JP2022046497A5 - - Google Patents
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- JP2022046497A5 JP2022046497A5 JP2021198476A JP2021198476A JP2022046497A5 JP 2022046497 A5 JP2022046497 A5 JP 2022046497A5 JP 2021198476 A JP2021198476 A JP 2021198476A JP 2021198476 A JP2021198476 A JP 2021198476A JP 2022046497 A5 JP2022046497 A5 JP 2022046497A5
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- alkyl
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- 150000001875 compounds Chemical class 0.000 claims description 51
- 150000003839 salts Chemical class 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 description 59
- 125000001475 halogen functional group Chemical group 0.000 description 20
- 230000001588 bifunctional effect Effects 0.000 description 19
- 125000003118 aryl group Chemical group 0.000 description 18
- 125000001072 heteroaryl group Chemical group 0.000 description 16
- 125000005647 linker group Chemical group 0.000 description 16
- 229910052799 carbon Inorganic materials 0.000 description 15
- 125000003545 alkoxy group Chemical group 0.000 description 14
- 125000000753 cycloalkyl group Chemical group 0.000 description 14
- 125000000623 heterocyclic group Chemical group 0.000 description 13
- 229910052760 oxygen Inorganic materials 0.000 description 13
- 239000000126 substance Substances 0.000 description 12
- 229910052739 hydrogen Inorganic materials 0.000 description 10
- 125000004429 atom Chemical group 0.000 description 9
- 229910052717 sulfur Inorganic materials 0.000 description 9
- 125000004122 cyclic group Chemical group 0.000 description 8
- 230000000707 stereoselective effect Effects 0.000 description 8
- -1 biheterocyclic Chemical group 0.000 description 7
- 125000005842 heteroatom Chemical group 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 229910052736 halogen Inorganic materials 0.000 description 6
- 150000002367 halogens Chemical class 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 6
- 125000003636 chemical group Chemical group 0.000 description 5
- 229910052757 nitrogen Inorganic materials 0.000 description 5
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 description 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 4
- 102100032783 Protein cereblon Human genes 0.000 description 4
- 102000001307 androgen receptors Human genes 0.000 description 4
- 108010080146 androgen receptors Proteins 0.000 description 4
- 125000000524 functional group Chemical group 0.000 description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 3
- 150000001408 amides Chemical class 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- AEOCXXJPGCBFJA-UHFFFAOYSA-N ethionamide Chemical compound CCC1=CC(C(N)=S)=CC=N1 AEOCXXJPGCBFJA-UHFFFAOYSA-N 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 150000003949 imides Chemical class 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 2
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 description 2
- 150000001204 N-oxides Chemical class 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 102000001708 Protein Isoforms Human genes 0.000 description 2
- 108010029485 Protein Isoforms Proteins 0.000 description 2
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 description 2
- 125000001931 aliphatic group Chemical group 0.000 description 2
- 239000002246 antineoplastic agent Substances 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 125000005841 biaryl group Chemical group 0.000 description 2
- 125000002619 bicyclic group Chemical group 0.000 description 2
- 239000012867 bioactive agent Substances 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 229960004942 lenalidomide Drugs 0.000 description 2
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 description 2
- 125000005544 phthalimido group Chemical group 0.000 description 2
- 229960000688 pomalidomide Drugs 0.000 description 2
- UVSMNLNDYGZFPF-UHFFFAOYSA-N pomalidomide Chemical compound O=C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O UVSMNLNDYGZFPF-UHFFFAOYSA-N 0.000 description 2
- 229960003433 thalidomide Drugs 0.000 description 2
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- 208000027747 Kennedy disease Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 description 1
- 125000002723 alicyclic group Chemical group 0.000 description 1
- 125000002877 alkyl aryl group Chemical group 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 150000001721 carbon Chemical class 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000000155 isotopic effect Effects 0.000 description 1
