JP2021535104A5 - - Google Patents
Info
- Publication number
- JP2021535104A5 JP2021535104A5 JP2021509151A JP2021509151A JP2021535104A5 JP 2021535104 A5 JP2021535104 A5 JP 2021535104A5 JP 2021509151 A JP2021509151 A JP 2021509151A JP 2021509151 A JP2021509151 A JP 2021509151A JP 2021535104 A5 JP2021535104 A5 JP 2021535104A5
- Authority
- JP
- Japan
- Prior art keywords
- piperazine
- pyrrolidine
- pharmaceutically acceptable
- imidazo
- fluorophenyl
- Prior art date
Links
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2018/101715 | 2018-08-22 | ||
| CN2018101715 | 2018-08-22 | ||
| CN2019086894 | 2019-05-14 | ||
| CNPCT/CN2019/086894 | 2019-05-14 | ||
| PCT/CN2019/101850 WO2020038415A1 (en) | 2018-08-22 | 2019-08-21 | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021535104A JP2021535104A (ja) | 2021-12-16 |
| JPWO2020038415A5 JPWO2020038415A5 (https=) | 2022-08-29 |
| JP2021535104A5 true JP2021535104A5 (https=) | 2022-08-29 |
| JP7472103B2 JP7472103B2 (ja) | 2024-04-22 |
Family
ID=69592803
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021509151A Active JP7472103B2 (ja) | 2018-08-22 | 2019-08-21 | トロポミオシン受容体キナーゼ（ｔｒｋ）分解化合物とその使用方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US12065442B2 (https=) |
| EP (1) | EP3841098B1 (https=) |
| JP (1) | JP7472103B2 (https=) |
| KR (1) | KR102850550B1 (https=) |
| CN (3) | CN115626927B (https=) |
| AU (2) | AU2019323446B2 (https=) |
| BR (1) | BR112021003098A2 (https=) |
| CA (1) | CA3110267A1 (https=) |
| DK (1) | DK3841098T3 (https=) |
| IL (1) | IL280984B2 (https=) |
| MX (1) | MX2021001957A (https=) |
| WO (1) | WO2020038415A1 (https=) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| MX2021001957A (es) | 2018-08-22 | 2021-07-15 | Cullgen Shanghai Inc | Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk). |
| 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 |
| GB201820165D0 (en) * | 2018-12-11 | 2019-01-23 | Ucb Biopharma Sprl | Therapeutic agents |
| BR112021026517A2 (pt) | 2019-06-28 | 2022-05-10 | Kymera Therapeutics Inc | Degradadores de irak e usos dos mesmos |
| WO2021011868A1 (en) | 2019-07-17 | 2021-01-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US12551564B2 (en) | 2019-12-10 | 2026-02-17 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| WO2021127190A1 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| JP2023508891A (ja) * | 2019-12-17 | 2023-03-06 | オリオニス バイオサイエンシズ，インコーポレイテッド | タンパク質の動員および／または分解のための二機能性剤 |
| JP2023507590A (ja) * | 2019-12-17 | 2023-02-24 | オリオニス バイオサイエンシズ，インコーポレイテッド | タンパク質の動員および／または分解を調節する化合物 |
| US20230219945A1 (en) * | 2019-12-17 | 2023-07-13 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CA3173262A1 (en) * | 2020-02-26 | 2021-09-02 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| US12528785B2 (en) * | 2020-03-19 | 2026-01-20 | Kymera Therapeutics, Inc. | MDM2 degraders and uses thereof |
| EP4121167A1 (en) * | 2020-03-21 | 2023-01-25 | Arvinas Operations, Inc. | Selective modulators of mutant lrrk2 proteolysis and associated methods of use |
| WO2021222542A1 (en) * | 2020-04-30 | 2021-11-04 | President And Fellows Of Harvard College | 5-amino-2-piperidinon-3-yl-1-oxoisoindoline derivatives for degradation of ikzf2 degraders |
| US11739101B2 (en) | 2020-05-06 | 2023-08-29 | Nurix Therapeutics, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| EP4157833A1 (en) * | 2020-05-28 | 2023-04-05 | Bristol-Myers Squibb Company | Galectin-3 inhibitors |
| CN113801062B (zh) * | 2020-06-15 | 2023-05-26 | 沈阳药科大学 | 3-氨基-5-(3,5-二氟苄基)-1h-吲唑的制备方法 |
| US20240100170A1 (en) * | 2020-08-27 | 2024-03-28 | Cullgen (Shanghai), Inc. | Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use |
| CN112125977B (zh) * | 2020-09-29 | 2022-03-08 | 西安交通大学 | 一种tweak-mv1偶联蛋白及其抗银屑病的应用 |
