JP2019511528A5 - - Google Patents
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- JP2019511528A5 JP2019511528A5 JP2018553365A JP2018553365A JP2019511528A5 JP 2019511528 A5 JP2019511528 A5 JP 2019511528A5 JP 2018553365 A JP2018553365 A JP 2018553365A JP 2018553365 A JP2018553365 A JP 2018553365A JP 2019511528 A5 JP2019511528 A5 JP 2019511528A5
- Authority
- JP
- Japan
- Prior art keywords
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- pharmaceutically acceptable
- acceptable salt
- solvate
- formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 0 **1C(*)=*C=C1* Chemical compound **1C(*)=*C=C1* 0.000 description 6
- LCNLCZYJDNFGLE-UHFFFAOYSA-N CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(C(NCCOCCOCCOCCOCCOCCOCCOCCNc(cccc2C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)=O)n1 Chemical compound CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(C(NCCOCCOCCOCCOCCOCCOCCOCCNc(cccc2C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)=O)n1 LCNLCZYJDNFGLE-UHFFFAOYSA-N 0.000 description 1
- KELXSFPNQGNTTJ-UHFFFAOYSA-N CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(CNCCCCNc2cccc(C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)n1 Chemical compound CC[n]1nc(C2CC2)cc1Nc1c(c(c([nH]2)c3)cc(OC)c3-c3c(C)[o]nc3C)c2nc(CNCCCCNc2cccc(C(N3C(CCC(N4)=O)C4=O)=O)c2C3=O)n1 KELXSFPNQGNTTJ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662321499P | 2016-04-12 | 2016-04-12 | |
| US62/321,499 | 2016-04-12 | ||
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| US62/393,888 | 2016-09-13 | ||
| PCT/US2017/026278 WO2017180417A1 (en) | 2016-04-12 | 2017-04-06 | Bet protein degraders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019511528A JP2019511528A (ja) | 2019-04-25 |
| JP2019511528A5 true JP2019511528A5 (https=) | 2020-05-14 |
| JP7072519B2 JP7072519B2 (ja) | 2022-05-20 |
Family
ID=58548921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018553365A Expired - Fee Related JP7072519B2 (ja) | 2016-04-12 | 2017-04-06 | Ｂｅｔタンパク質分解剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10633386B2 (https=) |
| EP (1) | EP3442976B1 (https=) |
| JP (1) | JP7072519B2 (https=) |
| KR (1) | KR20180132861A (https=) |
| CN (1) | CN109311890B (https=) |
| AU (1) | AU2017250076B2 (https=) |
| BR (1) | BR112018070859A2 (https=) |
| CA (1) | CA3020541A1 (https=) |
| IL (1) | IL262139B (https=) |
| MX (1) | MX384905B (https=) |
| RU (1) | RU2752677C2 (https=) |
| SG (1) | SG11201808729WA (https=) |
| UA (1) | UA123168C2 (https=) |
| WO (1) | WO2017180417A1 (https=) |
| ZA (1) | ZA201806969B (https=) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3445357B1 (en) | 2016-04-22 | 2021-05-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| 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 |
| 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 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| 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 |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| CN109422751B (zh) * | 2017-09-03 | 2022-04-22 | 上海美志医药科技有限公司 | 一类具有降解酪氨酸蛋白激酶jak3活性的化合物 |
| CN118206529A (zh) | 2017-09-04 | 2024-06-18 | C4医药公司 | 二氢苯并咪唑酮 |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| CN111278816B (zh) | 2017-09-04 | 2024-03-15 | C4医药公司 | 二氢喹啉酮 |
| WO2019094772A1 (en) * | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l degraders and methods of treatment therewith |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| 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 |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| 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 |
