AU2015284197B2 - Inhibitors of lysine specific demethylase-1 - Google Patents

Inhibitors of lysine specific demethylase-1 Download PDF

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Publication number
AU2015284197B2
AU2015284197B2 AU2015284197A AU2015284197A AU2015284197B2 AU 2015284197 B2 AU2015284197 B2 AU 2015284197B2 AU 2015284197 A AU2015284197 A AU 2015284197A AU 2015284197 A AU2015284197 A AU 2015284197A AU 2015284197 B2 AU2015284197 B2 AU 2015284197B2
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AU
Australia
Prior art keywords
carbonyl
methyl
fluorobenzonitrile
fluoro
methylindazol
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Ceased
Application number
AU2015284197A
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English (en)
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AU2015284197A1 (en
Inventor
Young K. Chen
Toufike Kanouni
Zhe Nie
Jeffrey Alan Stafford
James Marvin Veal
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Celgene Quanticel Research Inc
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Celgene Quanticel Research Inc
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Publication of AU2015284197A1 publication Critical patent/AU2015284197A1/en
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Ceased legal-status Critical Current
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
AU2015284197A 2014-07-03 2015-06-30 Inhibitors of lysine specific demethylase-1 Ceased AU2015284197B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462020758P 2014-07-03 2014-07-03
US62/020,758 2014-07-03
PCT/US2015/038661 WO2016004105A1 (en) 2014-07-03 2015-06-30 Inhibitors of lysine specific demethylase-1

Publications (2)

Publication Number Publication Date
AU2015284197A1 AU2015284197A1 (en) 2017-02-02
AU2015284197B2 true AU2015284197B2 (en) 2021-07-22

Family

ID=55019933

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015284197A Ceased AU2015284197B2 (en) 2014-07-03 2015-06-30 Inhibitors of lysine specific demethylase-1

Country Status (18)

Country Link
US (3) US10414750B2 (enExample)
EP (1) EP3164509B1 (enExample)
JP (2) JP6525422B2 (enExample)
KR (1) KR102450671B1 (enExample)
CN (1) CN106604997B (enExample)
AU (1) AU2015284197B2 (enExample)
BR (1) BR112017000042B1 (enExample)
CA (1) CA2954060A1 (enExample)
CL (1) CL2016003423A1 (enExample)
CO (1) CO2017000363A2 (enExample)
EA (1) EA201790082A1 (enExample)
EC (1) ECSP17006776A (enExample)
ES (1) ES2905280T3 (enExample)
IL (1) IL249876B (enExample)
MX (1) MX391865B (enExample)
SG (1) SG11201700007YA (enExample)
WO (1) WO2016004105A1 (enExample)
ZA (1) ZA201700072B (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2905280T3 (es) * 2014-07-03 2022-04-07 Celgene Quanticel Res Inc Inhibidores de la desmetilasa 1 específica de lisina
SG11201610975RA (en) * 2014-07-03 2017-01-27 Celgene Quanticel Res Inc Inhibitors of lysine specific demethylase-1
WO2016198649A1 (en) 2015-06-12 2016-12-15 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
AU2017233898B2 (en) 2016-03-15 2022-12-15 Oryzon Genomics, S.A. Combinations of LSD1 inhibitors for use in the treatment of solid tumors
ES3042059T3 (en) 2016-03-16 2025-11-18 Oryzon Genomics Sa Methods to determine kdm1a target engagement and chemoprobes useful therefor
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
MY204406A (en) 2017-08-03 2024-08-27 Oryzon Genomics Sa Methods of treating behavior alterations
AR112900A1 (es) 2017-09-13 2019-12-26 Hanmi Pharm Ind Co Ltd Compuesto derivado de pirazol y uso de este
BR112021016064A2 (pt) 2019-03-20 2021-10-05 Oryzon Genomics, S.A. Métodos de tratamento do transtorno de personalidade borderline
CN120837494A (zh) 2019-03-20 2025-10-28 奥莱松基因组股份有限公司 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法
JP2022546908A (ja) 2019-07-05 2022-11-10 オリゾン・ゲノミクス・ソシエダッド・アノニマ Kdm1a阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法
CA3231846A1 (en) 2021-04-08 2022-10-13 Tamara Maes Combinations of lsd1 inhibitors for treating myeloid cancers
EP4419504A4 (en) * 2021-10-18 2025-09-03 Imago Biosciences Inc KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
EP4522136A1 (en) 2022-05-09 2025-03-19 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
CN119497613A (zh) 2022-05-09 2025-02-21 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗nf1-突变肿瘤的方法
AU2023385514A1 (en) 2022-11-24 2025-07-10 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5776954A (en) * 1996-10-30 1998-07-07 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
WO2003057699A1 (en) * 2002-01-10 2003-07-17 Abbott Gmbh & Co. Kg Dibenzodiazepine derivates, their preparation and use
JP2003252854A (ja) * 2001-12-28 2003-09-10 Takeda Chem Ind Ltd アンドロゲン受容体拮抗剤
US20040132726A1 (en) * 2002-08-09 2004-07-08 Astrazeneca Ab And Nps Pharmaceuticals, Inc. New compounds
US20040176385A1 (en) * 2002-11-21 2004-09-09 Nuss John N. Small molecule PI 3-kinase inhibitors and methods of their use
US20050101657A1 (en) * 2001-12-28 2005-05-12 Takeda Chemical Industries Ltd. Androgen receptor antagonists
US20080081703A1 (en) * 2005-02-22 2008-04-03 American Axle & Manufacturing, Inc. Universal Joint
JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
JP2012162541A (ja) * 2008-06-16 2012-08-30 Univ Of Tennessee Research Foundation 癌を処置するための化合物
US20130035377A1 (en) * 2010-04-20 2013-02-07 Università Degli Studi Di Roma "La Sapienza" Tranylcypromine derivatives as inhibitors of histone demethylases lsd1 and/or lsd2
US20140155339A1 (en) * 2012-11-30 2014-06-05 Darlene E. McCord Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2731773T3 (es) 2013-03-14 2019-11-19 Celgene Quanticel Res Inc Inhibidores de la histona desmetilasa
ES2905280T3 (es) * 2014-07-03 2022-04-07 Celgene Quanticel Res Inc Inhibidores de la desmetilasa 1 específica de lisina

