JP2018502925A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- 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.)
- Granted
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP3247708A4 (https=) |
| JP (3) | JP6817962B2 (https=) |
| KR (5) | KR102564925B1 (https=) |
| CN (1) | CN107428734A (https=) |
| AU (4) | AU2016209349B2 (https=) |
| BR (1) | BR112017015497A2 (https=) |
| CA (1) | CA2974367A1 (https=) |
| HK (2) | HK1247204A1 (https=) |
| MX (2) | MX390189B (https=) |
| WO (1) | WO2016118666A1 (https=) |
Families Citing this family (169)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2861066C (en) | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| 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 |
| GB201504314D0 (en) * | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| US10730870B2 (en) * | 2015-03-18 | 2020-08-04 | Arvinas Operations, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017011371A1 (en) | 2015-07-10 | 2017-01-19 | Arvinas, Inc | Mdm2-based modulators of proteolysis and associated methods of use |
| WO2017024318A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| US9963433B2 (en) * | 2016-01-29 | 2018-05-08 | Wayne State University | Anticancer drugs including the chemical structures of an androgen receptor ligand and a histone deacetylase inhibitor |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| EP3445357B1 (en) | 2016-04-22 | 2021-05-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| GB2554071A (en) * | 2016-09-14 | 2018-03-28 | Univ Dundee | Small molecules |
| WO2018053354A1 (en) * | 2016-09-15 | 2018-03-22 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| WO2018071606A1 (en) | 2016-10-11 | 2018-04-19 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3535254A4 (en) * | 2016-11-01 | 2020-06-24 | Cornell University Cornell Center For Technology, Enterprise & Commercialization ("CCTEC") | COMPOUNDS FOR THE DEGRADATION OF MALT1 |
| IL290809B2 (en) | 2016-11-01 | 2024-01-01 | Arvinas Operations Inc | Tau-protein targeting protacs and associated methods of use |
| KR102674902B1 (ko) | 2016-12-01 | 2024-06-14 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| MX2019007646A (es) | 2016-12-23 | 2019-09-06 | Arvinas Operations Inc | Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. |
| CN117510491A (zh) | 2016-12-23 | 2024-02-06 | 阿尔维纳斯运营股份有限公司 | 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法 |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| AU2018211975B2 (en) | 2017-01-26 | 2022-05-26 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| BR112019015484A2 (pt) * | 2017-01-31 | 2020-04-28 | Arvinas Operations Inc | ligantes de cereblon e compostos bifuncionais compreendendo os mesmos |
| EP3580212A4 (en) | 2017-02-08 | 2021-03-17 | Dana Farber Cancer Institute, Inc. | REGULATION OF CHEMERIC ANTIGEN RECEPTORS |
| US10787443B2 (en) | 2017-04-28 | 2020-09-29 | Zamboni Chem Solutions Inc. | RAF-degrading conjugate compounds |
| AU2018261331C1 (en) | 2017-05-01 | 2022-08-04 | Spg Therapeutics, Inc. | Tripartite androgen receptor eliminators, methods and uses thereof |
| CN108976278B (zh) * | 2017-06-05 | 2021-04-06 | 海创药业股份有限公司 | 一种嵌合分子及其制备和应用 |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| SG10202110492YA (en) | 2017-06-22 | 2021-11-29 | Catalyst Biosciences Inc | Modified membrane type serine protease 1 (mtsp-1) polypeptides and methods of use |
| RU2020108515A (ru) * | 2017-07-28 | 2021-08-27 | Эрвинэс Оперейшнс, Инк. | Соединения и способы целевого расщепления андрогенного рецептора |
| CN118206529A (zh) | 2017-09-04 | 2024-06-18 | C4医药公司 | 二氢苯并咪唑酮 |
