PE20221724A1 - Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr) - Google Patents
Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr)Info
- Publication number
- PE20221724A1 PE20221724A1 PE2022001139A PE2022001139A PE20221724A1 PE 20221724 A1 PE20221724 A1 PE 20221724A1 PE 2022001139 A PE2022001139 A PE 2022001139A PE 2022001139 A PE2022001139 A PE 2022001139A PE 20221724 A1 PE20221724 A1 PE 20221724A1
- Authority
- PE
- Peru
- Prior art keywords
- egfr
- compounds
- growth factor
- factor receptor
- epidermal growth
- Prior art date
Links
- 102000001301 EGF receptor Human genes 0.000 title abstract 5
- 108060006698 EGF receptor Proteins 0.000 title abstract 5
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- 230000015556 catabolic process Effects 0.000 title 1
- 238000006731 degradation reaction Methods 0.000 title 1
- PXZQEOJJUGGUIB-UHFFFAOYSA-N isoindolin-1-one Chemical compound C1=CC=C2C(=O)NCC2=C1 PXZQEOJJUGGUIB-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 230000035772 mutation Effects 0.000 abstract 1
- IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical compound NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000004063 proteosomal degradation Effects 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 230000034512 ubiquitination Effects 0.000 abstract 1
- 238000010798 ubiquitination Methods 0.000 abstract 1
Classifications
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- 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
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- 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
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/009—Sachets, pouches characterised by the material or function of the envelope
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (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)
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- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
Abstract
Referida a compuestos de formula (I) que degradan el Receptor del Factor de Crecimiento Epidermico (EGFR), en donde A se selecciona de los sistemas de anillo AF, AG y AH; y B se selecciona del sistema del anillo AD y AE. Estos compuestos son seleccionados del grupo que consiste en 5-((2-(1-(6,7-dihidro-5H-pirrolo[1,2-c]imidazol-1-il)-2-oxo-2-(tiazol-2-ilamino)etil)-7-fluoro-3-oxoisoindolin-5-il)etinil)-N-(1-(2-(4-(4-((2,6-dioxopiperidin-3-il)amino)fenil)piperidin-1-il)acetil)piperidin-4-il)picolinamida, entre otros. Asimismo, la accion de dichos compuestos consiste en la ubiquitinacion de la proteina EGFR con una o mas mutaciones, tales como L858R, T790M o C797S, para finalizar con su degradacion proteasomica; ademas, los compuestos reclamados son utiles para el tratamiento o profilaxis del cancer de pulmon no pequeno con mutacion de EGFR en pacientes humanos.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962951467P | 2019-12-20 | 2019-12-20 | |
US201962951464P | 2019-12-20 | 2019-12-20 | |
PCT/US2020/066211 WO2021127561A1 (en) | 2019-12-20 | 2020-12-18 | Isoindolinone and indazole compounds for the degradation of egfr |
Publications (1)
Publication Number | Publication Date |
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PE20221724A1 true PE20221724A1 (es) | 2022-11-04 |
Family
ID=76478832
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2022001139A PE20221724A1 (es) | 2019-12-20 | 2020-12-18 | Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr) |
Country Status (15)
Country | Link |
---|---|
US (2) | US11673902B2 (es) |
EP (1) | EP4076450A4 (es) |
JP (1) | JP2023509375A (es) |
KR (1) | KR20220119415A (es) |
CN (1) | CN114901277B (es) |
AU (1) | AU2020405237A1 (es) |
BR (1) | BR112022011827A2 (es) |
CA (1) | CA3154073A1 (es) |
CL (1) | CL2022001641A1 (es) |
CO (1) | CO2022008604A2 (es) |
IL (1) | IL293999A (es) |
MX (1) | MX2022007659A (es) |
PE (1) | PE20221724A1 (es) |
TW (1) | TW202136265A (es) |
WO (1) | WO2021127561A1 (es) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
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AU2022280070A1 (en) * | 2021-05-26 | 2023-11-16 | C4 Therapeutics, Inc. | Egfr degraders to treat cancer metastasis to the brain or cns |
EP4367113A1 (en) | 2021-07-07 | 2024-05-15 | Biogen MA Inc. | Compounds for targeting degradation of irak4 proteins |
TW202329964A (zh) | 2021-11-17 | 2023-08-01 | 大陸商浙江同源康醫藥股份有限公司 | 用於egfr蛋白降解的化合物及其用途 |
TW202333670A (zh) * | 2022-01-04 | 2023-09-01 | 大陸商海思科醫藥集團股份有限公司 | 抑制並降解irak4的化合物及其藥物组合物和藥學上的應用 |
CN115109055B (zh) * | 2022-05-26 | 2023-11-28 | 北京康辰药业股份有限公司 | 一种用于egfr降解的双功能化合物及其应用 |
CN115160311B (zh) * | 2022-05-26 | 2024-03-15 | 北京康辰药业股份有限公司 | 一种用于egfr降解的双功能化合物及其应用 |
WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
WO2024097994A1 (en) * | 2022-11-03 | 2024-05-10 | Board Of Regents, The University Of Texas System | Methods for the detection and treatment of non-small-cell lung cancer |
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2020
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- 2020-12-18 JP JP2022537517A patent/JP2023509375A/ja active Pending
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- 2020-12-18 WO PCT/US2020/066211 patent/WO2021127561A1/en active Application Filing
- 2020-12-18 PE PE2022001139A patent/PE20221724A1/es unknown
- 2020-12-18 KR KR1020227024551A patent/KR20220119415A/ko unknown
- 2020-12-18 AU AU2020405237A patent/AU2020405237A1/en active Pending
- 2020-12-18 CN CN202080088015.1A patent/CN114901277B/zh active Active
- 2020-12-18 IL IL293999A patent/IL293999A/en unknown
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IL293999A (en) | 2022-08-01 |
CA3154073A1 (en) | 2021-06-24 |
AU2020405237A1 (en) | 2022-07-07 |
CO2022008604A2 (es) | 2022-07-08 |
CL2022001641A1 (es) | 2023-03-17 |
KR20220119415A (ko) | 2022-08-29 |
BR112022011827A2 (pt) | 2022-08-30 |
CN114901277B (zh) | 2024-05-17 |
TW202136265A (zh) | 2021-10-01 |
MX2022007659A (es) | 2022-07-19 |
US20240076300A1 (en) | 2024-03-07 |
US11673902B2 (en) | 2023-06-13 |
CN114901277A (zh) | 2022-08-12 |
JP2023509375A (ja) | 2023-03-08 |
EP4076450A1 (en) | 2022-10-26 |
EP4076450A4 (en) | 2024-01-10 |
US20230110648A1 (en) | 2023-04-13 |
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