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5776954A (en) * 1996-10-30 1998-07-07 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
JP2003252854A (ja) * 2001-12-28 2003-09-10 Takeda Chem Ind Ltd アンドロゲン受容体拮抗剤
US20050101657A1 (en) * 2001-12-28 2005-05-12 Takeda Chemical Industries Ltd. Androgen receptor antagonists
WO2003057699A1 (en) * 2002-01-10 2003-07-17 Abbott Gmbh & Co. Kg Dibenzodiazepine derivates, their preparation and use
US20040132726A1 (en) * 2002-08-09 2004-07-08 Astrazeneca Ab And Nps Pharmaceuticals, Inc. New compounds
US20040176385A1 (en) * 2002-11-21 2004-09-09 Nuss John N. Small molecule PI 3-kinase inhibitors and methods of their use
US20080081703A1 (en) * 2005-02-22 2008-04-03 American Axle & Manufacturing, Inc. Universal Joint
JP2012162541A (ja) * 2008-06-16 2012-08-30 Univ Of Tennessee Research Foundation 癌を処置するための化合物
JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
US20130035377A1 (en) * 2010-04-20 2013-02-07 Università Degli Studi Di Roma "La Sapienza" Tranylcypromine derivatives as inhibitors of histone demethylases lsd1 and/or lsd2
US20140155339A1 (en) * 2012-11-30 2014-06-05 Darlene E. McCord Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition

Also Published As

Publication number Publication date
JP6833896B2 (ja) 2021-02-24
US10626104B2 (en) 2020-04-21
US20190194162A1 (en) 2019-06-27
MX2017000170A (es) 2017-05-01
US20190194161A1 (en) 2019-06-27
KR102450671B1 (ko) 2022-10-04
EA201790082A1 (ru) 2017-08-31
BR112017000042B1 (pt) 2021-11-03
JP6525422B2 (ja) 2019-06-05
CA2954060A1 (en) 2016-01-07
BR112017000042A2 (pt) 2018-07-17
ZA201700072B (en) 2018-04-25
KR20170027822A (ko) 2017-03-10
US10626103B2 (en) 2020-04-21
ES2905280T3 (es) 2022-04-07
US20180265491A1 (en) 2018-09-20
MX391865B (es) 2025-03-21
IL249876B (en) 2020-06-30
CN106604997B (zh) 2021-02-19
AU2015284197A1 (en) 2017-02-02
EP3164509B1 (en) 2021-12-29
EP3164509A4 (en) 2018-02-28
EP3164509A1 (en) 2017-05-10
IL249876A0 (en) 2017-03-30
US10414750B2 (en) 2019-09-17
ECSP17006776A (es) 2017-03-31
WO2016004105A1 (en) 2016-01-07
JP2017521407A (ja) 2017-08-03
JP2019172676A (ja) 2019-10-10
CL2016003423A1 (es) 2017-11-10
CO2017000363A2 (es) 2017-04-10
SG11201700007YA (en) 2017-01-27
CN106604997A (zh) 2017-04-26

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired