CN106660982B - 组蛋白脱甲基酶抑制剂 - Google Patents

组蛋白脱甲基酶抑制剂 Download PDF

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Publication number
CN106660982B
CN106660982B CN201580045921.2A CN201580045921A CN106660982B CN 106660982 B CN106660982 B CN 106660982B CN 201580045921 A CN201580045921 A CN 201580045921A CN 106660982 B CN106660982 B CN 106660982B
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optionally substituted
alkyl
compound
pharmaceutically acceptable
acceptable salt
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Chinese (zh)
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CN106660982A (zh
Inventor
阿莫格·博卢尔
扬·K·陈
迈克尔·布伦南·华莱士
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Celgene Quanticel Research Inc
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Quanticel Pharmaceuticals Inc
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
CN201580045921.2A 2014-06-25 2015-06-25 组蛋白脱甲基酶抑制剂 Active CN106660982B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202010813617.0A CN111909083B (zh) 2014-06-25 2015-06-25 组蛋白脱甲基酶抑制剂

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

Related Child Applications (1)

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Publications (2)

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CN106660982A CN106660982A (zh) 2017-05-10
CN106660982B true CN106660982B (zh) 2020-09-08

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US (7) US10385047B2 (enExample)
EP (3) EP3160952B1 (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)
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EC (1) ECSP17004931A (enExample)
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HR (1) HRP20210299T1 (enExample)
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IL (1) IL249629A0 (enExample)
LT (1) LT3160952T (enExample)
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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) TWI715533B (enExample)
WO (1) WO2015200709A1 (enExample)

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ES2718495T3 (es) 2012-12-21 2019-07-02 Celgene Quanticel Res Inc Inhibidores de la histona desmetilasa
SG11201610813TA (en) 2014-06-25 2017-01-27 Quanticel Pharmaceuticals Inc Histone demethylase inhibitors
AU2015317806A1 (en) 2014-09-17 2017-04-13 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10030017B2 (en) 2014-09-17 2018-07-24 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10059687B2 (en) 2015-12-28 2018-08-28 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
ES2921009T3 (es) * 2016-03-15 2022-08-16 Celgene Quanticel Res Inc Inhibidores de desmetilasas de histonas
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US20200039938A1 (en) 2017-03-30 2020-02-06 Albert-Ludwigs-University Freiburg Kdm4 inhibitors
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
EP4319748A4 (en) * 2021-04-09 2025-02-26 Tachyon Therapeutics, Inc. TREATMENT OF CANCER WITH KDM4 INHIBITORS
US20250129056A1 (en) * 2021-08-18 2025-04-24 Celgene Corporation Process for preparing histone demethylase inhibitors
US20250134874A1 (en) * 2021-12-23 2025-05-01 Tachyon Therapeutics, Inc. Pharmaceutical formulations comprising 3-({[(4r)-7-{methyl[4-(propan-2-yl)phenyl]amino}-3,4-dihydro-2h-1-benzopyran-4-yl]methyl}amino)pyridine-4-carboxylic acid
WO2023240253A2 (en) 2022-06-10 2023-12-14 Forward Therapeutics, Inc. Modulators of tnf-alpha activity
CA3260514A1 (en) * 2022-06-23 2023-12-28 Cleveland Clinic Found 3.BETA.HSD1 INHIBITORS AND THEIR COMPOSITIONS AND USES
CA3268325A1 (en) * 2022-09-21 2024-03-28 Celgene Corp CRYSTALLINE FORMS OF L-LYSINE SALT OF 3-({[(4R)-7-{METHYL[4-(PROPAN-2-YL)PHENYL]AMINO}-3,4-DIHYDRO-2H-1-BENZOPYRAN-4-YL]METHYL}AMINO)PYRIDINE-4-CARBOXYLIC ACID AS A HISTONE DEMETHYLASE INHIBITOR
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
WO2025085527A1 (en) * 2023-10-16 2025-04-24 The Cleveland Clinic Foundation 3βHSD1 INHIBITORS AND COMPOSITIONS AND USES THEREOF

