CA3234831A1 - Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a - Google Patents

Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a Download PDF

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Publication number
CA3234831A1
CA3234831A1 CA3234831A CA3234831A CA3234831A1 CA 3234831 A1 CA3234831 A1 CA 3234831A1 CA 3234831 A CA3234831 A CA 3234831A CA 3234831 A CA3234831 A CA 3234831A CA 3234831 A1 CA3234831 A1 CA 3234831A1
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CA
Canada
Prior art keywords
amine
pyrrolo
triazin
imidazo
41triazin
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
CA3234831A
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English (en)
French (fr)
Inventor
Gopi Kumar Mittapalli
Sunil Kumar Kc
Chi Ching Mak
Brian Joseph HOFILENA
Lewis Daniel TURNER
Brian Walter Eastman
Ramkrishna Reddy VAKITI
Joseph Timothy Marakovits
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.)
Biosplice Therapeutics Inc
Original Assignee
Biosplice Therapeutics 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 Biosplice Therapeutics Inc filed Critical Biosplice Therapeutics Inc
Publication of CA3234831A1 publication Critical patent/CA3234831A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA3234831A 2021-10-12 2022-10-12 Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a Pending CA3234831A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202163254733P 2021-10-12 2021-10-12
US63/254,733 2021-10-12
US202263347757P 2022-06-01 2022-06-01
US63/347,757 2022-06-01
PCT/US2022/046416 WO2023064366A1 (en) 2021-10-12 2022-10-12 Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a

Publications (1)

Publication Number Publication Date
CA3234831A1 true CA3234831A1 (en) 2023-04-20

Family

ID=84330173

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3234831A Pending CA3234831A1 (en) 2021-10-12 2022-10-12 Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a

Country Status (12)

Country Link
US (2) US12134625B2 (enExample)
EP (1) EP4415816B1 (enExample)
JP (1) JP2024539620A (enExample)
KR (1) KR20240089275A (enExample)
AU (1) AU2022367222A1 (enExample)
CA (1) CA3234831A1 (enExample)
IL (1) IL312157A (enExample)
MX (1) MX2024004552A (enExample)
PY (1) PY2289204A (enExample)
TW (1) TW202322800A (enExample)
UY (1) UY39979A (enExample)
WO (1) WO2023064366A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2023212957A1 (en) * 2022-01-25 2024-08-22 Kinnate Biopharma Inc. Inhibitors of cdk4/6 kinase
KR20250133646A (ko) * 2022-11-03 2025-09-08 바이오스플라이스 테라퓨틱스, 인크. 4-아미노피롤로[2,1-f][1,2,4]트라이아진 및 이의 제조 및 용도
WO2024211797A1 (en) * 2023-04-07 2024-10-10 Biosplice Therapeutics, Inc. Pyrrolo[2,1-f][1,2,4]triazines and preparation and uses thereof
CN119019402A (zh) * 2023-05-24 2024-11-26 中国科学院上海有机化学研究所 作为lrrk2激酶抑制剂的多环化合物及其制备方法和用途
AU2024298476A1 (en) * 2023-07-26 2026-03-05 Khora Spv 1, Llc Inhibitors of cdk2/4/6 kinase
US20250206746A1 (en) * 2023-12-22 2025-06-26 Biosplice Therapeutics, Inc. 4-alkoxypyrrolo[2,1-f][1,2,4]triazines and preparation and uses thereof

