JP2019535746A5 - - Google Patents
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- JP2019535746A5 JP2019535746A5 JP2019527358A JP2019527358A JP2019535746A5 JP 2019535746 A5 JP2019535746 A5 JP 2019535746A5 JP 2019527358 A JP2019527358 A JP 2019527358A JP 2019527358 A JP2019527358 A JP 2019527358A JP 2019535746 A5 JP2019535746 A5 JP 2019535746A5
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- JP
- Japan
- Prior art keywords
- alkyl
- independently
- cancer
- haloalkyl
- formula
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 65
- 150000001875 compounds Chemical class 0.000 claims description 61
- 230000001588 bifunctional Effects 0.000 claims description 58
- 125000001188 haloalkyl group Chemical group 0.000 claims description 32
- 229910052736 halogen Inorganic materials 0.000 claims description 25
- 150000002367 halogens Chemical class 0.000 claims description 25
- 125000003545 alkoxy group Chemical group 0.000 claims description 23
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 19
- 230000027455 binding Effects 0.000 claims description 18
- 239000003446 ligand Substances 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 229910052717 sulfur Chemical group 0.000 claims description 14
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
- 125000004429 atoms Chemical group 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000005842 heteroatoms Chemical group 0.000 claims description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000011780 sodium chloride Substances 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 7
- 206010017758 Gastric cancer Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 201000011549 stomach cancer Diseases 0.000 claims description 6
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims description 5
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 229910052757 nitrogen Chemical group 0.000 claims description 4
- 125000004043 oxo group Chemical group O=* 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 206010005949 Bone cancer Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010073071 Hepatocellular carcinoma Diseases 0.000 claims description 2
- 206010024324 Leukaemias Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010025310 Other lymphomas Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer 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
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 2
- 201000005216 brain cancer Diseases 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 230000002062 proliferating Effects 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 201000000053 blastoma Diseases 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 0 CC(C)(*)[C@](C(N(CCC1)[C@]1C(NCc(cc1)ccc1-c1c(C)nc[s]1)=*)=O)N*(C)=C Chemical compound CC(C)(*)[C@](C(N(CCC1)[C@]1C(NCc(cc1)ccc1-c1c(C)nc[s]1)=*)=O)N*(C)=C 0.000 description 2
- 229910052740 iodine Inorganic materials 0.000 description 2
- NFLUBBOGFHPRKD-UHFFFAOYSA-N CCC(C)(C=C)NCC Chemical compound CCC(C)(C=C)NCC NFLUBBOGFHPRKD-UHFFFAOYSA-N 0.000 description 1
- GGZXJZZUBNDABX-SSDOTTSWSA-N CCCN(CC1)C[C@@H]1O Chemical compound CCCN(CC1)C[C@@H]1O GGZXJZZUBNDABX-SSDOTTSWSA-N 0.000 description 1
- VLLRBPIIWLQFCD-UHFFFAOYSA-N Cc1c(-c2ccc(CNC)cc2)[s]cn1 Chemical compound Cc1c(-c2ccc(CNC)cc2)[s]cn1 VLLRBPIIWLQFCD-UHFFFAOYSA-N 0.000 description 1
- ONYGKYUQGHVRKU-RXMQYKEDSA-N NNCC(N(CC1)C[C@@H]1O)=O Chemical compound NNCC(N(CC1)C[C@@H]1O)=O ONYGKYUQGHVRKU-RXMQYKEDSA-N 0.000 description 1
- 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 Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662425211P | 2016-11-22 | 2016-11-22 | |
| US62/425,211 | 2016-11-22 | ||
| PCT/US2017/063027 WO2018098288A1 (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 (2)
| Publication Number | Publication Date |
|---|---|
| JP2019535746A JP2019535746A (ja) | 2019-12-12 |
| JP2019535746A5 true JP2019535746A5 (US07943609-20110517-C00101.png) | 2020-12-24 |
Family
ID=62195636
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019527358A Pending JP2019535746A (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)
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017117474A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| WO2018098288A1 (en) * | 2016-11-22 | 2018-05-31 | 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 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| CN109422752B (zh) * | 2017-09-03 | 2023-04-07 | 上海美志医药科技有限公司 | 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 |
| EP3746426A4 (en) * | 2018-01-29 | 2021-12-29 | 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 |
| WO2019170150A1 (zh) * | 2018-03-09 | 2019-09-12 | 上海科技大学 | 蛋白降解靶向bcr-abl化合物及其抗肿瘤应用 |
| WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| US20240108747A1 (en) | 2019-03-21 | 2024-04-04 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
| CN110204532B (zh) * | 2019-05-15 | 2022-03-08 | 浙江工业大学 | 一种靶向egfr蛋白降解的化合物及其制备方法和应用 |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| WO2021023233A1 (zh) * | 2019-08-05 | 2021-02-11 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| CN114521196A (zh) * | 2019-09-16 | 2022-05-20 | 诺华股份有限公司 | 双官能团降解剂及其使用方法 |
| WO2021058017A1 (en) * | 2019-09-29 | 2021-04-01 | Beigene, Ltd. | Degradation of androgen receptor (ar) by conjugation of ar antagonists with e3 ligase ligand and methods of use |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| CN114478532A (zh) * | 2020-10-26 | 2022-05-13 | 上海美志医药科技有限公司 | 靶向降解Btk的化合物及其抗肿瘤用途 |
| WO2022143856A1 (en) * | 2020-12-31 | 2022-07-07 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| WO2022152821A1 (en) | 2021-01-13 | 2022-07-21 | Monte Rosa Therapeutics Ag | Isoindolinone 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 |
| WO2023137225A1 (en) * | 2022-01-17 | 2023-07-20 | Newave Pharmaceutical Inc. | Btk degrader |
| WO2024054591A1 (en) | 2022-09-07 | 2024-03-14 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| WO2015106292A1 (en) * | 2014-01-13 | 2015-07-16 | Coferon, Inc. | Bcr-abl tyrosine-kinase ligands capable of dimerizing in an aqueous solution, and methods of using same |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| UY36660A (es) | 2015-04-30 | 2016-11-30 | Bayer Pharma AG | Combinaciones de inhibidores de irak4 |
| JP2018531983A (ja) | 2015-11-02 | 2018-11-01 | イエール ユニバーシティ | タンパク質分解誘導キメラ化合物ならびにその調製方法および使用方法 |
| WO2017117474A1 (en) * | 2015-12-30 | 2017-07-06 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds for her3 degradation and methods of use |
| WO2018098288A1 (en) * | 2016-11-22 | 2018-05-31 | 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 |
-
2017
- 2017-11-22 WO PCT/US2017/063027 patent/WO2018098288A1/en unknown
- 2017-11-22 EP EP17873156.8A patent/EP3544959A4/en not_active Withdrawn
- 2017-11-22 KR KR1020197018106A patent/KR20190080956A/ko unknown
- 2017-11-22 AU AU2017363265A patent/AU2017363265B2/en active Active
- 2017-11-22 US US16/343,979 patent/US10925967B2/en active Active
- 2017-11-22 CA CA3042294A patent/CA3042294A1/en active Pending
- 2017-11-22 JP JP2019527358A patent/JP2019535746A/ja active Pending
-
2020
- 2020-12-16 US US17/123,955 patent/US11730818B2/en active Active
-
2023
- 2023-06-27 US US18/214,825 patent/US20230338551A1/en active Pending
