PE20240894A1 - Compuesto inductor de la degradacion de plk1 novedoso - Google Patents
Compuesto inductor de la degradacion de plk1 novedosoInfo
- Publication number
- PE20240894A1 PE20240894A1 PE2024000208A PE2024000208A PE20240894A1 PE 20240894 A1 PE20240894 A1 PE 20240894A1 PE 2024000208 A PE2024000208 A PE 2024000208A PE 2024000208 A PE2024000208 A PE 2024000208A PE 20240894 A1 PE20240894 A1 PE 20240894A1
- Authority
- PE
- Peru
- Prior art keywords
- plk1
- 4alkyl
- alkyl
- formula
- linked
- Prior art date
Links
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 title abstract 4
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 108010056274 polo-like kinase 1 Proteins 0.000 title abstract 4
- 230000015556 catabolic process Effects 0.000 title abstract 3
- 238000006731 degradation reaction Methods 0.000 title abstract 3
- 230000001939 inductive effect Effects 0.000 title abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
Abstract
La presente invencion se refiere a un compuesto inductor de la degradacion de PLK1, a un metodo para preparar el mismo y al uso del mismo. Los compuestos de la presente invencion exhiben un efecto de induccion de la degradacion de PLK1, por lo tanto, pueden utilizarse para prevenir o tratar enfermedades relacionadas con PLK1 como cancer, un tumor benigno y un trastorno neurologico. Ademas, se refiere a un compuesto representado por la siguiente formula I, un estereoisomero del mismo o una sal farmaceuticamente aceptable del mismo [Formula I], donde ULM es un resto representado por la formula 1, PTM es un resto representado por la formula 2, el enlazador es un grupo que se une quimicamente a ULM y PTM; X1 y X2 son cada uno independientemente CH2, CH o N; el anillo U es fenilo o heteroarilo de 5 a 6 miembros unido a X1 o X2, en donde al menos un H del anillo fenilo o heteroarilo de 5 a 6 miembros puede estar sustituido por RU; RU es -alquilo C1-4, -hidroxialquilo C1-4, -aminoalquilo, entre otros; Y es CR7 o N; R1 es -alquilo C1-4; R2 es -H o -alquilo C1-4, o esta unido con R1 para formar un anillo de 5 a 6 miembros junto con un atomo de N; R3 y R4 son cada uno independientemente -H, -alquilo C1-4 o -halo, o R3 y R4 estan unidos entre si para formar un anillo de 3 a 6 miembros; R5 es -alquilo C1-4; R6 es -alquilo C1-4, -hidroxialquilo C1-4, -aminoalquilo C1-4, entre otros; y R7 es -H o -halo.
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20210105358 | 2021-08-10 | ||
| KR20210106488 | 2021-08-12 | ||
| KR20210117389 | 2021-09-03 | ||
| KR20210126757 | 2021-09-24 | ||
| KR20220008456 | 2022-01-20 | ||
| KR20220020996 | 2022-02-17 | ||
| KR20220054880 | 2022-05-03 | ||
| KR20220075838 | 2022-06-21 | ||
| PCT/KR2022/011961 WO2023018236A1 (en) | 2021-08-10 | 2022-08-10 | Novel plk1 degradation inducing compound |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240894A1 true PE20240894A1 (es) | 2024-04-24 |
Family
ID=85200656
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2024000208A PE20240894A1 (es) | 2021-08-10 | 2022-08-10 | Compuesto inductor de la degradacion de plk1 novedoso |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11912710B2 (es) |
| EP (4) | EP4157850A1 (es) |
| JP (2) | JP2024530495A (es) |
| KR (5) | KR20240060721A (es) |
| CN (2) | CN116261458B (es) |
| AU (1) | AU2022327025A1 (es) |
| CA (1) | CA3228601A1 (es) |
| CL (1) | CL2024000373A1 (es) |
| CO (1) | CO2024001256A2 (es) |
| CR (1) | CR20240120A (es) |
