JP2020504741A5 - - Google Patents
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- JP2020504741A5 JP2020504741A5 JP2019534245A JP2019534245A JP2020504741A5 JP 2020504741 A5 JP2020504741 A5 JP 2020504741A5 JP 2019534245 A JP2019534245 A JP 2019534245A JP 2019534245 A JP2019534245 A JP 2019534245A JP 2020504741 A5 JP2020504741 A5 JP 2020504741A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- group
- substituted
- ulm
- Prior art date
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Families Citing this family (145)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107412788B (zh) | 2012-12-21 | 2021-06-18 | 国立研究开发法人量子科学技术研究开发机构 | 用于对脑内所蓄积的Tau蛋白质进行成像的新的化合物 |
| CA2933701C (en) | 2013-12-18 | 2022-05-31 | The California Institute For Biomedical Research | Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| 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 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs 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 |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CA3087528C (en) | 2016-09-15 | 2024-01-30 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| JP7286539B2 (ja) | 2016-11-01 | 2023-06-05 | アルビナス・オペレーションズ・インコーポレイテッド | タウタンパク質標的化ｐｒｏｔａｃ、および関連使用方法 |
| BR112019011200B1 (pt) | 2016-12-01 | 2021-12-28 | Arvinas Operations, Inc | Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| CA3047784A1 (en) * | 2016-12-23 | 2018-06-28 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| EP3559002A4 (en) | 2016-12-23 | 2021-02-17 | Arvinas Operations, Inc. | CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma 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 |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2018140809A1 (en) | 2017-01-26 | 2018-08-02 | Arvinas, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| CN115974840A (zh) | 2017-01-31 | 2023-04-18 | 阿尔维纳斯运营股份有限公司 | 人小脑蛋白配体和包含其的双官能化合物 |
| JP2020518660A (ja) * | 2017-04-28 | 2020-06-25 | クォーツ セラピューティクス，インコーポレイティド | Ｒａｆ分解性結合体化合物 |
| EP3641762A4 (en) | 2017-06-20 | 2021-03-10 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONES AND DEGRONIMERS FOR PROTEIN DEGRADATION |
| TWI793151B (zh) | 2017-08-23 | 2023-02-21 | 瑞士商諾華公司 | 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途 |
| CN111315735B (zh) | 2017-09-04 | 2024-03-08 | C4医药公司 | 二氢苯并咪唑酮 |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| CN111278816B (zh) | 2017-09-04 | 2024-03-15 | C4医药公司 | 二氢喹啉酮 |
| US10632209B2 (en) | 2017-11-10 | 2020-04-28 | The Regents Of The University Of Michigan | ASH1L inhibitors and methods of treatment therewith |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| WO2019099926A1 (en) | 2017-11-17 | 2019-05-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| WO2019148055A1 (en) | 2018-01-26 | 2019-08-01 | Yale University | Imide-based modulators of proteolysis and 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 |
| EP3774777A2 (en) | 2018-04-04 | 2021-02-17 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| EP3778590A4 (en) | 2018-04-09 | 2021-12-22 | ShanghaiTech University | ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE |
| MX2020010571A (es) * | 2018-04-13 | 2021-01-08 | Arvinas Operations Inc | Ligandos de cereblon y compuestos bifuncionales que los comprenden. |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| MX2020011959A (es) | 2018-05-09 | 2021-02-17 | Aprinoia Therapeutics Ltd | Compuestos de heteroarilo y usos de los mismos. |