| CN111278816B (zh) | 2017-09-04 | 2024-03-15 | C4医药公司 | 二氢喹啉酮 |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| AU2018332634A1 (en) * | 2017-09-12 | 2020-04-30 | Agency For Science, Technology And Research | Compounds useful as inhibitors of isoprenylcysteine carboxyl methyltransferase |
| WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
| MX2020003190A (es) | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| CN107987055A (zh) * | 2017-12-19 | 2018-05-04 | 刘秀云 | 硫代咪唑二酮类雄激素受体拮抗剂及其用途 |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| US11220515B2 (en) | 2018-01-26 | 2022-01-11 | Yale University | Imide-based modulators of proteolysis and associated methods of use |
| JP2021519337A (ja) | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Ｉｋａｒｏｓの分解のためのセレブロン結合剤 |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| US20190300521A1 (en) * | 2018-04-01 | 2019-10-03 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| KR20210006356A (ko) | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| WO2019222272A1 (en) | 2018-05-14 | 2019-11-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| WO2019218904A1 (zh) * | 2018-05-18 | 2019-11-21 | 四川科伦博泰生物医药股份有限公司 | 非天然氨基酸类衍生物、其制备方法及用途 |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CN110684046B (zh) * | 2018-07-06 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 一种新的咪唑啉类衍生物的制备方法 |
| US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
| CN110746399B (zh) * | 2018-07-23 | 2022-04-22 | 上海美志医药科技有限公司 | 具有降解雄激素受体活性的化合物 |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| WO2020051235A1 (en) | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| JP7623943B2 (ja) | 2018-11-30 | 2025-01-29 | カイメラ セラピューティクス， インコーポレイテッド | Ｉｒａｋ分解剤およびそれらの使用 |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN109762045A (zh) * | 2018-12-14 | 2019-05-17 | 中山大学附属第一医院 | 一种双靶点构建protac的方法及其用途 |
| US11325889B2 (en) * | 2018-12-19 | 2022-05-10 | Celgene Corporation | Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith |
| PL3897636T3 (pl) | 2018-12-19 | 2025-04-28 | Celgene Corporation | Podstawione związki 3-((3-aminofenylo)amino)piperydyno-2,6-dionu, ich kompozycje i sposoby leczenia nimi |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| WO2020142228A1 (en) * | 2019-01-03 | 2020-07-09 | The Regents Of The University Of Michigan | Androgen receptor protein degraders |
| US11547759B2 (en) | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| JP7555938B2 (ja) * | 2019-01-30 | 2024-09-25 | モンテリノ・セラピューティクス・インコーポレイテッド | アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法 |
| WO2020163823A2 (en) * | 2019-02-08 | 2020-08-13 | University Of Florida Research Foundation, Incorporated | Therapeutic agents and methods of treatment |
| WO2020181232A1 (en) | 2019-03-06 | 2020-09-10 | C4 Therapeutics, Inc. | Heterocyclic compounds for medical treatment |
| WO2020198055A1 (en) * | 2019-03-22 | 2020-10-01 | Yale University | Allosteric bcr-abl proteolysis targeting chimeric compounds |
| US20220177459A1 (en) * | 2019-04-02 | 2022-06-09 | Hinova Pharmaceuticals Inc. | Aromatic amine compound and use thereof in preparation of ar and brd4 dual inhibitors and regulators |
| TWI875749B (zh) | 2019-04-05 | 2025-03-11 | 美商凱麥拉醫療公司 | Stat降解劑及其用途 |
| CN120172958A (zh) | 2019-04-12 | 2025-06-20 | C4医药公司 | Ikaros和aiolos的三环降解物 |
| US12414995B2 (en) | 2019-04-16 | 2025-09-16 | Northwestern University | Bifunctional compounds comprising Apcin-A and their use in the treatment of cancer |
| KR20220004100A (ko) * | 2019-04-18 | 2022-01-11 | 하이노바 파마슈티컬스 인코포레이티드 | 안드로겐 수용체를 표적 분해하는 이중 기능성의 키메라 헤테로 고리 화합물 및 이의 용도 |
| MX2021013531A (es) | 2019-05-05 | 2022-02-11 | Qilu Regor Therapeutics Inc | Inhibidores de cdk. |
