JP2021519785A - 共有結合性メニン阻害剤としてのピペリジン化合物 - Google Patents

共有結合性メニン阻害剤としてのピペリジン化合物 Download PDF

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JP2021519785A
JP2021519785A JP2020552868A JP2020552868A JP2021519785A JP 2021519785 A JP2021519785 A JP 2021519785A JP 2020552868 A JP2020552868 A JP 2020552868A JP 2020552868 A JP2020552868 A JP 2020552868A JP 2021519785 A JP2021519785 A JP 2021519785A
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pharmaceutically acceptable
acceptable salt
alkyl
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JP2021519785A5 (enExample
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シャオメン ワン，
シャオメン ワン，
シリン シュー，
シリン シュー，
アンジェロ アグイラー，
アンジェロ アグイラー，
リユエ ファン，
リユエ ファン，
ジェーン スタッキー，
ジェーン スタッキー，
メン ジャン，
メン ジャン，
Original Assignee
ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン
ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン
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    • 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
    • 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
    • A61K31/44—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
    • A61K31/535—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged 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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020552868A 2018-03-30 2019-03-29 共有結合性メニン阻害剤としてのピペリジン化合物 Pending JP2021519785A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862650777P 2018-03-30 2018-03-30
US62/650,777 2018-03-30
US201862740549P 2018-10-03 2018-10-03
US62/740,549 2018-10-03
PCT/US2019/024729 WO2019191526A1 (en) 2018-03-30 2019-03-29 Piperidine compounds as covalent menin inhibitors

Publications (2)

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JP2021519785A true JP2021519785A (ja) 2021-08-12
JP2021519785A5 JP2021519785A5 (enExample) 2022-04-06

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JP2020552868A Pending JP2021519785A (ja) 2018-03-30 2019-03-29 共有結合性メニン阻害剤としてのピペリジン化合物

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US (1) US20210115018A1 (enExample)
EP (1) EP3774731A4 (enExample)
JP (1) JP2021519785A (enExample)
KR (1) KR20200136958A (enExample)
CN (1) CN111936465A (enExample)
AU (1) AU2019243587A1 (enExample)
BR (1) BR112020020059A2 (enExample)
CA (1) CA3093454A1 (enExample)
IL (1) IL277659A (enExample)
MX (1) MX2020010181A (enExample)
PH (1) PH12020551580A1 (enExample)
SG (1) SG11202009543VA (enExample)
TW (1) TW202003465A (enExample)
WO (1) WO2019191526A1 (enExample)

Families Citing this family (11)

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Publication number Priority date Publication date Assignee Title
KR102916887B1 (ko) 2016-06-10 2026-01-22 비타이 파마슈티컬즈, 엘엘씨 메닌-mll 상호 작용의 억제제
WO2019075386A1 (en) * 2017-10-13 2019-04-18 The Regents Of The University Of California MODULATORS OF MTORC1
KR20210072787A (ko) * 2018-10-03 2021-06-17 더 리젠츠 오브 더 유니버시티 오브 미시간 저분자 메닌 억제제
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
WO2021207335A1 (en) 2020-04-07 2021-10-14 Syndax Pharmaceuticals, Inc. Combinations of menin inhibitors and cyp3a4 inhibitors and methods of use thereof
WO2021204159A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
CA3213074A1 (en) 2021-05-14 2022-11-17 Salvacion Cacatian Inhibitors of the menin-mll interaction
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
WO2025106862A1 (en) * 2023-11-17 2025-05-22 Kura Oncology, Inc. Methods of treating kit positive cancers with a menin inhibitor

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004089892A2 (en) * 2003-04-01 2004-10-21 Theravance, Inc. Diarylmethyl and related compounds having beta2 andrenergic receptor agonist and muscarinic receptor antagonist activity
US9212180B2 (en) * 2013-06-12 2015-12-15 The Regents Of The University Of Michigan Menin-MLL inhibitors and methods of use thereof
KR20190015275A (ko) * 2016-05-02 2019-02-13 더 리젠츠 오브 더 유니버시티 오브 미시간 메닌 억제제로서의 피페리딘
WO2018106818A1 (en) * 2016-12-07 2018-06-14 Kura Oncology, Inc. Methods of promoting beta cell proliferation
KR20190133224A (ko) * 2017-03-31 2019-12-02 더 리젠츠 오브 더 유니버시티 오브 미시간 공유 메닌 억제제로서의 피페리딘

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KR20200136958A (ko) 2020-12-08
TW202003465A (zh) 2020-01-16
BR112020020059A2 (pt) 2021-03-30
EP3774731A1 (en) 2021-02-17
SG11202009543VA (en) 2020-10-29
CA3093454A1 (en) 2019-10-03
EP3774731A4 (en) 2021-11-24
AU2019243587A1 (en) 2020-09-24
CN111936465A (zh) 2020-11-13
IL277659A (en) 2020-11-30
WO2019191526A1 (en) 2019-10-03
US20210115018A1 (en) 2021-04-22
MX2020010181A (es) 2021-01-15
PH12020551580A1 (en) 2021-09-13

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