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

Info

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
Authority
CN
China
Prior art keywords
compound
crystalline form
salt
peaks
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.)
Pending
Application number
CN201880077022.4A
Other languages
English (en)
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
Original Assignee
Epizyme Inc
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 Epizyme Inc filed Critical Epizyme Inc
Publication of CN111417628A publication Critical patent/CN111417628A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • 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)
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

Family

ID=66173899

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (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=)

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
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)
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
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
IL301746A (en) 2023-05-01
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
KR20200101330A (ko) 2020-08-27
AU2018353122A1 (en) 2020-06-04
US20200247790A1 (en) 2020-08-06
JP2021500334A (ja) 2021-01-07
EA202090959A1 (ru) 2020-07-13

Similar Documents

Publication Publication Date Title
CN111417628A (zh) 作为ehmt2抑制剂的胺取代的杂环化合物、其盐及其合成方法
CN108314677B (zh) 一种ezh2抑制剂及其用途
US9890168B2 (en) 2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof
JP6759514B2 (ja) ブロモドメインに対して活性な化合物
CN107556295B (zh) 喹唑啉衍生物及其制备方法
CA3133753A1 (en) Novel small molecule inhibitors of tead transcription factors
KR20190092542A (ko) Ehmt2 저해제로서의 아민-치환된 헤테로사이클릭 화합물 및 이의 사용 방법
CN111343988A (zh) 作为ehmt2抑制剂的胺取代的杂环化合物及其衍生物
JP7189153B2 (ja) Ｐｌｋ１阻害剤としてのピロール誘導体
PT1546127E (pt) Novos derivados de piridinamida e a sua utilização
BR112015017963B1 (pt) Composto de fenil amino pirimidina deuterado, método para preparar a composição farmacêutica, composição farmacêutica e uso do composto
US10689361B2 (en) Quinoline derivative and use thereof
US20240217977A1 (en) Diazepanone-fused pyrimidine compounds, compositions and medicinal applications thereof
RU2444515C2 (ru) Производное амида индазолакриловой кислоты
JP2019519534A (ja) 五員複素環［３，４−ｄ］ピリダジノン系化合物、その製造方法、医薬組成物及び応用
EP3760633B1 (en) Oxazino-quinazoline and oxazino-quinazoline type compound, preparation method therefor, and uses thereof
CN120051460A (zh) 血浆激肽释放酶抑制剂
US20250353831A1 (en) Novel heterobicyclic compound for inhibiting yap-tead interaction and pharmaceutical composition comprising same
TW202115023A (zh) 新型細胞凋亡訊號調節激酶1抑制劑
HK40042713A (en) Oxazino-quinazoline and oxazino-quinazoline type compound, preparation method therefor, and uses thereof
HK40042713B (en) Oxazino-quinazoline and oxazino-quinazoline type compound, preparation method therefor, and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20200714

WD01 Invention patent application deemed withdrawn after publication