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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- 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 (https=) | 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 (https=) |
| EP (3) | EP3660004B1 (https=) |
| JP (6) | JP7009466B2 (https=) |
| KR (3) | KR20250044800A (https=) |
| CN (2) | CN110506039A (https=) |
| AU (6) | AU2017341723B2 (https=) |
| CA (1) | CA3038979A1 (https=) |
| CO (1) | CO2019003642A2 (https=) |
| CY (1) | CY1126053T1 (https=) |
| DK (2) | DK3526202T3 (https=) |
| ES (2) | ES2945224T3 (https=) |
| FI (2) | FI3660004T3 (https=) |
| HR (2) | HRP20250181T1 (https=) |
| HU (2) | HUE070289T2 (https=) |
| IL (4) | IL283761B2 (https=) |
| LT (2) | LT3526202T (https=) |
| MX (3) | MX2019004278A (https=) |
| PL (2) | PL3526202T3 (https=) |
| PT (2) | PT3526202T (https=) |
| RS (2) | RS66647B1 (https=) |
| SI (2) | SI3660004T1 (https=) |
| SM (1) | SMT202300152T1 (https=) |
| WO (1) | WO2018071606A1 (https=) |
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| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| RU2738833C9 (ru) * | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| EP3319944A4 (en) | 2015-07-10 | 2019-04-24 | Arvinas, Inc. | MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS |
| US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| BR112018068906A2 (pt) | 2016-03-16 | 2019-01-22 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | composição, método, método de redução de risco, prevenção ou tratamento de um indivíduo que tem uma doença ou distúrbio autoimune, método de indução de degradação de uma proteína-alvo numa célula, método para reduzir o risco, prevenir ou tratar um estado da doença ou afecção num paciente em que a atividade proteica desregulada é responsável pelo referido estado da doença ou afecção, método para reduzir o risco, prevenir ou tratar câncer num indivíduo e método de tratamento de uma doença ou distúrbio genético num indivíduo |
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| KR102119465B1 (ko) | 2017-09-20 | 2020-06-08 | (주)아모레퍼시픽 | 트리메톡시 페닐 화합물 및 그를 포함하는 발모 또는 육모 촉진용 조성물 |
| WO2020047487A1 (en) | 2018-08-31 | 2020-03-05 | The Regents Of The University Of California | Methods for treating cancer with rorgamma inhibitors and statins |
| WO2020211822A1 (zh) | 2019-04-18 | 2020-10-22 | 成都海创药业有限公司 | 一类靶向降解雄激素受体的双功能嵌合体杂环化合物及其用途 |
| EP4034114A4 (en) | 2019-09-23 | 2023-07-26 | Accutar Biotechnology Inc. | NEW UREAES HAVING ANDROGEN RECEPTOR DEGRADING ACTIVITY AND THEIR USES |
| KR20220087482A (ko) | 2019-10-22 | 2022-06-24 | 아비나스 오퍼레이션스, 인코포레이티드 | 전립선암 치료 방법 |
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| JP2023547084A (ja) * | 2020-10-21 | 2023-11-09 | アルビナス・オペレーションズ・インコーポレイテッド | アンドロゲン受容体タンパク質の標的分解のための化合物および方法 |
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| JP2023552818A (ja) * | 2020-12-11 | 2023-12-19 | アルビナス・オペレーションズ・インコーポレイテッド | 前立腺癌を治療する方法 |
| US20250248999A1 (en) | 2022-04-21 | 2025-08-07 | Arvinas Operations, Inc. | Bavdegalutamide and combinations thereof for use in treating prostate cancer |
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