AU2015240775B2 - Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof - Google Patents

Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof Download PDF

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Publication number
AU2015240775B2
AU2015240775B2 AU2015240775A AU2015240775A AU2015240775B2 AU 2015240775 B2 AU2015240775 B2 AU 2015240775B2 AU 2015240775 A AU2015240775 A AU 2015240775A AU 2015240775 A AU2015240775 A AU 2015240775A AU 2015240775 B2 AU2015240775 B2 AU 2015240775B2
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Australia
Prior art keywords
cancer
compounds
compound
erastin
salt
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AU2015240775A
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English (en)
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AU2015240775A1 (en
Inventor
William Hawkins
Robert Mach
Dirk Spitzer
Brian Van Tine
Suwanna Vangveravong
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Washington University in St Louis WUSTL
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Washington University in St Louis WUSTL
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2015240775A 2014-04-01 2015-04-01 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof Active AU2015240775B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2019200353A AU2019200353B2 (en) 2014-04-01 2019-01-18 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461973366P 2014-04-01 2014-04-01
US61/973,366 2014-04-01
PCT/US2015/023954 WO2015153814A1 (en) 2014-04-01 2015-04-01 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2019200353A Division AU2019200353B2 (en) 2014-04-01 2019-01-18 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof

Publications (2)

Publication Number Publication Date
AU2015240775A1 AU2015240775A1 (en) 2016-10-20
AU2015240775B2 true AU2015240775B2 (en) 2019-01-03

Family

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Family Applications (2)

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AU2015240775A Active AU2015240775B2 (en) 2014-04-01 2015-04-01 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
AU2019200353A Active AU2019200353B2 (en) 2014-04-01 2019-01-18 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof

Family Applications After (1)

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AU2019200353A Active AU2019200353B2 (en) 2014-04-01 2019-01-18 Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof

Country Status (8)

Country Link
US (5) US10087175B2 (OSRAM)
EP (1) EP3126356B1 (OSRAM)
JP (1) JP6557253B2 (OSRAM)
CN (1) CN106459011B (OSRAM)
AU (2) AU2015240775B2 (OSRAM)
CA (1) CA2944069C (OSRAM)
ES (1) ES2743701T3 (OSRAM)
WO (1) WO2015153814A1 (OSRAM)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2944069C (en) 2014-04-01 2022-03-08 William Hawkins Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
US11175296B2 (en) * 2016-10-26 2021-11-16 Washington University Methods of diagnosing and treating cancer comprising ME1
WO2018218087A1 (en) * 2017-05-24 2018-11-29 K-Gen, Inc. Methods of cancer treatment
US11541116B1 (en) 2022-01-07 2023-01-03 Kojin Therapeutics, Inc. Methods and compositions for inducing ferroptosis in vivo

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040248221A1 (en) * 2003-01-29 2004-12-09 Whitehead Institute For Biomedical Research Identification of genotype-selective anti-tumor agents
WO2006081331A2 (en) * 2005-01-25 2006-08-03 Prolexys Pharmaceuticals, Inc. Quinoxaline derivatives as antitumor agents
WO2006081337A2 (en) * 2005-01-25 2006-08-03 Whitehead Institute For Biomedical Research Erastin analogues and their uses for killing cancer cells
WO2007076087A2 (en) * 2005-12-22 2007-07-05 Prolexys Pharmaceuticals, Inc. 3-aryl-substituted quinazolones, and uses thereof
US20070161644A1 (en) * 2005-01-25 2007-07-12 Stockwell Brent R Erastin analogs and uses thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006130426A2 (en) * 2005-05-27 2006-12-07 Kemia, Inc. Modulators of ccr-5 activity
WO2008013987A2 (en) * 2006-07-27 2008-01-31 Prolexys Pharmaceuticals, Inc. N-alkyl substituted piperazinylmethylquinazolinones and azepanylmethylquinazolinones
US8324251B2 (en) 2006-10-04 2012-12-04 Bristol-Myers Squibb Company Cyclic modulators of chemokine receptor activity
US8143222B2 (en) 2007-10-22 2012-03-27 Washington University Modular platform for targeted therapeutic delivery
CA2944069C (en) 2014-04-01 2022-03-08 William Hawkins Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040248221A1 (en) * 2003-01-29 2004-12-09 Whitehead Institute For Biomedical Research Identification of genotype-selective anti-tumor agents
WO2006081331A2 (en) * 2005-01-25 2006-08-03 Prolexys Pharmaceuticals, Inc. Quinoxaline derivatives as antitumor agents
WO2006081337A2 (en) * 2005-01-25 2006-08-03 Whitehead Institute For Biomedical Research Erastin analogues and their uses for killing cancer cells
US20070161644A1 (en) * 2005-01-25 2007-07-12 Stockwell Brent R Erastin analogs and uses thereof
WO2007076087A2 (en) * 2005-12-22 2007-07-05 Prolexys Pharmaceuticals, Inc. 3-aryl-substituted quinazolones, and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GARG et al., "Conjugation to a SMAC mimetic potentiates sigma-2 ligand induced tumor cell death in ovarian cancer.", Molecular Cancer, (2014-03-07), vol. 13, page 50. *

Also Published As

Publication number Publication date
CN106459011A (zh) 2017-02-22
CN106459011B (zh) 2019-11-15
CA2944069A1 (en) 2015-10-08
US10344029B2 (en) 2019-07-09
JP2017509672A (ja) 2017-04-06
AU2019200353A1 (en) 2019-02-07
NZ724819A (en) 2020-09-25
WO2015153814A1 (en) 2015-10-08
US20200123149A1 (en) 2020-04-23
US10087175B2 (en) 2018-10-02
AU2015240775A1 (en) 2016-10-20
US20190002457A1 (en) 2019-01-03
US20170015660A1 (en) 2017-01-19
AU2019200353B2 (en) 2020-01-30
US10975069B2 (en) 2021-04-13
JP6557253B2 (ja) 2019-08-07
EP3126356B1 (en) 2019-07-31
US20210221805A1 (en) 2021-07-22
EP3126356A1 (en) 2017-02-08
CA2944069C (en) 2022-03-08
EP3126356A4 (en) 2017-08-16
US20250145617A1 (en) 2025-05-08
ES2743701T3 (es) 2020-02-20
CN106459011A8 (zh) 2017-06-30

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