JP2020515571A - 共有結合性メニン阻害剤としてのピペリジン - Google Patents

共有結合性メニン阻害剤としてのピペリジン Download PDF

Info

Publication number
JP2020515571A
JP2020515571A JP2019553080A JP2019553080A JP2020515571A JP 2020515571 A JP2020515571 A JP 2020515571A JP 2019553080 A JP2019553080 A JP 2019553080A JP 2019553080 A JP2019553080 A JP 2019553080A JP 2020515571 A JP2020515571 A JP 2020515571A
Authority
JP
Japan
Prior art keywords
group
pharmaceutically acceptable
solvate
acceptable salt
cancer
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
JP2019553080A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020515571A5 (https=
Inventor
シャオメン ワン，
シャオメン ワン，
アンジェロ アグイラー，
アンジェロ アグイラー，
シリン シュー，
シリン シュー，
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，
シュー ティアンフェン，
シュー ティアンフェン，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Michigan System
University of Michigan Ann Arbor
Original Assignee
University of Michigan System
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 University of Michigan System filed Critical University of Michigan System
Publication of JP2020515571A publication Critical patent/JP2020515571A/ja
Publication of JP2020515571A5 publication Critical patent/JP2020515571A5/ja
Pending legal-status Critical Current

Links

Images

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
    • 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
    • A61K31/47—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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
JP2019553080A 2017-03-31 2018-03-30 共有結合性メニン阻害剤としてのピペリジン Pending JP2020515571A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762479520P 2017-03-31 2017-03-31
US62/479,520 2017-03-31
PCT/US2018/025417 WO2018183857A1 (en) 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors

Publications (2)

Publication Number Publication Date
JP2020515571A true JP2020515571A (ja) 2020-05-28
JP2020515571A5 JP2020515571A5 (https=) 2021-04-30

Family

ID=63677047

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019553080A Pending JP2020515571A (ja) 2017-03-31 2018-03-30 共有結合性メニン阻害剤としてのピペリジン

Country Status (14)

Country Link
US (1) US11045448B2 (https=)
EP (1) EP3600313A4 (https=)
JP (1) JP2020515571A (https=)
KR (1) KR20190133224A (https=)
CN (1) CN110636843A (https=)
AU (1) AU2018243586A1 (https=)
BR (1) BR112019020130A2 (https=)
CA (1) CA3058448A1 (https=)
EA (1) EA201992320A1 (https=)
IL (1) IL269542A (https=)
MX (1) MX2019011412A (https=)
PH (1) PH12019502263A1 (https=)
SG (1) SG11201909083UA (https=)
WO (1) WO2018183857A1 (https=)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017192543A1 (en) 2016-05-02 2017-11-09 Regents Of The University Of Michigan Piperidines as menin inhibitors
JP2021519785A (ja) * 2018-03-30 2021-08-12 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン 共有結合性メニン阻害剤としてのピペリジン化合物
BR112021006273A2 (pt) * 2018-10-03 2021-07-06 Agios Pharmaceuticals Inc inibidores de menin de pequenas moléculas
EP3906026A4 (en) * 2018-12-31 2022-10-19 Biomea Fusion, LLC IRREVERSIBLE INHIBITORS OF MENIN-MLL INTERACTION
TW202043205A (zh) 2018-12-31 2020-12-01 美商拜歐米富士恩有限公司 Menin-mll相互作用之抑制劑
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
US20240124467A1 (en) * 2020-12-16 2024-04-18 Biomea Fusion, Inc. Fused pyrimidine compounds as inhibitors of menin-mll interaction
AU2022325861A1 (en) 2021-08-11 2024-02-29 Biomea Fusion, Inc. Covalent inhibitors of menin-mll interaction for diabetes mellitus
IL310717A (en) 2021-08-20 2024-04-01 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, IRREVERSIBLE MENIN-MLL INHIBITOR FOR CANCER TREATMENT
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer
SE546936C2 (en) 2021-10-15 2025-03-11 Skechers Usa Inc Ii A shoe comprising a heel cup attached to an interior compressible layer
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
WO2024155710A1 (en) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6- yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2-pyridinecarboxamide as a covalent inhibitor of menin-mll interaction

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140371239A1 (en) * 2013-06-12 2014-12-18 The Regents Of The University Of Michigan Menin-mll inhibitors and methods of use thereof
JP6991585B2 (ja) * 2016-05-02 2022-01-12 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン メニン阻害剤としてのピペリジン

