Title:
(R)-N-ETHYL-5-FLUORO-N-ISOPROPYL-2-((5-(2-(6-((2-METHOXYETHYL)(METHYL)AMINO)-2-M ETHYLHEXAN-3-YL)-2,6-DIAZASPIRO[3.4]OCTAN-6-YL)-1,2,4-TRIAZIN-6-YL)OXY)BENZAMIDE BESYLATE SALT FOR THE TREATMENT OF DISEASES SUCH AS CANCER
Document Type and Number:
WIPO Patent Application WO/2022/262796
Kind Code:
A1
Abstract:
The present invention relates to (R) -N-ethyl-5-fluoro-N-isopropyl-2- ( (5- (2- (6- ( (2-methoxyethyl) (methyl) amino) -2-methylhexan-3-yl) -2, 6-diazaspiro [3.4] octan-6-yl) -1, 2, 4-triazin-6-yl) oxy) benzamide besylate salt and solvates thereof. This compound may be useful for therapy and/or prophylaxis in a mammal, pharmaceutical composition comprising such compound, and use as menin/MLL protein/protein interaction inhibitor, useful for treating diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN); and diabetes.
Inventors:
CAI WEI (CN)
DAI XUEDONG (CN)
QUEROLLE OLIVIER ALEXIS GEORGES (FR)
THURING JOHANNES WILHELMUS J (BE)
NG ALICIA TEE FUAY (CN)
DARVILLE NICOLAS FREDDY JACQUES BRUNO (BE)
GEERTMAN ROBERT MICHAEL (BE)
AHUJA DIPALI (BE)
LIU YINGTAO (CN)
PANDE VINEET (BE)
CLEATOR EDWARD (BE)
BEN HAIM CYRIL (BE)
SMOLDERS SIMON JAN C (BE)
DAI XUEDONG (CN)
QUEROLLE OLIVIER ALEXIS GEORGES (FR)
THURING JOHANNES WILHELMUS J (BE)
NG ALICIA TEE FUAY (CN)
DARVILLE NICOLAS FREDDY JACQUES BRUNO (BE)
GEERTMAN ROBERT MICHAEL (BE)
AHUJA DIPALI (BE)
LIU YINGTAO (CN)
PANDE VINEET (BE)
CLEATOR EDWARD (BE)
BEN HAIM CYRIL (BE)
SMOLDERS SIMON JAN C (BE)
Application Number:
PCT/CN2022/099089
Publication Date:
December 22, 2022
Filing Date:
June 16, 2022
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NV (BE)
JOHNSON & JOHNSON CHINA INVEST LTD (CN)
JOHNSON & JOHNSON CHINA INVEST LTD (CN)
International Classes:
C07D487/04; A61K31/53; A61P35/00; C07C1/00; C07D487/10
Domestic Patent References:
| WO2021121327A1 | 2021-06-24 | |||
| WO2011029054A1 | 2011-03-10 | |||
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| WO2016195776A1 | 2016-12-08 | |||
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| WO2017192543A1 | 2017-11-09 | |||
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IVAN KOPLJAR ET AL., JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, vol. 91, 2018, pages 80 - 86
LU ET AL., TOX SCI, vol. 170, no. 2, 2019, pages 345 - 356
KOPLJAR ET AL., STEM CELL REPORTS, November 2018 (2018-11-01), pages 1365 - 1377
KOPLJAR ET AL., STEM CELL REPORTS, vol. 11, 2018, pages 1365 - 1377
JOHNSON JI ET AL., BR J CANCER, vol. 84, no. 10, 2001, pages 1424 - 1431
TOMIZAWA ET AL., PEDIATR BLOOD CANCER, vol. 49, no. 2, 2007, pages 127 - 32
MISHRA ET AL., CELL REP, vol. 7, no. 4, 2014, pages 1239 - 47
MEYER ET AL., LEUKEMIA, vol. 27, 2013, pages 2165 - 2176
THIEL ET AL., BIOESSAYS, vol. 34, 2012, pages 771 - 80
CERMAKOVA ET AL., CANCER RES, vol. 15, 2014, pages 5139 - 51
YOKOYAMACLEARY, CANCER CELL, vol. 8, 2008, pages 36 - 46
CHEN ET AL., PROC NATL ACAD SCI, vol. 103, 2006, pages 1018 - 23
YOKOYAMA ET AL., CELL, vol. 123, 2005, pages 207 - 18
BORKIN ET AL., CANCER CELL, vol. 27, 2015, pages 589 - 602
CIERPICKIGREMBECKA, FUTURE MED CHEM, vol. 6, 2014, pages 447 - 462
LI ET AL., BLOOD, vol. 122, 2013, pages 2039 - 2046
MALIK ET AL., NAT MED, vol. 21, 2015, pages 344 - 52
J MED CHEM, vol. 59, 2016, pages 892 - 913
NATURE CHEMICAL BIOLOGY, vol. 8, March 2012 (2012-03-01), pages 277 - 284
REN, J. ET AL., BIOORG MED CHEM LETT, vol. 26, no. 18, 2016, pages 4472 - 4476
JMED CHEM, vol. 57, 2014, pages 1543 - 1556
KRIVTSOV ET AL., CANCER CELL, vol. 36, no. 6, 2019, pages 660 - 673
GENNARO ET AL.: "Remington's Pharmaceutical Sciences", 1990, MACK PUBLISHING COMPANY, article "Pharmaceutical preparations and their Manufacture"
IVAN KOPLJAR ET AL., JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, vol. 91, 2018, pages 80 - 86
LU ET AL., TOX SCI, vol. 170, no. 2, 2019, pages 345 - 356
KOPLJAR ET AL., STEM CELL REPORTS, November 2018 (2018-11-01), pages 1365 - 1377
KOPLJAR ET AL., STEM CELL REPORTS, vol. 11, 2018, pages 1365 - 1377
JOHNSON JI ET AL., BR J CANCER, vol. 84, no. 10, 2001, pages 1424 - 1431
Attorney, Agent or Firm:
NTD UNIVATION INTELLECTUAL PROPERTY AGENCY LTD. (CN)
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