| WO2019222272A1 (en) | 2018-05-14 | 2019-11-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| AR116109A1 (es) * | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| CR20210001A (es) | 2018-07-10 | 2021-04-19 | Novartis Ag | Derivados de 3-(5-hidroxi-1-oxoisoindolin-2-il)piperidina-2,6-diona y su uso en el tratamiento de trastornos dependientes de la proteina con dedos de zinc 2 de la familia ikaros (1kzf2) |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| AU2019323446B2 (en) | 2018-08-22 | 2025-01-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| KR20240028539A (ko) * | 2018-09-07 | 2024-03-05 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행형 섬유육종 폴리펩티드의 표적화 분해를 위한 다중 고리 화합물 및 방법 |
| WO2020064002A1 (zh) * | 2018-09-30 | 2020-04-02 | 中国科学院上海药物研究所 | 异吲哚啉类化合物、其制备方法、药物组合物及用途 |
| EP3864030A4 (en) * | 2018-10-12 | 2022-09-21 | The Scripps Research Institute | Compounds and methods for dcaf-mediated protein degradation |
| EP3891128A4 (en) * | 2018-12-05 | 2022-08-17 | Vividion Therapeutics, Inc. | SUBSTITUTED ISOINDOLINONES AS MODULATORS OF CEREBLON-MEDIATED NEOSUBSTRATE RECRUITMENT |
| US20220041578A1 (en) * | 2018-12-06 | 2022-02-10 | Shanghai Institute Of Meteria Medica, Chinese Academy Of Sciences | Isoindoline compound, and preparation method, pharmaceutical composition, and application of isoindoline compound |
| WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| US20220105188A1 (en) * | 2019-02-07 | 2022-04-07 | Korea Research Institute Of Chemical Technology | Target protein eed degradation-inducing degraducer, preparation method thereof, and pharmaceutical composition for preventing or treating diseases related to eed, ezh2, or prc2, comprising same as active ingredient |
| US11389438B2 (en) * | 2019-02-25 | 2022-07-19 | Chdi Foundation, Inc. | Compounds for targeting mutant huntingtin protein and uses thereof |
| CA3131804A1 (en) | 2019-03-01 | 2020-09-10 | Ontario Institute For Cancer Research (Oicr) | Amide-based proteolysis modulators of b-rapidly accelerated fibrosarcoma (braf) and associated uses |
| EA202192738A1 (ru) | 2019-04-12 | 2022-03-17 | С4 Терапьютикс, Инк. | Трициклические соединения, обеспечивающие разрушение белка ikaros и белка aiolos |
| WO2020214555A1 (en) | 2019-04-16 | 2020-10-22 | Northwestern University | Bifunctional compounds comprising apcin-a and their use in the treatment of cancer |
| BR112021022008A2 (pt) | 2019-05-14 | 2022-05-17 | Nuvation Bio Inc | Compostos de direcionamento a receptor de hormônio nuclear anticâncer |
| AU2020281410A1 (en) * | 2019-05-31 | 2021-10-07 | Haisco Pharmaceuticals Pte. Ltd. | BTK inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof |
| KR102776925B1 (ko) | 2019-06-25 | 2025-03-11 | 길리애드 사이언시즈, 인코포레이티드 | Flt3l-fc 융합 단백질 및 사용 방법 |
| US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
| WO2021016521A1 (en) * | 2019-07-25 | 2021-01-28 | Beth Israel Deaconess Medical Center, Inc. | Photo induced control of protein destruction |
| WO2021020585A1 (ja) | 2019-07-31 | 2021-02-04 | ファイメクス株式会社 | 複素環化合物 |
| JP2021024787A (ja) | 2019-07-31 | 2021-02-22 | ファイメクス株式会社 | 複素環化合物 |
| MX2022002415A (es) | 2019-08-26 | 2022-03-22 | Arvinas Operations Inc | Metodos de tratamiento del cancer de mama con derivados de tetrahidronaftaleno como degradadores del receptor de estrogenos. |
| WO2021061644A1 (en) * | 2019-09-23 | 2021-04-01 | Accutar Biotechnology Inc. | Novel substituted quinoline-8-carbonitrile derivatives with androgen receptor degradation activity and uses thereof |
| WO2021061642A1 (en) * | 2019-09-23 | 2021-04-01 | Accutar Biotechnology Inc. | Novel ureas having androgen receptor degradation activity and uses thereof |
| CA3155290A1 (en) * | 2019-09-23 | 2021-04-01 | Accutar Biotechnology Inc. | Novel substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof |
| AU2020368542B2 (en) | 2019-10-17 | 2024-02-29 | Arvinas Operations, Inc. | Bifunctional molecules containing an E3 ubiquitine ligase binding moiety linked to a BCL6 targeting moiety |
| CN114728071B (zh) | 2019-11-13 | 2024-12-06 | 新旭生技股份有限公司 | 用于降解tau蛋白聚集体的化合物及其用途 |