| WO2020051235A1 (en) | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| KR102672549B1 (ko) * | 2018-09-30 | 2024-06-10 | 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 | 이소인돌린계 화합물, 이의 제조 방법, 약학 조성물 및 용도 |
| EP3863642A4 (en) * | 2018-10-09 | 2022-06-29 | The Regents of the University of California | Covalent targeting of e3 ligases |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| US20220089589A1 (en) * | 2019-01-07 | 2022-03-24 | Dana-Farber Cancer Institute, Inc. | SMALL MOLECULE DEGRADERS OF FKBP12 VIA RECRUITMENT OF VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) E3 UBIQUITIN LIGASE, AND USES IN dTAG SYSTEMS |
| ES2934986T3 (es) * | 2019-01-22 | 2023-02-28 | Merck Patent Gmbh | Derivados heterocíclicos |
| WO2020181232A1 (en) | 2019-03-06 | 2020-09-10 | C4 Therapeutics, Inc. | Heterocyclic compounds for medical treatment |
| KR102758231B1 (ko) * | 2019-06-12 | 2025-01-23 | 상하이테크 유니버시티 | Alk 단백질 조절제 및 이의 항종양 용도 |
| TW202126638A (zh) * | 2019-09-30 | 2021-07-16 | 日商協和麒麟股份有限公司 | Bet分解劑 |
| 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 |
| AU2021231898A1 (en) | 2020-03-05 | 2022-10-27 | C4 Therapeutics, Inc. | Compounds for targeted degradation of BRD9 |
| CN113387932B (zh) * | 2020-03-14 | 2023-05-09 | 成都先导药物开发股份有限公司 | 一种诱导brd4蛋白降解的双功能化合物 |
| CN112920176B (zh) * | 2020-05-25 | 2022-11-04 | 四川大学华西医院 | 可诱导prc2蛋白复合物核心亚基降解的双功能化合物和药物组合物及应用 |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| WO2022051616A1 (en) * | 2020-09-03 | 2022-03-10 | Board Of Regents Of The University Of Nebraska | Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras |
| KR20240017814A (ko) | 2021-05-05 | 2024-02-08 | 바이오젠 엠에이 인코포레이티드 | 브루톤 티로신 키나제의 분해를 표적으로 하는 화합물 |
| CN113336801B (zh) * | 2021-06-08 | 2023-08-22 | 中国人民解放军空军军医大学 | 含有bet抑制剂的四价铂配合物与应用 |
| 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 |
| 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 |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| 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 |
| CN116585322B (zh) * | 2023-01-16 | 2023-10-13 | 中山大学中山眼科中心 | Bet蛋白降解剂在预防和治疗视网膜退行性改变相关疾病中的应用 |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| AU2024307234A1 (en) | 2023-06-30 | 2026-01-29 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras 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 |
| WO2025096855A1 (en) | 2023-11-02 | 2025-05-08 | Kumquat Biosciences Inc. | Degraders and uses thereof |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL63907A0 (en) | 1980-09-24 | 1981-12-31 | Cetus Corp | Diagnostic method and antibody probe for use therein |
| ATE53862T1 (de) | 1982-01-22 | 1990-06-15 | Cetus Corp | Verfahren zur charakterisierung von hla und die darin benutzten cdns-testmittel. |
| US4582788A (en) | 1982-01-22 | 1986-04-15 | Cetus Corporation | HLA typing method and cDNA probes used therein |
| US4683194A (en) | 1984-05-29 | 1987-07-28 | Cetus Corporation | Method for detection of polymorphic restriction sites and nucleic acid sequences |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| CA1284931C (en) | 1986-03-13 | 1991-06-18 | Henry A. Erlich | Process for detecting specific nucleotide variations and genetic polymorphisms present in nucleic acids |
| CA1338457C (en) | 1986-08-22 | 1996-07-16 | Henry A. Erlich | Purified thermostable enzyme |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| DE69717160T2 (de) | 1996-09-13 | 2003-05-08 | Mitsubishi Pharma Corp., Osaka | Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen |
| US7091353B2 (en) * | 2000-12-27 | 2006-08-15 | Celgene Corporation | Isoindole-imide compounds, compositions, and uses thereof |
| US20030045552A1 (en) * | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| FR2843126B1 (fr) | 2002-08-01 | 2006-01-27 | Cis Bio Int | "methode de determination d'une activite enzymatique endoglycosidase" |
