CR20220234A - Degradadores de moléculas pequeñas de helios y procedimientos de uso - Google Patents

Degradadores de moléculas pequeñas de helios y procedimientos de uso

Info

Publication number
CR20220234A
CR20220234A CR20220234A CR20220234A CR20220234A CR 20220234 A CR20220234 A CR 20220234A CR 20220234 A CR20220234 A CR 20220234A CR 20220234 A CR20220234 A CR 20220234A CR 20220234 A CR20220234 A CR 20220234A
Authority
CR
Costa Rica
Prior art keywords
helios
degradators
procedures
small molecule
compounds
Prior art date
Application number
CR20220234A
Other languages
English (en)
Inventor
Jianwei Che
Nathanael S Gray
Hu Liu
Tinghu Zhang
Lyn Howard Jones
Original Assignee
Dana Farber Cancer Inst Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Dana Farber Cancer Inst Inc filed Critical Dana Farber Cancer Inst Inc
Publication of CR20220234A publication Critical patent/CR20220234A/es

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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
    • C07D487/10—Spiro-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
    • A61K31/435—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
    • 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
    • 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
    • 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
    • A61K31/535—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur 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
    • C07D471/04—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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Se divulgan compuestos y sales, hidratos, solvatos, profármacos, estereoisómeros o tautómeros farmacéuticamente aceptables de los mismos que pueden provocar la degradación de diversas proteínas, por ejemplo, IKZF2 (Helios). También se divulgan composiciones farmacéuticas que los contienen y los procedimientos de producción y de uso de los compuestos para tratar enfermedades y trastornos asociados con Helios y que pueden beneficiarse de la degradación de Helios
CR20220234A 2019-10-30 2020-10-29 Degradadores de moléculas pequeñas de helios y procedimientos de uso CR20220234A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962928139P 2019-10-30 2019-10-30
US202063035272P 2020-06-05 2020-06-05
US202063047411P 2020-07-02 2020-07-02
PCT/US2020/057930 WO2021087093A1 (en) 2019-10-30 2020-10-29 Small molecule degraders of helios and methods of use

Publications (1)

Publication Number Publication Date
CR20220234A true CR20220234A (es) 2022-07-19

Family

ID=75715607

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220234A CR20220234A (es) 2019-10-30 2020-10-29 Degradadores de moléculas pequeñas de helios y procedimientos de uso

Country Status (16)

Country Link
US (1) US20230002397A1 (es)
EP (1) EP4051386A4 (es)
JP (1) JP7720833B2 (es)
KR (1) KR20220092920A (es)
CN (1) CN114650868A (es)
AU (1) AU2020374957A1 (es)
BR (1) BR112022007867A2 (es)
CA (1) CA3154942A1 (es)
CL (1) CL2022001111A1 (es)
CR (1) CR20220234A (es)
DO (1) DOP2022000091A (es)
IL (1) IL292173A (es)
MX (1) MX2022005232A (es)
PE (1) PE20221457A1 (es)
PH (1) PH12022550980A1 (es)
WO (1) WO2021087093A1 (es)

