JP2019526616A5 - - Google Patents
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- Publication number
- JP2019526616A5 JP2019526616A5 JP2019513958A JP2019513958A JP2019526616A5 JP 2019526616 A5 JP2019526616 A5 JP 2019526616A5 JP 2019513958 A JP2019513958 A JP 2019513958A JP 2019513958 A JP2019513958 A JP 2019513958A JP 2019526616 A5 JP2019526616 A5 JP 2019526616A5
- Authority
- JP
- Japan
- Prior art keywords
- diazepine
- thieno
- triazolo
- chlorophenyl
- ethynyl
- 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
- 0 C*NC1=**=C2*1C(NC(C1NC)=C)=C1C(c1ccccc1)=*C2 Chemical compound C*NC1=**=C2*1C(NC(C1NC)=C)=C1C(c1ccccc1)=*C2 0.000 description 2
- BEIYFCCFKMAEDF-UHFFFAOYSA-N CC1C=CC(C)(C)CC1 Chemical compound CC1C=CC(C)(C)CC1 BEIYFCCFKMAEDF-UHFFFAOYSA-N 0.000 description 1
- CBRVMHNCKYHAOV-UHFFFAOYSA-N CCC1=CN=C(C)CC=C1 Chemical compound CCC1=CN=C(C)CC=C1 CBRVMHNCKYHAOV-UHFFFAOYSA-N 0.000 description 1
- RHOOLJLEYYXKTK-UHFFFAOYSA-N Cc1cnc(C)nc1 Chemical compound Cc1cnc(C)nc1 RHOOLJLEYYXKTK-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662393923P | 2016-09-13 | 2016-09-13 | |
| US62/393,923 | 2016-09-13 | ||
| PCT/US2017/051286 WO2018052949A1 (en) | 2016-09-13 | 2017-09-13 | Fused 1,4-diazepines as bet protein degraders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019526616A JP2019526616A (ja) | 2019-09-19 |
| JP2019526616A5 true JP2019526616A5 (enExample) | 2020-10-22 |
| JP7035027B2 JP7035027B2 (ja) | 2022-03-14 |
Family
ID=60002003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019513958A Expired - Fee Related JP7035027B2 (ja) | 2016-09-13 | 2017-09-13 | Ｂｅｔタンパク質分解物質としての縮合１，４－ジアゼピン |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US10975093B2 (enExample) |
| EP (2) | EP3858837A1 (enExample) |
| JP (1) | JP7035027B2 (enExample) |
| CN (1) | CN110072866A (enExample) |
| AU (1) | AU2017326175B2 (enExample) |
| CA (1) | CA3036841A1 (enExample) |
| ES (1) | ES2857743T3 (enExample) |
| WO (1) | WO2018052949A1 (enExample) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| WO2018144789A1 (en) * | 2017-02-03 | 2018-08-09 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet bromodomain inhibitors |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| EP3679027A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Dihydrobenzimidazolones |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| WO2019099868A2 (en) | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| WO2019191112A1 (en) | 2018-03-26 | 2019-10-03 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| AU2019251151B2 (en) | 2018-04-09 | 2022-07-07 | Shanghaitech University | Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates |
| WO2019199816A1 (en) * | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| CA3093405C (en) * | 2018-04-30 | 2025-06-17 | Dana-Farber Cancer Institute, Inc. | POLYBROMO-1 SMALL MOLECULE DEGRADING AGENTS (PBRM1) |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| AR118784A1 (es) * | 2018-07-04 | 2021-11-03 | Mitsubishi Tanabe Pharma Corp | Compuesto de amida que tiene acción inductora de la degradación de la proteína bet y su uso como medicamento |
| CN110407854B (zh) * | 2018-08-17 | 2020-09-15 | 北京加科思新药研发有限公司 | 新的四环化合物 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| EP3841098A4 (en) | 2018-08-22 | 2022-05-04 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHOD OF USE |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| EP3880669A1 (en) * | 2018-11-13 | 2021-09-22 | Biotheryx, Inc. | Substituted isoindolinones |
| WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 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 |
| EP4045496A1 (en) | 2019-10-17 | 2022-08-24 | Arvinas Operations, Inc. | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| EP4076530A4 (en) * | 2019-12-17 | 2024-04-10 | Orionis Biosciences, Inc. | BIFUNCTIONAL AGENTS FOR RECRUITMENT AND/OR DEGRADATION OF PROTEINS |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CN115697989B (zh) | 2020-02-26 | 2025-03-18 | 上海睿跃生物科技有限公司 | 原肌球蛋白受体激酶(trk)降解化合物和使用方法 |
| CN115279370B (zh) | 2020-03-05 | 2025-01-10 | C4医药公司 | 用于brd9的靶向降解的化合物 |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| EP4277901A1 (en) | 2021-01-13 | 2023-11-22 | Monte Rosa Therapeutics, Inc. | Isoindolinone compounds |
| US20240299557A1 (en) * | 2021-01-22 | 2024-09-12 | Taibidi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | Compound for degrading deoxyribonucleic acid (dna) polymerase, and use thereof |
