CO2023016743A2 - Compuestos para direccionar la degradación de tirosina cinasa de bruton - Google Patents
Compuestos para direccionar la degradación de tirosina cinasa de brutonInfo
- Publication number
- CO2023016743A2 CO2023016743A2 CONC2023/0016743A CO2023016743A CO2023016743A2 CO 2023016743 A2 CO2023016743 A2 CO 2023016743A2 CO 2023016743 A CO2023016743 A CO 2023016743A CO 2023016743 A2 CO2023016743 A2 CO 2023016743A2
- Authority
- CO
- Colombia
- Prior art keywords
- btk
- compounds
- degradation
- dsm
- linker
- Prior art date
Links
- 230000015556 catabolic process Effects 0.000 title abstract 4
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000006731 degradation reaction Methods 0.000 title abstract 4
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 title 1
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 abstract 2
- 108090000623 proteins and genes Proteins 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 230000006663 ubiquitin-proteasome pathway Effects 0.000 abstract 2
- 230000003213 activating effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 230000034512 ubiquitination Effects 0.000 abstract 1
- 238000010798 ubiquitination Methods 0.000 abstract 1
Classifications
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente descripción se relaciona con compuestos de Fórmula (A): BTK—L—DSM (A) o una sal farmacéuticamente aceptable de estos, donde DSM es un resto de señalización de degradación que se une, de forma covalente, al enlazador L, L es un enlazador que une, de forma covalente, BTK a DSM, y BTK es un resto de unión a Btk representado por la Fórmula (I) o la Fórmula (II) que se une, de forma covalente, al enlazador L: en la que todas las variables son como se definen en la solicitud. Los compuestos o sales farmacéuticamente aceptables de estos son capaces de activar la ubiquitinación selectiva de proteínas Btk mediante las vías de ubiquitina-proteasoma (UPP) y causar la degradación de proteínas Btk. La presente descripción también proporciona métodos para tratar trastornos que responden a la modulación de la actividad de Btk y/o la degradación de Btk con al menos un compuesto descrito en la presente.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163184439P | 2021-05-05 | 2021-05-05 | |
| PCT/US2022/027888 WO2022235945A1 (en) | 2021-05-05 | 2022-05-05 | Compounds for targeting degradation of bruton's tyrosine kinase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2023016743A2 true CO2023016743A2 (es) | 2023-12-29 |
Family
ID=82115630
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2023/0016743A CO2023016743A2 (es) | 2021-05-05 | 2023-12-01 | Compuestos para direccionar la degradación de tirosina cinasa de bruton |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP4333899A1 (es) |
| JP (1) | JP2024519496A (es) |
| KR (1) | KR20240017814A (es) |
| CN (1) | CN117580592A (es) |
| AR (1) | AR125768A1 (es) |
| AU (1) | AU2022268977A1 (es) |
| BR (1) | BR112023023065A2 (es) |
| CA (1) | CA3217417A1 (es) |
| CO (1) | CO2023016743A2 (es) |
| IL (1) | IL308219A (es) |
| TW (1) | TW202309039A (es) |
| UY (1) | UY39756A (es) |
| WO (1) | WO2022235945A1 (es) |
Family Cites Families (50)
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| EP2548877A1 (en) * | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| WO2015160845A2 (en) | 2014-04-14 | 2015-10-22 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| WO2016105518A1 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| KR20200052995A (ko) | 2015-01-20 | 2020-05-15 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| BR112017019751A2 (pt) | 2015-03-18 | 2018-05-29 | Arvinas Inc | composto bifuncional, composição farmacêutica, e, métodos para tratar ou prevenir uma doença ou um distúrbio, e para degradar uma proteína alvo em uma célula |
| BR112017025975B1 (pt) | 2015-06-04 | 2023-12-12 | Arvinas Operations, Inc | Composto, composição, método in vitro para induzir degradação de uma proteína alvo em uma célula, e, uso de uma composição |
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| GB201516243D0 (en) | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
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| CN113788818A (zh) | 2016-04-06 | 2021-12-14 | 密执安大学评议会 | Mdm2蛋白质降解剂 |
| CA3020541A1 (en) | 2016-04-12 | 2017-10-19 | The Regents Of The University Of Michigan | Bet protein degraders |
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| EP3454856A4 (en) | 2016-05-10 | 2019-12-25 | C4 Therapeutics, Inc. | HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
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| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
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-
2022
- 2022-05-05 AR ARP220101179A patent/AR125768A1/es unknown
- 2022-05-05 WO PCT/US2022/027888 patent/WO2022235945A1/en active Application Filing
- 2022-05-05 JP JP2023567962A patent/JP2024519496A/ja active Pending
- 2022-05-05 EP EP22731839.1A patent/EP4333899A1/en active Pending
- 2022-05-05 KR KR1020237041952A patent/KR20240017814A/ko unknown
- 2022-05-05 TW TW111116998A patent/TW202309039A/zh unknown
- 2022-05-05 CN CN202280047793.5A patent/CN117580592A/zh active Pending
- 2022-05-05 AU AU2022268977A patent/AU2022268977A1/en active Pending
- 2022-05-05 UY UY0001039756A patent/UY39756A/es unknown
- 2022-05-05 BR BR112023023065A patent/BR112023023065A2/pt unknown
- 2022-05-05 IL IL308219A patent/IL308219A/en unknown
- 2022-05-05 CA CA3217417A patent/CA3217417A1/en active Pending
-
2023
- 2023-12-01 CO CONC2023/0016743A patent/CO2023016743A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW202309039A (zh) | 2023-03-01 |
| WO2022235945A1 (en) | 2022-11-10 |
| UY39756A (es) | 2022-11-30 |
| JP2024519496A (ja) | 2024-05-14 |
| IL308219A (en) | 2024-01-01 |
| KR20240017814A (ko) | 2024-02-08 |
| EP4333899A1 (en) | 2024-03-13 |
| CN117580592A (zh) | 2024-02-20 |
| AU2022268977A1 (en) | 2023-11-30 |
| CA3217417A1 (en) | 2022-11-10 |
| AR125768A1 (es) | 2023-08-09 |
| BR112023023065A2 (pt) | 2024-01-30 |
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