JP6525422B2 - リジン特異的なデメチラーゼ−１の阻害剤 - Google Patents

リジン特異的なデメチラーゼ−１の阻害剤 Download PDF

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Publication number
JP6525422B2
JP6525422B2 JP2016575769A JP2016575769A JP6525422B2 JP 6525422 B2 JP6525422 B2 JP 6525422B2 JP 2016575769 A JP2016575769 A JP 2016575769A JP 2016575769 A JP2016575769 A JP 2016575769A JP 6525422 B2 JP6525422 B2 JP 6525422B2
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optionally substituted
pharmaceutically acceptable
acceptable salt
calc
heterocyclyl
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JP2017521407A5 (enExample
JP2017521407A (ja
Inventor
チェン，ヤング，ケイ．
カノウニ，トウフィケ
ニエ，チェ
スタッフォード，ジェフリー，アラン
ヴィール，ジェイムス，マービン
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セルジーン クオンティセル リサーチ，インク．
セルジーン クオンティセル リサーチ，インク．
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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)
JP2016575769A 2014-07-03 2015-06-30 リジン特異的なデメチラーゼ−１の阻害剤 Expired - Fee Related JP6525422B2 (ja)

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

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JP2019086398A Division JP6833896B2 (ja) 2014-07-03 2019-04-26 リジン特異的なデメチラーゼ−１の阻害剤

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JP2017521407A JP2017521407A (ja) 2017-08-03
JP2017521407A5 JP2017521407A5 (enExample) 2018-05-31
JP6525422B2 true JP6525422B2 (ja) 2019-06-05

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JP2019086398A Active JP6833896B2 (ja) 2014-07-03 2019-04-26 リジン特異的なデメチラーゼ−１の阻害剤

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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)

Cited By (1)

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JP2019172676A (ja) * 2014-07-03 2019-10-10 セルジーン クオンティセル リサーチ，インク． リジン特異的なデメチラーゼ−１の阻害剤

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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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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
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Publication number Priority date Publication date Assignee Title
JP2019172676A (ja) * 2014-07-03 2019-10-10 セルジーン クオンティセル リサーチ，インク． リジン特異的なデメチラーゼ−１の阻害剤

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
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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