IL292173A - Small molecule degraders of helios and methods of use - Google Patents
Small molecule degraders of helios and methods of useInfo
- Publication number
- IL292173A IL292173A IL292173A IL29217322A IL292173A IL 292173 A IL292173 A IL 292173A IL 292173 A IL292173 A IL 292173A IL 29217322 A IL29217322 A IL 29217322A IL 292173 A IL292173 A IL 292173A
- Authority
- IL
- Israel
- Prior art keywords
- helios
- methods
- small compounds
- decomposing small
- decomposing
- Prior art date
Links
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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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 |
|---|---|
| IL292173A true IL292173A (en) | 2022-06-01 |
Family
ID=75715607
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL292173A IL292173A (en) | 2019-10-30 | 2022-04-12 | Small molecule degraders of helios and methods of use |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20230002397A1 (https=) |
| EP (1) | EP4051386A4 (https=) |
| JP (1) | JP7720833B2 (https=) |
| KR (1) | KR20220092920A (https=) |
| CN (1) | CN114650868A (https=) |
| AU (1) | AU2020374957A1 (https=) |
| BR (1) | BR112022007867A2 (https=) |
| CA (1) | CA3154942A1 (https=) |
| CL (1) | CL2022001111A1 (https=) |
| CR (1) | CR20220234A (https=) |
| DO (1) | DOP2022000091A (https=) |
| IL (1) | IL292173A (https=) |
| MX (1) | MX2022005232A (https=) |
| PE (1) | PE20221457A1 (https=) |
| PH (1) | PH12022550980A1 (https=) |
| WO (1) | WO2021087093A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20220092920A (ko) * | 2019-10-30 | 2022-07-04 | 다나-파버 캔서 인스티튜트 인크. | 헬리오스의 소분자 분해제 및 사용 방법 |
| 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 |
| JP7819176B2 (ja) * | 2020-08-03 | 2026-02-24 | ノバルティス アーゲー | ヘテロアリール置換３－（１－オキソイソインドリン－２－イル）ピペリジン－２，６－ジオン誘導体及びその使用 |
| IL301690A (en) * | 2020-10-16 | 2023-05-01 | Dana Farber Cancer Inst Inc | Piperidinyl small molecule degraders of helios and methods of use |
| US12122764B2 (en) | 2021-12-22 | 2024-10-22 | Gilead Sciences, Inc. | IKAROS zinc finger family degraders and uses thereof |
| WO2023116835A1 (zh) * | 2021-12-24 | 2023-06-29 | 苏州开拓药业股份有限公司 | 一种具有酰亚胺骨架的多蛋白降解剂 |
| 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 |
| WO2023178181A1 (en) | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| CN119731179A (zh) * | 2022-03-25 | 2025-03-28 | 密歇根大学董事会 | Ikzf2降解剂及其用途 |
| 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 |
| 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 |
| AU2023375457A1 (en) * | 2022-11-11 | 2025-05-01 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via 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 |
| 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 |
| WO2025097092A1 (en) * | 2023-11-02 | 2025-05-08 | Neomorph, Inc. | Substituted 3-(5-(4-hydroxypiperidin-4-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and 3-(2-(4-hydroxypiperidin-4-yl)-5-oxo-5,7-dihydro-6h-pyrrolo[3,4-b]pyridin-6-yl)piperidine-2,6-dione derivatives and uses thereof |
| WO2025245178A1 (en) * | 2024-05-21 | 2025-11-27 | Innovo Therapeutics, Inc. | Pak4, cstf2, or cstf2t protein degraders, pharmaceutical compositions, and therapeutic applications |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012170546A1 (en) * | 2011-06-06 | 2012-12-13 | University Of Iowa Research Foundation | Methods of inhibiting muscle atrophy |
