MX2023011940A - Moduladores de la proteolisis bcl6 y metodos de uso asociados. - Google Patents
Moduladores de la proteolisis bcl6 y metodos de uso asociados.Info
- Publication number
- MX2023011940A MX2023011940A MX2023011940A MX2023011940A MX2023011940A MX 2023011940 A MX2023011940 A MX 2023011940A MX 2023011940 A MX2023011940 A MX 2023011940A MX 2023011940 A MX2023011940 A MX 2023011940A MX 2023011940 A MX2023011940 A MX 2023011940A
- Authority
- MX
- Mexico
- Prior art keywords
- target protein
- bcl6
- modulators
- present disclosure
- proteolysis
- Prior art date
Links
- 101100381525 Mus musculus Bcl6 gene Proteins 0.000 title 1
- 230000017854 proteolysis Effects 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 abstract 6
- 108090000623 proteins and genes Proteins 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000001588 bifunctional effect Effects 0.000 abstract 3
- 102100021631 B-cell lymphoma 6 protein 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
- 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
- 101000971234 Homo sapiens B-cell lymphoma 6 protein Proteins 0.000 abstract 1
- 101000941994 Homo sapiens Protein cereblon Proteins 0.000 abstract 1
- 102100032783 Protein cereblon Human genes 0.000 abstract 1
- 108010090920 Proto-Oncogene Proteins c-bcl-6 Proteins 0.000 abstract 1
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
- A61K31/495—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D471/04—Ortho-condensed 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
- C07D487/10—Spiro-condensed 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Optical Modulation, Optical Deflection, Nonlinear Optics, Optical Demodulation, Optical Logic Elements (AREA)
Abstract
Los compuestos bifuncionales, que encuentran utilidad como moduladores de la proteína 6 del linfoma de linfocitos B (BCL6; proteína diana), se describen en la presente descripción. En particular, los compuestos bifuncionales de la presente descripción contienen en un extremo un ligando cereblon que se une a la ligasa de ubiquitina E3 respectiva y en el otro extremo un resto que se une a la proteína diana, de manera que la proteína diana se coloca cerca de la ligada de ubiquitina para efectuar la degradación (e inhibición) de la proteína diana. Los compuestos bifuncionales de la presente descripción exhiben 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 evitan con compuestos y composiciones de la presente descripción.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202163175678P | 2021-04-16 | 2021-04-16 | |
PCT/US2022/025041 WO2022221673A1 (en) | 2021-04-16 | 2022-04-15 | Modulators of bcl6 proteolysis and associated methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2023011940A true MX2023011940A (es) | 2023-12-07 |
Family
ID=81585349
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2023011940A MX2023011940A (es) | 2021-04-16 | 2022-04-15 | Moduladores de la proteolisis bcl6 y metodos de uso asociados. |
Country Status (16)
Country | Link |
---|---|
US (2) | US11986532B2 (es) |
EP (1) | EP4323352A1 (es) |
JP (1) | JP2024515619A (es) |
KR (1) | KR20230171979A (es) |
CN (2) | CN118388454A (es) |
AU (1) | AU2022259683A1 (es) |
BR (1) | BR112023021265A2 (es) |
CA (1) | CA3214806A1 (es) |
CL (1) | CL2023003021A1 (es) |
CO (1) | CO2023015015A2 (es) |
CR (1) | CR20230516A (es) |
EC (1) | ECSP23083532A (es) |
IL (1) | IL305860A (es) |
MX (1) | MX2023011940A (es) |
PE (1) | PE20240639A1 (es) |
WO (1) | WO2022221673A1 (es) |
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JP2024539269A (ja) * | 2021-10-22 | 2024-10-28 | グルータクス セラピューティクス (シャンハイ) カンパニー、リミテッド | Crbn e3リガーゼリガンド化合物、当該リガンド化合物に基づいて開発したタンパク質分解剤及びそれらの応用 |
EP4455133A1 (en) * | 2021-12-24 | 2024-10-30 | Suzhou Kintor Pharmaceuticals, Inc. | Multi-protein degradation agent having imide skeleton |
US20230339904A1 (en) * | 2022-04-18 | 2023-10-26 | Bio TheryX, Inc | Isoindolinones, pharmaceutical compositions, and therapeutic applications |
TW202404951A (zh) * | 2022-06-02 | 2024-02-01 | 大陸商西藏海思科製藥有限公司 | 抑制或降解Bcl6的化合物及其在醫藥中的應用 |
WO2023240038A1 (en) | 2022-06-06 | 2023-12-14 | Treeline Biosciences, Inc. | Tricyclic quinolone bcl6 bifunctional degraders |
WO2023244918A1 (en) | 2022-06-13 | 2023-12-21 | Treeline Biosciences, Inc. | Quinolone bcl6 bifunctional degraders |
TW202415655A (zh) | 2022-06-13 | 2024-04-16 | 美商樹線生物科學公司 | 1,8—萘啶—2—酮異雙功能bcl6降解劑 |
WO2024073475A1 (en) * | 2022-09-27 | 2024-04-04 | Oncopia Therapeutics, Inc. D/B/A Proteovant Therapeutics, Inc. | Cereblon ligands and uses thereof |
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TW202430187A (zh) | 2023-01-09 | 2024-08-01 | 美商亞文納營運公司 | Bcl6蛋白水解之調節劑及相關使用方法 |
US20240327381A1 (en) * | 2023-02-08 | 2024-10-03 | Celgene Corporation | Compounds and Compositions for Selective Degradation of Engineered Proteins |
WO2024193464A1 (zh) * | 2023-03-17 | 2024-09-26 | 西藏海思科制药有限公司 | 一种含氮三并环衍生物及其在医药上的应用 |
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