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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Communicable Diseases (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) |
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| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| CN121974842A (zh) | 2016-05-10 | 2026-05-05 | 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 |
| EP4717317A3 (en) | 2017-06-20 | 2026-06-03 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| 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 |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| CN111902141A (zh) | 2018-03-26 | 2020-11-06 | C4医药公司 | 用于ikaros降解的羟脑苷脂结合剂 |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| EP3778590A4 (en) | 2018-04-09 | 2021-12-22 | ShanghaiTech University | ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE |
| CA3095912A1 (en) * | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| 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 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| CN120468320A (zh) * | 2018-10-09 | 2025-08-12 | 加利福尼亚大学董事会 | E3连接酶的共价靶向 |
| JP2022507267A (ja) | 2018-11-13 | 2022-01-18 | バイオセリックス, インコーポレイテッド | 置換イソインドリノン |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| EP3932922A4 (en) | 2019-02-25 | 2022-05-11 | ShanghaiTech University | SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | C4 Therapeutics Inc | Heterocyclic compounds for medical treatment |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| WO2021023233A1 (zh) | 2019-08-05 | 2021-02-11 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| 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. |
| JP7629459B2 (ja) | 2019-11-19 | 2025-02-13 | ブリストル-マイヤーズ スクイブ カンパニー | Heliosタンパク質の阻害剤として有用な化合物 |
| JP7871189B2 (ja) * | 2019-12-17 | 2026-06-08 | 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/または分解を調節する化合物 |
| CN119823124A (zh) | 2020-03-05 | 2025-04-15 | C4医药公司 | 用于brd9的靶向降解的化合物 |
| TW202140441A (zh) | 2020-03-23 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 經取代之側氧基異吲哚啉化合物 |
| 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 |
| CN117242060B (zh) | 2021-01-13 | 2026-07-17 | 蒙特罗莎治疗股份有限公司 | 异吲哚啉酮化合物 |
| 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 |
| PE20231941A1 (es) | 2021-04-06 | 2023-12-05 | 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 |
| TW202317546A (zh) | 2021-07-09 | 2023-05-01 | 美商普萊克斯姆公司 | 調節ikzf2之芳基化合物及醫藥組合物 |
| 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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| 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 |
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| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| CA3014644A1 (en) * | 2016-02-15 | 2017-08-24 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors |
| EP3440082A1 (en) * | 2016-04-06 | 2019-02-13 | The Regents of The University of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
-
2017
- 2017-09-13 CA CA3036834A patent/CA3036834A1/en active Pending
- 2017-09-13 AU AU2017326171A patent/AU2017326171B2/en not_active Ceased
- 2017-09-13 CN CN201780069396.7A patent/CN110062759B/zh not_active Expired - Fee Related
- 2017-09-13 WO PCT/US2017/051282 patent/WO2018052945A1/en not_active Ceased
- 2017-09-13 US US16/332,533 patent/US11466028B2/en active Active
- 2017-09-13 JP JP2019513957A patent/JP6961684B2/ja not_active Expired - Fee Related
- 2017-09-13 EP EP17772214.7A patent/EP3512855B1/en not_active Not-in-force
Also Published As
| Publication number | Publication date |
|---|---|
| EP3512855B1 (en) | 2022-07-27 |
| US11466028B2 (en) | 2022-10-11 |
| US20210284657A1 (en) | 2021-09-16 |
| JP2019526615A (ja) | 2019-09-19 |
| CN110062759A (zh) | 2019-07-26 |
| AU2017326171B2 (en) | 2021-12-09 |
| WO2018052945A1 (en) | 2018-03-22 |
| EP3512855A1 (en) | 2019-07-24 |
| CA3036834A1 (en) | 2018-03-22 |
| CN110062759B (zh) | 2022-05-24 |
| AU2017326171A1 (en) | 2019-04-04 |
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