| TW202131930A (zh) | 2019-11-13 | 2021-09-01 | 美商諾維雪碧歐公司 | 抗癌核荷爾蒙受體標靶化合物 |
| KR20220103753A (ko) | 2019-11-19 | 2022-07-22 | 브리스톨-마이어스 스큅 컴퍼니 | 헬리오스 단백질의 억제제로서 유용한 화합물 |
| CN110950877B (zh) * | 2019-12-11 | 2022-06-28 | 齐鲁工业大学 | 一种双检测荧光探针、制备方法及其在检测硫化氢和铜离子中的应用 |
| AU2020404956A1 (en) * | 2019-12-17 | 2022-07-07 | Orionis Biosciences, Inc. | Compounds modulating protein recruitment and/or degradation |
| AU2020408333A1 (en) * | 2019-12-17 | 2022-07-07 | Orionis Biosciences, Inc. | Bifunctional agents for protein recruitment and/or degradation |
| IL293530A (en) | 2019-12-18 | 2022-08-01 | Novartis Ag | Derivatives of 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione and their uses |
| CN115175901B (zh) | 2019-12-19 | 2024-03-22 | 阿尔维纳斯运营股份有限公司 | 用于雄激素受体的靶向降解的化合物和方法 |
| IL293999B1 (en) | 2019-12-20 | 2025-10-01 | C4 Therapeutics Inc | Isoindolinone compounds with a phenylaminoglutarimide residue for degradation of EGFR |
| CR20220396A (es) | 2020-02-14 | 2022-11-14 | Jounce Therapeutics Inc | Anticuerpos y proteínas de fusión que se unen a ccr8 y usos de estos |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CA3173262A1 (en) | 2020-02-26 | 2021-09-02 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | Compounds for targeted degradation of brd9 |
| WO2021207172A1 (en) * | 2020-04-06 | 2021-10-14 | Arvinas Operations, Inc. | Compounds and methods for targeted degradation of kras |
| ES3034380T3 (en) | 2020-06-09 | 2025-08-18 | Prelude Therapeutics Inc | Brm targeting compounds and associated methods of use |
| WO2021257650A1 (en) * | 2020-06-17 | 2021-12-23 | Dana-Farber Cancer Institute, Inc. | Targeted aberrant alpha-synuclein species and induced ubiquitination and proteosomal clearance via co-recruitment of an e3-ligase system |
| WO2021255213A1 (en) * | 2020-06-19 | 2021-12-23 | F. Hoffmann-La Roche Ag | Heterobifunctional compounds as degraders of braf |
| KR20230040991A (ko) * | 2020-06-19 | 2023-03-23 | 씨4 테라퓨틱스, 인코포레이티드 | Braf 분해제 |
| KR102559329B1 (ko) * | 2020-07-02 | 2023-07-25 | 포항공과대학교 산학협력단 | 신규한 프로탁 키메라 화합물, 이를 포함하는 표적 단백질 분해를 통한 질환의 예방, 개선 또는 치료용 약학적 조성물 |
| KR102646850B1 (ko) * | 2020-07-21 | 2024-03-13 | 주식회사 유빅스테라퓨틱스 | 안드로겐 수용체 분해용 화합물 및 이들의 의약 용도 |
| CN116490186B (zh) | 2020-08-05 | 2025-10-31 | C4医药公司 | 用于ret的靶向降解的化合物 |
| US20230277553A1 (en) * | 2020-08-07 | 2023-09-07 | Cornell University | Therapeutic composition of cure-pro compounds for targeted degradation of bet domain proteins, and methods of making and usage |
| EP4192825A4 (en) * | 2020-08-07 | 2024-08-28 | Cornell University | CURE PRO MOLECULES THERAPEUTICALLY USEFUL FOR E3 LIGASE-MEDIATED PROTEIN DEGRADATION, AND METHODS OF PREPARATION AND USE THEREOF |
| CN117062814A (zh) * | 2020-08-28 | 2023-11-14 | 阿维纳斯运营公司 | 快速加速纤维肉瘤蛋白降解的化合物和相关使用方法 |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| 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 |
| IL301588A (en) | 2020-09-23 | 2023-05-01 | St Jude Childrens Res Hospital Inc | Analogs of N-(2-(2,6-deoxypyridin-3-yl)-1,3-dioxoindolin-5-yl)arylsulfonamide are converted as cereblon protein modulators |
| EP4277901A1 (en) | 2021-01-13 | 2023-11-22 | Monte Rosa Therapeutics, Inc. | Isoindolinone compounds |
| KR102532692B1 (ko) * | 2021-03-15 | 2023-05-16 | (주)피알지에스앤텍 | 신경섬유종증 2형 증후군 예방 또는 치료용 조성물 |
| WO2022204184A1 (en) | 2021-03-23 | 2022-09-29 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| WO2022216644A1 (en) | 2021-04-06 | 2022-10-13 | Bristol-Myers Squibb Company | Pyridinyl substituted oxoisoindoline compounds |
| PE20240639A1 (es) | 2021-04-16 | 2024-04-04 | Arvinas Operations Inc | Moduladores de la proteolisis bcl6 y metodos de uso asociados |
