CA3079273A1 - 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
CA3079273A1
CA3079273A1 CA3079273A CA3079273A CA3079273A1 CA 3079273 A1 CA3079273 A1 CA 3079273A1 CA 3079273 A CA3079273 A CA 3079273A CA 3079273 A CA3079273 A CA 3079273A CA 3079273 A1 CA3079273 A1 CA 3079273A1
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Prior art keywords
compound
crystalline form
salt
radiation
xrpd pattern
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Pending
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CA3079273A
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English (en)
French (fr)
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 CA3079273A1 publication Critical patent/CA3079273A1/en
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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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P7/06Antianaemics
    • 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • 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
    • 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
    • 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
    • C07D405/14Heterocyclic 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

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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)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
CA3079273A 2017-10-18 2018-10-18 Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof Pending CA3079273A1 (en)

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

Publications (1)

Publication Number Publication Date
CA3079273A1 true CA3079273A1 (en) 2019-04-25

Family

ID=66173899

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3079273A Pending CA3079273A1 (en) 2017-10-18 2018-10-18 Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof

Country Status (16)

Country Link
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
EP3582783B1 (en) 2017-02-17 2023-06-07 Trevena, Inc. 7-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same
CN110621316B (zh) 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
CN118063470A (zh) 2017-10-18 2024-05-24 因赛特公司 作为PI3K-γ抑制剂的由叔羟基取代的缩合咪唑衍生物
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
EP4236939A4 (en) * 2020-10-27 2024-08-07 Trevena, Inc. Crystalline and amorphous forms of a delta-opioid modulator
WO2025240956A1 (en) * 2024-05-17 2025-11-20 Yale University G9a/ehmt2 inhibitor use for prader-willi syndrome

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100584832C (zh) * 2003-09-18 2010-01-27 诺瓦提斯公司 可用于治疗增殖性病症的2,4-二(苯基氨基)嘧啶类
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
JP5191391B2 (ja) * 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
US9284272B2 (en) * 2014-03-28 2016-03-15 Abbvie Inc. Inhibitors of histone methyltransferase G9a
EP3154957B1 (en) * 2014-06-16 2019-11-20 Fundacion para la Investigacion Medica Aplicada Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases
US20170209444A1 (en) * 2014-06-23 2017-07-27 Genentech Inc. Methods of treating cancer and preventing cancer drug resistance
AU2017250369A1 (en) * 2016-04-15 2018-10-11 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as EHMT1 and EHMT2 inhibitors
BR112019012140A2 (pt) * 2016-12-19 2019-11-05 Epizyme Inc composto, composição farmacêutica, método para prevenir ou tratar um distúrbio sanguíneo, método para prevenir ou tratar um câncer e uso de um composto
EP3600318A4 (en) * 2017-03-31 2021-06-09 Epizyme, Inc. METHOD OF USING EHMT2 INHIBITORS
CN111343989A (zh) * 2017-10-18 2020-06-26 Epizyme股份有限公司 使用ehmt2抑制剂用于免疫疗法的方法

Also Published As

Publication number Publication date
IL273974A (en) 2020-05-31
WO2019079540A1 (en) 2019-04-25
MA50418A (fr) 2021-04-07
BR112020007632A2 (pt) 2020-09-29
US20200247790A1 (en) 2020-08-06
AU2018353122A1 (en) 2020-06-04
EA202090959A1 (ru) 2020-07-13
JP2023036991A (ja) 2023-03-14
CL2020001009A1 (es) 2020-12-18
IL301746B1 (en) 2024-09-01
IL273974B1 (en) 2023-04-01
CO2020005944A2 (es) 2020-07-31
AU2018353122B2 (en) 2023-11-23
MX2020007152A (es) 2020-12-10
US20220324851A1 (en) 2022-10-13
MX2024012124A (es) 2025-02-10
EP3697762A4 (en) 2021-04-07
CN111417628A (zh) 2020-07-14
SG11202003225YA (en) 2020-05-28
IL301746A (en) 2023-05-01
EP3697762A1 (en) 2020-08-26
KR20200101330A (ko) 2020-08-27
JP2021500334A (ja) 2021-01-07
IL301746B2 (en) 2025-01-01
IL273974B2 (en) 2023-08-01
AU2024201165A1 (en) 2024-03-14

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