CN111936465A - 作为共价menin抑制剂的哌啶化合物 - Google Patents

作为共价menin抑制剂的哌啶化合物 Download PDF

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Publication number
CN111936465A
CN111936465A CN201980023575.6A CN201980023575A CN111936465A CN 111936465 A CN111936465 A CN 111936465A CN 201980023575 A CN201980023575 A CN 201980023575A CN 111936465 A CN111936465 A CN 111936465A
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China
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compound
group
pharmaceutically acceptable
solvate
acceptable salt
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CN201980023575.6A
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English (en)
Chinese (zh)
Inventor
S.王
S.许
A.阿圭拉
L.黄
J.斯塔基
M.张
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University of Michigan Ann Arbor
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University of Michigan Ann Arbor
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Publication of CN111936465A publication Critical patent/CN111936465A/zh
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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
    • C07D401/14—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
    • 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
    • C07D401/02—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
    • 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)
CN201980023575.6A 2018-03-30 2019-03-29 作为共价menin抑制剂的哌啶化合物 Pending CN111936465A (zh)

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 (1)

Publication Number Publication Date
CN111936465A true CN111936465A (zh) 2020-11-13

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CN201980023575.6A Pending CN111936465A (zh) 2018-03-30 2019-03-29 作为共价menin抑制剂的哌啶化合物

Country Status (14)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113166059A (zh) * 2018-10-03 2021-07-23 密歇根大学董事会 小分子menin抑制剂

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3805215A1 (en) 2016-06-10 2021-04-14 Vitae Pharmaceuticals, LLC Inhibitors of the menin-mll interaction
WO2019075386A1 (en) 2017-10-13 2019-04-18 The Regents Of The University Of California MODULATORS OF MTORC1
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
MX2022012471A (es) 2020-04-07 2022-11-30 Syndax Pharmaceuticals Inc Combinaciones de inhibidores de menina e inhibidores de cyp3a4 y métodos de uso de las mismas.
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
TW202311262A (zh) 2021-05-14 2023-03-16 美商錫達斯醫藥股份有限公司 Menin-mll交互作用之抑制劑
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer
CN120529900A (zh) 2022-11-24 2025-08-22 奥莱松基因组股份有限公司 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合
WO2025106862A1 (en) * 2023-11-17 2025-05-22 Kura Oncology, Inc. Methods of treating kit positive cancers with a menin inhibitor

Citations (3)

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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
US20140371239A1 (en) * 2013-06-12 2014-12-18 The Regents Of The University Of Michigan Menin-mll inhibitors and methods of use thereof
WO2017192543A1 (en) * 2016-05-02 2017-11-09 Regents Of The University Of Michigan Piperidines as menin inhibitors

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018106818A1 (en) * 2016-12-07 2018-06-14 Kura Oncology, Inc. Methods of promoting beta cell proliferation
CA3058448A1 (en) * 2017-03-31 2018-10-04 The Regents Of The University Of Michigan Piperidines as covalent menin inhibitors

Patent Citations (3)

* 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
US20140371239A1 (en) * 2013-06-12 2014-12-18 The Regents Of The University Of Michigan Menin-mll inhibitors and methods of use thereof
WO2017192543A1 (en) * 2016-05-02 2017-11-09 Regents Of The University Of Michigan Piperidines as menin inhibitors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
HE, SHIHAN等: "High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein-Protein Interaction", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 4, pages 1543 - 1556, XP002771199, DOI: 10.1021/jm401868d *
SENTER, TIMOTHY等: "Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 25, no. 13, pages 2720 - 2725, XP029210446, DOI: 10.1016/j.bmcl.2015.04.026 *
XU, SHILIN等: "Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction", ANGEWANDTE CHEMIE, INTERNATIONAL EDITION, vol. 57, no. 6, pages 1601 - 1605, XP055644297, DOI: 10.1002/anie.201711828 *
常玉杰等: "MLL1小分子抑制剂研究进展", 药学进展, vol. 41, no. 09, pages 696 - 703 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113166059A (zh) * 2018-10-03 2021-07-23 密歇根大学董事会 小分子menin抑制剂

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JP2021519785A (ja) 2021-08-12
US20210115018A1 (en) 2021-04-22
TW202003465A (zh) 2020-01-16
SG11202009543VA (en) 2020-10-29
EP3774731A4 (en) 2021-11-24
PH12020551580A1 (en) 2021-09-13
MX2020010181A (es) 2021-01-15
WO2019191526A1 (en) 2019-10-03
KR20200136958A (ko) 2020-12-08
CA3093454A1 (en) 2019-10-03
IL277659A (en) 2020-11-30
EP3774731A1 (en) 2021-02-17
BR112020020059A2 (pt) 2021-03-30
AU2019243587A1 (en) 2020-09-24

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Application publication date: 20201113