| AU2022269568A1 (en) | 2021-05-03 | 2023-11-16 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| CA3217417A1 (en) | 2021-05-05 | 2022-11-10 | Kevin M. Guckian | Compounds for targeting degradation of bruton's tyrosine kinase |
| WO2022245671A1 (en) | 2021-05-18 | 2022-11-24 | Gilead Sciences, Inc. | Methods of using flt3l-fc fusion proteins |
| UY39796A (es) | 2021-06-03 | 2023-07-31 | Novartis Ag | Derivados de 3–((5–oxi)–1–oxoisoindolin–2–il)piperidina–2,6–diona y sus usos |
| WO2022261627A1 (en) * | 2021-06-07 | 2022-12-15 | The General Hospital Corporation | Inhibitors of ttbk1 |
| CN117940133A (zh) | 2021-06-08 | 2024-04-26 | C4医药公司 | 用于突变braf的降解的治疗剂 |
| JP2024522196A (ja) | 2021-06-09 | 2024-06-11 | ザ スクリプス リサーチ インスティテュート | 長時間作用型デュアルｇｉｐ／ｇｌｐ－１ペプチドコンジュゲートおよび使用方法 |
| US20240343733A1 (en) | 2021-07-07 | 2024-10-17 | Biogen Ma Inc. | Compounds for targeting degradation of irak4 proteins |
| EP4366834A1 (en) | 2021-07-07 | 2024-05-15 | Biogen MA Inc. | Compounds for targeting degradation of irak4 proteins |
| WO2023023941A1 (en) * | 2021-08-24 | 2023-03-02 | Biofront Ltd (Cayman) | Hpk1 degraders, compositions comprising the hpki degrader, and methods of using the same |
| EP4395549A1 (en) | 2021-09-01 | 2024-07-10 | Oerth Bio LLC | Compositions and methods for targeted degradation of proteins in a plant cell |
| US20250243210A1 (en) * | 2021-10-22 | 2025-07-31 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | Crbn e3 ligase ligand compound, protein degrader developed based thereon and their applications |
| AU2022375782A1 (en) | 2021-10-28 | 2024-05-02 | Gilead Sciences, Inc. | Pyridizin-3(2h)-one derivatives |
| EP4422756A1 (en) | 2021-10-29 | 2024-09-04 | Gilead Sciences, Inc. | Cd73 compounds |
| CN115894450B (zh) * | 2021-11-30 | 2023-09-12 | 山东如至生物医药科技有限公司 | 一种新型多环类化合物及其组合物和用途 |
| KR20240123836A (ko) | 2021-12-22 | 2024-08-14 | 길리애드 사이언시즈, 인코포레이티드 | 이카로스 아연 핑거 패밀리 분해제 및 이의 용도 |
| WO2023122615A1 (en) | 2021-12-22 | 2023-06-29 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| WO2023143494A1 (zh) * | 2022-01-28 | 2023-08-03 | 甘李药业股份有限公司 | 新型protac化合物 |
| ES2999273T3 (en) | 2022-03-17 | 2025-02-25 | Gilead Sciences Inc | Ikaros zinc finger family degraders and uses thereof |
| CN119487038A (zh) | 2022-04-21 | 2025-02-18 | 吉利德科学公司 | Kras g12d调节化合物 |
| AU2023283735A1 (en) | 2022-06-06 | 2024-10-31 | C4 Therapeutics, Inc. | Bicyclic-substituted glutarimide cereblon binders |
| WO2024006929A1 (en) | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Cd73 compounds |
| 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 |
| WO2024054591A1 (en) | 2022-09-07 | 2024-03-14 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| EP4638436A1 (en) | 2022-12-22 | 2025-10-29 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| KR20250120440A (ko) * | 2022-12-27 | 2025-08-08 | 글루탁스 테라퓨틱스 (상하이) 씨오., 엘티디. | 황/산소 치환 글루타르이미딜-이소인돌리논 모핵을 기반으로 하는 화합물 및 이의 응용 |
| EP4655073A2 (en) | 2023-01-26 | 2025-12-03 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs ans uses related thereto |
| US20240383922A1 (en) | 2023-04-11 | 2024-11-21 | Gilead Sciences, Inc. | KRAS Modulating Compounds |
| WO2024220917A1 (en) | 2023-04-21 | 2024-10-24 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2025006720A1 (en) | 2023-06-30 | 2025-01-02 | Gilead Sciences, Inc. | Kras modulating compounds |
| TW202502779A (zh) | 2023-06-30 | 2025-01-16 | 美商金橘生物科技公司 | 取代的雜芳族胺及其用途 |
| TW202519517A (zh) | 2023-07-26 | 2025-05-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| WO2025024663A1 (en) | 2023-07-26 | 2025-01-30 | Gilead Sciences, Inc. | Parp7 inhibitors |
| 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 |
| WO2025054347A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2025054530A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| WO2025096855A1 (en) | 2023-11-02 | 2025-05-08 | Kumquat Biosciences Inc. | Degraders and uses thereof |
