Title:
ANTITUMOR AGENT AND BROMODOMAIN INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2018/124180
Kind Code:
A1
Abstract:
The present invention addresses the problem of providing an antitumor agent that is exceptional as a treatment agent for the prevention and/or treatment of tumors involving bromodomains, and providing a bromodomain inhibitor that is useful as a treatment agent for diseases or conditions involving bromodomains. An antitumor agent and bromodomain inhibitor containing a compound represented by the general formula [in the formula, R1 represents a C1-6 alkyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a halogen atom, etc.; Z1, Z2, and Z3 represent CH, etc.; X1 represents CONH, etc.; ring A represents a phenyl group, etc.; R4 represents a halogen atom, etc.; and m represents an integer of 0-5] have exceptional bromodomain inhibitory activity and are useful as treatment agents for the prevention and/or treatment of tumors involving bromodomains.
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Inventors:
MAKITA KEIKO (JP)
SAEKI KAZUNORI (JP)
TANAKA TADASHI (JP)
FUJINO MASATAKA (JP)
NATSUME TOHRU (JP)
FURUYA KENTARO (JP)
SAEKI KAZUNORI (JP)
TANAKA TADASHI (JP)
FUJINO MASATAKA (JP)
NATSUME TOHRU (JP)
FURUYA KENTARO (JP)
Application Number:
PCT/JP2017/046901
Publication Date:
July 05, 2018
Filing Date:
December 27, 2017
Export Citation:
Assignee:
FUJIFILM CORP (JP)
TOYAMA CHEMICAL CO LTD (JP)
AIST (JP)
TOYAMA CHEMICAL CO LTD (JP)
AIST (JP)
International Classes:
A61K31/4704; A61K31/4709; A61K31/4725; A61K31/497; A61K31/5377; A61P35/00; A61P35/02; A61P43/00
Domestic Patent References:
| WO2016016316A1 | 2016-02-04 | |||
| WO2013027168A1 | 2013-02-28 | |||
| WO2016077656A2 | 2016-05-19 | |||
| WO2016016316A1 | 2016-02-04 | |||
| WO2009084693A1 | 2009-07-09 |
Other References:
PANAGIS F ET AL., NATURE REVIEWS DRUG DISCOVERY, vol. 13, 2014, pages 337 - 356
SUZUKI ET AL., MAGAZINE OF KYOTO PREFECTURAL UNIVERSITY OF MEDICINE, vol. 124, 2015, pages 839 - 847
"Greene's Protective Groups in Organic Synthesis", 2014, JOHN WILEY & SONS, INC, pages: 895 - 1193
RICHARD C. LAROCK ET AL.: "Comprehensive Organic Transformations", 1999, JOHN WILEY & SONS, INC., pages: 823 - 827
DELMORE JE ET AL., CELL, vol. 146, 2011, pages 904 - 917
DYANA T. SAENZ ET AL., LEUKEMIA, vol. 31, 2017, pages 678 - 687
P. NEWHAM ET AL.: "In vivo and in vitro models of bromodomain and extraterminal domain inhibitor-induced intestinal stem cell loss and villous atrophy reveal differential human vs pre-clinal species sensitivity", BASEL LIFE SCIENCES WEEK 2015, 21 September 2015 (2015-09-21)
See also references of EP 3563851A4
SUZUKI ET AL., MAGAZINE OF KYOTO PREFECTURAL UNIVERSITY OF MEDICINE, vol. 124, 2015, pages 839 - 847
"Greene's Protective Groups in Organic Synthesis", 2014, JOHN WILEY & SONS, INC, pages: 895 - 1193
RICHARD C. LAROCK ET AL.: "Comprehensive Organic Transformations", 1999, JOHN WILEY & SONS, INC., pages: 823 - 827
DELMORE JE ET AL., CELL, vol. 146, 2011, pages 904 - 917
DYANA T. SAENZ ET AL., LEUKEMIA, vol. 31, 2017, pages 678 - 687
P. NEWHAM ET AL.: "In vivo and in vitro models of bromodomain and extraterminal domain inhibitor-induced intestinal stem cell loss and villous atrophy reveal differential human vs pre-clinal species sensitivity", BASEL LIFE SCIENCES WEEK 2015, 21 September 2015 (2015-09-21)
See also references of EP 3563851A4
Attorney, Agent or Firm:
SIKS & CO. (JP)
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