| EP1887008B1 (en) | 2005-05-30 | 2021-04-21 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and a medicinal use thereof |
| WO2008092231A1 (en) | 2007-02-01 | 2008-08-07 | Resverlogix Corp. | Compounds for the prevention and treatment of cardiovascular diseases |
| WO2009084693A1 (ja) | 2007-12-28 | 2009-07-09 | Mitsubishi Tanabe Pharma Corporation | 抗癌剤 |
| KR101629356B1 (ko) | 2008-06-26 | 2016-06-13 | 리스버로직스 코퍼레이션 | 퀴나졸리논 유도체의 제조방법 |
| PE20110547A1 (es) * | 2008-10-29 | 2011-08-04 | Celgene Corp | Compuestos de isoindolina con actividad anticancerigena |
| KR20190091564A (ko) | 2009-04-22 | 2019-08-06 | 리스버로직스 코퍼레이션 | 신규한 소염제 |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| RS54645B1 (sr) | 2009-11-05 | 2016-08-31 | Glaxosmithkline Llc | Benzodiazepin kao inhibitor bromodomena |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| EP2536706B1 (en) * | 2010-02-11 | 2017-06-14 | Celgene Corporation | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| PL2902030T3 (pl) | 2010-05-14 | 2017-07-31 | Dana-Farber Cancer Institute, Inc. | Związki tienotriazolodiazepinowe do leczenia nowotworu |
| MX354217B (es) | 2010-05-14 | 2018-02-19 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| JO2998B1 (ar) * | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| US9085582B2 (en) | 2010-06-22 | 2015-07-21 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2677865A4 (en) | 2011-02-23 | 2015-04-22 | Icahn School Med Mount Sinai | BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| 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 |
| US20140079636A1 (en) * | 2012-04-16 | 2014-03-20 | Dinesh U. Chimmanamada | Targeted therapeutics |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| EP2838881B1 (en) | 2012-04-20 | 2018-08-08 | AbbVie Inc. | Isoindolone derivatives |
| JP6215315B2 (ja) | 2012-06-12 | 2017-10-18 | アッヴィ・インコーポレイテッド | ピリジノンおよびピリダジノン誘導体 |
| CA2902856C (en) * | 2013-02-28 | 2021-02-16 | Amgen Inc. | A benzoic acid derivative mdm2 inhibitor for the treatment of cancer |
| EP2970312B1 (en) * | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| US9580430B2 (en) * | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| AU2015247817C1 (en) * | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| EP3262045A1 (en) * | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors |
| EP3337476A4 (en) * | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| WO2017176958A1 (en) * | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
-
2017
- 2017-04-06 MX MX2018012379A patent/MX384905B/es unknown
- 2017-04-06 US US16/093,160 patent/US10633386B2/en active Active
- 2017-04-06 UA UAA201811059A patent/UA123168C2/uk unknown
- 2017-04-06 CA CA3020541A patent/CA3020541A1/en active Pending
- 2017-04-06 JP JP2018553365A patent/JP7072519B2/ja not_active Expired - Fee Related
- 2017-04-06 AU AU2017250076A patent/AU2017250076B2/en not_active Ceased
- 2017-04-06 SG SG11201808729WA patent/SG11201808729WA/en unknown
- 2017-04-06 KR KR1020187032621A patent/KR20180132861A/ko not_active Abandoned
- 2017-04-06 CN CN201780036434.9A patent/CN109311890B/zh not_active Expired - Fee Related
- 2017-04-06 BR BR112018070859A patent/BR112018070859A2/pt not_active IP Right Cessation
- 2017-04-06 EP EP17717993.4A patent/EP3442976B1/en active Active
- 2017-04-06 WO PCT/US2017/026278 patent/WO2017180417A1/en not_active Ceased
- 2017-04-06 RU RU2018139537A patent/RU2752677C2/ru active
-
2018
- 2018-10-04 IL IL262139A patent/IL262139B/en active IP Right Grant
- 2018-10-18 ZA ZA2018/06969A patent/ZA201806969B/en unknown
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