CN112771038B - 作为smarca2/4降解剂的哒嗪衍生物 - Google Patents
作为smarca2/4降解剂的哒嗪衍生物 Download PDFInfo
- Publication number
- CN112771038B CN112771038B CN201980041999.5A CN201980041999A CN112771038B CN 112771038 B CN112771038 B CN 112771038B CN 201980041999 A CN201980041999 A CN 201980041999A CN 112771038 B CN112771038 B CN 112771038B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06052—Val-amino acid
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201841015818 | 2018-04-26 | ||
| IN201841015818 | 2018-04-26 | ||
| PCT/IB2019/053443 WO2019207538A1 (en) | 2018-04-26 | 2019-04-26 | Pyridazine derivatives as smarca2/4 degraders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN112771038A CN112771038A (zh) | 2021-05-07 |
| CN112771038B true CN112771038B (zh) | 2024-09-24 |
Family
ID=68295093
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980041999.5A Active CN112771038B (zh) | 2018-04-26 | 2019-04-26 | 作为smarca2/4降解剂的哒嗪衍生物 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US12371426B2 (https=) |
| EP (1) | EP3784665A4 (https=) |
| JP (1) | JP7387630B2 (https=) |
| CN (1) | CN112771038B (https=) |
| CA (1) | CA3118354A1 (https=) |
| SG (1) | SG11202104495YA (https=) |
| WO (1) | WO2019207538A1 (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11771697B2 (en) * | 2018-04-30 | 2023-10-03 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of polybromo-1 (PBRM1) |
| CN113874016A (zh) | 2019-01-29 | 2021-12-31 | 福宏治疗公司 | 化合物及其用途 |
| AR119731A1 (es) | 2019-05-17 | 2022-01-05 | Novartis Ag | Inhibidores del inflamasoma nlrp3 |
| JP2022533260A (ja) * | 2019-05-24 | 2022-07-21 | バイオセリックス， インコーポレイテッド | タンパク質を標的とする化合物及びその医薬組成物並びにそれらの治療的応用 |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| WO2021022163A2 (en) | 2019-07-31 | 2021-02-04 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| PH12022550578A1 (en) * | 2019-09-12 | 2024-02-19 | Aurigene Discovery Tech Ltd | Method for identifying responders to smarca2/4 degraders |
| JP2023511471A (ja) * | 2019-10-28 | 2023-03-20 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 二官能性化合物 |
| JP2023511472A (ja) * | 2019-10-29 | 2023-03-20 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | がんの治療のための二官能性化合物 |
| CN110790746B (zh) * | 2019-11-18 | 2020-10-30 | 南京恒通医药开发有限公司 | 一种利用微通道反应器连续化制备泊马度胺的合成工艺 |
| EP4081308A4 (en) * | 2019-12-23 | 2024-01-24 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| WO2021142247A1 (en) | 2020-01-10 | 2021-07-15 | Amgen Inc. | Smarca2-vhl degraders |
| US12528825B2 (en) | 2020-01-29 | 2026-01-20 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| EP4096651A4 (en) | 2020-01-29 | 2024-01-24 | Foghorn Therapeutics Inc. | COMPOUNDS AND THEIR USES |
| US12599671B2 (en) | 2020-02-12 | 2026-04-14 | Dana-Farber Cancer Institute, Inc. | Compounds, compositions, and methods for protein degradation |
| WO2021207291A1 (en) * | 2020-04-06 | 2021-10-14 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| US11739101B2 (en) | 2020-05-06 | 2023-08-29 | Nurix Therapeutics, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
| US12570650B2 (en) * | 2020-08-04 | 2026-03-10 | Aurigene Oncology Limited | 6-substituted pyridazine compounds as SMARCA2 and/or SMARCA4 degraders |
| WO2022099117A1 (en) * | 2020-11-06 | 2022-05-12 | Prelude Therapeutics Incorporated | Brm targeting compounds and associated methods of use |
| JP7723743B2 (ja) * | 2020-11-20 | 2025-08-14 | フォグホーン セラピューティクス インコーポレイテッド | 化合物及びその使用 |
