JP2019535744A5 - - Google Patents
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- JP2019535744A5 JP2019535744A5 JP2019527335A JP2019527335A JP2019535744A5 JP 2019535744 A5 JP2019535744 A5 JP 2019535744A5 JP 2019527335 A JP2019527335 A JP 2019527335A JP 2019527335 A JP2019527335 A JP 2019527335A JP 2019535744 A5 JP2019535744 A5 JP 2019535744A5
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- Prior art keywords
- alkyl
- independently
- cancer
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 45
- 230000001588 bifunctional effect Effects 0.000 claims description 43
- 125000000217 alkyl group Chemical group 0.000 claims description 42
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 125000001188 haloalkyl group Chemical group 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- 239000003446 ligand Substances 0.000 claims description 13
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 claims description 11
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 claims description 11
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 8
- 229910052717 sulfur Chemical group 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 6
- 206010017758 gastric cancer Diseases 0.000 claims description 6
- 201000011549 stomach cancer Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 5
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 5
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 5
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 208000032612 Glial tumor Diseases 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 206010005949 Bone cancer Diseases 0.000 claims description 2
- 208000018084 Bone neoplasm Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 229910052757 nitrogen Chemical group 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000008685 targeting Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 5
- 239000003814 drug Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662425204P | 2016-11-22 | 2016-11-22 | |
| US62/425,204 | 2016-11-22 | ||
| PCT/US2017/063011 WO2018098275A1 (en) | 2016-11-22 | 2017-11-22 | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019535744A JP2019535744A (ja) | 2019-12-12 |
| JP2019535744A5 true JP2019535744A5 (enExample) | 2020-12-24 |
| JP7038712B2 JP7038712B2 (ja) | 2022-03-18 |
Family
ID=62195645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019527335A Active JP7038712B2 (ja) | 2016-11-22 | 2017-11-22 | ブルトン型チロシンキナーゼ（ｂｔｋ）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ｂｔｋの分解および使用法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10842878B2 (enExample) |
| EP (1) | EP3544975B1 (enExample) |
| JP (1) | JP7038712B2 (enExample) |
| KR (1) | KR102566109B1 (enExample) |
| AU (1) | AU2017363252B2 (enExample) |
| CA (1) | CA3042297A1 (enExample) |
| WO (1) | WO2018098275A1 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109153644B (zh) | 2016-03-16 | 2022-10-21 | H·李·莫菲特癌症中心研究有限公司 | 用以增强效应t细胞功能的针对cereblon的小分子 |
| FI3500299T3 (fi) | 2016-08-19 | 2024-02-14 | Beigene Switzerland Gmbh | Tsanubrutinibin yhdistelmä cd20-tai pd-1-vasta-aineen kanssa käytettäväksi syövän hoidossa |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| US11597768B2 (en) | 2017-06-26 | 2023-03-07 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
| US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
| CA3085457C (en) | 2018-01-29 | 2023-05-23 | Dana-Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| US11730726B2 (en) | 2018-07-11 | 2023-08-22 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Dimeric immuno-modulatory compounds against cereblon-based mechanisms |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| CN118955473A (zh) * | 2018-10-15 | 2024-11-15 | 紐力克斯治疗公司 | 通过泛素蛋白酶体途径降解btk的双官能化合物 |
| EP4671268A2 (en) | 2019-03-21 | 2025-12-31 | Lonza Sales AG | METHOD FOR PREPARING EXTRACELLULAR VESICLES |
| EP3941528A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Extracellular vesicle conjugates and uses thereof |
| MX2021012285A (es) | 2019-04-09 | 2021-12-15 | Nurix Therapeutics Inc | Compuestos de piperidina 3-sustituidos para inhibicion del protooncogen-b de linfoma de linea b de casitas (cbl-b) y uso de un inhibidor de cbl-b en combinacion con una vacuna contra el cancer y/o con un virus oncolitico. |
| AU2020278592B2 (en) | 2019-05-17 | 2024-10-10 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for Cbl-b inhibition and uses thereof |
