KR20180132861A - Bet 단백질 분해제 - Google Patents
Bet 단백질 분해제 Download PDFInfo
- Publication number
- KR20180132861A KR20180132861A KR1020187032621A KR20187032621A KR20180132861A KR 20180132861 A KR20180132861 A KR 20180132861A KR 1020187032621 A KR1020187032621 A KR 1020187032621A KR 20187032621 A KR20187032621 A KR 20187032621A KR 20180132861 A KR20180132861 A KR 20180132861A
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutically acceptable
- compound
- solvate
- acceptable salt
- group
- 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.)
- Abandoned
Links
- 0 Cc1n[o]c(C)c1C(C=C(C1C2)Nc3c1c(*)nc(C(N*)=O)n3)=C2OC Chemical compound Cc1n[o]c(C)c1C(C=C(C1C2)Nc3c1c(*)nc(C(N*)=O)n3)=C2OC 0.000 description 15
- DNHOYQWUALLLAC-UHFFFAOYSA-N CC(C)(C)OC(NCCCC#Cc1cccc2c1CN(C(CCC(N1)=O)C1=O)C2=O)=O Chemical compound CC(C)(C)OC(NCCCC#Cc1cccc2c1CN(C(CCC(N1)=O)C1=O)C2=O)=O DNHOYQWUALLLAC-UHFFFAOYSA-N 0.000 description 1
- WHHYAYNALHPDGJ-UHFFFAOYSA-N CC(C)(C)OC(NCCCOCCOCCOCCCN)=O Chemical compound CC(C)(C)OC(NCCCOCCOCCOCCCN)=O WHHYAYNALHPDGJ-UHFFFAOYSA-N 0.000 description 1
- QMKUVSASETXPPR-UHFFFAOYSA-N CC(C)(C)OC(NCCOCCOCCOCCOc(cccc1C(N2C(CCC(N3)=O)C3=O)=O)c1C2=O)=O Chemical compound CC(C)(C)OC(NCCOCCOCCOCCOc(cccc1C(N2C(CCC(N3)=O)C3=O)=O)c1C2=O)=O QMKUVSASETXPPR-UHFFFAOYSA-N 0.000 description 1
- YOKAOKGGWYZBQK-UHFFFAOYSA-N CCOC(C(c1cc(OC)c(C2C(C)=NOC2C)cc1[N+]([O-])=O)C#N)=O Chemical compound CCOC(C(c1cc(OC)c(C2C(C)=NOC2C)cc1[N+]([O-])=O)C#N)=O YOKAOKGGWYZBQK-UHFFFAOYSA-N 0.000 description 1
- DSICVZUZCUHARI-UHFFFAOYSA-N CC[n]1nc(C2CC2)cc1Nc1nc(C(O)=O)nc2c1c(cc(c(-c1c(C)[o]nc1C)c1)OC)c1[nH]2 Chemical compound CC[n]1nc(C2CC2)cc1Nc1nc(C(O)=O)nc2c1c(cc(c(-c1c(C)[o]nc1C)c1)OC)c1[nH]2 DSICVZUZCUHARI-UHFFFAOYSA-N 0.000 description 1
- FOSBAOWYMPDSMM-UHFFFAOYSA-N COc(c(Br)c1CC2[O]=N2)cc(F)c1[N+]([O-])=O Chemical compound COc(c(Br)c1CC2[O]=N2)cc(F)c1[N+]([O-])=O FOSBAOWYMPDSMM-UHFFFAOYSA-N 0.000 description 1
- UNVMVTXWKBUDDZ-UHFFFAOYSA-N Cc1n[o]c(C)c1C(C1)C1O Chemical compound Cc1n[o]c(C)c1C(C1)C1O UNVMVTXWKBUDDZ-UHFFFAOYSA-N 0.000 description 1
- ZZXXBKHLDNFHCQ-UHFFFAOYSA-N NCCCCCc1c(CN(C(CCC(N2)=O)C2=O)C2=O)c2ccc1 Chemical compound NCCCCCc1c(CN(C(CCC(N2)=O)C2=O)C2=O)c2ccc1 ZZXXBKHLDNFHCQ-UHFFFAOYSA-N 0.000 description 1
- SCZFMUWTABGOGF-UHFFFAOYSA-N O=C(c1cccc(Br)c1C1)N1C(CCC(N1)=O)C1=O Chemical compound O=C(c1cccc(Br)c1C1)N1C(CCC(N1)=O)C1=O SCZFMUWTABGOGF-UHFFFAOYSA-N 0.000 description 1
- LRGLFYOYKPSPJQ-UHFFFAOYSA-N OC(CNc1cccc(C(N2C(CCC(N3)=O)C3=O)=O)c1C2=O)=O Chemical compound OC(CNc1cccc(C(N2C(CCC(N3)=O)C3=O)=O)c1C2=O)=O LRGLFYOYKPSPJQ-UHFFFAOYSA-N 0.000 description 1
Images
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)
- 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)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662321499P | 2016-04-12 | 2016-04-12 | |
| US62/321,499 | 2016-04-12 | ||
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| US62/393,888 | 2016-09-13 | ||
| PCT/US2017/026278 WO2017180417A1 (en) | 2016-04-12 | 2017-04-06 | Bet protein degraders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20180132861A true KR20180132861A (ko) | 2018-12-12 |
Family
ID=58548921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187032621A Abandoned KR20180132861A (ko) | 2016-04-12 | 2017-04-06 | Bet 단백질 분해제 |
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 (45)
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| 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 |
| 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 |
| US11285218B2 (en) * | 2016-06-23 | 2022-03-29 | 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 |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| 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 |
