CA3181909A1 - 4-ethynylpyridine derivatives useful as gcn2 inhibitors - Google Patents

4-ethynylpyridine derivatives useful as gcn2 inhibitors Download PDF

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Publication number
CA3181909A1
CA3181909A1 CA3181909A CA3181909A CA3181909A1 CA 3181909 A1 CA3181909 A1 CA 3181909A1 CA 3181909 A CA3181909 A CA 3181909A CA 3181909 A CA3181909 A CA 3181909A CA 3181909 A1 CA3181909 A1 CA 3181909A1
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Prior art keywords
halogen
optionally substituted
group
independently selected
groups independently
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Pending
Application number
CA3181909A
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English (en)
French (fr)
Inventor
Gavin Whitlock
Matthew FUCHTER
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.)
Ip2ipo Innovations Ltd
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Individual
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Publication of CA3181909A1 publication Critical patent/CA3181909A1/en
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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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA3181909A 2020-06-09 2021-06-09 4-ethynylpyridine derivatives useful as gcn2 inhibitors Pending CA3181909A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB2008749.0 2020-06-09
GBGB2008749.0A GB202008749D0 (en) 2020-06-09 2020-06-09 Novel compounds
PCT/GB2021/051428 WO2021250399A1 (en) 2020-06-09 2021-06-09 4-ethynylpyridine derivatives useful as gcn2 inhibitors

Publications (1)

Publication Number Publication Date
CA3181909A1 true CA3181909A1 (en) 2021-12-16

Family

ID=71616023

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3181909A Pending CA3181909A1 (en) 2020-06-09 2021-06-09 4-ethynylpyridine derivatives useful as gcn2 inhibitors

Country Status (12)

Country Link
US (2) US20230271939A1 (https=)
EP (1) EP4161915A1 (https=)
JP (1) JP2023529926A (https=)
KR (1) KR20230058042A (https=)
CN (2) CN116113629B (https=)
AU (1) AU2021289535A1 (https=)
BR (1) BR112022025147A2 (https=)
CA (1) CA3181909A1 (https=)
GB (1) GB202008749D0 (https=)
IL (1) IL298860B1 (https=)
MX (1) MX2022015516A (https=)
WO (1) WO2021250399A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB202008749D0 (en) 2020-06-09 2020-07-22 Ip2Ipo Innovations Ltd Novel compounds
GB202104635D0 (en) 2021-03-31 2021-05-12 Imperial College Innovations Ltd Methods and compositions for identifying and treating GCN2-dependent cancers
GB202118096D0 (en) * 2021-12-14 2022-01-26 Ip2Ipo Innovations Ltd Novel compounds
GB202403113D0 (en) 2024-03-04 2024-04-17 Apollo Ap30 Ltd Novel compounds

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7037927B2 (en) 2003-10-16 2006-05-02 Abbott Laboratories Amides that inhibit vanilloid receptor subtype 1 (VR1) receptor
US20080146599A1 (en) 2005-02-01 2008-06-19 Astrazeneca Ab Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity
GB0502418D0 (en) 2005-02-05 2005-03-16 Astrazeneca Ab Compounds
US8546413B2 (en) 2009-06-15 2013-10-01 Nerviano Medical Sciences S.R.L. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
ES2655264T3 (es) 2012-01-28 2018-02-19 Merck Patent Gmbh Derivados de triazolo[4,5-d]pirimidina
US20150051202A1 (en) 2012-03-07 2015-02-19 Merck Patent Gmbh Triazolopyrazine derivatives
WO2014031928A2 (en) 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
ES2755772T3 (es) 2012-11-07 2020-04-23 Nerviano Medical Sciences Srl Pirimidinil y piridinilpirrolopiridinonas sustituidas, proceso para su preparación y su uso como inhibidores de cinasas
EP2964648B1 (en) 2013-03-05 2016-11-16 Merck Patent GmbH 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents
AU2014224975B2 (en) 2013-03-05 2017-09-14 Merck Patent Gmbh Triazolo(4,5-d)pyrimidine derivatives for the treatment of diseases such as cancer
CN105732614B (zh) 2014-12-09 2018-06-12 中国科学院广州生物医药与健康研究院 磺酰胺基芳基炔类化合物及其用途
CN104829613B (zh) 2015-04-13 2020-06-09 赤峰蒙广生物科技有限公司 二芳基取代的吡唑并环类衍生物、其制备方法及其在医药领域的应用
HRP20241768T1 (hr) * 2016-08-10 2025-02-28 Takeda Pharmaceutical Company Limited Heterociklički spoj
CN108473476B (zh) 2016-10-13 2021-02-19 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白激酶活性的炔基杂环类化合物
JP7229257B2 (ja) 2018-01-29 2023-02-28 メルク パテント ゲーエムベーハー Gcn2阻害剤およびその使用
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
EP3802544A1 (en) 2018-06-05 2021-04-14 RAPT Therapeutics, Inc. Pyrazolo-pyrimidin-amino-cycloalkyl compounds and their therapeutic uses
US20220388964A1 (en) 2019-04-12 2022-12-08 Hibercell, Inc. (aza)indazolyl-aryl sulfonamide and related compounds and their use in treating medical conditions
WO2021155253A1 (en) 2020-01-31 2021-08-05 Atomwise Inc. Anat inhibitors and methods of use thereof
JP2023514328A (ja) 2020-02-17 2023-04-05 アレスタ・セラピューティクス・ベスローテン・フェンノートシャップ Gcn2モジュレーター化合物
WO2021222147A1 (en) 2020-04-27 2021-11-04 Hibercell, Inc. Heterocyclic gcn2 modulators
GB202008749D0 (en) 2020-06-09 2020-07-22 Ip2Ipo Innovations Ltd Novel compounds
IL302807A (en) 2020-11-18 2023-07-01 Deciphera Pharmaceuticals Llc Gcn2 and perk kinase inhibitors and methods of use thereof
BR112023014723A2 (pt) 2021-01-22 2023-10-03 Hibercell Inc Compostos moduladores de gcn2 e usos dos mesmos
US20240150345A1 (en) 2021-01-22 2024-05-09 Hibercell, Inc. Gcn2 modulating compounds and uses thereof

Also Published As

Publication number Publication date
MX2022015516A (es) 2023-03-22
WO2021250399A1 (en) 2021-12-16
AU2021289535A1 (en) 2023-02-09
JP2023529926A (ja) 2023-07-12
GB202008749D0 (en) 2020-07-22
US20230271939A1 (en) 2023-08-31
KR20230058042A (ko) 2023-05-02
US20230250082A1 (en) 2023-08-10
US11945799B2 (en) 2024-04-02
CN119661503A (zh) 2025-03-21
CN116113629B (zh) 2024-12-31
IL298860B1 (en) 2026-04-01
CN116113629A (zh) 2023-05-12
IL298860A (en) 2023-02-01
EP4161915A1 (en) 2023-04-12
BR112022025147A2 (pt) 2023-04-25

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