JP6961684B2 - Betタンパク質分解物質としての縮合1,4−オキサゼピン - Google Patents
Betタンパク質分解物質としての縮合1,4−オキサゼピン Download PDFInfo
- Publication number
- JP6961684B2 JP6961684B2 JP2019513957A JP2019513957A JP6961684B2 JP 6961684 B2 JP6961684 B2 JP 6961684B2 JP 2019513957 A JP2019513957 A JP 2019513957A JP 2019513957 A JP2019513957 A JP 2019513957A JP 6961684 B2 JP6961684 B2 JP 6961684B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- oxazepine
- benzyl
- thieno
- triazolo
- 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.)
- Expired - Fee Related
Links
- 0 B*Ic1c(*)c(C(*)(*C(*)(*)c2nnc(*)[n]2-2)*=*)c-2[s]1 Chemical compound B*Ic1c(*)c(C(*)(*C(*)(*)c2nnc(*)[n]2-2)*=*)c-2[s]1 0.000 description 8
- GWQAYTOUHWBOTG-UHFFFAOYSA-N CCc1n[o]c(C)c1C Chemical compound CCc1n[o]c(C)c1C GWQAYTOUHWBOTG-UHFFFAOYSA-N 0.000 description 2
- AJETYHOJNRQQFC-UHFFFAOYSA-N CC1=[N]=C(COC2)N1c1c2c(Cc2ccccc2)c(C#Cc2c[n](CCCC(Cc(cc3)c(CN(C(CCC(N4)=O)C4=O)C4=O)c4c3F)=C)cn2)[s]1 Chemical compound CC1=[N]=C(COC2)N1c1c2c(Cc2ccccc2)c(C#Cc2c[n](CCCC(Cc(cc3)c(CN(C(CCC(N4)=O)C4=O)C4=O)c4c3F)=C)cn2)[s]1 AJETYHOJNRQQFC-UHFFFAOYSA-N 0.000 description 1
- RXYPXQSKLGGKOL-UHFFFAOYSA-N CN1CCN(C)CC1 Chemical compound CN1CCN(C)CC1 RXYPXQSKLGGKOL-UHFFFAOYSA-N 0.000 description 1
- HUVAAOZUPLEYBH-UHFFFAOYSA-N Cc1c(C)[nH]nc1C Chemical compound Cc1c(C)[nH]nc1C HUVAAOZUPLEYBH-UHFFFAOYSA-N 0.000 description 1
- GGRRWFKQGMXXQS-UHFFFAOYSA-N Cc1c(C)[s]nc1C Chemical compound Cc1c(C)[s]nc1C GGRRWFKQGMXXQS-UHFFFAOYSA-N 0.000 description 1
- PUEJOCVNXNAMGP-UHFFFAOYSA-N Cc1cccc(C(N2C(CCC(N3)=O)C3=O)=O)c1C2=O Chemical compound Cc1cccc(C(N2C(CCC(N3)=O)C3=O)=O)c1C2=O PUEJOCVNXNAMGP-UHFFFAOYSA-N 0.000 description 1
- XGWXDMJKXOJAPJ-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c([s]1)c2c(Cc2ccccc2)c1Br Chemical compound Cc1nnc(COC2)[n]1-c([s]1)c2c(Cc2ccccc2)c1Br XGWXDMJKXOJAPJ-UHFFFAOYSA-N 0.000 description 1
- LGENJTSWXCLCAV-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2c[nH]cn2)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2c[nH]cn2)[s]1 LGENJTSWXCLCAV-UHFFFAOYSA-N 0.000 description 1
- ZTDJXVBUQNJGQF-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2c[nH]nc2)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2c[nH]nc2)[s]1 ZTDJXVBUQNJGQF-UHFFFAOYSA-N 0.000 description 1
- JAHSNRNNJAROFM-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2c[n](CCCC=C)cn2)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2c[n](CCCC=C)cn2)[s]1 JAHSNRNNJAROFM-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662393904P | 2016-09-13 | 2016-09-13 | |
| US62/393,904 | 2016-09-13 | ||
| PCT/US2017/051282 WO2018052945A1 (en) | 2016-09-13 | 2017-09-13 | Fused 1,4-oxazepines as bet protein degraders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019526615A JP2019526615A (ja) | 2019-09-19 |
| JP2019526615A5 JP2019526615A5 (enExample) | 2020-10-22 |
| JP6961684B2 true JP6961684B2 (ja) | 2021-11-05 |
Family
ID=59955689
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019513957A Expired - Fee Related JP6961684B2 (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−オキサゼピン |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11466028B2 (enExample) |
| EP (1) | EP3512855B1 (enExample) |
| JP (1) | JP6961684B2 (enExample) |
| CN (1) | CN110062759B (enExample) |
| AU (1) | AU2017326171B2 (enExample) |
| CA (1) | CA3036834A1 (enExample) |
| WO (1) | WO2018052945A1 (enExample) |
Families Citing this family (33)
| 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 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| EP4483875A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| 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 |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| EP3679027A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Dihydrobenzimidazolones |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| 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 |
