CN114599428A - 双功能化合物 - Google Patents
双功能化合物 Download PDFInfo
- Publication number
- CN114599428A CN114599428A CN202080074772.3A CN202080074772A CN114599428A CN 114599428 A CN114599428 A CN 114599428A CN 202080074772 A CN202080074772 A CN 202080074772A CN 114599428 A CN114599428 A CN 114599428A
- Authority
- CN
- China
- Prior art keywords
- formula
- absent
- group
- title compound
- amino
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
- C07D487/08—Bridged systems
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19205545 | 2019-10-28 | ||
| EP19205545.7 | 2019-10-28 | ||
| PCT/US2020/057356 WO2021086785A1 (en) | 2019-10-28 | 2020-10-26 | Bifunctional compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN114599428A true CN114599428A (zh) | 2022-06-07 |
Family
ID=68382246
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080074772.3A Pending CN114599428A (zh) | 2019-10-28 | 2020-10-26 | 双功能化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230002367A1 (https=) |
| EP (1) | EP4054724A4 (https=) |
| JP (1) | JP2023511471A (https=) |
| CN (1) | CN114599428A (https=) |
| WO (1) | WO2021086785A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024002375A1 (zh) * | 2022-06-30 | 2024-01-04 | 甘李药业股份有限公司 | 一种用作smarca2/4抑制剂的化合物及其应用 |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| WO2021133917A1 (en) | 2019-12-23 | 2021-07-01 | Kymera Therapeutics, Inc. | Smarca inhibitors and uses thereof |
| BR112022012410A2 (pt) | 2019-12-23 | 2022-08-30 | Kymera Therapeutics Inc | Degradadores smarca e usos dos mesmos |
| WO2021207291A1 (en) * | 2020-04-06 | 2021-10-14 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| EP4259144A4 (en) * | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| US11993599B2 (en) | 2021-08-09 | 2024-05-28 | Genentech, Inc. | Therapeutic compounds |
| WO2023129506A1 (en) * | 2021-12-28 | 2023-07-06 | Board Of Regents, The University Of Texas System | Potent and selective smarca2 degrading chimeric molecules as cancer therapeutics |
| EP4476225A4 (en) * | 2022-02-09 | 2026-01-14 | Aurigene Oncology Ltd | PYRIDAZINE 3-SUBSTITUTED COMPOUNDS USED AS SMARCA2 AND/OR SMARCA4 DEGRADING AGENTS |
| KR20250023362A (ko) * | 2022-06-15 | 2025-02-18 | 씨4 테라퓨틱스, 인코포레이티드 | Smarca2의 표적화된 분해를 위한 화합물 |
| WO2024064316A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 inhibitors and uses thereof |
| WO2024064328A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 degraders and uses thereof |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| WO2024137742A1 (en) | 2022-12-20 | 2024-06-27 | Blueprint Medicines Corporation | Compounds and compositions as fgfr3 degraders and uses thereof |
| WO2025096976A1 (en) * | 2023-11-01 | 2025-05-08 | Cornell University | Arid1a is a prognostic marker for aggressive lymphoma transformation and presents a vulnerability to pharmacological inhibition of smarca4/2 |
| WO2025129116A1 (en) * | 2023-12-14 | 2025-06-19 | C4 Therapeutics, Inc. | Compounds for the targeted degradation of smarca2 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019195201A1 (en) * | 2018-04-01 | 2019-10-10 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| CN112771038A (zh) * | 2018-04-26 | 2021-05-07 | 奥里吉恩发现科技有限公司 | 作为smarca2/4降解剂的哒嗪衍生物 |
| CN114375192A (zh) * | 2019-09-12 | 2022-04-19 | 奥瑞基尼探索技术有限公司 | 鉴定smarca2/4降解剂的应答者的方法 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019213005A1 (en) * | 2018-04-30 | 2019-11-07 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of polybromo-1 (pbrm1) |
-
2020
- 2020-10-26 JP JP2022523943A patent/JP2023511471A/ja active Pending
- 2020-10-26 EP EP20880820.4A patent/EP4054724A4/en not_active Withdrawn
- 2020-10-26 WO PCT/US2020/057356 patent/WO2021086785A1/en not_active Ceased
- 2020-10-26 US US17/771,127 patent/US20230002367A1/en not_active Abandoned
- 2020-10-26 CN CN202080074772.3A patent/CN114599428A/zh active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019195201A1 (en) * | 2018-04-01 | 2019-10-10 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| CN112771038A (zh) * | 2018-04-26 | 2021-05-07 | 奥里吉恩发现科技有限公司 | 作为smarca2/4降解剂的哒嗪衍生物 |
| CN114375192A (zh) * | 2019-09-12 | 2022-04-19 | 奥瑞基尼探索技术有限公司 | 鉴定smarca2/4降解剂的应答者的方法 |
Non-Patent Citations (3)
| Title |
|---|
| KWOK-HO CHAN，等: "Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 61, no. 2, pages 504 - 513, XP055930443, DOI: 10.1021/acs.jmedchem.6b01912 * |
| SAMUEL H. YALKOWSKY，等: "Correlation and Prediction of Mass Transport across Membranes 11: Influence of Vehicle Polarity on Flux from Solutions and Suspensions", 《JOURNAL OF PHARMACEUTICAL SCIENCES》, vol. 63, no. 8, pages 1276 - 1280 * |
| WILLIAM FARNABY，等: "BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design", 《NAT URE CHEMICA L BIOLOGY》, vol. 15, pages 672, XP036824718, DOI: 10.1038/s41589-019-0294-6 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024002375A1 (zh) * | 2022-06-30 | 2024-01-04 | 甘李药业股份有限公司 | 一种用作smarca2/4抑制剂的化合物及其应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021086785A1 (en) | 2021-05-06 |
| EP4054724A1 (en) | 2022-09-14 |
| US20230002367A1 (en) | 2023-01-05 |
| JP2023511471A (ja) | 2023-03-20 |
| EP4054724A4 (en) | 2023-12-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 40068906 Country of ref document: HK |
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| SE01 | Entry into force of request for substantive examination | ||
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| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20220607 |