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EA201992320A1 - Пиперидины в качестве ковалентных ингибиторов менина - Google Patents

Пиперидины в качестве ковалентных ингибиторов менина

Info

Publication number
EA201992320A1
EA201992320A1 EA201992320A EA201992320A EA201992320A1 EA 201992320 A1 EA201992320 A1 EA 201992320A1 EA 201992320 A EA201992320 A EA 201992320A EA 201992320 A EA201992320 A EA 201992320A EA 201992320 A1 EA201992320 A1 EA 201992320A1
Authority
EA
Eurasian Patent Office
Prior art keywords
piperidines
covalent
menin
menin inhibitors
formula
Prior art date
Application number
EA201992320A
Other languages
English (en)
Inventor
Шаомэн Ван
Анхело Агилар
Шилинь Сюй
Лиюэ Хуан
Джинн Стаки
Сюй Тяньфэн
Original Assignee
Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган
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 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган filed Critical Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган
Publication of EA201992320A1 publication Critical patent/EA201992320A1/ru

Links

Classifications

    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • 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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение раскрывает соединения, представленные формулой Iи их фармацевтически приемлемые соли и сольваты, где A, R, R, R, R, R, R, R, R, R, X, Z, m и n имеют значения, определенные в описании. Настоящее изобретение также представляет соединения формулы I для применения для лечения состояния или расстройства, чувствительного к ингибированию менина, такого как рак.
EA201992320A 2017-03-31 2018-03-30 Пиперидины в качестве ковалентных ингибиторов менина EA201992320A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762479520P 2017-03-31 2017-03-31
PCT/US2018/025417 WO2018183857A1 (en) 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors

Publications (1)

Publication Number Publication Date
EA201992320A1 true EA201992320A1 (ru) 2020-04-22

Family

ID=63677047

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201992320A EA201992320A1 (ru) 2017-03-31 2018-03-30 Пиперидины в качестве ковалентных ингибиторов менина

Country Status (13)

Country Link
US (1) US11045448B2 (ru)
EP (1) EP3600313A4 (ru)
JP (1) JP2020515571A (ru)
KR (1) KR20190133224A (ru)
CN (1) CN110636843A (ru)
AU (1) AU2018243586A1 (ru)
BR (1) BR112019020130A2 (ru)
CA (1) CA3058448A1 (ru)
EA (1) EA201992320A1 (ru)
IL (1) IL269542A (ru)
MX (1) MX2019011412A (ru)
SG (1) SG11201909083UA (ru)
WO (1) WO2018183857A1 (ru)

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CN109415337B (zh) 2016-05-02 2022-01-18 密执安大学评议会 作为多发性内分泌腺瘤蛋白抑制剂的哌啶
BR112020020059A2 (pt) * 2018-03-30 2021-03-30 The Regents Of The University Of Michigan Compostos de piperidina como inibidores de menin covalentes
SG11202101733TA (en) 2018-10-03 2021-03-30 Univ Michigan Regents Small molecule menin inhibitors
US11174263B2 (en) 2018-12-31 2021-11-16 Biomea Fusion, Inc. Inhibitors of menin-MLL interaction
JP7536767B2 (ja) 2018-12-31 2024-08-20 バイオメア フュージョン，インコーポレイテッド メニン－ｍｌｌ相互作用の不可逆的阻害剤
TW202126636A (zh) 2019-09-30 2021-07-16 美商阿吉歐斯製藥公司 作為ｍｅｎｉｎ抑制劑之六氫吡啶化合物
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
TW202204333A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
CA3202151A1 (en) * 2020-12-16 2022-06-23 Biomea Fusion, Inc. Fused pyrimidine compounds as inhibitors of menin-mll interaction
EP4387972A1 (en) 2021-08-20 2024-06-26 Biomea Fusion, Inc. Crystalline form of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(r)-[(1-oxo -2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide, an irreversible menin-mll inhibitor for the treatment of cancer
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

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JP7536767B2 (ja) 2018-12-31 2024-08-20 バイオメア フュージョン，インコーポレイテッド メニン－ｍｌｌ相互作用の不可逆的阻害剤
US11174263B2 (en) 2018-12-31 2021-11-16 Biomea Fusion, Inc. Inhibitors of menin-MLL interaction

Also Published As

Publication number Publication date
CN110636843A (zh) 2019-12-31
EP3600313A1 (en) 2020-02-05
AU2018243586A1 (en) 2019-10-17
JP2020515571A (ja) 2020-05-28
KR20190133224A (ko) 2019-12-02
MX2019011412A (es) 2020-02-07
SG11201909083UA (en) 2019-10-30
US20200022953A1 (en) 2020-01-23
IL269542A (en) 2019-11-28
BR112019020130A2 (pt) 2020-04-22
WO2018183857A1 (en) 2018-10-04
US11045448B2 (en) 2021-06-29
CA3058448A1 (en) 2018-10-04
EP3600313A4 (en) 2020-09-23

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