| 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 |
| CN110357889B (zh) * | 2018-04-09 | 2022-03-15 | 上海科技大学 | 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用 |
| KR20210003804A (ko) * | 2018-04-13 | 2021-01-12 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레브론 리간드 및 이를 포함하는 2작용성 화합물 |
| 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 |
| 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 |
| 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 |
| WO2020076996A1 (en) * | 2018-10-09 | 2020-04-16 | The Regents Of The University Of California | Covalent targeting of e3 ligases |
| WO2020102195A1 (en) | 2018-11-13 | 2020-05-22 | Biotheryx, Inc. | Substituted isoindolinones |
| WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
| CN119019369A (zh) | 2019-10-17 | 2024-11-26 | 阿尔维纳斯运营股份有限公司 | 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子 |
| KR20220103753A (ko) | 2019-11-19 | 2022-07-22 | 브리스톨-마이어스 스큅 컴퍼니 | 헬리오스 단백질의 억제제로서 유용한 화합물 |
| WO2021126973A1 (en) * | 2019-12-17 | 2021-06-24 | Orionis Biosciences, Inc. | Compounds modulating protein recruitment and/or degradation |
| CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | Compounds for targeted degradation of brd9 |
| CN111499644B (zh) * | 2020-04-24 | 2021-07-20 | 苏州大学 | 咪唑并[1,5-a]喹唑啉-5(4H)-酮类衍生物及其制备方法和用途 |
| EP4277901A1 (en) | 2021-01-13 | 2023-11-22 | Monte Rosa Therapeutics, Inc. | Isoindolinone compounds |
| CN112979657A (zh) * | 2021-02-03 | 2021-06-18 | 福建医科大学 | 一种靶向降解Hsp90蛋白的化合物及其制备方法与应用 |
| AR125298A1 (es) | 2021-04-06 | 2023-07-05 | Bristol Myers Squibb Co | Compuestos de oxoisoindolina sustituidos con piridinilo |
| CN118388454A (zh) | 2021-04-16 | 2024-07-26 | 阿尔维纳斯运营股份有限公司 | Bcl6蛋白水解的调节剂和其相关使用方法 |
| CA3226162A1 (en) | 2021-07-09 | 2023-01-12 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| CN116410205B (zh) * | 2021-12-29 | 2024-07-05 | 上海皓元生物医药科技有限公司 | 一种3-取代-9-甲基-噻吩并三唑并噁嗪类化合物的制备方法 |
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| DE69717160T2 (de) | 1996-09-13 | 2003-05-08 | Mitsubishi Pharma Corp., Osaka | Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen |
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| 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 |
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| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| ES2882066T3 (es) * | 2016-02-15 | 2021-12-01 | Univ Michigan Regents | 1,4-oxazepinas fusionadas y análogos relacionados como inhibidores de bromodominio BET |
| JP7001614B2 (ja) * | 2016-04-06 | 2022-02-03 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | リガンド依存性の標的タンパク質分解のための単官能性中間体 |
| EP4483875A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
-
2017
- 2017-09-13 AU AU2017326171A patent/AU2017326171B2/en not_active Ceased
- 2017-09-13 EP EP17772214.7A patent/EP3512855B1/en active Active
- 2017-09-13 US US16/332,533 patent/US11466028B2/en active Active
- 2017-09-13 CN CN201780069396.7A patent/CN110062759B/zh not_active Expired - Fee Related
- 2017-09-13 JP JP2019513957A patent/JP6961684B2/ja not_active Expired - Fee Related
- 2017-09-13 CA CA3036834A patent/CA3036834A1/en active Pending
- 2017-09-13 WO PCT/US2017/051282 patent/WO2018052945A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| AU2017326171B2 (en) | 2021-12-09 |
| CN110062759A (zh) | 2019-07-26 |
| JP2019526615A (ja) | 2019-09-19 |
| US20210284657A1 (en) | 2021-09-16 |
| CA3036834A1 (en) | 2018-03-22 |
| EP3512855A1 (en) | 2019-07-24 |
| US11466028B2 (en) | 2022-10-11 |
| AU2017326171A1 (en) | 2019-04-04 |
| EP3512855B1 (en) | 2022-07-27 |
| WO2018052945A1 (en) | 2018-03-22 |
| CN110062759B (zh) | 2022-05-24 |
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