JP2021500334A - Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 - Google Patents

Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 Download PDF

Info

Publication number
JP2021500334A
JP2021500334A JP2020521599A JP2020521599A JP2021500334A JP 2021500334 A JP2021500334 A JP 2021500334A JP 2020521599 A JP2020521599 A JP 2020521599A JP 2020521599 A JP2020521599 A JP 2020521599A JP 2021500334 A JP2021500334 A JP 2021500334A
Authority
JP
Japan
Prior art keywords
compound
crystalline form
rays
compound according
xrpd pattern
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.)
Withdrawn
Application number
JP2020521599A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021500334A5 (enExample
Inventor
ジョン エマーソン キャンベル，
ジョン エマーソン キャンベル，
ケネス ウィリアム ダンカン，
ケネス ウィリアム ダンカン，
ジェイムズ エドワード ジョン ミルズ，
ジェイムズ エドワード ジョン ミルズ，
マイケル ジョン マンチホフ，
マイケル ジョン マンチホフ，
Original Assignee
エピザイム，インコーポレイティド
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by エピザイム，インコーポレイティド filed Critical エピザイム，インコーポレイティド
Publication of JP2021500334A publication Critical patent/JP2021500334A/ja
Publication of JP2021500334A5 publication Critical patent/JP2021500334A5/ja
Priority to JP2023002371A priority Critical patent/JP2023036991A/ja
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
JP2020521599A 2017-10-18 2018-10-18 Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 Withdrawn JP2021500334A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023002371A JP2023036991A (ja) 2017-10-18 2023-01-11 Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法

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)

Application Number Title Priority Date Filing Date
JP2023002371A Division JP2023036991A (ja) 2017-10-18 2023-01-11 Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法

Publications (2)

Publication Number Publication Date
JP2021500334A true JP2021500334A (ja) 2021-01-07
JP2021500334A5 JP2021500334A5 (enExample) 2021-10-07

Family

ID=66173899

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2020521599A Withdrawn JP2021500334A (ja) 2017-10-18 2018-10-18 Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法
JP2023002371A Pending JP2023036991A (ja) 2017-10-18 2023-01-11 Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2023002371A Pending JP2023036991A (ja) 2017-10-18 2023-01-11 Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法

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)

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
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)
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

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2009513703A (ja) * 2005-11-01 2009-04-02 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
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
JP2017524668A (ja) * 2014-06-16 2017-08-31 ファンダシオン パラ ラ インベスティガシオン メディカ アプリカダＦｕｎｄａｃｉｏｎ Ｐａｒａ Ｌａ Ｉｎｖｅｓｔｉｇａｓｉｏｎ Ｍｅｄｉｃａ Ａｐｌｉｃａｄａ ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物
JP2020504715A (ja) * 2016-12-19 2020-02-13 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物およびその使用方法
JP7041070B2 (ja) * 2016-04-15 2022-03-23 エピザイム，インコーポレイティド Ｅｈｍｔ１およびｅｈｍｔ２阻害剤としてのアミン置換アリールまたはヘテロアリール化合物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
AU2018243749A1 (en) * 2017-03-31 2019-11-21 Epizyme, Inc. Methods of using EHMT2 inhibitors
EP3697420A4 (en) * 2017-10-18 2021-11-24 Epizyme, Inc. METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2009513703A (ja) * 2005-11-01 2009-04-02 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
JP2017524668A (ja) * 2014-06-16 2017-08-31 ファンダシオン パラ ラ インベスティガシオン メディカ アプリカダＦｕｎｄａｃｉｏｎ Ｐａｒａ Ｌａ Ｉｎｖｅｓｔｉｇａｓｉｏｎ Ｍｅｄｉｃａ Ａｐｌｉｃａｄａ ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物
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
JP7041070B2 (ja) * 2016-04-15 2022-03-23 エピザイム，インコーポレイティド Ｅｈｍｔ１およびｅｈｍｔ２阻害剤としてのアミン置換アリールまたはヘテロアリール化合物
JP2022081606A (ja) * 2016-04-15 2022-05-31 エピザイム，インコーポレイティド Ｅｈｍｔ１およびｅｈｍｔ２阻害剤としてのアミン置換アリールまたはヘテロアリール化合物
JP2020504715A (ja) * 2016-12-19 2020-02-13 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物およびその使用方法

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
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
CN111417628A (zh) 2020-07-14

Similar Documents

Publication Publication Date Title
JP2021500334A (ja) Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法
US9890168B2 (en) 2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof
US10259820B2 (en) EGFR inhibitor, preparation method and use thereof
CN108314677B (zh) 一种ezh2抑制剂及其用途
JP2022110080A (ja) Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物およびその使用方法
JP7425724B2 (ja) Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物及びその誘導体
AU2017226005A1 (en) Inhibitors of WDR5 protein-protein binding
JP6257835B2 (ja) 新規なトリアゾロピリミジノン又はトリアゾロピリジノン誘導体、及びこれらの用途
JP7187449B2 (ja) Ｅｈｍｔ２阻害剤としての置換された融合二環式または三環式複素環化合物
TWI669300B (zh) 嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途
EP3992189A1 (en) Quinazoline and cinnoline derivatives as dna-pk inhibitor
JP2022504620A (ja) 甲状腺ホルモン受容体ベータアゴニスト化合物
AU2024245104A1 (en) Compound acting as wrn helicase inhibitor
JP7776418B2 (ja) イソクエン酸デヒドロゲナーゼ（ｉｄｈ）阻害剤
JP2023502279A (ja) Ｃｐｓ１を阻害するためのピペラジン化合物
US10323043B2 (en) Derivatives of macrocyclic N-aryl-tricyclopyrimidine-2-amine polyethers as inhibitors of FTL3 and JAK
US10179785B2 (en) Imidazotriazinone or imidazopyrazinone derivatives, and use thereof
CN115894376B (zh) 一种芳香族酰胺类化合物、药物组合物及其用途

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210824

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210824

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220708

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220712

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20221011

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20221116

A761 Written withdrawal of application

Free format text: JAPANESE INTERMEDIATE CODE: A761

Effective date: 20230201