AU2018350989A1 - Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof - Google Patents

Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof Download PDF

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Publication number
AU2018350989A1
AU2018350989A1 AU2018350989A AU2018350989A AU2018350989A1 AU 2018350989 A1 AU2018350989 A1 AU 2018350989A1 AU 2018350989 A AU2018350989 A AU 2018350989A AU 2018350989 A AU2018350989 A AU 2018350989A AU 2018350989 A1 AU2018350989 A1 AU 2018350989A1
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AU
Australia
Prior art keywords
compound
halo
alkyl
optionally substituted
cyano
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
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AU2018350989A
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English (en)
Inventor
John Emmerson Campbell
Kenneth William Duncan
James Edward John Mills
Michael John Munchhof
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Epizyme Inc
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Epizyme Inc
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Publication date
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of AU2018350989A1 publication Critical patent/AU2018350989A1/en
Priority to AU2023251449A priority Critical patent/AU2023251449A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2018350989A 2017-10-17 2018-10-17 Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof Abandoned AU2018350989A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2023251449A AU2023251449A1 (en) 2017-10-17 2023-10-18 Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201762573442P 2017-10-17 2017-10-17
US62/573,442 2017-10-17
US201862681804P 2018-06-07 2018-06-07
US62/681,804 2018-06-07
US201862746252P 2018-10-16 2018-10-16
US201862746495P 2018-10-16 2018-10-16
US62/746,252 2018-10-16
US62/746,495 2018-10-16
PCT/US2018/056333 WO2019079485A1 (en) 2017-10-17 2018-10-17 AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS AND DERIVATIVES THEREOF

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2023251449A Division AU2023251449A1 (en) 2017-10-17 2023-10-18 Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof

Publications (1)

Publication Number Publication Date
AU2018350989A1 true AU2018350989A1 (en) 2020-05-28

Family

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Family Applications (2)

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AU2018350989A Abandoned AU2018350989A1 (en) 2017-10-17 2018-10-17 Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof
AU2023251449A Abandoned AU2023251449A1 (en) 2017-10-17 2023-10-18 Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2023251449A Abandoned AU2023251449A1 (en) 2017-10-17 2023-10-18 Amine-substituted heterocyclic compounds as EHMT2 inhibitors and derivatives thereof

Country Status (7)

Country Link
US (1) US20200317642A1 (enExample)
EP (1) EP3697419A4 (enExample)
JP (2) JP7425724B2 (enExample)
CN (1) CN111343988A (enExample)
AU (2) AU2018350989A1 (enExample)
CA (1) CA3079260A1 (enExample)
WO (1) WO2019079485A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018195450A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
CA3079412A1 (en) * 2017-10-18 2019-04-25 Epizyme, Inc. Methods of using ehmt2 inhibitors in immunotherapies
WO2020097398A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
US20230002374A1 (en) * 2019-11-08 2023-01-05 Heptares Therapeutics Limited Gpr52 modulator compounds
CA3181537A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN115160297B (zh) 2020-12-22 2023-03-31 益方生物科技(上海)股份有限公司 杂芳基化合物及其制备方法和用途
WO2022140527A1 (en) 2020-12-23 2022-06-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
TW202325289A (zh) 2021-11-09 2023-07-01 美商雅捷可斯治療公司 Jak2抑制劑之形式及組合物
TW202334139A (zh) 2021-11-09 2023-09-01 美商雅捷可斯治療公司 作為jak2抑制劑之6-雜芳氧基苯并咪唑及氮雜苯并咪唑
KR20230091052A (ko) * 2021-12-14 2023-06-22 (주)프레이저테라퓨틱스 폴리유비퀴틴화에 의한 표적 단백질 또는 폴리펩티드의 분해용 신규 화합물

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2443305A (en) * 1948-06-15 Pyrimidine derivatives
US6596747B2 (en) * 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
WO2003040141A1 (en) * 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
US7419984B2 (en) * 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
CA2538413A1 (en) * 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
JP5781943B2 (ja) * 2009-01-21 2015-09-24 ライジェル ファーマシューティカルズ, インコーポレイテッド 炎症性疾患、自己免疫疾患または増殖性疾患の治療に有用なn2−(3−ピリジルまたはフェニル)−n4−(4−ピペリジル)−2,4−ピリミジンジアミン誘導体
RU2618475C2 (ru) * 2010-09-10 2017-05-03 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
KR101682417B1 (ko) * 2011-02-25 2016-12-06 주식회사유한양행 다이아미노피리미딘 유도체 및 그의 제조방법
AU2014214846A1 (en) * 2013-02-08 2015-07-23 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
EP3442947B1 (en) * 2016-04-15 2023-06-07 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
EP3555070B1 (en) * 2016-12-19 2023-08-09 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
US20200113901A1 (en) * 2017-03-31 2020-04-16 Epizyme, Inc. Methods of using ehmt2 inhibitors
WO2018195450A1 (en) * 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors

Also Published As

Publication number Publication date
US20200317642A1 (en) 2020-10-08
JP2020537645A (ja) 2020-12-24
EP3697419A4 (en) 2021-08-18
AU2023251449A1 (en) 2023-11-16
JP7425724B2 (ja) 2024-01-31
JP2024038447A (ja) 2024-03-19
EP3697419A1 (en) 2020-08-26
CA3079260A1 (en) 2019-04-25
CN111343988A (zh) 2020-06-26
WO2019079485A1 (en) 2019-04-25

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