| US20250154172A1 (en) | 2023-11-03 | 2025-05-15 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2025137500A1 (en) | 2023-12-21 | 2025-06-26 | Dana-Farber Cancer Institute, Inc. | Kinase inhibition and degradation |
| WO2025137640A1 (en) | 2023-12-22 | 2025-06-26 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
| WO2025235298A1 (en) * | 2024-05-07 | 2025-11-13 | Nikang Therapeutics, Inc. | Bifunctional compounds containing thiazolyl derivatives for degrading certain cyclin-dependent kinase via ubiquitin proteasome pathway |
| US20250376484A1 (en) | 2024-05-21 | 2025-12-11 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
Family Cites Families (124)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4065567B2 (ja) | 1996-07-24 | 2008-03-26 | セルジーン コーポレイション | 置換２―（２，６―ジオキソピペリジン―３―イル）フタルイミド類及び―１―オキソイソインドリン類ならびにＴＮＦαレベルの減少方法 |
| CA2287387C (en) | 1997-05-14 | 2010-02-16 | Sloan-Kettering Institute For Cancer Research | Methods and compositions for destruction of selected proteins |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| WO2000066119A1 (en) | 1999-05-05 | 2000-11-09 | Merck & Co., Inc. | Novel prolines as antimicrobial agents |
| AU2001295041A1 (en) | 2000-09-08 | 2002-03-22 | 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 |
| CN1264858C (zh) | 2001-02-16 | 2006-07-19 | 纳幕尔杜邦公司 | 血管生成抑制三肽、组合物及其使用方法 |
| 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 |
| US7030141B2 (en) | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| AU2003249920A1 (en) | 2002-07-02 | 2004-01-23 | Novartis Ag | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| EP1651595A2 (en) | 2003-05-30 | 2006-05-03 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| JP2007522116A (ja) | 2004-01-16 | 2007-08-09 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | コンホメーションが制約されたＳｍａｃ模倣物およびその使用 |
| CA2558615C (en) | 2004-03-23 | 2013-10-29 | Genentech, Inc. | Azabicyclo-octane inhibitors of iap |
| PE20110102A1 (es) | 2004-04-07 | 2011-02-07 | Novartis Ag | Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap) |
| KR100984459B1 (ko) | 2004-07-02 | 2010-09-29 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| KR20120127754A (ko) | 2004-12-20 | 2012-11-23 | 제넨테크, 인크. | Ｉａｐ의 피롤리딘 억제제 |
| TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| AU2006216450C1 (en) | 2005-02-25 | 2013-01-10 | Medivir Ab | Dimeric IAP inhibitors |
| 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 |
| BRPI0611863B1 (pt) | 2005-06-22 | 2021-11-23 | Plexxikon, Inc | Composto, bem como composição e kit compreendendo o mesmo, composto intermediário na preparação do mesmo, método para tratamento e uso do mesmo |
| RU2008112221A (ru) | 2005-08-31 | 2009-10-10 | Селджин Корпорейшн (Us) | Соединения ряда изоиндолимидов, их композиции и способы применения |
| MX2008011128A (es) | 2006-03-03 | 2008-09-08 | Novartis Ag | Compuestos de n-formil-hidroxilamina. |
| WO2007101347A1 (en) | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| EA017279B1 (ru) | 2006-05-05 | 2012-11-30 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | БИВАЛЕНТНЫЕ МИМЕТИКИ Smac И ИХ ПРИМЕНЕНИЯ |
| 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 |
| WO2008014236A1 (en) | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| EP2057143B1 (en) | 2006-08-30 | 2013-07-24 | Celgene Corporation | 5-substituted isoindoline compounds |
| RU2448101C2 (ru) | 2006-08-30 | 2012-04-20 | Селджин Корпорейшн | 5-замещенные изоиндолиновые соединения |
| WO2008054827A2 (en) | 2006-11-03 | 2008-05-08 | 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 |
| BRPI0810178A2 (pt) | 2007-04-12 | 2014-09-23 | Joyant Pharmaceuticals Inc | Dímeros e trímeros miméticos de smac úteis como agentes anticâncer |