| GB201906705D0 (en) | 2019-05-13 | 2019-06-26 | Phoremost Ltd | Methods |
| CN113811333B (zh) | 2019-05-14 | 2024-03-12 | 诺维逊生物股份有限公司 | 靶向抗癌核激素受体的化合物 |
| JP2022533147A (ja) * | 2019-05-17 | 2022-07-21 | ヒノバ ファーマシューティカルズ インコーポレイテッド | 芳香族アミン類のａｒ及びｂｅｔを標的とするタンパク質分解キメラ化合物及び使用 |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| BR112021026517A2 (pt) | 2019-06-28 | 2022-05-10 | Kymera Therapeutics Inc | Degradadores de irak e usos dos mesmos |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| WO2021011868A1 (en) | 2019-07-17 | 2021-01-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CN112390852B (zh) * | 2019-08-14 | 2022-10-18 | 上海济煜医药科技有限公司 | 作为蛋白降解剂的化合物及其制备方法和应用 |
| IL320609A (en) | 2019-08-26 | 2025-07-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| CN112457367B (zh) * | 2019-09-06 | 2022-08-23 | 上海济煜医药科技有限公司 | 作为蛋白降解剂的连环类化合物及其制备方法和应用 |
| CN118085015A (zh) * | 2019-09-06 | 2024-05-28 | 江西济民可信集团有限公司 | 作为蛋白降解剂的并环类化合物及其制备方法和用途 |
| CN118930604A (zh) * | 2019-09-29 | 2024-11-12 | 江西济民可信集团有限公司 | 作为蛋白降解剂杂环类化合物及包含其的药物组合物和应用 |
| CN115397821B (zh) | 2019-10-17 | 2024-09-03 | 阿尔维纳斯运营股份有限公司 | 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子 |
| WO2021097046A1 (en) | 2019-11-13 | 2021-05-20 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| US12551564B2 (en) | 2019-12-10 | 2026-02-17 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| CN110845348A (zh) * | 2019-12-10 | 2020-02-28 | 苏州国匡医药科技有限公司 | 一种arv-110中间体的制备方法 |
| WO2021127190A1 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CA3165168A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| CA3162523A1 (en) | 2019-12-23 | 2021-07-01 | Hongfu LU | Protein degradation agent compound preparation method and application |
| BR112022012410A2 (pt) | 2019-12-23 | 2022-08-30 | Kymera Therapeutics Inc | Degradadores smarca e usos dos mesmos |
| CN113149981B (zh) * | 2020-01-22 | 2022-07-05 | 苏州德亘生物医药有限公司 | 一种降解雄激素受体的蛋白降解靶向嵌合体 |
| AU2021231898A1 (en) | 2020-03-05 | 2022-10-27 | C4 Therapeutics, Inc. | Compounds for targeted degradation of BRD9 |
| CN113387930B (zh) * | 2020-03-11 | 2022-07-12 | 苏州开拓药业股份有限公司 | 一种双官能化合物及其制备方法和用途 |
| US12528785B2 (en) | 2020-03-19 | 2026-01-20 | Kymera Therapeutics, Inc. | MDM2 degraders 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 |
| US20230357249A1 (en) * | 2020-05-14 | 2023-11-09 | The Regents Of The University Of Michigan | Androgen receptor protein degraders with a tricyclic cereblon ligand |
| WO2021236695A1 (en) * | 2020-05-18 | 2021-11-25 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| CN113801098B (zh) | 2020-06-12 | 2023-05-30 | 上海济煜医药科技有限公司 | 酞嗪酮类化合物及其制备方法和医药用途 |
| JP7778095B2 (ja) * | 2020-06-24 | 2025-12-01 | セルジーン コーポレーション | セレブロン結合化合物、その組成物及びそれによる治療方法 |
| KR20230027214A (ko) * | 2020-06-24 | 2023-02-27 | 셀진 코포레이션 | 세레블론 결합 화합물, 이의 조성물, 및 이에 의한 치료 방법 |
| PE20231746A1 (es) * | 2020-06-24 | 2023-11-06 | Celgene Corp | Compuestos de union a cereblon, composiciones de estos y metodos de tratamiento con estos |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| JP7834721B2 (ja) | 2020-08-28 | 2026-03-24 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| CN114163444B (zh) * | 2020-09-11 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用 |
| AR123492A1 (es) | 2020-09-14 | 2022-12-07 | Arvinas Operations Inc | Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógeno |
| CN114181277A (zh) * | 2020-09-15 | 2022-03-15 | 江苏恒瑞医药股份有限公司 | 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用 |
| CN113527273B (zh) * | 2020-10-28 | 2023-08-22 | 中国药科大学 | 靶向泛素化降解hmgcr的化合物或其可药用的盐、制备方法及用途 |