| CN116583509A (zh) * | 2020-10-07 | 2023-08-11 | 上海睿跃生物科技有限公司 | 治疗癌症的化合物和方法 |
| 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 |
| CN116867494A (zh) | 2021-02-15 | 2023-10-10 | 凯麦拉医疗公司 | Irak4降解剂和其用途 |
| WO2022218289A1 (en) * | 2021-04-12 | 2022-10-20 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| CN113402467B (zh) * | 2021-06-18 | 2022-05-13 | 山东汇海医药化工有限公司 | 一种氟班色林的合成方法 |
| BR112023025403A2 (pt) | 2021-06-25 | 2024-02-20 | Korea Res Inst Chemical Tech | Composto heterocíclico bifuncional tendo função de degradação de btk por meio da via ubiquitina proteassoma e uso do mesmo |
| CN113278023B (zh) * | 2021-07-22 | 2021-10-15 | 上海睿跃生物科技有限公司 | 含氮杂环化合物及其制备方法和应用 |
| AU2022370021B2 (en) * | 2021-10-22 | 2026-04-16 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications |
| US12187744B2 (en) | 2021-10-29 | 2025-01-07 | Kymera Therapeutics, Inc. | IRAK4 degraders and synthesis thereof |
| EP4430052A1 (en) | 2021-11-10 | 2024-09-18 | Nurix Therapeutics, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| EP4180428A1 (en) | 2021-11-12 | 2023-05-17 | Genzyme Corporation | Crystalline imidazo[4,5-b]pyridine compound, pharmaceutical compositions, and their use in treating medical conditions |
| CN114230518A (zh) * | 2021-12-13 | 2022-03-25 | 海南梵圣生物科技有限公司 | 一种5-苄基-1h-吲唑-3-胺类化合物的制备方法 |
| CN118401512A (zh) * | 2021-12-24 | 2024-07-26 | 苏州开拓药业股份有限公司 | 一种具有酰亚胺骨架的多蛋白降解剂 |
| CN116217578B (zh) * | 2021-12-30 | 2026-02-24 | 清华大学 | 一类抑制mTOR同时降解GSPT1蛋白的双功能化合物 |
| WO2023239629A1 (en) | 2022-06-06 | 2023-12-14 | Plexium, Inc. | Compounds and pharmaceutical compositions that degrade cdk2 |
| WO2023249994A1 (en) * | 2022-06-22 | 2023-12-28 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| TW202412851A (zh) * | 2022-08-05 | 2024-04-01 | 大陸商深圳市新樾生物科技有限公司 | 蛋白激酶降解劑、藥物及應用 |
| JP2026508813A (ja) * | 2023-01-13 | 2026-03-13 | シェンツェン ニューデル バイオテック カンパニー リミテッド | 化合物ａの塩及び結晶形、その製造方法、並びにその用途 |
| KR20250173033A (ko) * | 2024-05-31 | 2025-12-10 | 국민대학교산학협력단 | 알티라티닙을 유효성분으로 포함하는 관절염 예방 또는 치료용 조성물 |
Family Cites Families (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| PH12013501594A1 (en) | 2007-07-20 | 2014-05-12 | Nerviano Medical Sciences Srl | Substituted indazole derivatives active as kinase inhibitors |
| WO2009140128A2 (en) | 2008-05-13 | 2009-11-19 | Irm Llc | Compounds and compositions as kinase inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| SG186389A1 (en) | 2010-06-30 | 2013-01-30 | Univ Brandeis | Small-molecule-targeted protein degradation |
| WO2012037155A2 (en) | 2010-09-13 | 2012-03-22 | Gtx, Inc. | Tyrosine kinase inhibitors |
| AU2011338615B2 (en) | 2010-12-07 | 2017-07-27 | Yale University | Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same |
| 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 |
| US20150119435A1 (en) | 2012-05-11 | 2015-04-30 | Yale University | Compounds useful for promoting protein degradation and methods using same |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| SG11201605917SA (en) | 2014-01-24 | 2016-08-30 | Abbvie Inc | 6-phenyl- or 6-(pyridin-3-yl)indazole derivatives and methods of use |
| WO2015143652A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| 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 |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US10336707B2 (en) * | 2014-12-16 | 2019-07-02 | Eudendron S.R.L. | Heterocyclic derivatives modulating activity of certain protein kinases |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| 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 |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| AU2016275051A1 (en) | 2015-06-10 | 2017-12-07 | Epizyme, Inc. | EZH2 inhibitors for treating lymphoma |
| CN105085620B (zh) | 2015-06-25 | 2018-05-08 | 中山大学附属第一医院 | 一种靶向泛素化降解Smad3的化合物 |
| 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 |