| WO2008128171A2 (en) | 2007-04-13 | 2008-10-23 | The Regents Of The University Of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| PE20090211A1 (es) | 2007-04-30 | 2009-04-02 | Genentech Inc | Inhibidores de las iap |
| US20100203012A1 (en) | 2007-05-30 | 2010-08-12 | Aegera Therapeutics, Inc. | Iap bir domain binding compounds |
| KR20100038108A (ko) | 2007-07-25 | 2010-04-12 | 브리스톨-마이어스 스큅 컴퍼니 | 트리아진 키나제 억제제 |
| EP2058312A1 (en) | 2007-11-09 | 2009-05-13 | Universita' degli Studi di Milano | SMAC mimetic compounds as apoptosis inducers |
| HUE026105T2 (en) | 2008-10-29 | 2016-05-30 | Celgene Corp | Isoindole compounds for use in the treatment of cancer |
| 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 |
| WO2011059763A2 (en) | 2009-10-28 | 2011-05-19 | Joyant Pharmaceuticals, Inc. | Dimeric smac mimetics |
| RS59275B1 (sr) | 2010-02-11 | 2019-10-31 | Celgene Corp | Derivati arilmetoksi izoindolina i kompozicije koje ih obuhvataju i postupci njihove primene |
| US9765019B2 (en) | 2010-06-30 | 2017-09-19 | Brandeis University | Small-molecule-targeted protein degradation |
| CN103261169A (zh) | 2010-09-24 | 2013-08-21 | 密歇根大学董事会 | 脱泛素酶抑制剂及其应用方法 |
| EP2649099A4 (en) | 2010-12-07 | 2016-10-19 | Univ Yale | SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS |
| WO2012090104A1 (en) | 2010-12-31 | 2012-07-05 | Kareus Therapeutics, Sa | Methods and compositions for designing novel conjugate therapeutics |
| US8889684B2 (en) * | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| EA028821B9 (ru) * | 2011-02-07 | 2018-10-31 | Плексксикон, Инк. | Соединения и способы для модуляции киназ, а также показания к их применению |
| WO2012149299A2 (en) | 2011-04-29 | 2012-11-01 | Celgene Corporaiton | Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor |
| WO2013049250A1 (en) | 2011-09-27 | 2013-04-04 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| WO2013071039A1 (en) | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| US20140309265A1 (en) | 2011-11-09 | 2014-10-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| CN103159736B (zh) * | 2011-12-10 | 2015-05-13 | 通化济达医药有限公司 | 取代的吡唑激酶抑制剂 |
| CN103596926B (zh) * | 2011-12-31 | 2015-11-25 | 百济神州有限公司 | 作为raf激酶抑制剂的稠合三环化合物 |
| EP2802608A4 (en) | 2012-01-12 | 2015-08-05 | Univ Yale | COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY E3 UBIQUITIN LIGASE |
| WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| WO2013169858A1 (en) * | 2012-05-08 | 2013-11-14 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
| 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 |
| WO2013178570A1 (en) | 2012-05-30 | 2013-12-05 | F. Hoffmann-La Roche Ag | Substituted pyrrolidine-2-carboxamides |
| EP2872521B1 (en) | 2012-07-10 | 2016-08-24 | Bristol-Myers Squibb Company | Iap antagonists |
| US20150159222A1 (en) | 2012-07-31 | 2015-06-11 | Novartis Ag | Markers associated with human double minute 2 inhibitors |
| US9453048B2 (en) | 2012-08-09 | 2016-09-27 | Bristol-Myers Squibb Company | IAP antagonists |
| 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 |
| EP2897949B1 (en) | 2012-09-18 | 2018-01-10 | Bristol-Myers Squibb Company | Iap antagonists |
| JP6407504B2 (ja) | 2012-09-21 | 2018-10-17 | アログ・ファーマシューティカルズ・インコーポレイテッドＡｒｏｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | 恒常的に活性であるリン酸化型ｆｌｔ３キナーゼの阻害方法 |
| US9603889B2 (en) | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| EP2917218B1 (en) | 2012-11-09 | 2017-01-04 | Ensemble Therapeutics Corporation | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| MX373639B (es) | 2012-12-20 | 2020-05-04 | Merck Sharp & Dohme | Imidazopiridinas sustituidas como inhibidores de doble minuto 2 humana. |
| EP2934535B1 (en) | 2012-12-20 | 2017-07-19 | Merck Sharp & Dohme Corp. | Substituted pyrrolopyrimidines as hdm2 inhibitors |
