EA201992320A1 - Пиперидины в качестве ковалентных ингибиторов менина - Google Patents

Пиперидины в качестве ковалентных ингибиторов менина

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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

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    • 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • 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
    • A61K31/454Non 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
    • 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
    • A61K31/4709Non-condensed quinolines and 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic 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
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (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)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU2019243587A1 (en) * 2018-03-30 2020-09-24 The Regents Of The University Of Michigan Piperidine compounds as covalent menin inhibitors
CN113166059A (zh) 2018-10-03 2021-07-23 密歇根大学董事会 小分子menin抑制剂
WO2020142559A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction
SG11202106304RA (en) 2018-12-31 2021-07-29 Biomea Fusion Llc Irreversible inhibitors of menin-mll interaction
WO2021067215A1 (en) 2019-09-30 2021-04-08 Agios Pharmaceuticals, Inc. Piperidine compounds as menin inhibitors
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
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
WO2022133064A1 (en) * 2020-12-16 2022-06-23 Biomea Fusion, Inc. Fused pyrimidine compounds as inhibitors of menin-mll interaction
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer

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Also Published As

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

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