JP2019519476A5 - - Google Patents
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- JP2019519476A5 JP2019519476A5 JP2018554702A JP2018554702A JP2019519476A5 JP 2019519476 A5 JP2019519476 A5 JP 2019519476A5 JP 2018554702 A JP2018554702 A JP 2018554702A JP 2018554702 A JP2018554702 A JP 2018554702A JP 2019519476 A5 JP2019519476 A5 JP 2019519476A5
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- Prior art keywords
- diastereomer
- stereoisomer
- enantiomer
- cancer
- pharmaceutically acceptable
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 36
- 150000003839 salts Chemical class 0.000 claims 33
- 230000001588 bifunctional effect Effects 0.000 claims 32
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 102000001301 EGF receptor Human genes 0.000 claims 6
- 108060006698 EGF receptor Proteins 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 4
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
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- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
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- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
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- 0 CCCCCC[C@](CC)*[C@@](*(C)C)[C@](C1)[C@]1[C@@]1C[C@@](CCCCC)CC1 Chemical compound CCCCCC[C@](CC)*[C@@](*(C)C)[C@](C1)[C@]1[C@@]1C[C@@](CCCCC)CC1 0.000 description 2
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 |
|---|---|
| JP2019519476A JP2019519476A (ja) | 2019-07-11 |
| JP2019519476A5 true JP2019519476A5 (cg-RX-API-DMAC7.html) | 2020-05-28 |
| JP6968823B2 JP6968823B2 (ja) | 2021-11-17 |
Family
ID=60116448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018554702A Active JP6968823B2 (ja) | 2016-04-22 | 2017-04-21 | Ｅｇｆｒの分解のための二官能性分子、及び使用方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10450310B2 (cg-RX-API-DMAC7.html) |
| EP (2) | EP3445357B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6968823B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN109475528B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2017254713C1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA3021358A1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2017185036A1 (cg-RX-API-DMAC7.html) |
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| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| AU2016232705C1 (en) | 2015-03-18 | 2021-06-17 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| US20180147202A1 (en) | 2015-06-05 | 2018-05-31 | 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 |
| 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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| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
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