AU2017254713C1 - Bifunctional molecules for degradation of EGFR and methods of use - Google Patents
Bifunctional molecules for degradation of EGFR and methods of use Download PDFInfo
- Publication number
- AU2017254713C1 AU2017254713C1 AU2017254713A AU2017254713A AU2017254713C1 AU 2017254713 C1 AU2017254713 C1 AU 2017254713C1 AU 2017254713 A AU2017254713 A AU 2017254713A AU 2017254713 A AU2017254713 A AU 2017254713A AU 2017254713 C1 AU2017254713 C1 AU 2017254713C1
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- cancer
- formula
- egfr
- alkyl
- compound
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- 0 *=C(c1c2cccc1NCCOCCCCCCC(N(CC1)CCN1c(cc1)ccc1-c1cc(C(N(C3)C(C(Nc4ncc[s]4)=O)C(CC(C=C4)F)=C4O)=O)c3cc1)=O)N(C(CCC(*1)=O)C1=N)C2=O Chemical compound *=C(c1c2cccc1NCCOCCCCCCC(N(CC1)CCN1c(cc1)ccc1-c1cc(C(N(C3)C(C(Nc4ncc[s]4)=O)C(CC(C=C4)F)=C4O)=O)c3cc1)=O)N(C(CCC(*1)=O)C1=N)C2=O 0.000 description 1
- IZIJTCGOBSORDO-UHFFFAOYSA-N CC(CCC(N1)=O)(C1=O)N(C(c1cccc(NCCOCCOCCOCCC(N(CC2)CCN2c(cc2)ccc2-c2ccc(CN(C(C(Nc3ncc[s]3)=C)c3ccccc3)C3=C)c3c2)=O)c11)=O)C1=O Chemical compound CC(CCC(N1)=O)(C1=O)N(C(c1cccc(NCCOCCOCCOCCC(N(CC2)CCN2c(cc2)ccc2-c2ccc(CN(C(C(Nc3ncc[s]3)=C)c3ccccc3)C3=C)c3c2)=O)c11)=O)C1=O IZIJTCGOBSORDO-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- 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
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326574P | 2016-04-22 | 2016-04-22 | |
| US62/326,574 | 2016-04-22 | ||
| PCT/US2017/028950 WO2017185036A1 (en) | 2016-04-22 | 2017-04-21 | Bifunctional molecules for degradation of egfr and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| AU2017254713A1 AU2017254713A1 (en) | 2018-10-18 |
| AU2017254713B2 AU2017254713B2 (en) | 2020-11-19 |
| AU2017254713C1 true AU2017254713C1 (en) | 2021-04-29 |
Family
ID=60116448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017254713A Active AU2017254713C1 (en) | 2016-04-22 | 2017-04-21 | Bifunctional molecules for degradation of EGFR and methods of use |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10450310B2 (enExample) |
| EP (2) | EP3892272B1 (enExample) |
| JP (1) | JP6968823B2 (enExample) |
| CN (1) | CN109475528B (enExample) |
| AU (1) | AU2017254713C1 (enExample) |
| CA (1) | CA3021358A1 (enExample) |
| WO (1) | WO2017185036A1 (enExample) |
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| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
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| JP7269731B2 (ja) | 2015-03-18 | 2023-05-09 | アルビナス・オペレーションズ・インコーポレイテッド | 標的タンパク質の分解向上のための化合物および方法 |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2017185036A1 (en) | 2016-04-22 | 2017-10-26 | Dana Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| JP6927999B2 (ja) * | 2016-04-22 | 2021-09-01 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ９（ｃｄｋ９）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ９の分解および使用法 |
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