| 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. |
| EP2961735B1 (en) | 2013-02-28 | 2017-09-27 | Amgen Inc. | A benzoic acid derivative mdm2 inhibitor for the treatment of cancer |
| US9758495B2 (en) | 2013-03-14 | 2017-09-12 | Amgen Inc. | Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US9637518B2 (en) | 2013-07-12 | 2017-05-02 | Bristol-Myers Squibb Company | IAP antagonists |
| US20150259288A1 (en) | 2014-03-14 | 2015-09-17 | City Of Hope | 5-bromo-indirubins |
| KR102320082B1 (ko) * | 2014-04-14 | 2021-10-29 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, 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 |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| 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 |
| 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 |
| MX385750B (es) | 2015-03-18 | 2025-03-18 | Arvinas Inc | Compuestos y métodos para la degradación mejorada de proteinas específicas. |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| KR20250171392A (ko) * | 2015-06-04 | 2025-12-08 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드계 조절인자 및 관련된 이용 방법 |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | 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 |
| CA2988430A1 (en) | 2015-07-10 | 2017-01-19 | Arvinas, Inc. | Mdm2-based modulators of proteolysis and associated methods of use |
| EP3322986A4 (en) | 2015-07-13 | 2018-09-05 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| WO2017024317A2 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CN108350062B (zh) | 2015-08-06 | 2022-10-14 | 达纳-法伯癌症研究所股份有限公司 | 靶向蛋白降解以减弱过继性t细胞疗法相关的不良炎症反应 |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| GB201516243D0 (en) | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US9938264B2 (en) * | 2015-11-02 | 2018-04-10 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| JP7264642B2 (ja) | 2016-03-16 | 2023-04-25 | エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド | エフェクターｔ細胞機能を増進するための、セレブロンを標的とする小分子 |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| AU2017254713C1 (en) | 2016-04-22 | 2021-04-29 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of EGFR and methods of use |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| CA3087528C (en) | 2016-09-15 | 2024-01-30 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| HUE070289T2 (hu) | 2016-10-11 | 2025-05-28 | Arvinas Operations Inc | Vegyületek és módszerek az androgénreceptor célzott lebontására |
| JP7286539B2 (ja) | 2016-11-01 | 2023-06-05 | アルビナス・オペレーションズ・インコーポレイテッド | タウタンパク質標的化ｐｒｏｔａｃ、および関連使用方法 |
| EP3544957B1 (en) | 2016-11-22 | 2024-05-29 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use |
| BR112019011200B1 (pt) | 2016-12-01 | 2021-12-28 | Arvinas Operations, Inc | Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio |
| EP3559002A4 (en) | 2016-12-23 | 2021-02-17 | Arvinas Operations, Inc. | CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE |
| CA3047784A1 (en) * | 2016-12-23 | 2018-06-28 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, 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 |
| WO2018140809A1 (en) | 2017-01-26 | 2018-08-02 | Arvinas, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| CN115974840A (zh) | 2017-01-31 | 2023-04-18 | 阿尔维纳斯运营股份有限公司 | 人小脑蛋白配体和包含其的双官能化合物 |
| AU2018219289A1 (en) | 2017-02-08 | 2019-09-05 | Dana-Farber Cancer Institute, Inc. | Regulating chimeric antigen receptors |
| JP2020518660A (ja) | 2017-04-28 | 2020-06-25 | クォーツ セラピューティクス，インコーポレイティド | Ｒａｆ分解性結合体化合物 |
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- 2017-12-22 CA CA3047784A patent/CA3047784A1/en active Pending
- 2017-12-22 WO PCT/US2017/068322 patent/WO2018119448A1/en not_active Ceased
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