KR102450671B1 - 리신 특이적 데메틸라제-1의 저해제 - Google Patents

리신 특이적 데메틸라제-1의 저해제 Download PDF

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KR102450671B1
KR102450671B1 KR1020177002953A KR20177002953A KR102450671B1 KR 102450671 B1 KR102450671 B1 KR 102450671B1 KR 1020177002953 A KR1020177002953 A KR 1020177002953A KR 20177002953 A KR20177002953 A KR 20177002953A KR 102450671 B1 KR102450671 B1 KR 102450671B1
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carbonyl
fluorobenzonitrile
methyl
fluoro
optionally substituted
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KR20170027822A (ko
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영 케이 첸
토우피케 카노우니
제 니
제프리 앨런 스태포드
제임스 마빈 빌
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셀젠 콴티셀 리서치, 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • 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
    • 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
    • C07D487/10—Spiro-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)
KR1020177002953A 2014-07-03 2015-06-30 리신 특이적 데메틸라제-1의 저해제 Active KR102450671B1 (ko)

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
KR20170027822A KR20170027822A (ko) 2017-03-10
KR102450671B1 true KR102450671B1 (ko) 2022-10-04

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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)

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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

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US20040132726A1 (en) 2002-08-09 2004-07-08 Astrazeneca Ab And Nps Pharmaceuticals, Inc. New compounds
JP4316232B2 (ja) * 2001-12-28 2009-08-19 武田薬品工業株式会社 アンドロゲン受容体拮抗剤
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

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US5776954A (en) * 1996-10-30 1998-07-07 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
US20050101657A1 (en) 2001-12-28 2005-05-12 Takeda Chemical Industries Ltd. Androgen receptor antagonists
US7026311B2 (en) * 2002-01-10 2006-04-11 Abbott Gmbh & Co., Kg Dibenzodiazepine derivatives, their preparation and use
EP2316831B1 (en) * 2002-11-21 2013-03-06 Novartis AG 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
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DK2959900T3 (en) * 2008-06-16 2017-06-26 Univ Tennessee Res Found CONNECTION TO TREATMENT OF CANCER
JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
EA022459B1 (ru) * 2010-04-20 2016-01-29 Университа' Дельи Студи Ди Рома "Ла Сапиенца" Производные транилципромина в качестве ингибиторов гистон деметилаз lsd1 и/или lsd2
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 (3)

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Publication number Priority date Publication date Assignee Title
JP4316232B2 (ja) * 2001-12-28 2009-08-19 武田薬品工業株式会社 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
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
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
AU2015284197B2 (en) 2021-07-22
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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