CA3037587A1 - Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors - Google Patents

Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors Download PDF

Info

Publication number
CA3037587A1
CA3037587A1 CA3037587A CA3037587A CA3037587A1 CA 3037587 A1 CA3037587 A1 CA 3037587A1 CA 3037587 A CA3037587 A CA 3037587A CA 3037587 A CA3037587 A CA 3037587A CA 3037587 A1 CA3037587 A1 CA 3037587A1
Authority
CA
Canada
Prior art keywords
halo
compound
optionally substituted
cyano
hydroxyl
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
CA3037587A
Other languages
English (en)
French (fr)
Inventor
John Emmerson Campbell
Kenneth William Duncan
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 CA3037587A1 publication Critical patent/CA3037587A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Indole Compounds (AREA)
CA3037587A 2016-09-30 2017-09-29 Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors Pending CA3037587A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662402863P 2016-09-30 2016-09-30
US62/402,863 2016-09-30
US201762509620P 2017-05-22 2017-05-22
US62/509,620 2017-05-22
PCT/US2017/054468 WO2018064557A1 (en) 2016-09-30 2017-09-29 Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors

Publications (1)

Publication Number Publication Date
CA3037587A1 true CA3037587A1 (en) 2018-04-05

Family

ID=60043417

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3037587A Pending CA3037587A1 (en) 2016-09-30 2017-09-29 Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors

Country Status (6)

Country Link
US (2) US20200039961A1 (OSRAM)
EP (2) EP4105203A1 (OSRAM)
JP (2) JP7187449B2 (OSRAM)
AU (3) AU2017336074A1 (OSRAM)
CA (1) CA3037587A1 (OSRAM)
WO (1) WO2018064557A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11672800B2 (en) 2017-04-21 2023-06-13 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
US12415816B2 (en) 2018-11-07 2025-09-16 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
EP4146639A1 (en) 2020-05-06 2023-03-15 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
TW202241889A (zh) 2020-12-23 2022-11-01 美商雅捷可斯治療公司 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑
WO2023086320A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of jak2
JP7782035B2 (ja) 2021-11-09 2025-12-08 エイジャックス セラピューティクス， インコーポレイテッド Ｊａｋ２阻害剤としての６－ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
CN116425642B (zh) * 2023-04-06 2025-06-10 浙江科聚生物医药有限公司 2-甲氧基-4-氟-5-胺基苯酚的制备方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE8604566D0 (sv) 1986-10-27 1986-10-27 Haessle Ab Novel compunds
GB8820231D0 (en) 1988-08-25 1988-09-28 Fujisawa Pharmaceutical Co New benzazole compounds processes for preparation thereof & pharmaceutical composition comprising same
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
US6025379A (en) 1996-03-11 2000-02-15 Eli Lilly And Company Methods of treating or preventing interstitial cystitis
US6391907B1 (en) * 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
CN1143847C (zh) * 1999-05-04 2004-03-31 美国家庭用品有限公司 硫代-羟吲哚衍生物
TW593278B (en) 2001-01-23 2004-06-21 Wyeth Corp 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
EP1682126B1 (en) * 2003-10-16 2009-07-01 Novartis Vaccines and Diagnostics, Inc. Substituted benzazoles and use thereof as inhibitors of raf kinase
US8214439B2 (en) * 2005-12-06 2012-07-03 Microsoft Corporation Document object model API for MIME
FR2897061B1 (fr) * 2006-02-03 2010-09-03 Sanofi Aventis Derives de n-heteroaryl-carboxamides tricycliques contenant un motif benzimidazole, leur preparation et leur application en therapeutique.
CN103172637B (zh) * 2013-03-13 2015-05-27 上海大学 嘧啶并[1,2-a]苯并咪唑类化合物及其制备方法
US9284272B2 (en) * 2014-03-28 2016-03-15 Abbvie Inc. Inhibitors of histone methyltransferase G9a
US20170209444A1 (en) 2014-06-23 2017-07-27 Genentech Inc. Methods of treating cancer and preventing cancer drug resistance
TW202411220A (zh) * 2016-12-19 2024-03-16 美商雅酶股份有限公司 作為ehmt2抑制劑之胺取代的雜環化合物及其使用方法
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
BR112020007585A2 (pt) * 2017-10-18 2020-09-24 Epizyme, Inc. método para prevenir ou tratar um distúrbio sanguíneo, inibidor de ehmt2 e uso de um inibidor de ehmt2

Also Published As

Publication number Publication date
WO2018064557A1 (en) 2018-04-05
JP2019533650A (ja) 2019-11-21
AU2017336074A1 (en) 2019-03-28
JP7187449B2 (ja) 2022-12-12
US20200039961A1 (en) 2020-02-06
AU2021277619B2 (en) 2023-11-09
US20220274961A1 (en) 2022-09-01
AU2024200781A1 (en) 2024-02-29
AU2021277619A1 (en) 2021-12-23
EP4105203A1 (en) 2022-12-21
EP3519393A1 (en) 2019-08-07
EP3519393B1 (en) 2022-05-18
JP2023022230A (ja) 2023-02-14

Similar Documents

Publication Publication Date Title
EP3555070B1 (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
AU2021245168B2 (en) Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
AU2021277619B2 (en) Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
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
WO2015010078A2 (en) Substituted 6,5-fused bicyclic heteroaryl compounds
HK40098892A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
HK40016100B (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
HK40016100A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
NZ795530A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
OA19666A (en) Amine-substituted heterocyclic compounds as Ehmt2 inhibitors and methods of use thereof.
HK40012431A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
OA19500A (en) Amine-substituted Aryl or Heteroaryl compounds as Ehmt1 and Ehmt2 inhibitors.

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20220929

EEER Examination request

Effective date: 20220929

EEER Examination request

Effective date: 20220929

EEER Examination request

Effective date: 20220929