KR20200101330A - Ehmt2 저해제로서의 아민-치환된 헤테로사이클릭 화합물, 이의 염, 및 이들의 합성 방법 - Google Patents

Ehmt2 저해제로서의 아민-치환된 헤테로사이클릭 화합물, 이의 염, 및 이들의 합성 방법 Download PDF

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KR20200101330A
KR20200101330A KR1020207013781A KR20207013781A KR20200101330A KR 20200101330 A KR20200101330 A KR 20200101330A KR 1020207013781 A KR1020207013781 A KR 1020207013781A KR 20207013781 A KR20207013781 A KR 20207013781A KR 20200101330 A KR20200101330 A KR 20200101330A
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compound
crystalline form
salt
radiation
xrpd pattern
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존 에머슨 캠벨
케네스 윌리엄 던칸
제임스 에드워드 존 밀스
마이클 존 먼초프
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에피자임, 인코포레이티드
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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)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020207013781A 2017-10-18 2018-10-18 Ehmt2 저해제로서의 아민-치환된 헤테로사이클릭 화합물, 이의 염, 및 이들의 합성 방법 Ceased KR20200101330A (ko)

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
KR20200101330A true KR20200101330A (ko) 2020-08-27

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KR1020207013781A Ceased KR20200101330A (ko) 2017-10-18 2018-10-18 Ehmt2 저해제로서의 아민-치환된 헤테로사이클릭 화합물, 이의 염, 및 이들의 합성 방법

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

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
US11225487B2 (en) 2017-02-17 2022-01-18 Trevena, Inc. 7-membered aza-heterocyclic containing δ-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
KR20240152947A (ko) 2017-10-18 2024-10-22 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
JP2023546729A (ja) * 2020-10-27 2023-11-07 トレベナ・インコーポレイテッド デルタオピオイドモジュレーターの結晶形及び非晶形
WO2025240956A1 (en) * 2024-05-17 2025-11-20 Yale University G9a/ehmt2 inhibitor use for prader-willi syndrome

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MXPA06003054A (es) * 2003-09-18 2006-05-31 Novartis Ag 2,4-di-(fenil-amino)-pirimidinas utiles en el tratamiento de trastornos proliferativos.
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
CN103626742B (zh) * 2005-11-01 2017-04-26 塔格根公司 激酶的联-芳基间-嘧啶抑制剂
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
EP3157524A4 (en) * 2014-06-23 2017-12-06 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
HUE064145T2 (hu) * 2016-04-15 2024-03-28 Epizyme Inc Amin-szubsztituált aril- vagy heteroaril vegyületek, mint EHMT1 és EHMT2 inhibitorok
ES2955132T3 (es) * 2016-12-19 2023-11-28 Epizyme Inc Compuestos heterocíclicos sustituidos con amina como inhibidores de EHMT2 y métodos de uso de los mismos
EP3600318A4 (en) * 2017-03-31 2021-06-09 Epizyme, Inc. METHOD OF USING EHMT2 INHIBITORS
EP3697420A4 (en) * 2017-10-18 2021-11-24 Epizyme, Inc. METHOD OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPY

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Publication number Publication date
IL301746A (en) 2023-05-01
CN111417628A (zh) 2020-07-14
CO2020005944A2 (es) 2020-07-31
BR112020007632A2 (pt) 2020-09-29
SG11202003225YA (en) 2020-05-28
EP3697762A4 (en) 2021-04-07
JP2023036991A (ja) 2023-03-14
IL301746B2 (en) 2025-01-01
CL2020001009A1 (es) 2020-12-18
MX2024012124A (es) 2025-02-10
IL301746B1 (en) 2024-09-01
MA50418A (fr) 2021-04-07
US20220324851A1 (en) 2022-10-13
AU2024201165A1 (en) 2024-03-14
EP3697762A1 (en) 2020-08-26
IL273974B1 (en) 2023-04-01
MX2020007152A (es) 2020-12-10
CA3079273A1 (en) 2019-04-25
AU2018353122B2 (en) 2023-11-23
IL273974B2 (en) 2023-08-01
IL273974A (en) 2020-05-31
WO2019079540A1 (en) 2019-04-25
AU2018353122A1 (en) 2020-06-04
US20200247790A1 (en) 2020-08-06
JP2021500334A (ja) 2021-01-07
EA202090959A1 (ru) 2020-07-13

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