CA2953437C - Histone demethylase inhibitors - Google Patents

Histone demethylase inhibitors Download PDF

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Publication number
CA2953437C
CA2953437C CA2953437A CA2953437A CA2953437C CA 2953437 C CA2953437 C CA 2953437C CA 2953437 A CA2953437 A CA 2953437A CA 2953437 A CA2953437 A CA 2953437A CA 2953437 C CA2953437 C CA 2953437C
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CA
Canada
Prior art keywords
optionally substituted
compound
methyl
pharmaceutically acceptable
acceptable salt
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Active
Application number
CA2953437A
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English (en)
French (fr)
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CA2953437A1 (en
Inventor
Amogh Boloor
Young K. Chen
Michael Brennan Wallace
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Celgene Quanticel Research Inc
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Celgene Quanticel Research Inc
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Publication of CA2953437A1 publication Critical patent/CA2953437A1/en
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Active legal-status Critical Current
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • 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
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
CA2953437A 2014-06-25 2015-06-25 Histone demethylase inhibitors Active CA2953437C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462017201P 2014-06-25 2014-06-25
US62/017,201 2014-06-25
PCT/US2015/037812 WO2015200709A1 (en) 2014-06-25 2015-06-25 Histone demethylase inhibitors

Publications (2)

Publication Number Publication Date
CA2953437A1 CA2953437A1 (en) 2015-12-30
CA2953437C true CA2953437C (en) 2022-08-30

Family

ID=54929774

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2953437A Active CA2953437C (en) 2014-06-25 2015-06-25 Histone demethylase inhibitors

Country Status (29)

Country Link
US (7) US10385047B2 (enExample)
EP (3) EP3738960A1 (enExample)
JP (1) JP6521535B2 (enExample)
KR (1) KR102591897B1 (enExample)
CN (2) CN106660982B (enExample)
AR (1) AR100997A1 (enExample)
AU (1) AU2015279719B2 (enExample)
BR (1) BR112016030367A2 (enExample)
CA (1) CA2953437C (enExample)
CL (1) CL2016003301A1 (enExample)
CO (1) CO2017000359A2 (enExample)
CY (1) CY1123906T1 (enExample)
DK (1) DK3160952T3 (enExample)
EA (1) EA031200B1 (enExample)
EC (1) ECSP17004931A (enExample)
ES (1) ES2862648T3 (enExample)
HR (1) HRP20210299T1 (enExample)
HU (1) HUE053876T2 (enExample)
IL (1) IL249629A0 (enExample)
LT (1) LT3160952T (enExample)
MX (1) MX375219B (enExample)
NZ (1) NZ728120A (enExample)
PL (1) PL3160952T3 (enExample)
PT (1) PT3160952T (enExample)
SA (1) SA516380585B1 (enExample)
SG (1) SG11201610813TA (enExample)
SI (1) SI3160952T1 (enExample)
TW (2) TWI758004B (enExample)
WO (1) WO2015200709A1 (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2895808A1 (en) 2012-12-21 2014-06-26 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
CN106660982B (zh) 2014-06-25 2020-09-08 赛尔基因昆蒂赛尔研究公司 组蛋白脱甲基酶抑制剂
SG11201702147TA (en) 2014-09-17 2017-04-27 Celgene Quanticel Res Inc Histone demethylase inhibitors
US10030017B2 (en) 2014-09-17 2018-07-24 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3397617A4 (en) * 2015-12-28 2019-05-22 Celgene Quanticel Research, Inc. HISTONDEMETHYLASEINHIBITOREN
WO2017161012A1 (en) * 2016-03-15 2017-09-21 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
ES2991090T3 (es) 2017-03-30 2024-12-02 Univ Freiburg Albert Ludwigs Inhibidores de KDM4
CN109825551B (zh) * 2019-02-21 2022-08-02 深圳大学 一种评价组蛋白赖氨酸去甲基转移酶活性的方法
CN111679072B (zh) * 2020-06-15 2022-04-29 温州医科大学 Kdm6b蛋白在乳腺癌预后评估试剂盒、诊断试剂盒中的应用
US20250025451A1 (en) * 2021-04-09 2025-01-23 Celgene Corporation Treatment of cancer with kdm4 inhibitors
AU2022331536A1 (en) * 2021-08-18 2024-02-22 Celgene Corporation Process for preparing histone demethylase inhibitors
WO2023122221A1 (en) * 2021-12-23 2023-06-29 Tachyon Therapeutics, Inc. Pharmaceutical formulations comprising 3-({[(4r)-7-{methyl[4-(propan-2-yl)phenyl]amino}-3,4-dihydro-2h-l-benzopyran-4-yl]methyl}amino)pyridine-4-carboxylic acid
AR129578A1 (es) 2022-06-10 2024-09-11 Forward Therapeutics Inc MODULADORES DE LA ACTIVIDAD DE TNF-a
US20250241905A1 (en) * 2022-06-23 2025-07-31 The Cleveland Clinic Foundation 3-beta-hsd1 inhibitors and compositions and uses thereof
JP2025532101A (ja) * 2022-09-21 2025-09-29 セルジーン コーポレーション 3-({[(4r)-7-{メチル[4-(プロパン-2-イル)フェニル]アミノ}-3,4-ジヒドロ-2h-1-ベンゾピラン-4-イル]メチル}アミノ)ピリジン-4-カルボン酸のl-リジン塩、ヒストンデメチラーゼ阻害剤
CN115974647B (zh) * 2022-12-05 2024-09-03 江苏宏邦化工科技有限公司 以四氢-4-甲基-2-苯基-2h-吡喃-4-醇为原料制备苯乐戊醇的方法
IL327679A (en) * 2023-10-16 2026-06-01 Cleveland Clinic Found 3?hsd1 inhibitors and compositions and uses thereof

