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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
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

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

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US (7) US10385047B2 (https=)
EP (3) EP3741749A1 (https=)
JP (1) JP6521535B2 (https=)
KR (1) KR102591897B1 (https=)
CN (2) CN106660982B (https=)
AR (1) AR100997A1 (https=)
AU (1) AU2015279719B2 (https=)
BR (1) BR112016030367A2 (https=)
CA (1) CA2953437C (https=)
CL (1) CL2016003301A1 (https=)
CO (1) CO2017000359A2 (https=)
CY (1) CY1123906T1 (https=)
DK (1) DK3160952T3 (https=)
EA (1) EA031200B1 (https=)
EC (1) ECSP17004931A (https=)
ES (1) ES2862648T3 (https=)
HR (1) HRP20210299T1 (https=)
HU (1) HUE053876T2 (https=)
IL (1) IL249629A0 (https=)
LT (1) LT3160952T (https=)
MX (1) MX375219B (https=)
NZ (1) NZ728120A (https=)
PL (1) PL3160952T3 (https=)
PT (1) PT3160952T (https=)
SA (1) SA516380585B1 (https=)
SG (1) SG11201610813TA (https=)
SI (1) SI3160952T1 (https=)
TW (2) TWI715533B (https=)
WO (1) WO2015200709A1 (https=)

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BR112015014968A2 (pt) 2012-12-21 2017-07-11 Quanticel Pharmaceuticals Inc inibidores de histona-desmetilase
SI3160952T1 (sl) 2014-06-25 2021-07-30 Celgene Quanticel Research, Inc. Zaviralci histon demetilaz
ES2910226T3 (es) 2014-09-17 2022-05-12 Celgene Quanticel Res Inc Inhibidores de desmetilasa de histonas
US10030017B2 (en) 2014-09-17 2018-07-24 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
WO2017117154A1 (en) * 2015-12-28 2017-07-06 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3430008B1 (en) * 2016-03-15 2022-05-18 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3600301B1 (en) * 2017-03-30 2024-07-03 Albert-Ludwigs-Universität 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
JP2024518712A (ja) * 2021-04-09 2024-05-02 タキオン セラピューティクス，インコーポレーテッド Ｋｄｍ４阻害剤による癌の処置
WO2023023112A1 (en) * 2021-08-18 2023-02-23 Celgene Corporation Process for preparing histone demethylase inhibitors
EP4452249A4 (en) * 2021-12-23 2026-03-11 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
TW202412816A (zh) 2022-06-10 2024-04-01 美商弗沃德醫療公司 ＴＮＦ—α活性調節劑
WO2023250480A1 (en) * 2022-06-23 2023-12-28 The Cleveland Clinic Foundation 3-βHSD1 INHIBITORS AND COMPOSITIONS AND USES THEREOF
KR20250067936A (ko) * 2022-09-21 2025-05-15 셀진 코포레이션 3-(｛[(4r)-7-｛메틸[4-(프로판-2-일)페닐]아미노｝-3,4-디하이드로-2h-1-벤조피란-4-일]메틸｝아미노)피리딘-4-카르복실산l-라이신 염의 결정형, 히스톤 탈메틸화효소 억제제
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
DE102004039876A1 (de) 2004-06-23 2006-01-26 Lanxess Deutschland Gmbh Herstellung von fluorierten 1,3-Benzodioxanen
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
CN101466670B (zh) * 2006-04-07 2013-04-17 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
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CA2834548C (en) * 2011-04-28 2021-06-01 The Broad Institute, Inc. Inhibitors of histone deacetylase
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CA2894399A1 (en) * 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
SMT201800070T1 (it) 2012-12-19 2018-03-08 Celgene Quanticel Res Inc Inibiorti di istone demetilasi
SI3160952T1 (sl) 2014-06-25 2021-07-30 Celgene Quanticel Research, Inc. Zaviralci histon demetilaz
EP3600301B1 (en) * 2017-03-30 2024-07-03 Albert-Ludwigs-Universität 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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EA031200B1 (ru) 2018-11-30
MX375219B (es) 2025-03-06
TWI758004B (zh) 2022-03-11
CO2017000359A2 (es) 2017-04-10
EP3160952A1 (en) 2017-05-03
ES2862648T3 (es) 2021-10-07
HRP20210299T1 (hr) 2021-04-16
ECSP17004931A (es) 2017-03-31
US9242968B2 (en) 2016-01-26
HUE053876T2 (hu) 2021-07-28
EP3741749A1 (en) 2020-11-25
KR102591897B1 (ko) 2023-10-19
US9994561B2 (en) 2018-06-12
CA2953437A1 (en) 2015-12-30
KR20170018079A (ko) 2017-02-15
CA2953437C (en) 2022-08-30
SI3160952T1 (sl) 2021-07-30
LT3160952T (lt) 2021-05-10
US20170114055A1 (en) 2017-04-27
PT3160952T (pt) 2021-03-08
CN111909083A (zh) 2020-11-10
CL2016003301A1 (es) 2021-03-05
EP3738960A1 (en) 2020-11-18
JP2017523152A (ja) 2017-08-17
US20160107995A1 (en) 2016-04-21
DK3160952T3 (da) 2021-03-08
CN106660982A (zh) 2017-05-10
US10385047B2 (en) 2019-08-20
TWI715533B (zh) 2021-01-11
US10106534B2 (en) 2018-10-23
AU2015279719A1 (en) 2017-02-02
US20170158685A1 (en) 2017-06-08
PL3160952T3 (pl) 2021-07-19
AR100997A1 (es) 2016-11-16
MX2016017407A (es) 2017-04-27
SA516380585B1 (ar) 2020-12-06
EP3160952B1 (en) 2020-12-02
US20150376169A1 (en) 2015-12-31
TW201613882A (en) 2016-04-16
US20180044334A1 (en) 2018-02-15
US9586902B2 (en) 2017-03-07
WO2015200709A1 (en) 2015-12-30
AU2015279719B2 (en) 2019-03-21
BR112016030367A2 (pt) 2018-07-17
IL249629A0 (en) 2017-02-28
EA201692483A1 (ru) 2017-05-31
JP6521535B2 (ja) 2019-05-29
TW202124369A (zh) 2021-07-01
US9815828B2 (en) 2017-11-14
NZ728120A (en) 2023-06-30
SG11201610813TA (en) 2017-01-27
US9447046B2 (en) 2016-09-20
CY1123906T1 (el) 2022-05-27
CN111909083B (zh) 2023-08-15
EP3160952A4 (en) 2018-02-21
US20160332970A1 (en) 2016-11-17
US20180251458A1 (en) 2018-09-06

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