| IL303025A (en) * | 2020-11-18 | 2023-07-01 | Constellation Pharmaceuticals Inc | EZH2 inhibition therapies for prostate cancer with androgen receptor mutation |
| CA3199652A1 (en) * | 2020-11-20 | 2022-05-27 | Matthew Netherton | Compounds and uses thereof |
| CN114262319B (zh) * | 2020-12-01 | 2023-05-05 | 南昌奥瑞药业有限公司 | 一类双功能分子、其制备方法及其应用 |
| WO2022120355A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
| EP4259144A4 (en) | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| EP4023649A1 (en) * | 2020-12-30 | 2022-07-06 | Industrial Technology Research Institute | Androgen receptor binding bifunctional molecules |
| PH12023500015A1 (en) | 2020-12-30 | 2024-03-11 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| JP2024504932A (ja) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス， インコーポレイテッド | イソインドリノン化合物 |
| WO2022174268A1 (en) | 2021-02-15 | 2022-08-18 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| KR20230160299A (ko) | 2021-03-23 | 2023-11-23 | 누베이션 바이오 인크. | 항암 핵 호르몬 수용체 표적화 화합물 |
| CN117279910A (zh) | 2021-04-16 | 2023-12-22 | 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 |
| US12006314B2 (en) | 2021-05-03 | 2024-06-11 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| KR20240017814A (ko) | 2021-05-05 | 2024-02-08 | 바이오젠 엠에이 인코포레이티드 | 브루톤 티로신 키나제의 분해를 표적으로 하는 화합물 |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| WO2022262782A1 (zh) * | 2021-06-17 | 2022-12-22 | 南京明德新药研发有限公司 | 戊二酰亚胺取代的异噁唑稠环化合物及其应用 |
| EP4359407A4 (en) * | 2021-06-25 | 2025-04-30 | Celgene Corporation | CEREBLON-BINDING COMPOUNDS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT USING THEM |
| EP4359404A4 (en) * | 2021-06-25 | 2025-06-04 | Celgene Corporation | Cereblon-binding compounds, compositions thereof and methods of treatment therewith |
| JP2024526192A (ja) * | 2021-06-25 | 2024-07-17 | セルジーン コーポレーション | セレブロン結合化合物、その組成物及びそれによる治療方法 |
| KR20240035526A (ko) | 2021-07-07 | 2024-03-15 | 바이오젠 엠에이 인코포레이티드 | Irak4 단백질의 분해를 표적하는 화합물 |
| WO2023283372A1 (en) | 2021-07-07 | 2023-01-12 | Biogen Ma Inc. | Compounds for targeting degradation of irak4 proteins |
| CN115772210A (zh) * | 2021-09-08 | 2023-03-10 | 苏州开拓药业股份有限公司 | 硫代乙内酰脲化合物或其药用盐的无定形物、晶体、药物组合物、制备方法和用途 |
| US11981672B2 (en) | 2021-09-13 | 2024-05-14 | Montelino Therapeutics Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| WO2023039601A1 (en) * | 2021-09-13 | 2023-03-16 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| TW202330570A (zh) | 2021-09-30 | 2023-08-01 | 日商Ａｓｋａ製藥股份有限公司 | 分解誘導劑 |
| JP2024539280A (ja) | 2021-10-25 | 2024-10-28 | カイメラ セラピューティクス， インコーポレイテッド | Ｔｙｋ２分解剤およびそれらの使用 |
| US12187744B2 (en) | 2021-10-29 | 2025-01-07 | Kymera Therapeutics, Inc. | IRAK4 degraders and synthesis thereof |
| 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 |
| EP4472967A4 (en) | 2022-01-31 | 2026-04-15 | Kymera Therapeutics Inc | Iraqi Degradation Agents and Their Uses |
| JP2025523393A (ja) | 2022-06-06 | 2025-07-23 | シーフォー セラピューティクス， インコーポレイテッド | 二環式置換グルタルイミドセレブロンバインダー |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| TW202417425A (zh) | 2022-06-27 | 2024-05-01 | 美商傳達治療有限公司 | 雌激素受體α降解劑及其使用方法 |
| JP2025528193A (ja) * | 2022-08-19 | 2025-08-26 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | シクロヘキシル基を含む化合物 |
| WO2024050016A1 (en) | 2022-08-31 | 2024-03-07 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
| CN121039116A (zh) * | 2023-02-10 | 2025-11-28 | 南昌奥瑞药业有限公司 | 蛋白降解靶向嵌合体化合物及其用途 |
| WO2024211154A2 (en) * | 2023-04-03 | 2024-10-10 | Wisconsin Alumni Research Foundation | Ferritin-targeting protacs and methods of inducing pyroptosis |
| CN117209433B (zh) * | 2023-08-04 | 2026-02-10 | 南开大学 | 一种以降冰片胺为疏水基团的蛋白降解剂及其制备方法、药物组合物和应用 |
