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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JP2024539620A5 (enExample
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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 JP2024539620A5 publication Critical patent/JP2024539620A5/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)
  • 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)
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
JP2024539620A5 JP2024539620A5 (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

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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)

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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

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WO2016208595A1 (ja) * 2015-06-22 2016-12-29 小野薬品工業株式会社 Brk阻害化合物
JP2018526452A (ja) * 2015-09-03 2018-09-13 アリゾナ ボード オブ リージェンツ オン ビハーフ オブ ザ ユニバーシティー オブ アリゾナ Dyrk1aの小分子抑制剤およびその使用
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
WO2020061377A1 (en) * 2018-09-19 2020-03-26 Genentech, Inc. Spirocyclic 2,3-dihydro-7-azaindole compounds and uses thereof
WO2020150552A2 (en) * 2019-01-17 2020-07-23 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
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
WO2020253458A1 (zh) * 2019-06-18 2020-12-24 北京睿熙生物科技有限公司 Cdk激酶抑制剂

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* Cited by examiner, † Cited by third party
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US20120184508A1 (en) * 2011-01-19 2012-07-19 Wenjian Liu Pyrazolo pyrimidines
WO2016208595A1 (ja) * 2015-06-22 2016-12-29 小野薬品工業株式会社 Brk阻害化合物
JP2018526452A (ja) * 2015-09-03 2018-09-13 アリゾナ ボード オブ リージェンツ オン ビハーフ オブ ザ ユニバーシティー オブ アリゾナ Dyrk1aの小分子抑制剤およびその使用
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
WO2020061377A1 (en) * 2018-09-19 2020-03-26 Genentech, Inc. Spirocyclic 2,3-dihydro-7-azaindole compounds and uses thereof
WO2020150552A2 (en) * 2019-01-17 2020-07-23 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
WO2020253458A1 (zh) * 2019-06-18 2020-12-24 北京睿熙生物科技有限公司 Cdk激酶抑制剂

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EP4415816B1 (en) 2026-03-18
MX2024004552A (es) 2024-06-04
WO2023064366A1 (en) 2023-04-20
CA3234831A1 (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
PY2289204A (es) 2023-12-05
KR20240089275A (ko) 2024-06-20
US12134625B2 (en) 2024-11-05
AU2022367222A1 (en) 2024-05-02

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