KR102604802B1 - 신규 plk1 분해 유도 화합물 - Google Patents
신규 plk1 분해 유도 화합물 Download PDFInfo
- Publication number
- KR102604802B1 KR102604802B1 KR1020227036596A KR20227036596A KR102604802B1 KR 102604802 B1 KR102604802 B1 KR 102604802B1 KR 1020227036596 A KR1020227036596 A KR 1020227036596A KR 20227036596 A KR20227036596 A KR 20227036596A KR 102604802 B1 KR102604802 B1 KR 102604802B1
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- South Korea
- Prior art keywords
- mmol
- methyl
- cancer
- mixture
- μmol
- 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.)
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Classifications
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K47/545—Heterocyclic compounds
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (17)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20210105358 | 2021-08-10 | ||
| KR1020210105358 | 2021-08-10 | ||
| KR20210106488 | 2021-08-12 | ||
| KR1020210106488 | 2021-08-12 | ||
| KR1020210117389 | 2021-09-03 | ||
| KR20210117389 | 2021-09-03 | ||
| KR20210126757 | 2021-09-24 | ||
| KR1020210126757 | 2021-09-24 | ||
| KR1020220008456 | 2022-01-20 | ||
| KR20220008456 | 2022-01-20 | ||
| KR1020220020996 | 2022-02-17 | ||
| KR20220020996 | 2022-02-17 | ||
| KR20220054880 | 2022-05-03 | ||
| KR1020220054880 | 2022-05-03 | ||
| KR1020220075838 | 2022-06-21 | ||
| KR20220075838 | 2022-06-21 | ||
| PCT/KR2022/011963 WO2023018238A1 (en) | 2021-08-10 | 2022-08-10 | Novel plk1 degradation inducing compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20230024251A KR20230024251A (ko) | 2023-02-20 |
| KR102604802B1 true KR102604802B1 (ko) | 2023-11-22 |
Family
ID=85200656
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227036596A Active KR102604802B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020227042318A Active KR102604803B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020227036557A Active KR102604801B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020227046443A Active KR102662205B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020247013823A Pending KR20240060721A (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227042318A Active KR102604803B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020227036557A Active KR102604801B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020227046443A Active KR102662205B1 (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
| KR1020247013823A Pending KR20240060721A (ko) | 2021-08-10 | 2022-08-10 | 신규 plk1 분해 유도 화합물 |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US11939334B2 (enExample) |
| EP (4) | EP4157850A4 (enExample) |
| JP (4) | JP7555155B2 (enExample) |
| KR (5) | KR102604802B1 (enExample) |
| CN (2) | CN116261458B (enExample) |
| AU (1) | AU2022327025A1 (enExample) |
| CA (1) | CA3228601A1 (enExample) |
| CL (1) | CL2024000373A1 (enExample) |
| CO (1) | CO2024001256A2 (enExample) |
| CR (1) | CR20240120A (enExample) |
| EC (1) | ECSP24010109A (enExample) |
| IL (1) | IL310678A (enExample) |
| MX (1) | MX2024001774A (enExample) |
| PE (1) | PE20240894A1 (enExample) |
| WO (5) | WO2023017446A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20230158158A1 (en) * | 2020-03-27 | 2023-05-25 | Uppthera | Pyrazolo quinazoline derivative compounds inducing selective degradation of plk1 |
| JP7555155B2 (ja) * | 2021-08-10 | 2024-09-24 | オップテラ インコーポレイテッド | 新規ｐｌｋ１分解誘導化合物 |
| AU2022326463A1 (en) | 2021-08-10 | 2024-02-22 | Novartis Pharma Ag | Compounds and compositions for treating conditions associated with sting activity |
