AU2018353122B2 - Amine-substituted heterocyclic compounds as EHMT2 inhibitors, salts thereof, and methods of synthesis thereof - Google Patents

Amine-substituted heterocyclic compounds as EHMT2 inhibitors, salts thereof, and methods of synthesis thereof Download PDF

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Publication number
AU2018353122B2
AU2018353122B2 AU2018353122A AU2018353122A AU2018353122B2 AU 2018353122 B2 AU2018353122 B2 AU 2018353122B2 AU 2018353122 A AU2018353122 A AU 2018353122A AU 2018353122 A AU2018353122 A AU 2018353122A AU 2018353122 B2 AU2018353122 B2 AU 2018353122B2
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Prior art keywords
compound
crystalline form
radiation
xrpd pattern
salt
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AU2018353122A
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AU2018353122A1 (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 of AU2018353122B2 publication Critical patent/AU2018353122B2/en
Priority to AU2024201165A priority Critical patent/AU2024201165A1/en
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Anticipated expiration legal-status Critical

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    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2018353122A 2017-10-18 2018-10-18 Amine-substituted heterocyclic compounds as EHMT2 inhibitors, salts thereof, and methods of synthesis thereof Ceased AU2018353122B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2024201165A AU2024201165A1 (en) 2017-10-18 2024-02-22 Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762573917P 2017-10-18 2017-10-18
US62/573,917 2017-10-18
PCT/US2018/056428 WO2019079540A1 (en) 2017-10-18 2018-10-18 AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS INHIBITORS OF EHMT2, SALTS THEREOF, AND METHODS OF SYNTHESIS THEREOF

Related Child Applications (1)

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AU2024201165A Division AU2024201165A1 (en) 2017-10-18 2024-02-22 Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof

Publications (2)

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AU2018353122A1 AU2018353122A1 (en) 2020-06-04
AU2018353122B2 true AU2018353122B2 (en) 2023-11-23

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AU2018353122A Ceased AU2018353122B2 (en) 2017-10-18 2018-10-18 Amine-substituted heterocyclic compounds as EHMT2 inhibitors, salts thereof, and methods of synthesis thereof
AU2024201165A Abandoned AU2024201165A1 (en) 2017-10-18 2024-02-22 Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof

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US (2) US20200247790A1 (enExample)
EP (1) EP3697762A4 (enExample)
JP (2) JP2021500334A (enExample)
KR (1) KR20200101330A (enExample)
CN (1) CN111417628A (enExample)
AU (2) AU2018353122B2 (enExample)
BR (1) BR112020007632A2 (enExample)
CA (1) CA3079273A1 (enExample)
CL (1) CL2020001009A1 (enExample)
CO (1) CO2020005944A2 (enExample)
EA (1) EA202090959A1 (enExample)
IL (2) IL301746B2 (enExample)
MA (1) MA50418A (enExample)
MX (2) MX2020007152A (enExample)
SG (1) SG11202003225YA (enExample)
WO (1) WO2019079540A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110446495B (zh) 2017-02-17 2023-09-05 特维娜有限公司 含有7元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法
WO2018195450A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
KR102717072B1 (ko) 2017-10-18 2024-10-15 인사이트 코포레이션 Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
CN114249785B (zh) * 2020-09-23 2024-04-05 常州方圆制药有限公司 一种2-腺苷n-吡唑的衍生物瑞加德松的制备方法
CN116406268A (zh) * 2020-10-27 2023-07-07 特维娜有限公司 δ-阿片样物质调节剂的结晶和无定形形式
WO2025240956A1 (en) * 2024-05-17 2025-11-20 Yale University G9a/ehmt2 inhibitor use for prader-willi syndrome

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017181177A1 (en) * 2016-04-15 2017-10-19 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
WO2018118842A1 (en) * 2016-12-19 2018-06-28 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004272288B2 (en) * 2003-09-18 2008-11-13 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2007053452A1 (en) * 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US9284272B2 (en) * 2014-03-28 2016-03-15 Abbvie Inc. Inhibitors of histone methyltransferase G9a
DK3154957T3 (da) * 2014-06-16 2020-02-17 Fundacion Para La Investig Medica Aplicada Hidtil ukendte forbindelser som dobbelte inhibitorer af histonmethyltransferaser og dna-methyltransferaser
JP2017519017A (ja) * 2014-06-23 2017-07-13 ジェネンテック， インコーポレイテッド 癌の治療及び癌薬剤耐性の防止方法
AU2018243749A1 (en) * 2017-03-31 2019-11-21 Epizyme, Inc. Methods of using EHMT2 inhibitors
US20210213014A1 (en) * 2017-10-18 2021-07-15 Epizyme, Inc. Methods of using ehmt2 inhibitors in immunotherapies

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017181177A1 (en) * 2016-04-15 2017-10-19 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
WO2018118842A1 (en) * 2016-12-19 2018-06-28 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof

Also Published As

Publication number Publication date
US20220324851A1 (en) 2022-10-13
AU2018353122A1 (en) 2020-06-04
IL301746A (en) 2023-05-01
IL301746B2 (en) 2025-01-01
JP2021500334A (ja) 2021-01-07
CO2020005944A2 (es) 2020-07-31
MX2024012124A (es) 2025-02-10
IL273974B1 (en) 2023-04-01
CA3079273A1 (en) 2019-04-25
SG11202003225YA (en) 2020-05-28
KR20200101330A (ko) 2020-08-27
JP2023036991A (ja) 2023-03-14
MX2020007152A (es) 2020-12-10
CN111417628A (zh) 2020-07-14
BR112020007632A2 (pt) 2020-09-29
US20200247790A1 (en) 2020-08-06
EP3697762A1 (en) 2020-08-26
WO2019079540A1 (en) 2019-04-25
EA202090959A1 (ru) 2020-07-13
AU2024201165A1 (en) 2024-03-14
CL2020001009A1 (es) 2020-12-18
IL301746B1 (en) 2024-09-01
MA50418A (fr) 2021-04-07
EP3697762A4 (en) 2021-04-07
IL273974B2 (en) 2023-08-01
IL273974A (en) 2020-05-31

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