| 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 |
| AU2018351050B2 (en) | 2017-10-18 | 2025-09-18 | Novartis Ag | Compositions and methods for selective protein degradation |
| CN113490528B (zh) * | 2019-02-15 | 2024-12-03 | 诺华股份有限公司 | 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途 |
| CA3123519A1 (en) * | 2019-02-15 | 2020-08-20 | Novartis Ag | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| WO2020168172A1 (en) * | 2019-02-15 | 2020-08-20 | Zamboni Chem Solutions Inc. | Conjugate compounds for the degradation of raf |
| KR20220092920A (ko) * | 2019-10-30 | 2022-07-04 | 다나-파버 캔서 인스티튜트 인크. | 헬리오스의 소분자 분해제 및 사용 방법 |
| CN115397460A (zh) * | 2020-02-27 | 2022-11-25 | 诺华股份有限公司 | 制备表达嵌合抗原受体的细胞的方法 |
| KR20230027056A (ko) * | 2020-06-23 | 2023-02-27 | 노파르티스 아게 | 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 |
| IL301690A (en) * | 2020-10-16 | 2023-05-01 | Dana Farber Cancer Inst Inc | Piperidinyl small molecule degraders of helios and methods of use |
| WO2022232391A1 (en) * | 2021-04-29 | 2022-11-03 | Dana-Farber Cancer Institute, Inc. | Phthalimido cereblon complex binders and transcription factor degraders and methods of use |
| JP2024517772A (ja) * | 2021-04-29 | 2024-04-23 | ネオモルフ インコーポレイテッド | 置換された２－（２，６－ジオキソピペリジン－３－イル）－５－（１－ピペリジン－４－イル）イソインドリン－１，３－ジオン誘導体及びその使用 |
-
2020
- 2020-10-29 KR KR1020227017914A patent/KR20220092920A/ko active Pending
- 2020-10-29 MX MX2022005232A patent/MX2022005232A/es unknown
- 2020-10-29 PE PE2022000693A patent/PE20221457A1/es unknown
- 2020-10-29 US US17/772,384 patent/US20230002397A1/en active Pending
- 2020-10-29 CR CR20220234A patent/CR20220234A/es unknown
- 2020-10-29 BR BR112022007867A patent/BR112022007867A2/pt unknown
- 2020-10-29 WO PCT/US2020/057930 patent/WO2021087093A1/en not_active Ceased
- 2020-10-29 CN CN202080077672.6A patent/CN114650868A/zh active Pending
- 2020-10-29 JP JP2022524112A patent/JP7720833B2/ja active Active
- 2020-10-29 AU AU2020374957A patent/AU2020374957A1/en active Pending
- 2020-10-29 CA CA3154942A patent/CA3154942A1/en active Pending
- 2020-10-29 PH PH1/2022/550980A patent/PH12022550980A1/en unknown
- 2020-10-29 EP EP20882103.3A patent/EP4051386A4/en active Pending
-
2022
- 2022-04-12 IL IL292173A patent/IL292173A/en unknown
- 2022-04-27 DO DO2022000091A patent/DOP2022000091A/es unknown
- 2022-04-29 CL CL2022001111A patent/CL2022001111A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PE20221457A1 (es) | 2022-09-21 |
| US20230002397A1 (en) | 2023-01-05 |
| JP2023500611A (ja) | 2023-01-10 |
| EP4051386A4 (en) | 2024-05-22 |
| CR20220234A (es) | 2022-07-19 |
| CA3154942A1 (en) | 2021-05-06 |
| BR112022007867A2 (pt) | 2022-07-12 |
| EP4051386A1 (en) | 2022-09-07 |
| PH12022550980A1 (en) | 2023-10-09 |
| AU2020374957A1 (en) | 2022-04-28 |
| CL2022001111A1 (es) | 2022-11-18 |
| JP7720833B2 (ja) | 2025-08-08 |
| MX2022005232A (es) | 2022-06-08 |
| WO2021087093A1 (en) | 2021-05-06 |
| KR20220092920A (ko) | 2022-07-04 |
| CN114650868A (zh) | 2022-06-21 |
| DOP2022000091A (es) | 2022-08-31 |
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