WO2015013635A3 - Inhibitors of transcription factors and uses thereof - Google Patents

Inhibitors of transcription factors and uses thereof Download PDF

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Publication number
WO2015013635A3
WO2015013635A3 PCT/US2014/048230 US2014048230W WO2015013635A3 WO 2015013635 A3 WO2015013635 A3 WO 2015013635A3 US 2014048230 W US2014048230 W US 2014048230W WO 2015013635 A3 WO2015013635 A3 WO 2015013635A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
bromodomain
containing proteins
transcription factors
compounds
Prior art date
Application number
PCT/US2014/048230
Other languages
French (fr)
Other versions
WO2015013635A2 (en
Inventor
Jason J. MARINEAU
James E. Bradner
Wei Zhang
Jun Qi
Michael R. MCKEOWN
Harry Hongning FU
Shuai LIU
Original Assignee
Dana-Farber Cancer Institute, Inc.
University Of Massachusetts
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to US14/907,339 priority Critical patent/US9975896B2/en
Application filed by Dana-Farber Cancer Institute, Inc., University Of Massachusetts filed Critical Dana-Farber Cancer Institute, Inc.
Priority to AU2014292888A priority patent/AU2014292888B2/en
Priority to MX2016001037A priority patent/MX2016001037A/en
Priority to CA2918910A priority patent/CA2918910A1/en
Priority to RU2016105108A priority patent/RU2016105108A/en
Priority to JP2016530079A priority patent/JP2016531113A/en
Priority to EP14828728.7A priority patent/EP3024327B1/en
Priority to CN201480052916.XA priority patent/CN105611835A/en
Priority to KR1020167004492A priority patent/KR20160034379A/en
Priority to BR112016001457A priority patent/BR112016001457A2/en
Publication of WO2015013635A2 publication Critical patent/WO2015013635A2/en
Publication of WO2015013635A3 publication Critical patent/WO2015013635A3/en
Priority to HK16112643.8A priority patent/HK1224140A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Toxicology (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention provides novel compounds of any one of Formulae (I) to (IV), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I) to (IV) are believed to be inhibitors of bromodomain-containing proteins (e.g., bromo and extra terminal proteins (BETs)). Also provided are methods, uses, and kits using the inventive compounds and pharmaceutical compositions for inhibiting the activity of the bromodomain-containing proteins and for treating and/or preventing in a subject in need thereof diseases associated with bromodomain-containing proteins, such as proliferative diseases.
PCT/US2014/048230 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof WO2015013635A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
JP2016530079A JP2016531113A (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
AU2014292888A AU2014292888B2 (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
MX2016001037A MX2016001037A (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof.
CA2918910A CA2918910A1 (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
RU2016105108A RU2016105108A (en) 2013-07-25 2014-07-25 TRANSCRIPTION FACTOR INHIBITORS AND THEIR APPLICATION
US14/907,339 US9975896B2 (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
EP14828728.7A EP3024327B1 (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
BR112016001457A BR112016001457A2 (en) 2013-07-25 2014-07-25 TRANSCRIPTION FACTOR INHIBITORS AND THEIR USES
KR1020167004492A KR20160034379A (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
CN201480052916.XA CN105611835A (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof
HK16112643.8A HK1224140A1 (en) 2013-07-25 2016-11-03 Inhibitors of transcription factors and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361858521P 2013-07-25 2013-07-25
US61/858,521 2013-07-25

Publications (2)

Publication Number Publication Date
WO2015013635A2 WO2015013635A2 (en) 2015-01-29
WO2015013635A3 true WO2015013635A3 (en) 2015-04-02

Family

ID=52393987

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2014/048230 WO2015013635A2 (en) 2013-07-25 2014-07-25 Inhibitors of transcription factors and uses thereof

Country Status (12)

Country Link
US (1) US9975896B2 (en)
EP (1) EP3024327B1 (en)
JP (1) JP2016531113A (en)
KR (1) KR20160034379A (en)
CN (1) CN105611835A (en)
AU (1) AU2014292888B2 (en)
BR (1) BR112016001457A2 (en)
CA (1) CA2918910A1 (en)
HK (1) HK1224140A1 (en)
MX (1) MX2016001037A (en)
RU (1) RU2016105108A (en)
WO (1) WO2015013635A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors

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