Family Cites Families (15)

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Publication number Priority date Publication date Assignee Title
CA2465978C (en) * 2001-09-14 2015-04-07 Soon Hyung Woo Inhibitors of histone deacetylase
UA89035C2 (ru) 2003-12-03 2009-12-25 Лео Фарма А/С Эфиры гидроксамовых кислот и их фармацевтическое применение
DE102004039876A1 (de) 2004-06-23 2006-01-26 Lanxess Deutschland Gmbh Herstellung von fluorierten 1,3-Benzodioxanen
PE20071020A1 (es) 2006-03-07 2007-12-11 Smithkline Beecham Corp Compuestos derivados de glicina n-sustituidos como inhibidores de prolil hidroxilasa
CA2648804C (en) * 2006-04-07 2014-05-27 Methylgene Inc. Benzamide derivatives as inhibitors of histone deacetylase
US7898712B2 (en) 2008-06-27 2011-03-01 Lockheed Martin Corporation Risley integrated steering module
GB201112607D0 (en) * 2011-07-22 2011-09-07 Glaxo Group Ltd Novel compounds
WO2012149540A1 (en) 2011-04-28 2012-11-01 The Broad Institute Inc Inhibitors of histone deacetylase
WO2013143597A1 (en) 2012-03-29 2013-10-03 Glaxo Group Limited Demethylase enzymes inhibitors
US20140162266A1 (en) 2012-12-05 2014-06-12 Bio-Rad Laboratories, Inc. Methods for polymerase chain reaction copy number variation assays
US8987461B2 (en) * 2012-12-06 2015-03-24 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
SI2934145T1 (en) * 2012-12-19 2018-03-30 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
CA2895808A1 (en) * 2012-12-21 2014-06-26 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
CN106660982B (zh) 2014-06-25 2020-09-08 赛尔基因昆蒂赛尔研究公司 组蛋白脱甲基酶抑制剂
ES2991090T3 (es) * 2017-03-30 2024-12-02 Univ Freiburg Albert Ludwigs Inhibidores de KDM4

Also Published As

Publication number Publication date
CN106660982B (zh) 2020-09-08
US20170114055A1 (en) 2017-04-27
US9242968B2 (en) 2016-01-26
MX2016017407A (es) 2017-04-27
SI3160952T1 (sl) 2021-07-30
CN106660982A (zh) 2017-05-10
CY1123906T1 (el) 2022-05-27
JP2017523152A (ja) 2017-08-17
AU2015279719A1 (en) 2017-02-02
US20170158685A1 (en) 2017-06-08
NZ728120A (en) 2023-06-30
EP3160952B1 (en) 2020-12-02
EP3741749A1 (en) 2020-11-25
EP3160952A1 (en) 2017-05-03
US9994561B2 (en) 2018-06-12
HUE053876T2 (hu) 2021-07-28
US20180251458A1 (en) 2018-09-06
AU2015279719B2 (en) 2019-03-21
TW201613882A (en) 2016-04-16
WO2015200709A1 (en) 2015-12-30
KR102591897B1 (ko) 2023-10-19
CN111909083A (zh) 2020-11-10
TWI715533B (zh) 2021-01-11
CA2953437A1 (en) 2015-12-30
EP3738960A1 (en) 2020-11-18
SA516380585B1 (ar) 2020-12-06
US20150376169A1 (en) 2015-12-31
CO2017000359A2 (es) 2017-04-10
JP6521535B2 (ja) 2019-05-29
ECSP17004931A (es) 2017-03-31
PT3160952T (pt) 2021-03-08
US20180044334A1 (en) 2018-02-15
US9586902B2 (en) 2017-03-07
MX375219B (es) 2025-03-06
TWI758004B (zh) 2022-03-11
CN111909083B (zh) 2023-08-15
DK3160952T3 (da) 2021-03-08
LT3160952T (lt) 2021-05-10
EA201692483A1 (ru) 2017-05-31
US10385047B2 (en) 2019-08-20
US9815828B2 (en) 2017-11-14
EP3160952A4 (en) 2018-02-21
ES2862648T3 (es) 2021-10-07
PL3160952T3 (pl) 2021-07-19
CL2016003301A1 (es) 2021-03-05
IL249629A0 (en) 2017-02-28
KR20170018079A (ko) 2017-02-15
US20160107995A1 (en) 2016-04-21
BR112016030367A2 (pt) 2018-07-17
US10106534B2 (en) 2018-10-23
US9447046B2 (en) 2016-09-20
SG11201610813TA (en) 2017-01-27
HRP20210299T1 (hr) 2021-04-16
AR100997A1 (es) 2016-11-16
EA031200B1 (ru) 2018-11-30
TW202124369A (zh) 2021-07-01
US20160332970A1 (en) 2016-11-17

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