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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- 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 (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3017740A1 (en) | 2016-03-16 | 2017-09-21 | Pearlie BURNETTE | Small molecules against cereblon to enhance effector t cell function |
| PT3500299T (pt) | 2016-08-19 | 2024-02-21 | Beigene Switzerland Gmbh | Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | 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 |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| BR122023024103A2 (pt) * | 2018-10-15 | 2024-02-20 | Nurix Therapeutics, Inc. | Compostos bifuncionais para degradação de btk por meio da via de proteossoma de ubiquitina, composição farmacêutica compreendendo os mesmos, e seus usos |
| US20240108747A1 (en) | 2019-03-21 | 2024-04-04 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
| US12233356B2 (en) | 2019-03-21 | 2025-02-25 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| BR112021019722A2 (pt) | 2019-04-09 | 2021-12-14 | Nurix Therapeutics Inc | Compostos de piperidina 3-substituídos para inibição de cbl-b, e uso de inibidor de cbl-b em combinação com vacina contra câncer e/ou vírus oncolítico |
| EP3969447A1 (en) | 2019-05-17 | 2022-03-23 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof |
| JP2022538174A (ja) | 2019-06-26 | 2022-08-31 | ニューリックス セラピューティクス，インコーポレイテッド | Ｃｂｌ－ｂ阻害のための置換ベンジル－トリアゾール化合物、及びそのさらなる使用 |
| US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
| WO2021018018A1 (en) * | 2019-07-26 | 2021-02-04 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inidbitors with e3 ligase ligand and methods of use |
| WO2021061870A1 (en) | 2019-09-24 | 2021-04-01 | Nurix Therapeutics, Inc. | Cbl inhibitors and compositions for expansion of immune cells |
| AU2020368542B2 (en) | 2019-10-17 | 2024-02-29 | 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 |
| ES3033520T3 (en) * | 2019-12-04 | 2025-08-05 | Nurix Therapeutics Inc | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| PE20230114A1 (es) * | 2019-12-23 | 2023-01-27 | Shanghai Jemincare Pharmaceuticals Co Ltd | Metodo y aplicacion de preparacion de compuesto como agente de degradacion de proteinas |
| WO2021198966A1 (en) * | 2020-03-31 | 2021-10-07 | Orum Therapeutics, Inc. | Conjugates |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| CN116082311B (zh) | 2020-06-12 | 2025-04-25 | 上海济煜医药科技有限公司 | 酞嗪酮类化合物及其制备方法和医药用途 |
| 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 |
| EP4204418A1 (en) | 2020-08-28 | 2023-07-05 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| WO2022152821A1 (en) | 2021-01-13 | 2022-07-21 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| KR20230167407A (ko) | 2021-04-08 | 2023-12-08 | 누릭스 테라퓨틱스 인코포레이티드 | Cbl-b 억제제 화합물을 이용한 조합 요법 |
| EP4323352A1 (en) | 2021-04-16 | 2024-02-21 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| 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 |
| 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 |
| TW202432544A (zh) | 2022-09-07 | 2024-08-16 | 美商亞文納營運公司 | 快速加速纖維肉瘤降解化合物及相關使用方法 |
| 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 |
|---|---|---|---|---|
| CA2601628C (en) | 2005-03-10 | 2014-05-13 | Cgi Pharmaceuticals, 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 |
| WO2009137596A1 (en) * | 2008-05-06 | 2009-11-12 | Cgi Pharmaceuticals, Inc. | Substituted amides, method of making, and use as btk inhibitors |
| PL2300459T3 (pl) * | 2008-07-02 | 2013-10-31 | Hoffmann La Roche | Nowe fenylopirazynony jako inhibitory kinazy |
| 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 |
| KR102438072B1 (ko) | 2012-01-12 | 2022-08-31 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| KR20250127179A (ko) | 2014-04-14 | 2025-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | 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 | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| HK1249058A1 (zh) | 2015-03-18 | 2018-10-26 | Arvinas, Inc. | 用於增强靶向蛋白质降解的化合物和方法 |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
-
2017
- 2017-11-22 WO PCT/US2017/063011 patent/WO2018098275A1/en not_active Ceased
- 2017-11-22 CA CA3042297A patent/CA3042297A1/en active Pending
- 2017-11-22 US US16/343,974 patent/US10842878B2/en active Active
- 2017-11-22 JP JP2019527335A patent/JP7038712B2/ja active Active
- 2017-11-22 KR KR1020197018105A patent/KR102566109B1/ko active Active
- 2017-11-22 EP EP17873155.0A patent/EP3544975B1/en active Active
- 2017-11-22 AU AU2017363252A patent/AU2017363252B2/en not_active Ceased