- 238000000370 laser capture micro-dissection Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022210062A JP7590399B2 (ja) | 2016-10-11 | 2022-12-27 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2024198850A JP2025026916A (ja) | 2016-10-11 | 2024-11-14 | アンドロゲン受容体の標的分解のための化合物および方法 |
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662406888P | 2016-10-11 | 2016-10-11 | |
| US62/406,888 | 2016-10-11 | ||
| US201762528385P | 2017-07-03 | 2017-07-03 | |
| US62/528,385 | 2017-07-03 | ||
| JP2019519731A JP7009466B2 (ja) | 2016-10-11 | 2017-10-11 | アンドロゲン受容体の標的分解のための化合物および方法 |
| PCT/US2017/056234 WO2018071606A1 (en) | 2016-10-11 | 2017-10-11 | Compounds and methods for the targeted degradation of androgen receptor |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019519731A Division JP7009466B2 (ja) | 2016-10-11 | 2017-10-11 | アンドロゲン受容体の標的分解のための化合物および方法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022210062A Division JP7590399B2 (ja) | 2016-10-11 | 2022-12-27 | アンドロゲン受容体の標的分解のための化合物および方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022046497A JP2022046497A (ja) | 2022-03-23 |
| JP2022046497A5 true JP2022046497A5 (enExample) | 2022-11-09 |
| JP7203936B2 JP7203936B2 (ja) | 2023-01-13 |
Family
ID=61830620
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019519731A Active JP7009466B2 (ja) | 2016-10-11 | 2017-10-11 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2020032037A Active JP6972210B2 (ja) | 2016-10-11 | 2020-02-27 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2021113423A Active JP7178532B2 (ja) | 2016-10-11 | 2021-07-08 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2021198476A Active JP7203936B2 (ja) | 2016-10-11 | 2021-12-07 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2022210062A Active JP7590399B2 (ja) | 2016-10-11 | 2022-12-27 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2024198850A Pending JP2025026916A (ja) | 2016-10-11 | 2024-11-14 | アンドロゲン受容体の標的分解のための化合物および方法 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019519731A Active JP7009466B2 (ja) | 2016-10-11 | 2017-10-11 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2020032037A Active JP6972210B2 (ja) | 2016-10-11 | 2020-02-27 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2021113423A Active JP7178532B2 (ja) | 2016-10-11 | 2021-07-08 | アンドロゲン受容体の標的分解のための化合物および方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022210062A Active JP7590399B2 (ja) | 2016-10-11 | 2022-12-27 | アンドロゲン受容体の標的分解のための化合物および方法 |
| JP2024198850A Pending JP2025026916A (ja) | 2016-10-11 | 2024-11-14 | アンドロゲン受容体の標的分解のための化合物および方法 |
Country Status (23)
| Country | Link |
|---|---|
| US (8) | US10584101B2 (enExample) |
| EP (3) | EP3660004B1 (enExample) |
| JP (6) | JP7009466B2 (enExample) |
| KR (3) | KR102173463B1 (enExample) |
| CN (2) | CN110506039A (enExample) |
| AU (6) | AU2017341723B2 (enExample) |
| CA (1) | CA3038979A1 (enExample) |
| CO (1) | CO2019003642A2 (enExample) |
| CY (1) | CY1126053T1 (enExample) |
| DK (2) | DK3526202T3 (enExample) |
| ES (2) | ES3023040T3 (enExample) |
| FI (2) | FI3526202T3 (enExample) |
| HR (2) | HRP20250181T1 (enExample) |
| HU (2) | HUE070289T2 (enExample) |
| IL (4) | IL265806B2 (enExample) |
| LT (2) | LT3660004T (enExample) |
| MX (3) | MX2019004278A (enExample) |
| PL (2) | PL3660004T3 (enExample) |
| PT (2) | PT3526202T (enExample) |
| RS (2) | RS64208B1 (enExample) |
| SI (2) | SI3526202T1 (enExample) |
| SM (1) | SMT202300152T1 (enExample) |
| WO (1) | WO2018071606A1 (enExample) |
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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 |
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| EP4034114A4 (en) | 2019-09-23 | 2023-07-26 | Accutar Biotechnology Inc. | Novel ureas having androgen receptor degradation activity and uses thereof |
| US20210113557A1 (en) * | 2019-10-22 | 2021-04-22 | Arvinas Operations, Inc. | Methods of treating prostate cancer |
| 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 |
| KR20230015934A (ko) | 2020-05-12 | 2023-01-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 전립선암 치료 방법 |
| WO2022087125A1 (en) * | 2020-10-21 | 2022-04-28 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor protein |
| EP4240733A1 (en) | 2020-11-06 | 2023-09-13 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor and associated methods of use |
| US20220184078A1 (en) * | 2020-12-11 | 2022-06-16 | Arvinas Operations, Inc. | Methods of treating prostate cancer |
| WO2023205481A1 (en) | 2022-04-21 | 2023-10-26 | Arvinas Operations, Inc. | A combination for use in treating prostate cancer comprising arv-100 and abiraterone |
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2017
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