CA3192393A1 - Piperidinyl small molecule degraders of helios and methods of use - Google Patents

Piperidinyl small molecule degraders of helios and methods of use

Info

Publication number
CA3192393A1
CA3192393A1 CA3192393A CA3192393A CA3192393A1 CA 3192393 A1 CA3192393 A1 CA 3192393A1 CA 3192393 A CA3192393 A CA 3192393A CA 3192393 A CA3192393 A CA 3192393A CA 3192393 A1 CA3192393 A1 CA 3192393A1
Authority
CA
Canada
Prior art keywords
alkyl
group
aryl
cycloalkyl
heteroaryl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3192393A
Other languages
English (en)
French (fr)
Inventor
Hu Liu
Tinghu Zhang
Lyn Jones
Jianwei Che
Brian Bear
Whitney PETRILLI
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Neomorph Inc
Dana Farber Cancer Institute Inc
Original Assignee
Neomorph Inc
Dana Farber Cancer Institute 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 Neomorph Inc, Dana Farber Cancer Institute Inc filed Critical Neomorph Inc
Publication of CA3192393A1 publication Critical patent/CA3192393A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
CA3192393A 2020-10-16 2021-10-15 Piperidinyl small molecule degraders of helios and methods of use Pending CA3192393A1 (en)

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 (1)

Publication Number Publication Date
CA3192393A1 true CA3192393A1 (en) 2022-04-21

Family

ID=81208657

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3192393A Pending CA3192393A1 (en) 2020-10-16 2021-10-15 Piperidinyl small molecule degraders of helios and methods of use

Country Status (13)

Country Link
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP7585034B2 (ja) * 2017-10-18 2024-11-18 ノバルティス アーゲー 選択的タンパク質分解のための組成物及び方法
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
CN113874016A (zh) * 2019-01-29 2021-12-31 福宏治疗公司 化合物及其用途
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
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

Also Published As

Publication number Publication date
JP2023545396A (ja) 2023-10-30
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
IL301690A (en) 2023-05-01

Similar Documents

Publication Publication Date Title
CA3192393A1 (en) Piperidinyl small molecule degraders of helios and methods of use
AU2022287562B2 (en) 2-amino-N-heteroaryl-nicotinamides as NAV1.8 inhibitors
JP7720833B2 (ja) Heliosの低分子分解誘導剤および使用方法
AU2019294835B2 (en) Ligands to cereblon (CRBN)
AU2019293235B2 (en) Immunomodulatory compounds
JP2024525740A (ja) 小分子サイクリン依存性キナーゼ4/6(cdk4/6)およびikzf2(helios)分解剤並びにその使用方法
CA3178450A1 (en) Amide compounds and uses thereof
CA3172589A1 (en) Piperidine-2,6-diones as small molecule degraders of helios and methods of use
EP4367115A1 (en) Degraders of wild-type and mutant forms of lrrk2 and uses thereof
CA3113065A1 (en) Macrocyclic inhibitors of alk, trka, trkb, and ros1
US20250129070A1 (en) Bifunctional androgen receptor compounds
WO2022076304A1 (en) Potent and selective inhibitors of her2
CN116669769A (zh) Helios的哌啶基小分子降解剂和使用方法
CN116801878A (zh) Her2的有效和选择性抑制剂

Legal Events

Date Code Title Description
MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 3RD ANNIV.) - STANDARD

Year of fee payment: 3

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241011

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20241011

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 4TH ANNIV.) - STANDARD

Year of fee payment: 4

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20251010

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20251010

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D11-D117 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION RECEIVED

Effective date: 20251014

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - VOLUNTARY AMENDMENT

Effective date: 20251014

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20251014

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D118 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20251215

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D11-D155 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: ALL REQUIREMENTS FOR EXAMINATION DETERMINED COMPLIANT

Effective date: 20251215

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20251215

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20251215

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20251215

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20251217