| 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 |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| CA3082077A1 (en) * | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l degraders 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 |
| 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 |
| 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 |
| US12065442B2 (en) | 2018-08-22 | 2024-08-20 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| 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 |
| WO2020064002A1 (zh) * | 2018-09-30 | 2020-04-02 | 中国科学院上海药物研究所 | 异吲哚啉类化合物、其制备方法、药物组合物及用途 |
| WO2020076996A1 (en) * | 2018-10-09 | 2020-04-16 | The Regents Of The University Of California | Covalent targeting of e3 ligases |
| WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| WO2020146250A1 (en) * | 2019-01-07 | 2020-07-16 | Dana-Farber Cancer Institute, Inc. | SMALL MOLECULE DEGRADERS OF FKBP12 VIA RECRUITMENT OF VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) E3 UBIQUITIN LIGASE, AND USES IN dTAG SYSTEMS |
| BR112021014220A2 (pt) * | 2019-01-22 | 2022-01-18 | Merck Patent Gmbh | Derivados heterocíclicos |
| KR102758231B1 (ko) * | 2019-06-12 | 2025-01-23 | 상하이테크 유니버시티 | Alk 단백질 조절제 및 이의 항종양 용도 |
| AU2020360170A1 (en) * | 2019-09-30 | 2022-05-19 | Kyowa Kirin Co., Ltd. | Bet degrader |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US12410171B2 (en) | 2020-02-26 | 2025-09-09 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | Compounds for targeted degradation of brd9 |
| 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 |
| CA3188313A1 (en) | 2020-08-05 | 2022-02-10 | C4 Therapeutics, Inc. | Compounds for targeted degradation 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 |
| EP4333899A1 (en) | 2021-05-05 | 2024-03-13 | Biogen MA Inc. | Compounds for targeting degradation of bruton's tyrosine kinase |
| 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 |
| KR20240035526A (ko) | 2021-07-07 | 2024-03-15 | 바이오젠 엠에이 인코포레이티드 | Irak4 단백질의 분해를 표적하는 화합물 |
| US20250018046A1 (en) | 2021-07-07 | 2025-01-16 | Biogen Ma Inc | Compounds for targeting degradation of irak4 proteins |
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| CN105121407B (zh) * | 2013-02-28 | 2017-07-18 | 美国安进公司 | 用于治疗癌症的苯甲酸衍生物mdm2抑制剂 |
| CN105377851B (zh) | 2013-03-11 | 2018-07-20 | 密执安州立大学董事会 | Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法 |
| WO2015131005A1 (en) * | 2014-02-28 | 2015-09-03 | The Regents Of The University Of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| JP6778114B2 (ja) * | 2014-04-14 | 2020-10-28 | 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. | イミド系タンパク質分解モジュレーター及び関連する使用方法 |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| EP3262045A1 (en) * | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors |
| US10772962B2 (en) * | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| 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 |
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| UA123168C2 (uk) | 2021-02-24 |
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| IL262139A (en) | 2018-11-29 |
| US20190169195A1 (en) | 2019-06-06 |
| JP7072519B2 (ja) | 2022-05-20 |
| RU2018139537A (ru) | 2020-05-14 |
| RU2752677C2 (ru) | 2021-07-29 |
| MX2018012379A (es) | 2019-07-04 |
| CN109311890B (zh) | 2021-08-31 |
| MX384905B (es) | 2025-03-14 |
| CA3020541A1 (en) | 2017-10-19 |
| JP2019511528A (ja) | 2019-04-25 |
| US10633386B2 (en) | 2020-04-28 |
| EP3442976B1 (en) | 2022-07-20 |
| BR112018070859A2 (pt) | 2019-02-05 |
| WO2017180417A1 (en) | 2017-10-19 |
| AU2017250076B2 (en) | 2021-07-22 |
| CN109311890A (zh) | 2019-02-05 |
| AU2017250076A1 (en) | 2018-11-08 |
| EP3442976A1 (en) | 2019-02-20 |
| IL262139B (en) | 2021-05-31 |
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