| AU2022259683A1 (en) | 2021-04-16 | 2023-10-19 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| KR20240035820A (ko) | 2021-07-09 | 2024-03-18 | 플렉시움 인코포레이티드 | Ikzf2를 조절하는 아릴 화합물 및 약학 조성물 |
| CN115611881B (zh) * | 2021-07-13 | 2024-09-20 | 复旦大学 | 一种合成新型vhl配体4-f-vh032的方法 |
| WO2023074780A1 (ja) * | 2021-10-27 | 2023-05-04 | 国立大学法人愛媛大学 | 治療薬組成物 |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| 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 |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| WO2025011624A1 (en) * | 2023-07-11 | 2025-01-16 | Etern Biopharma (Shanghai) Co., Ltd. | Bifunctional compounds for androgen receptor degradation and methods of use |
| TW202523291A (zh) | 2023-11-02 | 2025-06-16 | 美商金橘生物科技公司 | 降解劑及其用途 |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57501692A (enExample) | 1980-09-24 | 1982-09-16 | ||
| EP0084796B1 (en) | 1982-01-22 | 1990-05-02 | Cetus Corporation | Hla typing method and cdna probes used therein |
| 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 |
| GB9614098D0 (en) | 1996-07-05 | 1996-09-04 | Orion Yhtymae Oy | Transdermal delivery of levosimendan |
| WO1998011111A1 (en) | 1996-09-13 | 1998-03-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Thienotriazolodiazepine compounds and medicinal uses thereof |
| FR2843126B1 (fr) | 2002-08-01 | 2006-01-27 | Cis Bio Int | "methode de determination d'une activite enzymatique endoglycosidase" |
| EP1761508A1 (en) * | 2004-06-30 | 2007-03-14 | Wisys Technology Foundation, Inc. | Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects |
| US8044042B2 (en) | 2005-05-30 | 2011-10-25 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and medicinal use thereof |
| KR101444489B1 (ko) | 2007-02-01 | 2014-09-24 | 리스버로직스 코퍼레이션 | 심혈관 질환을 예방 및 치료하기 위한 화합물 |
| EP2239264A4 (en) | 2007-12-28 | 2012-01-11 | Mitsubishi Tanabe Pharma Corp | ANTITUMORAL MEDIUM |
| WO2009158404A1 (en) | 2008-06-26 | 2009-12-30 | Resverlogix Corp. | Methods of preparing quinazolinone derivatives |
| CN107252429B (zh) | 2009-04-22 | 2023-06-16 | 雷斯韦洛吉克斯公司 | 新抗炎剂 |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| ES2654423T3 (es) | 2009-11-05 | 2018-02-13 | Glaxosmithkline Llc | Inhibidor de bromodominio de benzodiacepina |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| US8981083B2 (en) | 2010-05-14 | 2015-03-17 | Dana Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| JP5844358B2 (ja) | 2010-06-22 | 2016-01-13 | グラクソスミスクライン エルエルシー | ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤 |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| EP2677865A4 (en) | 2011-02-23 | 2015-04-22 | Icahn School Med Mount Sinai | BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION |
| US9422292B2 (en) | 2011-05-04 | 2016-08-23 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | 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 |
| 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 |
| WO2013185284A1 (en) | 2012-06-12 | 2013-12-19 | Abbott Laboratories | Pyridinone and pyridazinone derivatives |
| WO2014164596A1 (en) | 2013-03-11 | 2014-10-09 | The Regents Of The University Of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| WO2014159392A1 (en) * | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| 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 |
| KR20250127179A (ko) * | 2014-04-14 | 2025-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| US10759808B2 (en) * | 2016-04-06 | 2020-09-01 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
-
2017
- 2017-09-13 WO PCT/US2017/051286 patent/WO2018052949A1/en not_active Ceased
- 2017-09-13 EP EP20216642.7A patent/EP3858837A1/en not_active Withdrawn
- 2017-09-13 CN CN201780069335.0A patent/CN110072866A/zh active Pending
- 2017-09-13 US US16/332,544 patent/US10975093B2/en active Active
- 2017-09-13 EP EP17778012.9A patent/EP3512853B1/en not_active Not-in-force
- 2017-09-13 ES ES17778012T patent/ES2857743T3/es active Active
- 2017-09-13 JP JP2019513958A patent/JP7035027B2/ja not_active Expired - Fee Related
- 2017-09-13 AU AU2017326175A patent/AU2017326175B2/en not_active Ceased
- 2017-09-13 CA CA3036841A patent/CA3036841A1/en active Pending
-
2021
- 2021-04-12 US US17/227,641 patent/US20220356192A1/en not_active Abandoned
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