CA3036841A1 - Fused 1,4-diazepines as bet protein degraders - Google Patents
Fused 1,4-diazepines as bet protein degraders Download PDFInfo
- Publication number
- CA3036841A1 CA3036841A1 CA3036841A CA3036841A CA3036841A1 CA 3036841 A1 CA3036841 A1 CA 3036841A1 CA 3036841 A CA3036841 A CA 3036841A CA 3036841 A CA3036841 A CA 3036841A CA 3036841 A1 CA3036841 A1 CA 3036841A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- pharmaceutically acceptable
- group
- acceptable salt
- cancer
- 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.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- C07K5/06—Dipeptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3036841A1 true CA3036841A1 (en) | 2018-03-22 |
Family
ID=60002003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3036841A Pending CA3036841A1 (en) | 2016-09-13 | 2017-09-13 | Fused 1,4-diazepines as bet protein degraders |
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 |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic 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 |
| US11046709B2 (en) * | 2017-02-03 | 2021-06-29 | 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 |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | 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 |
| 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 |
| KR20210018199A (ko) | 2018-03-26 | 2021-02-17 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스의 분해를 위한 세레블론 결합제 |
| JP7367908B2 (ja) * | 2018-04-09 | 2023-10-24 | 上海科技大学 | 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用 |
| JP2021521192A (ja) * | 2018-04-13 | 2021-08-26 | 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. | セレブロンリガンドおよび同リガンドを含む二機能性化合物 |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| AU2019261938B2 (en) * | 2018-04-30 | 2024-06-13 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of polybromo-1 (PBRM1) |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| WO2020009176A1 (ja) * | 2018-07-04 | 2020-01-09 | 田辺三菱製薬株式会社 | Bet蛋白質分解誘導作用を有するアミド化合物及びその医薬としての用途 |
| 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 |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| EP3841098A4 (en) | 2018-08-22 | 2022-05-04 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHOD OF USE |
| CA3119343C (en) | 2018-11-13 | 2024-01-16 | Biotheryx, Inc. | Substituted isoindolinones |
| CN113453679B (zh) | 2018-12-20 | 2025-07-08 | C4医药公司 | 靶向蛋白降解 |
| JP7548992B2 (ja) | 2019-07-17 | 2024-09-10 | 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化合物および関連する使用方法 |
| MX2022004526A (es) | 2019-10-17 | 2022-07-21 | Arvinas Operations Inc | Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6. |
| 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 |
| 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 |
| EP4114392A4 (en) | 2020-03-05 | 2024-04-10 | C4 Therapeutics, Inc. | Compounds for targeted degradation of brd9 |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| 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 |
| CN116802180B (zh) * | 2021-01-22 | 2024-05-28 | 泰比棣医药科技(石家庄)有限公司 | 一种降解脱氧核糖核酸(dna)聚合酶的化合物及其用途 |
| JP2024515619A (ja) | 2021-04-16 | 2024-04-10 | アルビナス・オペレーションズ・インコーポレイテッド | Bcl6タンパク質分解の調節因子および関連する使用方法 |
| JP2024529298A (ja) | 2021-07-09 | 2024-08-06 | プレキシウム インコーポレイテッド | Ikzf2を調節するアリール化合物及び医薬組成物 |
| 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 |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | 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 |
| 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 |
| WO2025011624A1 (en) * | 2023-07-11 | 2025-01-16 | Etern Biopharma (Shanghai) Co., Ltd. | Bifunctional compounds for androgen receptor degradation and methods of use |
| WO2025096855A1 (en) | 2023-11-02 | 2025-05-08 | Kumquat Biosciences Inc. | Degraders and uses thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO1982001011A1 (en) | 1980-09-24 | 1982-04-01 | Corp Cetus | Diagnostic method and probe |
| US4582788A (en) | 1982-01-22 | 1986-04-15 | Cetus Corporation | HLA typing method and cDNA probes used therein |
| EP0084796B1 (en) | 1982-01-22 | 1990-05-02 | 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 |
| ATE227727T1 (de) | 1996-09-13 | 2002-11-15 | Mitsubishi Pharma Corp | Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen |
| FR2843126B1 (fr) | 2002-08-01 | 2006-01-27 | Cis Bio Int | "methode de determination d'une activite enzymatique endoglycosidase" |
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-
2017
- 2017-09-13 WO PCT/US2017/051286 patent/WO2018052949A1/en not_active Ceased
- 2017-09-13 CA CA3036841A patent/CA3036841A1/en active Pending
- 2017-09-13 ES ES17778012T patent/ES2857743T3/es active Active
- 2017-09-13 EP EP20216642.7A patent/EP3858837A1/en not_active Withdrawn
- 2017-09-13 JP JP2019513958A patent/JP7035027B2/ja not_active Expired - Fee Related
- 2017-09-13 EP EP17778012.9A patent/EP3512853B1/en not_active Not-in-force
- 2017-09-13 AU AU2017326175A patent/AU2017326175B2/en not_active Ceased
- 2017-09-13 US US16/332,544 patent/US10975093B2/en active Active
- 2017-09-13 CN CN201780069335.0A patent/CN110072866A/zh active Pending
-
2021
- 2021-04-12 US US17/227,641 patent/US20220356192A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20220356192A1 (en) | 2022-11-10 |
| EP3512853A1 (en) | 2019-07-24 |
| AU2017326175B2 (en) | 2022-01-27 |
| CN110072866A (zh) | 2019-07-30 |
| US10975093B2 (en) | 2021-04-13 |
| JP7035027B2 (ja) | 2022-03-14 |
| ES2857743T3 (es) | 2021-09-29 |
| EP3512853B1 (en) | 2020-12-23 |
| WO2018052949A1 (en) | 2018-03-22 |
| AU2017326175A1 (en) | 2019-04-04 |
| EP3858837A1 (en) | 2021-08-04 |
| JP2019526616A (ja) | 2019-09-19 |
| US20190263827A1 (en) | 2019-08-29 |
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| EEER | Examination request |
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