IL262139B - Bet protein degraders - Google Patents
Bet protein degradersInfo
- Publication number
- IL262139B IL262139B IL262139A IL26213918A IL262139B IL 262139 B IL262139 B IL 262139B IL 262139 A IL262139 A IL 262139A IL 26213918 A IL26213918 A IL 26213918A IL 262139 B IL262139 B IL 262139B
- Authority
- IL
- Israel
- Prior art keywords
- bet protein
- protein degraders
- degraders
- bet
- protein
- Prior art date
Links
- 239000001064 degrader Substances 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662321499P | 2016-04-12 | 2016-04-12 | |
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| PCT/US2017/026278 WO2017180417A1 (en) | 2016-04-12 | 2017-04-06 | Bet protein degraders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL262139A IL262139A (en) | 2018-11-29 |
| IL262139B true IL262139B (en) | 2021-05-31 |
Family
ID=58548921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL262139A IL262139B (en) | 2016-04-12 | 2018-10-04 | Bet protein degraders |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10633386B2 (enExample) |
| EP (1) | EP3442976B1 (enExample) |
| JP (1) | JP7072519B2 (enExample) |
| KR (1) | KR20180132861A (enExample) |
| CN (1) | CN109311890B (enExample) |
| AU (1) | AU2017250076B2 (enExample) |
| BR (1) | BR112018070859A2 (enExample) |
| CA (1) | CA3020541A1 (enExample) |
| IL (1) | IL262139B (enExample) |
| MX (1) | MX384905B (enExample) |
| RU (1) | RU2752677C2 (enExample) |
| SG (1) | SG11201808729WA (enExample) |
| UA (1) | UA123168C2 (enExample) |
| WO (1) | WO2017180417A1 (enExample) |
| ZA (1) | ZA201806969B (enExample) |
Families Citing this family (46)
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| AU2017254713C1 (en) | 2016-04-22 | 2021-04-29 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of EGFR and methods of use |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | 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 |
| WO2017223452A1 (en) * | 2016-06-23 | 2017-12-28 | 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 |
| 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 |
| 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 |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| WO2019094773A1 (en) * | 2017-11-10 | 2019-05-16 | 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 |
| EP3773576A4 (en) | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| JP7472103B2 (ja) | 2018-08-22 | 2024-04-22 | クルゲン(シャンハイ),インク. | 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 |
| 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 |
| AU2019348094B2 (en) * | 2018-09-30 | 2022-12-22 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Isoindoline compound, preparation method, pharmaceutical composition and use thereof |
| 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 |
| EP3908291A4 (en) * | 2019-01-07 | 2023-01-11 | Dana-Farber Cancer Institute, Inc. | SMALL MOLECULAR DEGRADERS OF FKBP12 VIA RECRUITMENT OF THE VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) AND USE IN DTAG SYSTEMS |
| KR20210118884A (ko) * | 2019-01-22 | 2021-10-01 | 메르크 파텐트 게엠베하 | 헤테로시클릭 유도체 |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | 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 |
| CN120623106A (zh) * | 2019-09-30 | 2025-09-12 | 协和麒麟株式会社 | Bet降解剂 |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| EP4110772A4 (en) | 2020-02-26 | 2024-04-03 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE |
| TW202146412A (zh) | 2020-03-05 | 2021-12-16 | 美商C4醫藥公司 | 用於標靶降解brd9之化合物 |
| 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 |
| IL300397A (en) | 2020-08-05 | 2023-04-01 | C4 Therapeutics Inc | Compounds for targeted knockdown 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 |
| TW202309039A (zh) | 2021-05-05 | 2023-03-01 | 美商百健Ma公司 | 用於靶向布魯頓氏酪胺酸激酶降解之化合物 |
| 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 |
| EP4367113A1 (en) | 2021-07-07 | 2024-05-15 | Biogen MA Inc. | Compounds for targeting degradation of irak4 proteins |
| US20250018046A1 (en) | 2021-07-07 | 2025-01-16 | Biogen Ma Inc | Compounds for targeting degradation of irak4 proteins |
| JP2025521686A (ja) | 2022-06-27 | 2025-07-10 | リレー セラピューティクス, インコーポレイテッド | エストロゲン受容体アルファ分解剤及びその使用 |
| 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 |
| PE20252789A1 (es) | 2023-05-24 | 2025-12-22 | Kumquat Biosciences Inc | Compuestos heterociclicos y usos de estos |
| CN121263417A (zh) | 2023-06-30 | 2026-01-02 | 金橘生物科技公司 | 取代的稠合三环胺化合物及其作为ras抑制剂的用途 |
| 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 |
| AU2024374420A1 (en) | 2023-11-02 | 2026-04-16 | Kumquat Biosciences Inc. | Degraders and uses thereof |
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-
2017
- 2017-04-06 KR KR1020187032621A patent/KR20180132861A/ko not_active Abandoned
- 2017-04-06 WO PCT/US2017/026278 patent/WO2017180417A1/en not_active Ceased
- 2017-04-06 AU AU2017250076A patent/AU2017250076B2/en not_active Ceased
- 2017-04-06 CA CA3020541A patent/CA3020541A1/en active Pending
- 2017-04-06 US US16/093,160 patent/US10633386B2/en active Active
- 2017-04-06 MX MX2018012379A patent/MX384905B/es unknown
- 2017-04-06 RU RU2018139537A patent/RU2752677C2/ru active
- 2017-04-06 JP JP2018553365A patent/JP7072519B2/ja not_active Expired - Fee Related
- 2017-04-06 BR BR112018070859A patent/BR112018070859A2/pt not_active IP Right Cessation
- 2017-04-06 SG SG11201808729WA patent/SG11201808729WA/en unknown
- 2017-04-06 CN CN201780036434.9A patent/CN109311890B/zh not_active Expired - Fee Related
- 2017-04-06 EP EP17717993.4A patent/EP3442976B1/en active Active
- 2017-04-06 UA UAA201811059A patent/UA123168C2/uk unknown
-
2018
- 2018-10-04 IL IL262139A patent/IL262139B/en active IP Right Grant
- 2018-10-18 ZA ZA2018/06969A patent/ZA201806969B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2019511528A (ja) | 2019-04-25 |
| JP7072519B2 (ja) | 2022-05-20 |
| MX384905B (es) | 2025-03-14 |
| CN109311890A (zh) | 2019-02-05 |
| AU2017250076B2 (en) | 2021-07-22 |
| IL262139A (en) | 2018-11-29 |
| ZA201806969B (en) | 2019-12-18 |
| US10633386B2 (en) | 2020-04-28 |
| UA123168C2 (uk) | 2021-02-24 |
| BR112018070859A2 (pt) | 2019-02-05 |
| CN109311890B (zh) | 2021-08-31 |
| US20190169195A1 (en) | 2019-06-06 |
| MX2018012379A (es) | 2019-07-04 |
| RU2752677C2 (ru) | 2021-07-29 |
| RU2018139537A (ru) | 2020-05-14 |
| SG11201808729WA (en) | 2018-11-29 |
| EP3442976A1 (en) | 2019-02-20 |
| RU2018139537A3 (enExample) | 2020-08-11 |
| AU2017250076A1 (en) | 2018-11-08 |
| WO2017180417A1 (en) | 2017-10-19 |
| KR20180132861A (ko) | 2018-12-12 |
| CA3020541A1 (en) | 2017-10-19 |
| EP3442976B1 (en) | 2022-07-20 |
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