| WO2025049555A1 (en) | 2023-08-31 | 2025-03-06 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| WO2025068704A1 (en) | 2023-09-28 | 2025-04-03 | Phoremost Limited | Methods of protein engineering and functional screening |
| 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 |
| TW202543650A (zh) | 2024-03-08 | 2025-11-16 | 美商海爾達醫療運營公司 | 異雙官能化合物及其在治療疾病中之用途 |
Family Cites Families (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ333903A (en) | 1996-07-24 | 2000-02-28 | Celgene Corp | Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1oxoisoindolines and method of reducing TNF-alpha levels in a mammal |
| CA2287387C (en) | 1997-05-14 | 2010-02-16 | Sloan-Kettering Institute For Cancer Research | Methods and compositions for destruction of selected proteins |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| US6333344B1 (en) | 1999-05-05 | 2001-12-25 | Merck & Co. | Prolines as antimicrobial agents |
| BR0111298A (pt) | 2000-06-28 | 2005-05-10 | Bristol Myers Squibb Co | Moduladores seletivos dos receptores de andrógenos e métodos para identificação, projeto e uso dos mesmos |
| US7041298B2 (en) | 2000-09-08 | 2006-05-09 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| US7208157B2 (en) | 2000-09-08 | 2007-04-24 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| US20030045552A1 (en) | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| CA2432932A1 (en) | 2001-02-16 | 2002-08-29 | Mark A. Scialdone | Angiogenesis-inhibitory tripeptides, compositions and their methods of use |
| HN2002000136A (es) | 2001-06-11 | 2003-07-31 | Basf Ag | Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis |
| TWI263640B (en) * | 2001-12-19 | 2006-10-11 | Bristol Myers Squibb Co | Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function |
| WO2004005248A1 (en) | 2002-07-02 | 2004-01-15 | Novartis Ag | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| US7915293B2 (en) | 2003-05-30 | 2011-03-29 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| US7932382B2 (en) | 2004-01-16 | 2011-04-26 | The Regents Of The University Of Michigan | Conformationally constrained Smac mimetics and the uses thereof |
| WO2005094818A1 (en) | 2004-03-23 | 2005-10-13 | Genentech, Inc. | Azabicyclo-octane inhibitors of iap |
| RS52545B (sr) | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
| BRPI0511350A (pt) | 2004-07-02 | 2007-12-04 | Genentech Inc | composto, métodos de indução da apoptose em uma célula, de sensibilização de uma célula à um sinal apoptótico, de inibição da ligação de uma proteìna iap e de tratamento de uma doença e cáncer e usos de um composto |
| EP1781598A1 (en) | 2004-07-08 | 2007-05-09 | Warner-Lambert Company LLC | Androgen modulators |
| TW200621723A (en) * | 2004-09-09 | 2006-07-01 | Chugai Pharmaceutical Co Ltd | Novel imidazolidine derivative and use thereof |
| MX2007007195A (es) | 2004-12-20 | 2007-10-08 | Genentech Inc | Inhibidores de pirrolidina de iap. |
| ES2456671T3 (es) | 2005-02-25 | 2014-04-23 | Tetralogic Pharmaceuticals Corporation | Inhibidores diméricos de IAP |
| CN100383139C (zh) | 2005-04-07 | 2008-04-23 | 天津和美生物技术有限公司 | 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物 |
| WO2006113942A2 (en) | 2005-04-20 | 2006-10-26 | Schering Corporation | Method of inhibiting cathepsin activity |
| JP4644737B2 (ja) * | 2005-05-13 | 2011-03-02 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | ジアリールヒダントイン化合物 |
| KR20080042158A (ko) | 2005-08-31 | 2008-05-14 | 셀진 코포레이션 | 이소인돌-이미드 화합물과 이를 포함하는 조성물 및 이를이용한 방법 |
| BRPI0708524A2 (pt) | 2006-03-03 | 2011-05-31 | Novartis Ag | compostos de n-formil hidroxilamina |
| WO2007101347A1 (en) | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| CN101032483B (zh) * | 2006-03-09 | 2011-05-04 | 陈德桂 | 调节雄激素受体活性的乙内酰脲衍生物及其应用 |
