JP2018502925A5 - - Google Patents
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- JP2018502925A5 JP2018502925A5 JP2017556797A JP2017556797A JP2018502925A5 JP 2018502925 A5 JP2018502925 A5 JP 2018502925A5 JP 2017556797 A JP2017556797 A JP 2017556797A JP 2017556797 A JP2017556797 A JP 2017556797A JP 2018502925 A5 JP2018502925 A5 JP 2018502925A5
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- Prior art keywords
- alkyl
- optionally substituted
- halo
- independently
- substituted
- 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 140
- 125000005843 halogen group Chemical group 0.000 claims description 70
- 229910052799 carbon Inorganic materials 0.000 claims description 36
- 150000001875 compounds Chemical class 0.000 claims description 36
- 125000003545 alkoxy group Chemical group 0.000 claims description 34
- 125000003118 aryl group Chemical group 0.000 claims description 32
- 125000001072 heteroaryl group Chemical group 0.000 claims description 32
- 125000005842 heteroatom Chemical group 0.000 claims description 26
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 22
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 22
- 229910052760 oxygen Inorganic materials 0.000 claims description 22
- 230000001588 bifunctional effect Effects 0.000 claims description 20
- 125000004429 atom Chemical group 0.000 claims description 16
- 125000004122 cyclic group Chemical group 0.000 claims description 16
- 125000001188 haloalkyl group Chemical group 0.000 claims description 16
- 125000002723 alicyclic group Chemical group 0.000 claims description 14
- 125000003342 alkenyl group Chemical group 0.000 claims description 14
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- 229910052717 sulfur Inorganic materials 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 10
- 102000001307 androgen receptors Human genes 0.000 claims description 10
- 108010080146 androgen receptors Proteins 0.000 claims description 10
- -1 hydroxylprolyl moiety Chemical group 0.000 claims description 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 10
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 8
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 8
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 8
- 125000005647 linker group Chemical group 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- PIGFYZPCRLYGLF-UHFFFAOYSA-N Aluminum nitride Chemical compound [Al]#N PIGFYZPCRLYGLF-UHFFFAOYSA-N 0.000 claims description 4
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 claims description 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 4
- 125000005129 aryl carbonyl group Chemical group 0.000 claims description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- VLJNHYLEOZPXFW-UHFFFAOYSA-N pyrrolidine-2-carboxamide Chemical compound NC(=O)C1CCCN1 VLJNHYLEOZPXFW-UHFFFAOYSA-N 0.000 claims description 4
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 3
- XXTZLIAFLLLNOR-USAYTKQKSA-N (2S,4R)-1-[(2S)-2-amino-3,3-dimethylbutanoyl]-N-[(4-chlorophenyl)methyl]-4-hydroxypyrrolidine-2-carboxamide hydrochloride Chemical compound Cl.CC(C)(C)[C@H](N)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(Cl)cc1 XXTZLIAFLLLNOR-USAYTKQKSA-N 0.000 claims description 2
- PAQNZLPEBCDUAS-GBEOHXTHSA-N (2S,4R)-1-[(2S)-2-amino-3,3-dimethylbutanoyl]-N-[(4-cyanophenyl)methyl]-4-hydroxypyrrolidine-2-carboxamide hydrochloride Chemical compound Cl.CC(C)(C)[C@H](N)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(cc1)C#N PAQNZLPEBCDUAS-GBEOHXTHSA-N 0.000 claims description 2
- ZLOXMSNKPDWMEF-ZIFCJYIRSA-N (2s,4r)-1-[(2s)-2-amino-3,3-dimethylbutanoyl]-4-hydroxy-n-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide Chemical compound N1=CSC(C=2C=CC(CNC(=O)[C@H]3N(C[C@H](O)C3)C(=O)[C@@H](N)C(C)(C)C)=CC=2)=C1C ZLOXMSNKPDWMEF-ZIFCJYIRSA-N 0.000 claims description 2
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- 208000027747 Kennedy disease Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 239000012867 bioactive agent Substances 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 2
- 230000000155 isotopic effect Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 239000000651 prodrug Substances 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562105210P | 2015-01-20 | 2015-01-20 | |
| US62/105,210 | 2015-01-20 | ||
| PCT/US2016/014187 WO2016118666A1 (en) | 2015-01-20 | 2016-01-20 | Compounds and methods for the targeted degradation of the androgen receptor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020046636A Division JP2020111590A (ja) | 2015-01-20 | 2020-03-17 | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018502925A JP2018502925A (ja) | 2018-02-01 |
| JP2018502925A5 true JP2018502925A5 (enExample) | 2018-09-27 |
| JP6817962B2 JP6817962B2 (ja) | 2021-01-20 |
Family
ID=56417710
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017556797A Active JP6817962B2 (ja) | 2015-01-20 | 2016-01-20 | 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 |
| JP2020046636A Pending JP2020111590A (ja) | 2015-01-20 | 2020-03-17 | 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 |
| JP2022206686A Pending JP2023040072A (ja) | 2015-01-20 | 2022-12-23 | 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020046636A Pending JP2020111590A (ja) | 2015-01-20 | 2020-03-17 | 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 |
| JP2022206686A Pending JP2023040072A (ja) | 2015-01-20 | 2022-12-23 | 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 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US11352351B2 (enExample) |
| EP (1) | EP3247708A4 (enExample) |
| JP (3) | JP6817962B2 (enExample) |
| KR (5) | KR20200052995A (enExample) |
| CN (1) | CN107428734A (enExample) |
| AU (4) | AU2016209349B2 (enExample) |
| BR (1) | BR112017015497A2 (enExample) |
| CA (1) | CA2974367A1 (enExample) |
| HK (2) | HK1245791A1 (enExample) |
| MX (2) | MX390189B (enExample) |
| WO (1) | WO2016118666A1 (enExample) |
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| KR102668696B1 (ko) | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| US10071164B2 (en) | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| 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 |
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