JP2024539620A - Ｄｙｒｋ１ａ阻害剤としてのピロロ［２，１－ｆ］［１，２，４］トリアジン誘導体 - Google Patents

Ｄｙｒｋ１ａ阻害剤としてのピロロ［２，１－ｆ］［１，２，４］トリアジン誘導体 Download PDF

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JP2024539620A
JP2024539620A JP2024522052A JP2024522052A JP2024539620A JP 2024539620 A JP2024539620 A JP 2024539620A JP 2024522052 A JP2024522052 A JP 2024522052A JP 2024522052 A JP2024522052 A JP 2024522052A JP 2024539620 A JP2024539620 A JP 2024539620A
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triazin
pyrrolo
amine
imidazo
methyl
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JP2024522052A
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JPWO2023064366A5 (enExample
Inventor
ゴピ クマル ミッタパリ
ケーシー スニル クマル
チ チン マク
ブライアン ジョセフ ホフィレナ
ルイス ダニエル ターナー
ブライアン ウォルター イーストマン
ラムクリシュナ レディ ヴァキティ
ジョセフ ティモシー マーコビッツ
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バイオスプライス セラピューティクス インコーポレイテッド
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Publication of JP2024539620A publication Critical patent/JP2024539620A/ja
Publication of JPWO2023064366A5 publication Critical patent/JPWO2023064366A5/ja
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    • 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
    • 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
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2024522052A 2021-10-12 2022-10-12 Ｄｙｒｋ１ａ阻害剤としてのピロロ［２，１－ｆ］［１，２，４］トリアジン誘導体 Pending JP2024539620A (ja)

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 (2)

Publication Number Publication Date
JP2024539620A true JP2024539620A (ja) 2024-10-29
JPWO2023064366A5 JPWO2023064366A5 (enExample) 2025-10-21

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JP2024522052A Pending JP2024539620A (ja) 2021-10-12 2022-10-12 Ｄｙｒｋ１ａ阻害剤としてのピロロ［２，１－ｆ］［１，２，４］トリアジン誘導体

Country Status (11)

Country Link
US (2) US12134625B2 (enExample)
EP (1) EP4415816A1 (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)
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
CN119013030A (zh) * 2022-01-25 2024-11-22 金耐特生物制药公司 Cdk4/6激酶的抑制剂
US20240199649A1 (en) * 2022-11-03 2024-06-20 Biosplice Therapeutics, Inc. 4-aminopyrrolo[2,1-f][1,2,4]triazines and preparation and uses thereof
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
WO2025024707A1 (en) * 2023-07-26 2025-01-30 Kinnate Biopharma Inc. Inhibitors of cdk2/4/6 kinase
WO2025137469A1 (en) * 2023-12-22 2025-06-26 Biosplice Therapeutics, Inc. 4-alkoxypyrrolo[2,1-f][1,2,4]triazines and preparation and uses thereof

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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
PT1730146E (pt) 2004-03-30 2011-07-11 Vertex Pharma Azaindoles úteis como inibidores de jak e outras proteínas quinases
CA2594963A1 (en) 2005-01-24 2006-07-27 Neurosystec Corporation Apparatus and method for delivering therapeutic and/or other agents to the inner ear and to other tissues
JP2011526931A (ja) 2008-07-03 2011-10-20 エグゼリクシス， インコーポレイテッド Ｃｄｋモジュレーター
WO2011018894A1 (en) 2009-08-10 2011-02-17 Raqualia Pharma Inc. Pyrrolopyrimidine derivatives as potassium channel modulators
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
EP2935248B1 (en) 2012-12-21 2018-02-28 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
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
JP2020536920A (ja) * 2017-10-10 2020-12-17 サイロス ファーマシューティカルズ， インコーポレイテッド ピロロトリアジン化合物およびｔａｍキナーゼを阻害する方法
US20200039989A1 (en) 2018-03-01 2020-02-06 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of dyrk/clk and uses thereof
EP3759072A4 (en) 2018-03-01 2021-11-03 The Trustees of Columbia University in the City of New York COMPOUNDS, COMPOSITIONS AND METHODS FOR RELATING TOXIC STRESS FROM ENDOPLASMIC RETICULUM
WO2020006115A1 (en) 2018-06-26 2020-01-02 Betty Tam Methods of treating cancer using a clk inhibitor
CN112867493A (zh) 2018-10-16 2021-05-28 达纳-法伯癌症研究所有限公司 野生型和突变型lrrk2的氮杂吲哚抑制剂
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WO2021257863A1 (en) * 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
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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
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Publication number Publication date
US20230312605A1 (en) 2023-10-05
IL312157A (en) 2024-06-01
WO2023064366A1 (en) 2023-04-20
EP4415816A1 (en) 2024-08-21
CA3234831A1 (en) 2023-04-20
MX2024004552A (es) 2024-06-04
AU2022367222A1 (en) 2024-05-02
US12134625B2 (en) 2024-11-05
TW202322800A (zh) 2023-06-16
US20250171466A1 (en) 2025-05-29
UY39979A (es) 2023-04-14
KR20240089275A (ko) 2024-06-20

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