CL2020002546A1 - Compuestos dirigidos a brm y métodos de uso asociados - Google Patents
Compuestos dirigidos a brm y métodos de uso asociadosInfo
- Publication number
- CL2020002546A1 CL2020002546A1 CL2020002546A CL2020002546A CL2020002546A1 CL 2020002546 A1 CL2020002546 A1 CL 2020002546A1 CL 2020002546 A CL2020002546 A CL 2020002546A CL 2020002546 A CL2020002546 A CL 2020002546A CL 2020002546 A1 CL2020002546 A1 CL 2020002546A1
- Authority
- CL
- Chile
- Prior art keywords
- target protein
- present disclosure
- brm
- compounds
- associated methods
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 230000008685 targeting Effects 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 abstract 6
- 108090000623 proteins and genes Proteins 0.000 abstract 6
- 101000702559 Homo sapiens Probable global transcription activator SNF2L2 Proteins 0.000 abstract 2
- 102100031021 Probable global transcription activator SNF2L2 Human genes 0.000 abstract 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 2
- 230000001588 bifunctional effect Effects 0.000 abstract 2
- 230000015556 catabolic process Effects 0.000 abstract 2
- 238000006731 degradation reaction Methods 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 238000009825 accumulation Methods 0.000 abstract 1
- 230000002776 aggregation Effects 0.000 abstract 1
- 238000004220 aggregation Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
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- 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
- 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
- A61K47/06—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
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- 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
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (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)
Abstract
La presente divulgación se refiere a compuestos bifuncionales, que encuentran utilidad como moduladores de SMARCA2 o BRM (proteína diana). En particular, la presente divulgación está dirigida a compuestos bifuncionales, que contienen en un extremo un ligando que se une a la ubiquitina ligasa de Von Hippel-Lindau E3, y en el otro extremo un resto que se une a la proteína diana, de modo que la proteína diana es colocada cerca de la ubiquitina ligasa para efectuar la degradación (e inhibición) de la proteína diana. La presente divulgación exhibe una amplia gama de actividades farmacológicas asociadas con la degradación / inhibición de la proteína diana. Las enfermedades o trastornos que resultan de la agregación o acumulación de la proteína diana se tratan o se previenen con compuestos y composiciones de la presente divulgación.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862651186P | 2018-04-01 | 2018-04-01 | |
US201962797754P | 2019-01-28 | 2019-01-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
CL2020002546A1 true CL2020002546A1 (es) | 2021-01-29 |
Family
ID=66175525
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CL2020002546A CL2020002546A1 (es) | 2018-04-01 | 2020-10-01 | Compuestos dirigidos a brm y métodos de uso asociados |
Country Status (17)
Country | Link |
---|---|
US (2) | US20190300521A1 (es) |
EP (1) | EP3774789A1 (es) |
JP (2) | JP2021520350A (es) |
KR (2) | KR102697733B1 (es) |
CN (1) | CN112166114B (es) |
AU (3) | AU2019249849C1 (es) |
BR (1) | BR112020020196A2 (es) |
CA (1) | CA3094305A1 (es) |
CL (1) | CL2020002546A1 (es) |
CO (1) | CO2020013762A2 (es) |
CR (1) | CR20200527A (es) |
IL (1) | IL277677A (es) |
MX (2) | MX2020010368A (es) |
PE (1) | PE20212108A1 (es) |
PH (1) | PH12020500663A1 (es) |
SG (1) | SG11202008898UA (es) |
WO (1) | WO2019195201A1 (es) |
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KR20240095318A (ko) | 2018-04-04 | 2024-06-25 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
EP3784665A4 (en) * | 2018-04-26 | 2022-01-26 | Aurigene Discovery Technologies Limited | PYRIDAZINE DERIVATIVES AS SMARCA2/4 DEGRADERS |
EP3787747A4 (en) * | 2018-04-30 | 2022-01-12 | Dana-Farber Cancer Institute, Inc. | POLYBROMO-1 (PBRM1) SMALL MOLECULE DEGRADATION PRODUCTS |
JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのe3ユビキチンリガーゼ結合活性を有するキメラ(protac)化合物を標的とし、アルファ-シヌクレインタンパク質を標的とするタンパク質分解 |
TW202037381A (zh) | 2018-10-24 | 2020-10-16 | 瑞士商赫孚孟拉羅股份公司 | 綴合化學降解誘導劑及使用方法 |
CN113453679A (zh) | 2018-12-20 | 2021-09-28 | C4医药公司 | 靶向蛋白降解 |
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CN114787159B (zh) * | 2019-10-01 | 2024-09-27 | 阿尔维纳斯运营股份有限公司 | Brm靶向化合物及相关使用方法 |
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CN114599428A (zh) * | 2019-10-28 | 2022-06-07 | 豪夫迈·罗氏有限公司 | 双功能化合物 |
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CN107698657A (zh) * | 2017-09-26 | 2018-02-16 | 中国药科大学 | 基于vhl配体和bet抑制剂诱导bet降解的双功能分子及其制备和应用 |
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2019
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2020
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2022
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2023
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2024
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MX2024000329A (es) | 2024-01-25 |
AU2024203058A1 (en) | 2024-05-30 |
AU2019249849B2 (en) | 2022-03-17 |
US20190300521A1 (en) | 2019-10-03 |
RU2020135754A3 (es) | 2022-05-04 |
US20240076295A1 (en) | 2024-03-07 |
BR112020020196A2 (pt) | 2021-01-26 |
CR20200527A (es) | 2021-04-09 |
MX2020010368A (es) | 2021-01-08 |
KR20210005037A (ko) | 2021-01-13 |
RU2020135754A (ru) | 2022-05-04 |
AU2019249849A1 (en) | 2020-10-01 |
KR20240130153A (ko) | 2024-08-28 |
JP2023071767A (ja) | 2023-05-23 |
WO2019195201A1 (en) | 2019-10-10 |
CO2020013762A2 (es) | 2021-01-18 |
PH12020500663A1 (en) | 2021-06-07 |
NZ767872A (en) | 2024-04-26 |
IL277677A (en) | 2020-11-30 |
KR102697733B1 (ko) | 2024-08-26 |
AU2022204042A1 (en) | 2022-06-30 |
CN112166114A (zh) | 2021-01-01 |
SG11202008898UA (en) | 2020-10-29 |
CN112166114B (zh) | 2024-11-19 |
JP2021520350A (ja) | 2021-08-19 |
CA3094305A1 (en) | 2019-10-10 |
PE20212108A1 (es) | 2021-11-04 |
EP3774789A1 (en) | 2021-02-17 |
AU2019249849C1 (en) | 2022-09-29 |
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