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998054167A1 (en) 1997-05-28 1998-12-03 Mitsubishi-Tokyo Pharmaceuticals, Inc. Indole compounds
US7576082B2 (en) 2005-06-24 2009-08-18 Hoffman-La Roche Inc. Oxindole derivatives
US8242078B2 (en) 2006-10-19 2012-08-14 The University Of Chicago Therapeutics to inhibit MLL-menin interaction for treating leukemia
EP2473054B1 (en) 2009-09-04 2017-06-14 The Regents of the University of Michigan Compositions and methods for treatment of leukemia
WO2011060321A1 (en) 2009-11-16 2011-05-19 Chdi, Inc. Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof
WO2012154194A1 (en) * 2011-05-09 2012-11-15 Forma Tm, Llc Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (nampt)
AU2012324015A1 (en) 2011-12-01 2013-06-20 Purdue Pharma L.P. Azetidine-substituted quinoxaline-type piperidine compounds and uses thererof
KR20150130389A (ko) 2013-03-13 2015-11-23 더 리젠츠 오브 더 유니버시티 오브 미시간 티에노피리미딘 및 티에노피리딘 화합물을 포함하는 조성물 및 이의 사용 방법
WO2014200479A1 (en) 2013-06-12 2014-12-18 The Regents Of The University Of Michigan Menin-mll inhibitors and methods of use thereof
WO2016040330A1 (en) * 2014-09-09 2016-03-17 The Regents Of The University Of Michigan Thienopyrimidine and thienopyridine compounds and methods of use thereof
WO2016197027A1 (en) 2015-06-04 2016-12-08 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
AR104020A1 (es) 2015-06-04 2017-06-21 Kura Oncology Inc Métodos y composiciones para inhibir la interacción de menina con proteínas mill
AU2016378579A1 (en) 2015-12-22 2018-06-14 Vitae Pharmaceuticals, Inc. Inhibitors of the menin-MLL interaction
CN109152784B (zh) 2016-03-16 2021-12-28 库拉肿瘤学公司 经取代的menin-mll抑制剂及使用方法
CN109640987B (zh) 2016-03-16 2022-12-02 库拉肿瘤学公司 Menin-mll的桥联双环抑制剂及使用方法
EP3805215A1 (en) 2016-06-10 2021-04-14 Vitae Pharmaceuticals, LLC Inhibitors of the menin-mll interaction
US10899758B2 (en) 2016-09-16 2021-01-26 Vitae Pharmaceuticals, Llc Inhibitors of the menin-MLL interaction
WO2018106818A1 (en) 2016-12-07 2018-06-14 Kura Oncology, Inc. Methods of promoting beta cell proliferation
CN110691779B (zh) 2017-03-24 2023-10-10 库拉肿瘤学公司 治疗血液系统恶性肿瘤和尤因肉瘤的方法
US11542248B2 (en) 2017-06-08 2023-01-03 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with MLL proteins
US11649251B2 (en) 2017-09-20 2023-05-16 Kura Oncology, Inc. Substituted inhibitors of menin-MLL and methods of use
US11325921B2 (en) 2018-03-30 2022-05-10 Sumitomo Dainippon Pharma Co., Ltd. Optically active crosslinked cyclic secondary amine derivative
EP3856173A4 (en) 2018-09-26 2022-07-06 Kura Oncology, Inc. TREATMENT OF HEMATOLOGICAL MALIGNITIES WITH MENIN INHIBITORS
EP3906026A4 (en) 2018-12-31 2022-10-19 Biomea Fusion, LLC IRREVERSIBLE INHIBITORS OF MENIN-MLL INTERACTION
TW202043205A (zh) 2018-12-31 2020-12-01 美商拜歐米富士恩有限公司 Menin-mll相互作用之抑制劑

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140371239A1 (en) * 2013-06-12 2014-12-18 The Regents Of The University Of Michigan Menin-mll inhibitors and methods of use thereof
JP6991585B2 (ja) * 2016-05-02 2022-01-12 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン メニン阻害剤としてのピペリジン

Also Published As

Publication number Publication date
IL269542A (en) 2019-11-28
EP3600313A1 (en) 2020-02-05
SG11201909083UA (en) 2019-10-30
US20200022953A1 (en) 2020-01-23
MX2019011412A (es) 2020-02-07
CA3058448A1 (en) 2018-10-04
EP3600313A4 (en) 2020-09-23
WO2018183857A1 (en) 2018-10-04
BR112019020130A2 (pt) 2020-04-22
EA201992320A1 (ru) 2020-04-22
US11045448B2 (en) 2021-06-29
AU2018243586A1 (en) 2019-10-17
PH12019502263A1 (en) 2020-10-26
CN110636843A (zh) 2019-12-31
KR20190133224A (ko) 2019-12-02

Similar Documents

Publication Publication Date Title
JP2020515571A (ja) 共有結合性メニン阻害剤としてのピペリジン
CN110062759B (zh) 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬
KR102387316B1 (ko) Mdm2 단백질 분해제
JP7352284B2 (ja) ＬＳＤ－１インヒビターとしてのピロロ〔２，３－ｃ〕ピリジン及び関連類似体
EP3416969B1 (en) Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors
AU2019243587A1 (en) Piperidine compounds as covalent menin inhibitors
CN112119080B (zh) 作为lsd-1抑制剂的咪唑并[4,5-c]吡啶化合物
WO2022187419A1 (en) Small molecule degraders of androgen receptor
WO2020072391A1 (en) Small molecule menin inhibitors
WO2021067215A1 (en) Piperidine compounds as menin inhibitors
TW202204334A (zh) Menin抑制劑及治療癌症之使用方法
WO2023056589A1 (en) Menin inhibitors and methods of use for treating cancer
HK40041770A (en) Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors
HK40022861B (en) Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors
HK40041770B (en) Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors
HK40022861A (en) Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210317

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210317

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220221

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220224

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20220921