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WO2012052390A1 (en) * 2010-10-19 2012-04-26 Glaxo Group Limited N-2-(2-pyridinyl)-4-pyrimidinyl-beta-alanine derivatives as inhibitors of histone demethylase jmjd3
WO2013143597A1 (en) * 2012-03-29 2013-10-03 Glaxo Group Limited Demethylase enzymes inhibitors
WO2014100818A1 (en) * 2012-12-21 2014-06-26 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors

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UA89035C2 (ru) 2003-12-03 2009-12-25 Лео Фарма А/С Эфиры гидроксамовых кислот и их фармацевтическое применение
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AR059733A1 (es) 2006-03-07 2008-04-23 Smithkline Beecham Corp Compuesto derivado de glicina n- sustituida con heteroaromaticos bicicicos, composicion farmaceutica que lo comprende, uso para preparar un medicamento para tratar la anemia y proceso para su preparacion
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WO2014100463A1 (en) 2012-12-19 2014-06-26 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
SG11201610813TA (en) 2014-06-25 2017-01-27 Quanticel Pharmaceuticals Inc Histone demethylase inhibitors
US20200039938A1 (en) * 2017-03-30 2020-02-06 Albert-Ludwigs-University Freiburg Kdm4 inhibitors

Patent Citations (3)

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WO2012052390A1 (en) * 2010-10-19 2012-04-26 Glaxo Group Limited N-2-(2-pyridinyl)-4-pyrimidinyl-beta-alanine derivatives as inhibitors of histone demethylase jmjd3
WO2013143597A1 (en) * 2012-03-29 2013-10-03 Glaxo Group Limited Demethylase enzymes inhibitors
WO2014100818A1 (en) * 2012-12-21 2014-06-26 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors

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CO2017000359A2 (es) 2017-04-10
EP3160952A4 (en) 2018-02-21
KR20170018079A (ko) 2017-02-15
US9815828B2 (en) 2017-11-14
JP2017523152A (ja) 2017-08-17
US20180044334A1 (en) 2018-02-15
US9586902B2 (en) 2017-03-07
US10385047B2 (en) 2019-08-20
AU2015279719A1 (en) 2017-02-02
CA2953437C (en) 2022-08-30
US20170158685A1 (en) 2017-06-08
SA516380585B1 (ar) 2020-12-06
CY1123906T1 (el) 2022-05-27
LT3160952T (lt) 2021-05-10
CL2016003301A1 (es) 2021-03-05
EA031200B1 (ru) 2018-11-30
US9447046B2 (en) 2016-09-20
MX2016017407A (es) 2017-04-27
TW201613882A (en) 2016-04-16
EP3160952B1 (en) 2020-12-02
DK3160952T3 (da) 2021-03-08
EP3160952A1 (en) 2017-05-03
WO2015200709A1 (en) 2015-12-30
US10106534B2 (en) 2018-10-23
HRP20210299T1 (hr) 2021-04-16
TWI715533B (zh) 2021-01-11
MX375219B (es) 2025-03-06
EA201692483A1 (ru) 2017-05-31
US20180251458A1 (en) 2018-09-06
EP3738960A1 (en) 2020-11-18
CN106660982A (zh) 2017-05-10
US20170114055A1 (en) 2017-04-27
CN111909083A (zh) 2020-11-10
HUE053876T2 (hu) 2021-07-28
CA2953437A1 (en) 2015-12-30
CN111909083B (zh) 2023-08-15
EP3741749A1 (en) 2020-11-25
SG11201610813TA (en) 2017-01-27
TWI758004B (zh) 2022-03-11
AU2015279719B2 (en) 2019-03-21
SI3160952T1 (sl) 2021-07-30
US20160107995A1 (en) 2016-04-21
BR112016030367A2 (pt) 2018-07-17
PT3160952T (pt) 2021-03-08
US20150376169A1 (en) 2015-12-31
US9242968B2 (en) 2016-01-26
AR100997A1 (es) 2016-11-16
TW202124369A (zh) 2021-07-01
US20160332970A1 (en) 2016-11-17
NZ728120A (en) 2023-06-30
PL3160952T3 (pl) 2021-07-19
KR102591897B1 (ko) 2023-10-19
ECSP17004931A (es) 2017-03-31
ES2862648T3 (es) 2021-10-07
IL249629A0 (en) 2017-02-28
US9994561B2 (en) 2018-06-12
JP6521535B2 (ja) 2019-05-29

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