| 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 |
| WO2017176958A1 (en) | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| AU2017246452C1 (en) | 2016-04-06 | 2021-06-03 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| MX384905B (es) | 2016-04-12 | 2025-03-14 | Univ Michigan Regents | Degradadores de proteínas de bromodominio y dominioextraterminal (bet). |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic 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 |
| 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 |
| WO2017201069A1 (en) | 2016-05-18 | 2017-11-23 | Biotheryx, Inc. | Oxoindoline derivatives as protein function modulators |
| KR101825065B1 (ko) | 2016-05-24 | 2018-02-05 | 한국화학연구원 | Alk 단백질의 분해를 유도하는 약학적 조성물 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| GB201610156D0 (en) | 2016-06-10 | 2016-07-27 | Otsuka Pharma Co Ltd | Cliptac compositions |
| AU2017281903B2 (en) | 2016-06-23 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use |
| CA3036841A1 (en) | 2016-09-13 | 2018-03-22 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet protein degraders |
| 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 |
| CN106543185B (zh) | 2016-11-10 | 2017-12-15 | 吉林大学 | 一种靶向泛素化降解plk1和brd4蛋白的化合物及其应用 |
| US10925868B2 (en) | 2016-11-10 | 2021-02-23 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use |
| CA3043938A1 (en) | 2016-12-21 | 2018-06-28 | Biotheryx, Inc. | Thienopyrrole derivatives for use in targeting proteins, compositions, methods, and uses thereof |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase 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 |
| 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 |
| EP3609889B1 (en) | 2017-04-14 | 2023-07-05 | University Of Dundee | Small molecules |
| 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 |
| WO2018226542A1 (en) | 2017-06-09 | 2018-12-13 | Arvinas, Inc. | Modulators of proteolysis and associated methods of use |
| CN109912655B (zh) * | 2017-12-13 | 2021-12-10 | 上海科技大学 | Alk蛋白降解剂及其抗肿瘤应用 |
| CN112789057A (zh) | 2018-07-24 | 2021-05-11 | 詹纽瑞治疗公司 | 纳米颗粒组合物 |
| MX2021001957A (es) | 2018-08-22 | 2021-07-15 | Cullgen Shanghai Inc | Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk). |
| US11969472B2 (en) * | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| CA3173262A1 (en) * | 2020-02-26 | 2021-09-02 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| WO2023055952A1 (en) | 2021-09-29 | 2023-04-06 | C4 Therapeutics, Inc. | Neurotrophic tyrosine receptor kinase (ntrk) degrading compounds |
-
2019
- 2019-08-21 MX MX2021001957A patent/MX2021001957A/es unknown
- 2019-08-21 CN CN202210693243.2A patent/CN115626927B/zh active Active
- 2019-08-21 KR KR1020217008232A patent/KR102850550B1/ko active Active
- 2019-08-21 BR BR112021003098-0A patent/BR112021003098A2/pt unknown
- 2019-08-21 CN CN201980067402.4A patent/CN112888681B/zh active Active
- 2019-08-21 CA CA3110267A patent/CA3110267A1/en active Pending
- 2019-08-21 JP JP2021509151A patent/JP7472103B2/ja active Active
- 2019-08-21 DK DK19852808.5T patent/DK3841098T3/da active
- 2019-08-21 CN CN202311721460.9A patent/CN118530239A/zh active Pending
- 2019-08-21 AU AU2019323446A patent/AU2019323446B2/en active Active
- 2019-08-21 US US17/269,670 patent/US12065442B2/en active Active
- 2019-08-21 EP EP19852808.5A patent/EP3841098B1/en active Active
- 2019-08-21 WO PCT/CN2019/101850 patent/WO2020038415A1/en not_active Ceased
- 2019-08-21 IL IL280984A patent/IL280984B2/en unknown
-
2024
- 2024-05-03 US US18/654,554 patent/US20240400570A1/en not_active Abandoned
-
2025
- 2025-04-11 AU AU2025202596A patent/AU2025202596A1/en active Pending
- 2025-08-19 US US19/304,433 patent/US20250388587A1/en active Pending
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