CA3235383A1 - Therapeutic targeting of gastrointestinal stromal tumor (gist) by disrupting the menin-mll epigenetic complex - Google Patents

Therapeutic targeting of gastrointestinal stromal tumor (gist) by disrupting the menin-mll epigenetic complex Download PDF

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Publication number
CA3235383A1
CA3235383A1 CA3235383A CA3235383A CA3235383A1 CA 3235383 A1 CA3235383 A1 CA 3235383A1 CA 3235383 A CA3235383 A CA 3235383A CA 3235383 A CA3235383 A CA 3235383A CA 3235383 A1 CA3235383 A1 CA 3235383A1
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Prior art keywords
inhibitor
menin
gist
moz
vtp
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Pending
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CA3235383A
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English (en)
French (fr)
Inventor
Scott A. Armstrong
Matthew L. HEMMING
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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Publication of CA3235383A1 publication Critical patent/CA3235383A1/en
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    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic 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
    • A61K31/435—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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3235383A 2021-12-15 2022-12-14 Therapeutic targeting of gastrointestinal stromal tumor (gist) by disrupting the menin-mll epigenetic complex Pending CA3235383A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163289943P 2021-12-15 2021-12-15
US63/289,943 2021-12-15
PCT/US2022/081587 WO2023114867A2 (en) 2021-12-15 2022-12-14 Therapeutic targeting of gastrointestinal stromal tumor (gist) by disrupting the menin-mll epigenetic complex

Publications (1)

Publication Number Publication Date
CA3235383A1 true CA3235383A1 (en) 2023-06-22

Family

ID=86773651

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3235383A Pending CA3235383A1 (en) 2021-12-15 2022-12-14 Therapeutic targeting of gastrointestinal stromal tumor (gist) by disrupting the menin-mll epigenetic complex

Country Status (10)

Country Link
US (1) US20250041299A1 (cg-RX-API-DMAC10.html)
EP (1) EP4447972A4 (cg-RX-API-DMAC10.html)
JP (1) JP2025503385A (cg-RX-API-DMAC10.html)
KR (1) KR20240121720A (cg-RX-API-DMAC10.html)
CN (1) CN118234497A (cg-RX-API-DMAC10.html)
AU (1) AU2022410890A1 (cg-RX-API-DMAC10.html)
CA (1) CA3235383A1 (cg-RX-API-DMAC10.html)
IL (1) IL311862A (cg-RX-API-DMAC10.html)
MX (1) MX2024007201A (cg-RX-API-DMAC10.html)
WO (1) WO2023114867A2 (cg-RX-API-DMAC10.html)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2831084T3 (es) 2016-06-10 2021-06-07 Vitae Pharmaceuticals Inc Inhibidores de la interacción menina-MLL
UY38988A (es) 2019-12-19 2021-06-30 Janssen Pharmaceutica Nv Derivados espiráncos sustituidos de cadena lineal
IL297039A (en) 2020-04-07 2022-12-01 Syndax Pharmaceuticals Inc Combinations of menin inhibitors and cyp3a4 inhibitors and methods of use thereof
US12187732B2 (en) 2022-03-28 2025-01-07 Isosterix, Inc. Inhibitors of the myst family of lysine acetyl transferases
AR132185A1 (es) 2023-03-24 2025-06-04 Acerta Pharma Bv COMPUESTOS DE 1-H-PIRROLO[2,3-c]PIRIDINA
JP2026525148A (ja) * 2023-07-17 2026-07-29 クラ オンコロジー,インク. メニン阻害剤を含む医薬組成物
IL325861A (en) 2023-07-17 2026-03-01 Kura Oncology Inc Crystalline forms of a menin inhibitor
KR20260099138A (ko) * 2023-10-20 2026-06-26 얀센 파마슈티카 엔브이 암 치료에 사용하기 위한, (r)-n-에틸-5-플루오로-n-아이소프로필-2-((5-(2-(6-((2-메톡시에틸)(메틸)아미노)-2-메틸헥산-3-일)-2,6-다이아자스피로[3.4]옥탄-6-일)-1,2,4-트라이아진-6-일)옥시)벤즈아미드, 이의 제제 및 이의 투여 요법
IL328224A (en) * 2023-11-17 2026-07-01 Kura Oncology Inc Methods for treating KIT-positive cancer with a menin inhibitor

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016197027A1 (en) * 2015-06-04 2016-12-08 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
US10752639B2 (en) * 2016-03-16 2020-08-25 Kura Oncology, Inc. Bridged bicyclic inhibitors of menin-MLL and methods of use
WO2017161028A1 (en) * 2016-03-16 2017-09-21 Kura Oncology, Inc. Substituted inhibitors of menin-mll and methods of use
JP2022503792A (ja) * 2018-09-26 2022-01-12 クラ オンコロジー,インク. メニン阻害剤を用いた血液悪性腫瘍の処置

Also Published As

Publication number Publication date
IL311862A (en) 2024-06-01
WO2023114867A2 (en) 2023-06-22
KR20240121720A (ko) 2024-08-09
CN118234497A (zh) 2024-06-21
US20250041299A1 (en) 2025-02-06
EP4447972A2 (en) 2024-10-23
EP4447972A4 (en) 2025-12-31
WO2023114867A3 (en) 2023-07-27
MX2024007201A (es) 2024-08-06
AU2022410890A1 (en) 2024-05-02
JP2025503385A (ja) 2025-02-04

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