CN111417628A - 作为ehmt2抑制剂的胺取代的杂环化合物、其盐及其合成方法 - Google Patents

作为ehmt2抑制剂的胺取代的杂环化合物、其盐及其合成方法 Download PDF

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Publication number
CN111417628A
CN111417628A CN201880077022.4A CN201880077022A CN111417628A CN 111417628 A CN111417628 A CN 111417628A CN 201880077022 A CN201880077022 A CN 201880077022A CN 111417628 A CN111417628 A CN 111417628A
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compound
crystalline form
salt
peaks
xrpd pattern
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CN201880077022.4A
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Chinese (zh)
Inventor
约翰·埃默森·坎贝尔
肯尼思·W·邓肯
詹姆斯·爱德华·约翰·米尔斯
迈克尔·约翰·芒赤霍夫
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Epizyme Inc
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Epizyme Inc
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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
CN201880077022.4A 2017-10-18 2018-10-18 作为ehmt2抑制剂的胺取代的杂环化合物、其盐及其合成方法 Pending CN111417628A (zh)

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
CN111417628A true CN111417628A (zh) 2020-07-14

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CN201880077022.4A Pending CN111417628A (zh) 2017-10-18 2018-10-18 作为ehmt2抑制剂的胺取代的杂环化合物、其盐及其合成方法

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)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114249785A (zh) * 2020-09-23 2022-03-29 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

Families Citing this family (6)

* 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
US11672800B2 (en) 2017-04-21 2023-06-13 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
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

Citations (7)

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US9284272B2 (en) * 2014-03-28 2016-03-15 Abbvie Inc. Inhibitors of histone methyltransferase G9a
US20170121316A1 (en) * 2014-06-16 2017-05-04 Fundación Para La Investigación Médica 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
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
WO2018183923A1 (en) * 2017-03-31 2018-10-04 Epizyme, Inc. Methods of using ehmt2 inhibitors
WO2019079596A1 (en) * 2017-10-18 2019-04-25 Epizyme, Inc. METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES

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JP2007505858A (ja) * 2003-09-18 2007-03-15 ノバルティス アクチエンゲゼルシャフト 増殖性障害の処置に有用な２，４−ジ（フェニルアミノ）ピリミジン
NZ592990A (en) * 2005-11-01 2013-01-25 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

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9284272B2 (en) * 2014-03-28 2016-03-15 Abbvie Inc. Inhibitors of histone methyltransferase G9a
US20170121316A1 (en) * 2014-06-16 2017-05-04 Fundación Para La Investigación Médica 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
WO2017181177A1 (en) * 2016-04-15 2017-10-19 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
CN109153650A (zh) * 2016-04-15 2019-01-04 Epizyme股份有限公司 作为ehmt1和ehmt2抑制剂的胺取代的芳基或杂芳基化合物
WO2018118842A1 (en) * 2016-12-19 2018-06-28 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
CN110088099A (zh) * 2016-12-19 2019-08-02 Epizyme股份有限公司 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法
WO2018183923A1 (en) * 2017-03-31 2018-10-04 Epizyme, Inc. Methods of using ehmt2 inhibitors
WO2019079596A1 (en) * 2017-10-18 2019-04-25 Epizyme, Inc. METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114249785A (zh) * 2020-09-23 2022-03-29 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
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

Also Published As

Publication number Publication date
US20220324851A1 (en) 2022-10-13
IL301746B1 (en) 2024-09-01
SG11202003225YA (en) 2020-05-28
AU2018353122B2 (en) 2023-11-23
CA3079273A1 (en) 2019-04-25
CL2020001009A1 (es) 2020-12-18
EA202090959A1 (ru) 2020-07-13
MX2024012124A (es) 2025-02-10
IL273974B2 (en) 2023-08-01
KR20200101330A (ko) 2020-08-27
EP3697762A4 (en) 2021-04-07
IL301746B2 (en) 2025-01-01
MA50418A (fr) 2021-04-07
CO2020005944A2 (es) 2020-07-31
JP2021500334A (ja) 2021-01-07
IL273974B1 (en) 2023-04-01
MX2020007152A (es) 2020-12-10
WO2019079540A1 (en) 2019-04-25
US20200247790A1 (en) 2020-08-06
AU2024201165A1 (en) 2024-03-14
IL301746A (en) 2023-05-01
IL273974A (en) 2020-05-31
BR112020007632A2 (pt) 2020-09-29
JP2023036991A (ja) 2023-03-14
EP3697762A1 (en) 2020-08-26
AU2018353122A1 (en) 2020-06-04

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