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WO2021087093A1 (en) * 2019-10-30 2021-05-06 Dana-Farber Cancer Institute, Inc. Small molecule degraders of helios and methods of use
JP7629459B2 (ja) 2019-11-19 2025-02-13 ブリストル-マイヤーズ スクイブ カンパニー Heliosタンパク質の阻害剤として有用な化合物
EP4188549A1 (en) * 2020-08-03 2023-06-07 Novartis AG Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
IL301690A (en) * 2020-10-16 2023-05-01 Dana Farber Cancer Inst Inc Piperidinyl small molecule degraders of helios and methods of use
CN118488948A (zh) * 2021-12-22 2024-08-13 吉利德科学公司 Ikaros锌指家族降解剂及其用途
EP4455133A4 (en) * 2021-12-24 2026-04-15 Suzhou Kintor Pharmaceuticals Inc MULTI-PROTEIN DEGRADING AGENT WITH AN IMIDE SKELETON
CN116640122A (zh) * 2022-02-16 2023-08-25 苏州国匡医药科技有限公司 Ikzf2降解剂及包含其的药物组合物和用途
PL4245756T3 (pl) 2022-03-17 2025-02-17 Gilead Sciences, Inc. Środki degradujące palec cynkowy z rodziny ikaros i ich zastosowania
TW202341988A (zh) * 2022-03-25 2023-11-01 密西根大學董事會 Ikzf2降解劑及其用途
WO2023201012A1 (en) * 2022-04-15 2023-10-19 Regents Of The University Of Michigan Ikzf2 degraders and uses thereof
WO2023208165A1 (zh) * 2022-04-29 2023-11-02 四川海思科制药有限公司 一种含氮杂环衍生物及其组合物和药学上的应用
CN117065022A (zh) * 2022-05-17 2023-11-17 海创药业股份有限公司 一种治疗三阴乳腺癌的药物
US20260028326A1 (en) * 2022-08-10 2026-01-29 Gluetacs Therapeutics (Shanghai) Co., Ltd. Compound based on isoindoline-substituted glutarimide backbone and use thereof
WO2024073871A1 (en) * 2022-10-04 2024-04-11 Biofront Ltd Gspt1 degraders, compositions comprising the degrader, and methods of using the same
CN117982498A (zh) * 2022-11-01 2024-05-07 苏州开拓药业股份有限公司 一种含蛋白降解剂或抑制剂的组合物及其用途
IL320316A (en) * 2022-11-11 2025-06-01 Nikang Therapeutics Inc Bifunctional compounds containing pyrimidine derivatives with substitutions at positions 2 and 5, for degradation of cyclin-dependent kinase 2 (CDK2) via the ubiquitin-proteasome pathway
WO2024109918A1 (zh) * 2022-11-24 2024-05-30 西藏海思科制药有限公司 一种gspt1降解剂及其在医药上的应用
EP4660193A1 (en) * 2023-01-31 2025-12-10 Korea Research Institute of Chemical Technology Indole compound decomposing ikzf2, and use thereof
WO2024222918A1 (zh) * 2023-04-28 2024-10-31 中国药科大学 一种苯并六元杂环类gspt1蛋白降解剂及其应用
WO2025011624A1 (en) * 2023-07-11 2025-01-16 Etern Biopharma (Shanghai) Co., Ltd. Bifunctional compounds for androgen receptor degradation and methods of use
CN121532386A (zh) * 2023-07-28 2026-02-13 杭州中美华东制药有限公司 具有蛋白降解作用的芳胺类化合物
IL328173A (en) * 2023-11-02 2026-07-01 Neomorph Inc History of 3-(5-(4-hydroxypiperidin-4-yl)-1-oxoindolin-2-yl)piperidine-6,2-dione and history of 3-(2-(4-hydroxypiperidin-4-yl)-5-oxo-7,5-dihydro-6H-pyrrolo[4,3-B]pyridin-6-yl)piperidine-6,2-dione derivatives and their uses
WO2025245178A1 (en) * 2024-05-21 2025-11-27 Innovo Therapeutics, Inc. Pak4, cstf2, or cstf2t protein degraders, pharmaceutical compositions, and therapeutic applications

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TWI793151B (zh) * 2017-08-23 2023-02-21 瑞士商諾華公司 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途
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WO2020168172A1 (en) * 2019-02-15 2020-08-20 Zamboni Chem Solutions Inc. Conjugate compounds for the degradation of raf
WO2021087093A1 (en) * 2019-10-30 2021-05-06 Dana-Farber Cancer Institute, Inc. Small molecule degraders of helios and methods of use
IL295878A (en) * 2020-02-27 2022-10-01 Novartis Ag Methods for producing cells expressing a chimeric antigen receptor
EP4168007A1 (en) * 2020-06-23 2023-04-26 Novartis AG Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
IL301690A (en) * 2020-10-16 2023-05-01 Dana Farber Cancer Inst Inc Piperidinyl small molecule degraders of helios and methods of use
EP4329746A4 (en) * 2021-04-29 2025-03-19 Dana-Farber Cancer Institute, Inc. Phthalimido cereblon complex binders and transcription factor degraders and methods of use
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Also Published As

Publication number Publication date
BR112022007867A2 (pt) 2022-07-12
PE20221457A1 (es) 2022-09-21
US20230002397A1 (en) 2023-01-05
IL292173A (en) 2022-06-01
PH12022550980A1 (en) 2023-10-09
JP2023500611A (ja) 2023-01-10
KR20220092920A (ko) 2022-07-04
MX2022005232A (es) 2022-06-08
EP4051386A1 (en) 2022-09-07
CA3154942A1 (en) 2021-05-06
DOP2022000091A (es) 2022-08-31
CN114650868A (zh) 2022-06-21
EP4051386A4 (en) 2024-05-22
CL2022001111A1 (es) 2022-11-18
WO2021087093A1 (en) 2021-05-06
AU2020374957A1 (en) 2022-04-28
JP7720833B2 (ja) 2025-08-08

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