JP2023545396A - Heliosのピペリジニル低分子分解剤および使用方法 - Google Patents

Heliosのピペリジニル低分子分解剤および使用方法 Download PDF

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JP2023545396A
JP2023545396A JP2023520211A JP2023520211A JP2023545396A JP 2023545396 A JP2023545396 A JP 2023545396A JP 2023520211 A JP2023520211 A JP 2023520211A JP 2023520211 A JP2023520211 A JP 2023520211A JP 2023545396 A JP2023545396 A JP 2023545396A
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alkyl
group
cycloalkyl
aryl
heteroaryl
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JP2023545396A5 (https=
JPWO2022081976A5 (https=
Inventor
ブライアン ベア,
ホイットニー ペトリリ,
フー リウ,
ティンフー ジャン,
リン ジョーンズ,
ジャンウェイ チェ,
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Neomorph Inc
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Neomorph Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2023520211A 2020-10-16 2021-10-15 Heliosのピペリジニル低分子分解剤および使用方法 Pending JP2023545396A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063092610P 2020-10-16 2020-10-16
US63/092,610 2020-10-16
US202163153599P 2021-02-25 2021-02-25
US63/153,599 2021-02-25
PCT/US2021/055186 WO2022081976A1 (en) 2020-10-16 2021-10-15 Piperidinyl small molecule degraders of helios and methods of use

Publications (3)

Publication Number Publication Date
JP2023545396A true JP2023545396A (ja) 2023-10-30
JP2023545396A5 JP2023545396A5 (https=) 2024-10-22
JPWO2022081976A5 JPWO2022081976A5 (https=) 2024-10-22

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JP2023520211A Pending JP2023545396A (ja) 2020-10-16 2021-10-15 Heliosのピペリジニル低分子分解剤および使用方法

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US (1) US20240034723A1 (https=)
EP (1) EP4228651A4 (https=)
JP (1) JP2023545396A (https=)
KR (1) KR20230090318A (https=)
AU (1) AU2021361060A1 (https=)
CA (1) CA3192393A1 (https=)
CL (1) CL2023000655A1 (https=)
CR (1) CR20230143A (https=)
DO (1) DOP2023000072A (https=)
IL (1) IL301690A (https=)
MX (1) MX2023004149A (https=)
PE (1) PE20231190A1 (https=)
WO (1) WO2022081976A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20220234A (es) * 2019-10-30 2022-07-19 Dana Farber Cancer Inst Inc Degradadores de moléculas pequeñas de helios y procedimientos de uso
AU2021330835B2 (en) 2020-08-24 2023-12-14 Gilead Sciences, Inc. Phospholipid compounds and uses thereof
TW202344257A (zh) 2020-10-16 2023-11-16 美商基利科學股份有限公司 磷脂化合物及其用途
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
EP4452415B1 (en) 2021-12-22 2026-02-25 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
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
KR20240161147A (ko) 2022-03-14 2024-11-12 슬랩 파마슈티컬스 엘엘씨 다중 사이클릭 화합물
CA3253296A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Zinc Finger Degradation Agents of the Ikaros Family and Their Uses
US20240327381A1 (en) * 2023-02-08 2024-10-03 Celgene Corporation Compounds and Compositions for Selective Degradation of Engineered Proteins
WO2025011624A1 (en) * 2023-07-11 2025-01-16 Etern Biopharma (Shanghai) Co., Ltd. Bifunctional compounds for androgen receptor degradation and methods of use
WO2025117881A1 (en) * 2023-12-01 2025-06-05 Casma Therapeutics, Inc. Compounds and methods for inhibiting autophagy
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors
WO2025245178A1 (en) * 2024-05-21 2025-11-27 Innovo Therapeutics, Inc. Pak4, cstf2, or cstf2t protein degraders, pharmaceutical compositions, and therapeutic applications

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019038717A1 (en) * 2017-08-23 2019-02-28 Novartis Ag 3- (1-OXOISOINDOLIN-2-YL) PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
WO2019079569A1 (en) * 2017-10-18 2019-04-25 Novartis Ag COMPOSITIONS AND METHODS FOR SELECTIVE DEGRADATION OF A PROTEIN
WO2020160192A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020165833A1 (en) * 2019-02-15 2020-08-20 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12227488B2 (en) * 2018-12-03 2025-02-18 Dana-Farber Cancer Institute, Inc. Small molecule degraders of Helios and methods of use
KR20210106437A (ko) * 2018-12-20 2021-08-30 노파르티스 아게 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물
CR20220234A (es) * 2019-10-30 2022-07-19 Dana Farber Cancer Inst Inc Degradadores de moléculas pequeñas de helios y procedimientos de uso
CA3161455A1 (en) * 2019-11-13 2021-05-20 Aprinoia Therapeutics Limited Compounds for degrading tau protein aggregates and uses thereof
CA3162523A1 (en) * 2019-12-23 2021-07-01 Hongfu LU Protein degradation agent compound preparation method and application
KR20220147109A (ko) * 2020-02-27 2022-11-02 노파르티스 아게 키메라 항원 수용체 발현 세포의 제조 방법

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019038717A1 (en) * 2017-08-23 2019-02-28 Novartis Ag 3- (1-OXOISOINDOLIN-2-YL) PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
WO2019079569A1 (en) * 2017-10-18 2019-04-25 Novartis Ag COMPOSITIONS AND METHODS FOR SELECTIVE DEGRADATION OF A PROTEIN
WO2020160192A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020165833A1 (en) * 2019-02-15 2020-08-20 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof

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Publication number Publication date
US20240034723A1 (en) 2024-02-01
PE20231190A1 (es) 2023-08-15
DOP2023000072A (es) 2023-09-29
MX2023004149A (es) 2023-07-10
EP4228651A4 (en) 2024-11-27
AU2021361060A1 (en) 2023-03-30
EP4228651A1 (en) 2023-08-23
KR20230090318A (ko) 2023-06-21
WO2022081976A1 (en) 2022-04-21
CL2023000655A1 (es) 2023-08-11
CR20230143A (es) 2023-07-28
CA3192393A1 (en) 2022-04-21
IL301690A (en) 2023-05-01

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