| AU2020303696A1 (en) | 2019-06-26 | 2022-01-06 | Nurix Therapeutics, Inc. | Substituted benzyl-triazole compounds for Cbl-b inhibition, and further uses thereof |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| CN114174299B (zh) * | 2019-07-26 | 2024-10-25 | 百济神州有限公司 | 通过btk抑制剂与e3连接酶配体缀合对布鲁顿氏酪氨酸激酶(btk)的降解以及使用方法 |
| EP4034141A1 (en) | 2019-09-24 | 2022-08-03 | Nurix Therapeutics, Inc. | Cbl inhibitors and compositions for expansion of immune cells |
| WO2021077010A1 (en) | 2019-10-17 | 2021-04-22 | Arvinas Operations, Inc. | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| WO2021091575A1 (en) * | 2019-11-08 | 2021-05-14 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| MX2022006672A (es) * | 2019-12-04 | 2022-08-08 | Nurix Therapeutics Inc | Compuestos bifuncionales para la degradacion de btk a traves de la via de proteosomas de ubiquitina. |
| US12441706B2 (en) * | 2019-12-23 | 2025-10-14 | Shanghai Jemincare Pharmaceuticals Co., Ltd. | Protein degradation agent compound preparation method and application |
| EP4126068A4 (en) * | 2020-03-31 | 2024-12-04 | Orum Therapeutics Inc. | CONJUGATES |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| AU2021286738A1 (en) | 2020-06-12 | 2023-01-19 | Jiangxi Jemincare Group Co., Ltd | Phthalazinone compound, and preparation method therefor and medical use thereof |
| CN113943293A (zh) * | 2020-07-16 | 2022-01-18 | 百济神州(北京)生物科技有限公司 | 用于制备作为protac btk降解剂的双官能化合物的方法 |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| MX2023008296A (es) | 2021-01-13 | 2023-09-29 | Monte Rosa Therapeutics Inc | Compuestos de isoindolinona. |
| WO2022217123A2 (en) | 2021-04-08 | 2022-10-13 | Nurix Therapeutics, Inc. | Combination therapies with cbl-b inhibitor compounds |
| CN118388454A (zh) | 2021-04-16 | 2024-07-26 | 阿尔维纳斯运营股份有限公司 | Bcl6蛋白水解的调节剂和其相关使用方法 |
| IL312357A (en) | 2021-10-26 | 2024-06-01 | Nurix Therapeutics Inc | Piperidinylpyrazine-carboxamide compounds for the treatment and prevention of cancer and to restore BTK |
| EP4434992A1 (en) * | 2021-11-18 | 2024-09-25 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Fused imide derivative |
| IL313509A (en) * | 2021-12-30 | 2024-08-01 | Beigene Switzerland Gmbh | Reduction of proton tyrosine kinase (btk) by fusing btk inhibitors with an e3 ligase ligand and methods of use |
| JP2023140319A (ja) | 2022-03-22 | 2023-10-04 | アッヴィ・インコーポレイテッド | ブルトン型チロシンキナーゼを分解するためのピリミジン |
| CN114853735B (zh) * | 2022-07-06 | 2022-10-21 | 北京鑫开元医药科技有限公司 | 靶向泛素化降解trk的化合物及其制备方法、组合物和用途 |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| CN116283929B (zh) * | 2023-01-10 | 2023-11-07 | 暨南大学 | 诱导egfr降解的化合物及其应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006223409B2 (en) * | 2005-03-10 | 2011-07-21 | Gilead Connecticut, Inc. | Certain substituted amides, method of making, and method of use thereof |
| CL2008002793A1 (es) | 2007-09-20 | 2009-09-04 | Cgi Pharmaceuticals Inc | Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras |
| AU2009244291B2 (en) * | 2008-05-06 | 2014-02-13 | Genentech, Inc. | Substituted amides, method of making, and use as Btk inhibitors |
| MX2010013478A (es) | 2008-07-02 | 2010-12-20 | Hoffmann La Roche | Nuevas fenilpirazinonas como inhibidores de cinasa. |
| JP2013104687A (ja) * | 2011-11-10 | 2013-05-30 | Carna Biosciences Inc | 新規な蛍光プローブ及びキナーゼ阻害剤の新規スクリーニング方法 |
| WO2013106643A2 (en) * | 2012-01-12 | 2013-07-18 | Yale University | Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase |
| KR20220101015A (ko) * | 2014-04-14 | 2022-07-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3256470B1 (en) * | 2014-12-23 | 2023-07-26 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| KR102616762B1 (ko) * | 2015-03-18 | 2023-12-20 | 아비나스 오퍼레이션스, 인코포레이티드 | 타겟화된 단백질들의 향상된 분해를 위한 화합물들 및 방법들 |
| GB201506871D0 (en) * | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
-
2017
- 2017-11-22 KR KR1020197018105A patent/KR102566109B1/ko active Active
- 2017-11-22 CA CA3042297A patent/CA3042297A1/en active Pending
- 2017-11-22 JP JP2019527335A patent/JP7038712B2/ja active Active
- 2017-11-22 WO PCT/US2017/063011 patent/WO2018098275A1/en not_active Ceased
- 2017-11-22 AU AU2017363252A patent/AU2017363252B2/en not_active Ceased
- 2017-11-22 EP EP17873155.0A patent/EP3544975B1/en active Active
- 2017-11-22 US US16/343,974 patent/US10842878B2/en active Active