| EP4259144A4 (en) * | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| CN117337178A (zh) * | 2021-05-10 | 2024-01-02 | 福宏治疗公司 | 化合物及其用途 |
| KR20240004983A (ko) * | 2021-05-10 | 2024-01-11 | 포그혼 쎄라퓨틱스 인크. | 화합물 및 이의 용도 |
| US11767330B2 (en) | 2021-07-06 | 2023-09-26 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
| CN115611881B (zh) * | 2021-07-13 | 2024-09-20 | 复旦大学 | 一种合成新型vhl配体4-f-vh032的方法 |
| KR20240046498A (ko) | 2021-08-09 | 2024-04-09 | 제넨테크, 인크. | Brm의 조절에 사용하기 위한 페놀 유도체 |
| US20250145609A1 (en) * | 2022-02-09 | 2025-05-08 | Aurigene Oncology Limited | 3-substituted pyridazine compounds as smarca2 and/or smarca4 degraders |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
| WO2024064328A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 degraders and uses thereof |
| WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| WO2024064316A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 inhibitors and uses thereof |
| WO2024137742A1 (en) | 2022-12-20 | 2024-06-27 | Blueprint Medicines Corporation | Compounds and compositions as fgfr3 degraders and uses thereof |
| PE20260307A1 (es) | 2023-06-14 | 2026-02-11 | Astrazeneca Ab | Degradadores de smarca2 y usos de estos |
| PE20260301A1 (es) | 2023-06-14 | 2026-02-10 | Astrazeneca Ab | Derivados de 3-[3-amino-6-(2-hidroxifenil)piridazin-4-il]-3,8-diazabiciclo[3.2.1]octano como protacs degradantes de smarca2 para el tratamiento del cancer |
| CN121816356A (zh) * | 2023-07-28 | 2026-04-07 | 甘李药业股份有限公司 | 一种选择性降解smarca2/4的化合物及其应用 |
| CN118406019B (zh) * | 2024-07-02 | 2024-09-20 | 苏州源起材料科技有限公司 | 一种噻唑化合物生物医药砌块的合成方法 |
| WO2026061475A1 (zh) * | 2024-09-19 | 2026-03-26 | 标新生物医药科技(上海)有限公司 | 含有芳基取代杂芳基的双功能蛋白降解剂及其应用 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016138114A1 (en) * | 2015-02-25 | 2016-09-01 | Genentech, Inc. | Therapeutic pyridazine compounds and uses thereof |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| US20190300521A1 (en) * | 2018-04-01 | 2019-10-03 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| US11771697B2 (en) * | 2018-04-30 | 2023-10-03 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of polybromo-1 (PBRM1) |
| PH12022550578A1 (en) * | 2019-09-12 | 2024-02-19 | Aurigene Discovery Tech Ltd | Method for identifying responders to smarca2/4 degraders |
-
2019
- 2019-04-26 EP EP19792591.0A patent/EP3784665A4/en active Pending
- 2019-04-26 CA CA3118354A patent/CA3118354A1/en active Pending
- 2019-04-26 JP JP2020554235A patent/JP7387630B2/ja active Active
- 2019-04-26 SG SG11202104495YA patent/SG11202104495YA/en unknown
- 2019-04-26 WO PCT/IB2019/053443 patent/WO2019207538A1/en not_active Ceased
- 2019-04-26 US US17/050,792 patent/US12371426B2/en active Active
- 2019-04-26 CN CN201980041999.5A patent/CN112771038B/zh active Active
-
2024
- 2024-03-19 US US18/609,175 patent/US20240270734A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016138114A1 (en) * | 2015-02-25 | 2016-09-01 | Genentech, Inc. | Therapeutic pyridazine compounds and uses thereof |
| CN107531668A (zh) * | 2015-02-25 | 2018-01-02 | 基因泰克公司 | 治疗性哒嗪化合物及其用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2019207538A1 (en) | 2019-10-31 |
| CA3118354A1 (en) | 2019-10-31 |
| JP7387630B2 (ja) | 2023-11-28 |
| US20240270734A1 (en) | 2024-08-15 |
| JP2021520372A (ja) | 2021-08-19 |
| EP3784665A4 (en) | 2022-01-26 |
| SG11202104495YA (en) | 2021-05-28 |
| CN112771038A (zh) | 2021-05-07 |
| US12371426B2 (en) | 2025-07-29 |
| EP3784665A1 (en) | 2021-03-03 |
| US20210253564A1 (en) | 2021-08-19 |
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