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 PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- triazin
- pyrrolo
- amine
- imidazo
- methyl
- 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
Links
Classifications
-
- 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
Landscapes
- 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)
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 |
Family
ID=84330173
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 (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)
| 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 |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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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| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| 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 |
| 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 |
| 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 |
| US20220062240A1 (en) | 2018-06-26 | 2022-03-03 | Biosplice Therapeutics, Inc. | Methods of treating cancer using a clk inhibitor |
| 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 |
| 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 |
-
2022
- 2022-10-12 MX MX2024004552A patent/MX2024004552A/es unknown
- 2022-10-12 KR KR1020247014718A patent/KR20240089275A/ko active Pending
- 2022-10-12 WO PCT/US2022/046416 patent/WO2023064366A1/en not_active Ceased
- 2022-10-12 AU AU2022367222A patent/AU2022367222A1/en active Pending
- 2022-10-12 IL IL312157A patent/IL312157A/en unknown
- 2022-10-12 JP JP2024522052A patent/JP2024539620A/ja active Pending
- 2022-10-12 TW TW111138697A patent/TW202322800A/zh unknown
- 2022-10-12 UY UY0001039979A patent/UY39979A/es unknown
- 2022-10-12 EP EP22801289.4A patent/EP4415816B1/en active Active
- 2022-10-12 CA CA3234831A patent/CA3234831A1/en active Pending
- 2022-10-12 PY PY202202289204A patent/PY2289204A/es unknown
- 2022-10-12 US US17/964,489 patent/US12134625B2/en active Active
-
2024
- 2024-08-15 US US18/806,231 patent/US20250171466A1/en active Pending
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| 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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