| KR101456722B1 (ko) | 2006-03-29 | 2014-10-31 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 디아릴티오히단토인 화합물 |
| JP5230610B2 (ja) | 2006-05-05 | 2013-07-10 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | 二価ｓｍａｃ模倣物およびその使用 |
| JP2009544620A (ja) | 2006-07-20 | 2009-12-17 | リガンド・ファーマシューティカルズ・インコーポレイテッド | 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト |
| US20100056495A1 (en) | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| RU2448101C2 (ru) | 2006-08-30 | 2012-04-20 | Селджин Корпорейшн | 5-замещенные изоиндолиновые соединения |
| MX2009001989A (es) | 2006-08-30 | 2009-03-09 | Celgene Corp | Compuestos de isoindolina 5-substituidos. |
| CA2668286C (en) | 2006-11-03 | 2014-09-16 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| WO2008109057A1 (en) | 2007-03-02 | 2008-09-12 | Dana-Farber Cancer Institute, Inc. | Organic compounds and their uses |
| JP5454943B2 (ja) | 2007-04-12 | 2014-03-26 | ジョイアント ファーマスーティカルズ、インク． | 抗癌剤として有用なｓｍａｃ模倣二量体及び三量体 |
| WO2008128171A2 (en) | 2007-04-13 | 2008-10-23 | The Regents Of The University Of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| PE20130150A1 (es) | 2007-04-30 | 2013-02-27 | Genentech Inc | Inhibidores de las iap |
| WO2008144925A1 (en) | 2007-05-30 | 2008-12-04 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| KR20100038108A (ko) | 2007-07-25 | 2010-04-12 | 브리스톨-마이어스 스큅 컴퍼니 | 트리아진 키나제 억제제 |
| CN101820765A (zh) * | 2007-07-31 | 2010-09-01 | 安德鲁科技有限公司 | 包含雄激素受体降解(ard)增强剂的组合物和预防性或治疗性治疗皮肤病与脱发的方法 |
| EP2058312A1 (en) | 2007-11-09 | 2009-05-13 | Universita' degli Studi di Milano | SMAC mimetic compounds as apoptosis inducers |
| PE20110547A1 (es) | 2008-10-29 | 2011-08-04 | Celgene Corp | Compuestos de isoindolina con actividad anticancerigena |
| US20120135089A1 (en) | 2009-03-17 | 2012-05-31 | Stockwell Brent R | E3 ligase inhibitors |
| WO2010141805A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heterocyclic amides as modulators of trpa1 |
| JP2012532929A (ja) | 2009-07-13 | 2012-12-20 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | 二機能性のステープリングされたポリペプチドおよびそれらの使用 |
| AR078793A1 (es) | 2009-10-27 | 2011-12-07 | Orion Corp | Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros |
| EP2784076A1 (en) | 2009-10-28 | 2014-10-01 | Joyant Pharmaceuticals, Inc. | Dimeric SMAC mimetics |
| EP2536706B1 (en) | 2010-02-11 | 2017-06-14 | Celgene Corporation | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| WO2011103202A2 (en) * | 2010-02-16 | 2011-08-25 | Aragon Pharmaceuticals, Inc. | Androgen receptor modulators and uses thereof |
| SG186389A1 (en) | 2010-06-30 | 2013-01-30 | Univ Brandeis | Small-molecule-targeted protein degradation |
| EP2619184B1 (en) | 2010-09-24 | 2018-05-23 | The Regents of the University of Michigan | Deubiquitinase inhibitors and methods for use of the same |
| AU2011338615B2 (en) | 2010-12-07 | 2017-07-27 | Yale University | Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same |
| US20140243282A1 (en) | 2010-12-31 | 2014-08-28 | Satish Reddy Kallam | Methods and compositions for designing novel conjugate therapeutics |
| ES2541295T3 (es) * | 2011-04-21 | 2015-07-17 | Orion Corporation | Carboxamidas que modulan el receptor de andrógenos |
| MX352672B (es) | 2011-09-27 | 2017-12-04 | Amgen Inc | Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer. |
| WO2013067151A1 (en) * | 2011-11-02 | 2013-05-10 | Medivation Prostate Therapeutics, Inc. | Treatment methods using diarylthiohydantoin derivatives |
| WO2013067142A1 (en) * | 2011-11-02 | 2013-05-10 | Medivation Technologies, Inc. | Compounds and treatment methods |
