 2002, pages 12557 - 12565
J. ORG. CHEM., vol. 78, 2013, pages 8250 - 8266
GAO T ET AL., METHODS MOL BIOL., vol. 981, 2013, pages 229 - 38
BERNDSEN CE, DENU JM. METHODS, vol. 36, 2005, pages 321 - 33
Attorney, Agent or Firm:
ISHIBASHI, Koki (JP)
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