| EC (1) | ECSP24010109A (es) |
| IL (1) | IL310678A (es) |
| MX (1) | MX2024001774A (es) |
| PE (1) | PE20240894A1 (es) |
| WO (5) | WO2023017442A1 (es) |
Families Citing this family (2)
| 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 |
| WO2024162828A1 (en) * | 2023-02-02 | 2024-08-08 | Uppthera, Inc. | Novel plk1 degradation inducing compound |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5313875B2 (ja) * | 2006-04-12 | 2013-10-09 | バーテックス ファーマシューティカルズ インコーポレイテッド | 増殖性疾患の処置のためのタンパク質キナーゼｐｌｋ１の阻害剤として有用な４，５−ジヒドロ−［１，２，４］トリアゾロ［４，３−ｆ］プテリジン |
| EP2303889A1 (en) | 2008-06-18 | 2011-04-06 | F. Hoffmann-La Roche AG | Halo-substituted pyrimidodiazepines as plkl inhibitors |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| AU2016349781A1 (en) | 2015-11-02 | 2018-05-10 | Yale University | Proteolysis targeting chimera compounds and methods of preparing and using same |
| 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 |
| CN106977584B (zh) * | 2017-04-19 | 2019-12-06 | 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 |
| 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) |
| CN109879877B (zh) | 2019-03-04 | 2021-08-10 | 吉林大学 | 一种可降解plk1和brd4蛋白的化合物及其应用 |
| US20220378919A1 (en) * | 2019-09-27 | 2022-12-01 | Dana-Farber Cancer Institute, Inc. | Erk5 degraders as therapeutics in cancer and inflammatory diseases |
-
2022
- 2022-08-10 CN CN202280006544.1A patent/CN116261458B/zh active Active
- 2022-08-10 JP JP2024507883A patent/JP2024530495A/ja active Pending
- 2022-08-10 US US18/019,047 patent/US11912710B2/en active Active
- 2022-08-10 CN CN202280006505.1A patent/CN116322700B/zh active Active
- 2022-08-10 MX MX2024001774A patent/MX2024001774A/es unknown
- 2022-08-10 WO PCT/IB2022/057471 patent/WO2023017442A1/en active Application Filing
- 2022-08-10 WO PCT/KR2022/011961 patent/WO2023018236A1/en active Application Filing
- 2022-08-10 CR CR20240120A patent/CR20240120A/es unknown
- 2022-08-10 EP EP22808931.4A patent/EP4157850A1/en active Pending
- 2022-08-10 WO PCT/KR2022/011963 patent/WO2023018238A1/en unknown
- 2022-08-10 AU AU2022327025A patent/AU2022327025A1/en active Pending
- 2022-08-10 US US18/019,034 patent/US11939334B2/en active Active
- 2022-08-10 EP EP22855629.6A patent/EP4384520A1/en active Pending
- 2022-08-10 JP JP2024507884A patent/JP2024530195A/ja active Pending
- 2022-08-10 WO PCT/KR2022/011962 patent/WO2023018237A1/en active Application Filing
- 2022-08-10 KR KR1020247013823A patent/KR20240060721A/ko active Application Filing
- 2022-08-10 IL IL310678A patent/IL310678A/en unknown
- 2022-08-10 KR KR1020227046443A patent/KR102662205B1/ko active IP Right Grant
- 2022-08-10 EP EP22808930.6A patent/EP4157849A1/en active Pending
- 2022-08-10 EP EP22856233.6A patent/EP4384521A1/en active Pending
- 2022-08-10 KR KR1020227036557A patent/KR102604801B1/ko active IP Right Grant
- 2022-08-10 CA CA3228601A patent/CA3228601A1/en active Pending
- 2022-08-10 KR KR1020227042318A patent/KR102604803B1/ko active IP Right Grant
- 2022-08-10 WO PCT/IB2022/057475 patent/WO2023017446A1/en active Application Filing
- 2022-08-10 PE PE2024000208A patent/PE20240894A1/es unknown
- 2022-08-10 KR KR1020227036596A patent/KR102604802B1/ko active IP Right Grant
-
2024
- 2024-02-06 CL CL2024000373A patent/CL2024000373A1/es unknown
- 2024-02-06 CO CONC2024/0001256A patent/CO2024001256A2/es unknown
- 2024-02-07 EC ECSENADI202410109A patent/ECSP24010109A/es unknown
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