| WO2013071039A1 (en) | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| WO2013071035A1 (en) | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| CA2861066C (en) * | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| US20150119435A1 (en) | 2012-05-11 | 2015-04-30 | Yale University | Compounds useful for promoting protein degradation and methods using same |
| EP2855483B1 (en) | 2012-05-24 | 2017-10-25 | Novartis AG | Pyrrolopyrrolidinone compounds |
| NZ631477A (en) | 2012-05-30 | 2016-12-23 | Hoffmann La Roche | Substituted pyrrolidine-2-carboxamides |
| US9345740B2 (en) | 2012-07-10 | 2016-05-24 | Bristol-Myers Squibb Company | IAP antagonists |
| US9371568B2 (en) | 2012-07-31 | 2016-06-21 | Novartis Ag | Markers associated with human double minute 2 inhibitors |
| WO2014025759A1 (en) | 2012-08-09 | 2014-02-13 | Bristol-Myers Squibb Company | Iap antagonists |
| RS61242B1 (sr) * | 2012-09-04 | 2021-01-29 | Shanghai hengrui pharmaceutical co ltd | Derivati imidazolina, postupci njihove pripreme i njihove primene u medicini |
| TWI586668B (zh) | 2012-09-06 | 2017-06-11 | 第一三共股份有限公司 | 二螺吡咯啶衍生物之結晶 |
| WO2014047024A1 (en) | 2012-09-18 | 2014-03-27 | Bristol-Myers Squibb Company | Iap antagonists |
| US9603889B2 (en) | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| TW201428002A (zh) | 2012-11-09 | 2014-07-16 | 必治妥美雅史谷比公司 | 用於抑制細胞凋亡抑制劑之巨環化合物 |
| US9637493B2 (en) | 2012-12-20 | 2017-05-02 | Merck Sharp & Dohme Corp. | Substituted pyrrolopyrimidines as HDM2 inhibitors |
| TW201429969A (zh) | 2012-12-20 | 2014-08-01 | Merck Sharp & Dohme | 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶 |
| EP2752191A1 (en) | 2013-01-07 | 2014-07-09 | Sanofi | Compositions and methods using hdm2 antagonist and mek inhibitor |
| GB201311910D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
| NL2011274C2 (en) | 2013-08-06 | 2015-02-09 | Illumicare Ip B V 51 | Groundbreaking platform technology for specific binding to necrotic cells. |
| CA2902856C (en) | 2013-02-28 | 2021-02-16 | Amgen Inc. | A benzoic acid derivative mdm2 inhibitor for the treatment of cancer |
| AU2014236812B2 (en) | 2013-03-14 | 2018-03-01 | Amgen Inc. | Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer |
| TW201534586A (zh) * | 2013-06-11 | 2015-09-16 | Orion Corp | 新穎ｃｙｐ１７抑制劑／抗雄激素劑 |
| 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 |
| EP3019517A1 (en) | 2013-07-12 | 2016-05-18 | Bristol-Myers Squibb Company | Iap antagonists |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| AU2015247817C1 (en) * | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| TW201613916A (en) | 2014-06-03 | 2016-04-16 | Gilead Sciences Inc | TANK-binding kinase inhibitor compounds |
| US20160022642A1 (en) | 2014-07-25 | 2016-01-28 | Yale University | Compounds Useful for Promoting Protein Degradation and Methods Using Same |
| US10071164B2 (en) | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| 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 |
| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| US10730870B2 (en) | 2015-03-18 | 2020-08-04 | Arvinas Operations, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2017011371A1 (en) | 2015-07-10 | 2017-01-19 | Arvinas, Inc | Mdm2-based modulators of proteolysis and associated methods of use |
| CA2988436A1 (en) | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| WO2017024318A1 (en) * | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| WO2017024317A2 (en) * | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| AU2016349781A1 (en) | 2015-11-02 | 2018-05-10 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| WO2018071606A1 (en) | 2016-10-11 | 2018-04-19 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| IL290809B2 (en) | 2016-11-01 | 2024-01-01 | Arvinas Operations Inc | Tau-protein targeting protacs and associated methods of use |
