JPWO2020198711A5 - - Google Patents
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- Publication number
- JPWO2020198711A5 JPWO2020198711A5 JP2021557652A JP2021557652A JPWO2020198711A5 JP WO2020198711 A5 JPWO2020198711 A5 JP WO2020198711A5 JP 2021557652 A JP2021557652 A JP 2021557652A JP 2021557652 A JP2021557652 A JP 2021557652A JP WO2020198711 A5 JPWO2020198711 A5 JP WO2020198711A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- independently
- halogen
- bond
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 53
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 27
- 150000002367 halogens Chemical class 0.000 claims 27
- 239000001257 hydrogen Substances 0.000 claims 24
- 150000002431 hydrogen Chemical class 0.000 claims 20
- -1 substituted Chemical class 0.000 claims 17
- 125000004093 cyano group Chemical group *C#N 0.000 claims 15
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 125000005647 linker group Chemical group 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000004429 atom Chemical group 0.000 claims 7
- 125000003636 chemical group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 5
- 229910052805 deuterium Inorganic materials 0.000 claims 5
- 239000000651 prodrug Substances 0.000 claims 5
- 229940002612 prodrug Drugs 0.000 claims 5
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 101000941994 Homo sapiens Protein cereblon Proteins 0.000 claims 2
- 102100032783 Protein cereblon Human genes 0.000 claims 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 1
- 102000001307 androgen receptors Human genes 0.000 claims 1
- 108010080146 androgen receptors Proteins 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- ACGUYXCXAPNIKK-UHFFFAOYSA-N hexachlorophene Chemical compound OC1=C(Cl)C=C(Cl)C(Cl)=C1CC1=C(O)C(Cl)=CC(Cl)=C1Cl ACGUYXCXAPNIKK-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962825387P | 2019-03-28 | 2019-03-28 | |
| US62/825,387 | 2019-03-28 | ||
| PCT/US2020/025542 WO2020198711A1 (en) | 2019-03-28 | 2020-03-27 | Androgen receptor modulators and methods for use as proteolysis targeting chimera ligands |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022521825A JP2022521825A (ja) | 2022-04-12 |
| JP2022521825A5 JP2022521825A5 (https=) | 2023-04-04 |
| JPWO2020198711A5 true JPWO2020198711A5 (https=) | 2023-04-04 |
Family
ID=72611232
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021557652A Pending JP2022521825A (ja) | 2019-03-28 | 2020-03-27 | アンドロゲン受容体モジュレーター及びタンパク質分解誘導キメラリガンドとして使用するための方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230078913A1 (https=) |
| EP (1) | EP3946292A4 (https=) |
| JP (1) | JP2022521825A (https=) |
| KR (1) | KR20220004978A (https=) |
| CN (1) | CN114269331A (https=) |
| AU (1) | AU2020247255A1 (https=) |
| CA (1) | CA3134546A1 (https=) |
| IL (1) | IL286723A (https=) |
| MX (1) | MX2021011827A (https=) |
| WO (1) | WO2020198711A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10471023B2 (en) | 2015-03-12 | 2019-11-12 | British Columbia Cancer Agency Branch | Bisphenol ether derivatives and methods for using the same |
| US20170298033A1 (en) | 2016-04-15 | 2017-10-19 | The University Of British Columbia | Bisphenol derivatives and their use as androgen receptor activity modulators |
| WO2019226991A1 (en) | 2018-05-25 | 2019-11-28 | Essa Pharma, Inc. | Androgen receptor modulators and methods for their use |
| WO2020198712A1 (en) | 2019-03-28 | 2020-10-01 | Essa Pharma, Inc. | Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof |
| CA3165168A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| AU2021255723A1 (en) | 2020-04-17 | 2022-12-08 | Essa Pharma, Inc. | Solid forms of an N-terminal domain androgen receptor inhibitor and uses thereof |
| CN115996918A (zh) | 2020-05-09 | 2023-04-21 | 阿尔维纳斯运营股份有限公司 | 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型 |
| CN116529248B (zh) * | 2020-11-25 | 2025-10-17 | 西藏海思科制药有限公司 | 一种苯环衍生物及其组合物和药学上的应用 |
| EP4023649A1 (en) | 2020-12-30 | 2022-07-06 | Industrial Technology Research Institute | Androgen receptor binding bifunctional molecules |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| CA3227457A1 (en) * | 2021-07-30 | 2023-02-02 | Wu Du | Bifunctional chimeric heterocyclic compound and use thereof as androgen receptor degrader |
| WO2023046283A1 (en) * | 2021-09-22 | 2023-03-30 | Fundació Institut De Recerca Biomèdica (Irb Barcelona) | Compounds and their use in a method for modulating ar (androgen receptor) transcriptional activity |
| JP2024543129A (ja) | 2021-11-25 | 2024-11-19 | 江蘇恒瑞医薬股▲ふん▼有限公司 | アンドロゲン受容体タンパク質の標的分解のためのキメラ化合物、その調製方法及びその医薬的使用 |
| AU2022424178A1 (en) | 2021-12-30 | 2024-07-11 | Beone Medicines I Gmbh | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| CN119301111A (zh) | 2022-03-24 | 2025-01-10 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物 |
| WO2024006207A1 (en) * | 2022-06-26 | 2024-01-04 | Essa Pharma Inc. | An n-terminal domain androgen receptor inhibitor and uses thereof |
| US12496301B2 (en) | 2023-12-08 | 2025-12-16 | Arvinas Operations, Inc. | Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy |
| CN119684303A (zh) * | 2023-12-28 | 2025-03-25 | 上海超阳药业有限公司 | 一种双功能可降解雄激素受体的杂环化合物及其应用 |
| WO2025152998A1 (en) * | 2024-01-17 | 2025-07-24 | Foshan Ionova Biotherapeutics Co., Inc. | Compounds for the targeted degradation of androgen receptor and use thereof |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101516835A (zh) * | 2006-07-19 | 2009-08-26 | 俄亥俄州立大学研究基金会 | 选择性雄激素受体调节剂、它们的类似物和衍生物以及它们的用途 |
| MA37975B2 (fr) * | 2012-09-11 | 2021-03-31 | Genzyme Corp | Inhibiteurs de synthase de glucosylcéramide |
| US20180228907A1 (en) * | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| JP6884100B2 (ja) * | 2015-01-13 | 2021-06-09 | ブリティッシュ コロンビア キャンサー エージェンシー ブランチ | がんの画像化及び治療用のヘテロ環式化合物ならびにそれらの使用方法 |
| US10471023B2 (en) * | 2015-03-12 | 2019-11-12 | British Columbia Cancer Agency Branch | Bisphenol ether derivatives and methods for using the same |
| WO2017185031A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| JP2020514252A (ja) * | 2016-12-08 | 2020-05-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Ｃｄｋ４／６媒介性がんを治療するための組成物および方法 |
| MX2019007646A (es) * | 2016-12-23 | 2019-09-06 | Arvinas Operations Inc | Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. |
-
2020
- 2020-03-27 AU AU2020247255A patent/AU2020247255A1/en not_active Abandoned
- 2020-03-27 KR KR1020217034497A patent/KR20220004978A/ko not_active Ceased
- 2020-03-27 EP EP20778151.9A patent/EP3946292A4/en not_active Withdrawn
- 2020-03-27 WO PCT/US2020/025542 patent/WO2020198711A1/en not_active Ceased
- 2020-03-27 CN CN202080036492.3A patent/CN114269331A/zh active Pending
- 2020-03-27 MX MX2021011827A patent/MX2021011827A/es unknown
- 2020-03-27 CA CA3134546A patent/CA3134546A1/en active Pending
- 2020-03-27 JP JP2021557652A patent/JP2022521825A/ja active Pending
- 2020-03-27 US US17/599,341 patent/US20230078913A1/en not_active Abandoned
-
2021
- 2021-09-26 IL IL286723A patent/IL286723A/en unknown