| CN120603831A (zh) * | 2022-11-29 | 2025-09-05 | 厄普特拉株式会社 | 具有增加的刚性的plk1降解诱导化合物 |
| EP4658658A1 (en) * | 2023-02-02 | 2025-12-10 | Uppthera, Inc. | Novel plk1 degradation inducing compound |
| CN118946561A (zh) * | 2023-03-10 | 2024-11-12 | 标新生物医药科技(上海)有限公司 | 新颖的e3泛素连接酶配体、蛋白降解剂及其应用 |
| TW202502750A (zh) | 2023-06-08 | 2025-01-16 | 美商新銳思生物製藥股份有限公司 | Smarca2之雙官能選擇性降解劑及其治療用途 |
| EP4759807A1 (en) | 2023-08-11 | 2026-06-17 | Shenzhen Zhongge Biological Technology Co., Ltd. | Proteolysis targeting chimera compound for degrading irak4 and use thereof |
| CN117126133B (zh) * | 2023-08-14 | 2026-06-30 | 中国海洋大学 | 一种化合物及其用途 |
| EP4780815A1 (en) | 2023-09-20 | 2026-07-29 | Aurigene Oncology Limited | Heterocyclic compounds as cbp selective degraders |
| US20250197411A1 (en) | 2023-12-14 | 2025-06-19 | Astrazeneca Ab | Irak4 protacs |
| WO2025239662A1 (ko) * | 2024-05-13 | 2025-11-20 | (주) 업테라 | 분해 약물-항체 접합체용 plk1 분해 유도 화합물 |
| CN118724841B (zh) * | 2024-06-14 | 2026-06-19 | 南通华祥医药科技有限公司 | 一种n-氨基哌啶二盐酸盐的制备方法 |
| WO2026013576A1 (en) * | 2024-07-10 | 2026-01-15 | Monte Rosa Therapeutics Ag | Dihydrouracil derivatives useful for the targeted degradation of vav1 |
| WO2026013577A1 (en) * | 2024-07-10 | 2026-01-15 | Monte Rosa Therapeutics Ag | Piperidine-2, 6-dione derivatives useful for the targeted degradation of vav1 |
| WO2026026773A1 (zh) * | 2024-07-29 | 2026-02-05 | 杭州胶联生物医药科技有限公司 | 作为vav1蛋白靶点降解剂的新型取代杂环类化合物 |
| WO2026041138A1 (zh) * | 2024-08-22 | 2026-02-26 | 武汉人福创新药物研发中心有限公司 | 作为vav1降解剂的苯并杂环类化合物及其用途 |
| WO2026114368A1 (zh) * | 2024-11-28 | 2026-06-04 | 西藏海思科制药有限公司 | 一种vav1靶向降解剂及其用途 |
| WO2026114367A1 (zh) * | 2024-11-28 | 2026-06-04 | 西藏海思科制药有限公司 | Vav1靶向降解剂及其用途 |
| WO2026114343A1 (zh) * | 2024-11-29 | 2026-06-04 | 上海美悦生物科技发展有限公司 | 杂环化合物、及其药物组合物和用途 |
| WO2026158584A1 (zh) * | 2025-01-25 | 2026-07-30 | 杭州和正医药有限公司 | 多杂环类vav1降解分子衍生物及其用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009153197A1 (en) | 2008-06-18 | 2009-12-23 | F. Hoffmann-La Roche Ag | Halo-substituted pyrimidodiazepines as plkl inhibitors |
| CN106977584A (zh) | 2017-04-19 | 2017-07-25 | 吉林大学 | 靶向泛素化降解plk1和brd4蛋白的化合物及其应用 |
| CN109879877A (zh) | 2019-03-04 | 2019-06-14 | 吉林大学 | 一种可降解plk1和brd4蛋白的化合物及其应用 |
| US20200038513A1 (en) | 2018-07-26 | 2020-02-06 | Arvinas Operations, Inc. | Modulators of fak proteolysis and associated methods of use |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2010542B1 (en) * | 2006-04-12 | 2012-01-25 | Vertex Pharmaceuticals Incorporated | 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridines as plk1 protein kinase inhibitors for the treatment of proliferative disorders |
| TW200808325A (en) | 2006-07-06 | 2008-02-16 | Astrazeneca Ab | Novel compounds |
| CN101636399B (zh) | 2007-03-22 | 2012-04-18 | 武田药品工业株式会社 | 可用作plk1抑制剂的取代的嘧啶并二氮杂* |
| BRPI0817315A2 (pt) * | 2007-09-25 | 2015-03-17 | Takeda Pharmaceutical | Inibidores de quinase do tipo polo |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| BR112018008918A8 (pt) | 2015-11-02 | 2019-02-26 | Univ Yale | compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos |
| CN106543185B (zh) * | 2016-11-10 | 2017-12-15 | 吉林大学 | 一种靶向泛素化降解plk1和brd4蛋白的化合物及其应用 |
| IL319363A (en) * | 2017-01-31 | 2025-05-01 | Arvinas Operations Inc | Cervalon ligands and bifunctional compounds containing them |
| CN111018857B (zh) * | 2018-10-09 | 2023-06-02 | 嘉兴优博生物技术有限公司 | 靶向蛋白酶降解平台(ted) |
| EP4031247A1 (en) | 2019-09-16 | 2022-07-27 | Novartis AG | Bifunctional degraders and their methods of use |