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4164559A (en) 1977-09-21 1979-08-14 Cornell Research Foundation, Inc. Collagen drug delivery device
US4474752A (en) 1983-05-16 1984-10-02 Merck & Co., Inc. Drug delivery system utilizing thermosetting gels
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US6440102B1 (en) 1998-07-23 2002-08-27 Durect Corporation Fluid transfer and diagnostic system for treating the inner ear
DE19853299C2 (de) 1998-11-19 2003-04-03 Thomas Lenarz Katheter zur Applikation von Medikamenten in Flüssigkeitsräumen des menschlichen Innenohrs
US6120484A (en) 1999-02-17 2000-09-19 Silverstein; Herbert Otological implant for delivery of medicament and method of using same
US6967023B1 (en) 2000-01-10 2005-11-22 Foamix, Ltd. Pharmaceutical and cosmetic carrier or composition for topical application
US6648873B2 (en) 2001-09-21 2003-11-18 Durect Corp. Aural catheter system including anchor balloon and balloon inflation device
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
JP2008537684A (ja) 2005-01-24 2008-09-25 ニューロシステック コーポレイション 内耳およびその他の組織へ治療薬および/またはその他の薬剤を送達するための装置および方法
CA2728559A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
WO2011018894A1 (en) 2009-08-10 2011-02-17 Raqualia Pharma Inc. Pyrrolopyrimidine derivatives as potassium channel modulators
US8362023B2 (en) * 2011-01-19 2013-01-29 Hoffmann-La Roche Inc. Pyrazolo pyrimidines
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
ME03000B (me) 2012-12-21 2018-10-20 Plexxikon Inc Jedinjenja i metode modulacije kinaze i povezane indikacije
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
BR112017027951A2 (pt) * 2015-06-22 2018-08-28 Ono Pharmaceutical Co., Ltd. composto inibitório de brk
AU2016315881B2 (en) * 2015-09-03 2019-09-19 The Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK1A and uses thereof
FR3041640B1 (fr) 2015-09-30 2019-05-17 Les Laboratoires Servier NOUVEAUX DERIVES DE PYRROLO[2,3-d]PYRIMIDINE, LEUR PROCEDE DE PREPRATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
EP3694860A1 (en) * 2017-10-10 2020-08-19 Syros Pharmaceuticals, Inc. Pyrrolotriazine compounds and methods of inhibiting tam kinases
CA3092828A1 (en) 2018-03-01 2019-09-06 The Trustees Of Columbia University In The City Of New York Compounds, compositions, and methods for suppressing toxic endoplasmic reticulum stress
US12528810B2 (en) * 2018-03-01 2026-01-20 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
US20220062240A1 (en) 2018-06-26 2022-03-03 Biosplice Therapeutics, Inc. Methods of treating cancer using a clk inhibitor
CN113015526A (zh) * 2018-09-19 2021-06-22 豪夫迈·罗氏有限公司 螺环2,3-二氢-7-氮杂吲哚化合物及其用途
JP7503054B2 (ja) 2018-10-16 2024-06-19 ダナ-ファーバー キャンサー インスティテュート,インコーポレイテッド Lrrk2の野生型および変異型のアザインドール阻害剤
EP3911317A2 (en) * 2019-01-17 2021-11-24 BioSplice Therapeutics, Inc. Methods of treating cartilage disorders through inhibition of clk and dyrk
CN112094272A (zh) * 2019-06-18 2020-12-18 北京睿熙生物科技有限公司 Cdk激酶抑制剂
WO2021257863A1 (en) * 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
CA3185649A1 (en) 2020-07-20 2022-01-27 Bakary-Barry Toure Indole compounds as androgen receptor modulators
TW202330533A (zh) 2021-10-12 2023-08-01 美商生物銜接醫療公司 7h-吡咯并[2,3-d]嘧啶及其製備及用途
WO2023064349A1 (en) 2021-10-12 2023-04-20 Biosplice Therapeutics, Inc. 1h-pyrrolo[2,3-b]pyridines as dyrk1a inhibitors
EP4543886A1 (en) 2022-06-23 2025-04-30 BioSplice Therapeutics, Inc. 4-alkoxypyrrolo[2,1-f][1,2,4]triazines and preparation and uses thereof

Also Published As

Publication number Publication date
EP4415816B1 (en) 2026-03-18
MX2024004552A (es) 2024-06-04
WO2023064366A1 (en) 2023-04-20
UY39979A (es) 2023-04-14
US20250171466A1 (en) 2025-05-29
TW202322800A (zh) 2023-06-16
IL312157A (en) 2024-06-01
US20230312605A1 (en) 2023-10-05
EP4415816A1 (en) 2024-08-21
JP2024539620A (ja) 2024-10-29
PY2289204A (es) 2023-12-05
KR20240089275A (ko) 2024-06-20
US12134625B2 (en) 2024-11-05
AU2022367222A1 (en) 2024-05-02

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