| KR102674902B1 (ko) | 2016-12-01 | 2024-06-14 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| CN117510491A (zh) | 2016-12-23 | 2024-02-06 | 阿尔维纳斯运营股份有限公司 | 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法 |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
-
2016
- 2016-01-20 JP JP2017556797A patent/JP6817962B2/ja active Active
- 2016-01-20 KR KR1020227037454A patent/KR102564925B1/ko active Active
- 2016-01-20 KR KR1020227006656A patent/KR20220029783A/ko not_active Ceased
- 2016-01-20 KR KR1020177023120A patent/KR102110566B1/ko active Active
- 2016-01-20 US US15/002,303 patent/US11352351B2/en active Active
- 2016-01-20 EP EP16740708.9A patent/EP3247708A4/en active Pending
- 2016-01-20 WO PCT/US2016/014187 patent/WO2016118666A1/en not_active Ceased
- 2016-01-20 KR KR1020207013156A patent/KR20200052995A/ko not_active Abandoned
- 2016-01-20 HK HK18106942.6A patent/HK1247204A1/zh unknown
- 2016-01-20 HK HK18105390.5A patent/HK1245791A1/zh unknown
- 2016-01-20 BR BR112017015497-8A patent/BR112017015497A2/pt not_active Application Discontinuation
- 2016-01-20 CA CA2974367A patent/CA2974367A1/en active Pending
- 2016-01-20 CN CN201680014250.8A patent/CN107428734A/zh active Pending
- 2016-01-20 MX MX2017009454A patent/MX390189B/es unknown
- 2016-01-20 AU AU2016209349A patent/AU2016209349B2/en active Active
- 2016-01-20 KR KR1020237026413A patent/KR20230119040A/ko not_active Ceased
-
2017
- 2017-07-19 MX MX2022002016A patent/MX2022002016A/es unknown
-
2018
- 2018-07-27 US US16/048,191 patent/US20180346461A1/en not_active Abandoned
-
2020
- 2020-03-17 JP JP2020046636A patent/JP2020111590A/ja active Pending
- 2020-08-07 AU AU2020213376A patent/AU2020213376B2/en active Active
-
2021
- 2021-10-27 AU AU2021257970A patent/AU2021257970A1/en not_active Abandoned
-
2022
- 2022-12-20 US US18/085,500 patent/US20240059686A1/en active Pending
- 2022-12-23 JP JP2022206686A patent/JP2023040072A/ja active Pending
-
2023
- 2023-12-19 AU AU2023285742A patent/AU2023285742A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018502925A5 (https=) | ||
| RU2020108515A (ru) | Соединения и способы целевого расщепления андрогенного рецептора | |
| JP2009532486A5 (https=) | ||
| NZ588830A (en) | Inhibitors of protein kinases | |
| JP2011509309A5 (https=) | ||
| JP2011219498A5 (https=) | ||
| JP2018522879A5 (https=) | ||
| JP2016506962A5 (https=) | ||
| JP2010532387A5 (https=) | ||
| PE20141824A1 (es) | Compuestos terapeuticamente activos y sus metodos de uso | |
| RU2015118647A (ru) | Аминопиримидиновые соединения в качестве ингибиторов содержащих т790м мутантных egfr | |
| JP2018502906A5 (https=) | ||
| JP2016506960A5 (https=) | ||
| JP2012515225A5 (https=) | ||
| JP2003528859A5 (https=) | ||
| JP2015500887A5 (https=) | ||
| JP2015514808A5 (https=) | ||
| TR201802944T4 (tr) | İlaç olarak azai̇ndazol veya di̇azai̇ndazol türünün türevleri̇ | |
| BRPI0815142B8 (pt) | forma cristalina do sal de dicloridrato ((1s)-1-(((2s)-2-(5-(4'-(2-((2s)-1-((2s)-2-((metoxicarbonil)amino)-3-metilbutanoil)-2-pirrolidinil)-1h-imidazol-5-il)-4-bifenilil)-1h-imidazol-2-il)-1-pirrolidinil)carbonil)-2-metilpropil)carbamato de metila. | |
| JP2014511892A5 (https=) | ||
| JP2011515483A5 (https=) | ||
| MX2013015370A (es) | Terapia de combinacion que comprende un inhibidor de cdk4/6 y un inhibidor de pi3kpara usarse en el tratamiento de cancer. | |
| JP2016506961A5 (https=) | ||
| JP2016503009A5 (https=) | ||
| JP2014532730A5 (ja) | オピオイド受容体の調節物質およびそれを含む薬学的組成物 |