| AU2020356484A1 (en) | 2019-09-27 | 2022-03-17 | Dana-Farber Cancer Institute, Inc. | ERK5 degraders as therapeutics in cancer and inflammatory diseases |
| US20230158158A1 (en) * | 2020-03-27 | 2023-05-25 | Uppthera | Pyrazolo quinazoline derivative compounds inducing selective degradation of plk1 |
| JP7555155B2 (ja) * | 2021-08-10 | 2024-09-24 | オップテラ インコーポレイテッド | 新規ｐｌｋ１分解誘導化合物 |
-
2022
- 2022-08-10 JP JP2023514149A patent/JP7555155B2/ja active Active
- 2022-08-10 IL IL310678A patent/IL310678A/en unknown
- 2022-08-10 KR KR1020227036596A patent/KR102604802B1/ko active Active
- 2022-08-10 EP EP22808931.4A patent/EP4157850A4/en active Pending
- 2022-08-10 US US18/019,034 patent/US11939334B2/en active Active
- 2022-08-10 EP EP22855629.6A patent/EP4384520A4/en active Pending
- 2022-08-10 WO PCT/IB2022/057475 patent/WO2023017446A1/en not_active Ceased
- 2022-08-10 WO PCT/KR2022/011963 patent/WO2023018238A1/en not_active Ceased
- 2022-08-10 EP EP22808930.6A patent/EP4157849A4/en active Pending
- 2022-08-10 US US18/580,553 patent/US20250114460A1/en active Pending
- 2022-08-10 US US18/019,047 patent/US11912710B2/en active Active
- 2022-08-10 CN CN202280006544.1A patent/CN116261458B/zh active Active
- 2022-08-10 WO PCT/KR2022/011961 patent/WO2023018236A1/en not_active Ceased
- 2022-08-10 WO PCT/KR2022/011962 patent/WO2023018237A1/en not_active Ceased
- 2022-08-10 EP EP22856233.6A patent/EP4384521A4/en active Pending
- 2022-08-10 JP JP2024507884A patent/JP2024530195A/ja active Pending
- 2022-08-10 KR KR1020227042318A patent/KR102604803B1/ko active Active
- 2022-08-10 KR KR1020227036557A patent/KR102604801B1/ko active Active
- 2022-08-10 CA CA3228601A patent/CA3228601A1/en active Pending
- 2022-08-10 AU AU2022327025A patent/AU2022327025A1/en active Pending
- 2022-08-10 CR CR20240120A patent/CR20240120A/es unknown
- 2022-08-10 WO PCT/IB2022/057471 patent/WO2023017442A1/en not_active Ceased
- 2022-08-10 KR KR1020227046443A patent/KR102662205B1/ko active Active
- 2022-08-10 US US18/580,506 patent/US20250101025A1/en active Pending
- 2022-08-10 MX MX2024001774A patent/MX2024001774A/es unknown
- 2022-08-10 JP JP2024507883A patent/JP2024530495A/ja active Pending
- 2022-08-10 JP JP2023514160A patent/JP7555156B2/ja active Active
- 2022-08-10 KR KR1020247013823A patent/KR20240060721A/ko active Pending
- 2022-08-10 PE PE2024000208A patent/PE20240894A1/es unknown
- 2022-08-10 CN CN202280006505.1A patent/CN116322700B/zh active Active
-
2024
- 2024-02-06 CO CONC2024/0001256A patent/CO2024001256A2/es unknown
- 2024-02-06 CL CL2024000373A patent/CL2024000373A1/es unknown
- 2024-02-07 EC ECSENADI202410109A patent/ECSP24010109A/es unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009153197A1 (en) | 2008-06-18 | 2009-12-23 | F. Hoffmann-La Roche Ag | Halo-substituted pyrimidodiazepines as plkl inhibitors |
| CN106977584A (zh) | 2017-04-19 | 2017-07-25 | 吉林大学 | 靶向泛素化降解plk1和brd4蛋白的化合物及其应用 |
| US20200038513A1 (en) | 2018-07-26 | 2020-02-06 | Arvinas Operations, Inc. | Modulators of fak proteolysis and associated methods of use |
| CN109879877A (zh) | 2019-03-04 | 2019-06-14 | 吉林大学 | 一种可降解plk1和brd4蛋白的化合物及其应用 |
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| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
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St.27 status event code: A-3-3-R10-R18-oth-X000 |
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| P11-X000 | Amendment of application requested |
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