JP2021534084A - ヒストンデメチラーゼ５阻害剤およびその使用 - Google Patents

ヒストンデメチラーゼ５阻害剤およびその使用 Download PDF

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Publication number
JP2021534084A
JP2021534084A JP2021505646A JP2021505646A JP2021534084A JP 2021534084 A JP2021534084 A JP 2021534084A JP 2021505646 A JP2021505646 A JP 2021505646A JP 2021505646 A JP2021505646 A JP 2021505646A JP 2021534084 A JP2021534084 A JP 2021534084A
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Prior art keywords
certain embodiments
optionally substituted
pharmaceutically acceptable
isotope
cancer
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JP2021505646A
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Japanese (ja)
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JP2021534084A5 (https=
JPWO2020033377A5 (https=
Inventor
ジュン チィー，
ポール エム． パーク，
チェンクイ ペイ，
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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Publication of JP2021534084A publication Critical patent/JP2021534084A/ja
Publication of JP2021534084A5 publication Critical patent/JP2021534084A5/ja
Publication of JPWO2020033377A5 publication Critical patent/JPWO2020033377A5/ja
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • 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)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021505646A 2018-08-06 2019-08-06 ヒストンデメチラーゼ５阻害剤およびその使用 Pending JP2021534084A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862715122P 2018-08-06 2018-08-06
US62/715,122 2018-08-06
US201862715687P 2018-08-07 2018-08-07
US62/715,687 2018-08-07
US201962803332P 2019-02-08 2019-02-08
US62/803,332 2019-02-08
PCT/US2019/045259 WO2020033377A1 (en) 2018-08-06 2019-08-06 Histone demethylase 5 inhibitors and uses thereof

Publications (3)

Publication Number Publication Date
JP2021534084A true JP2021534084A (ja) 2021-12-09
JP2021534084A5 JP2021534084A5 (https=) 2022-08-15
JPWO2020033377A5 JPWO2020033377A5 (https=) 2022-08-15

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JP2021505646A Pending JP2021534084A (ja) 2018-08-06 2019-08-06 ヒストンデメチラーゼ５阻害剤およびその使用

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US (1) US20230382865A1 (https=)
EP (1) EP3833347A4 (https=)
JP (1) JP2021534084A (https=)
AU (1) AU2019318046B2 (https=)
CA (1) CA3106548A1 (https=)
WO (1) WO2020033377A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11232861B1 (en) 2021-06-18 2022-01-25 Argos Health Inc. Systems and methods for displaying predetermined information for clinical use
WO2024233765A1 (en) * 2023-05-09 2024-11-14 Ohio State Innovation Foundation Therapeutic approach to block terminal exhaustion of t cells and synergize the efficacy of t cell immunotherapies

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015532295A (ja) * 2012-10-02 2015-11-09 エピセラピューティックス・エイ・ピー・エス ヒストン脱メチル化酵素の阻害剤
JP2016509047A (ja) * 2013-02-27 2016-03-24 エピセラピューティクス アーペーエス ヒストン脱メチル化酵素の阻害剤
JP2017512804A (ja) * 2014-03-31 2017-05-25 ギリアード サイエンシーズ， インコーポレイテッド ヒストン脱メチル化酵素の阻害剤
JP2017526675A (ja) * 2014-08-27 2017-09-14 ギリアード サイエンシーズ， インコーポレイテッド ヒストンデメチラーゼを阻害するための化合物および方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9408577D0 (en) * 1994-04-29 1994-06-22 Fujisawa Pharmaceutical Co New compound
BRPI0415179A (pt) * 2003-10-07 2006-11-28 Renovis Inc derivados de amida como ligandos de canal de ìon e composições farmacêuticas e métodos de empregar as mesmas
WO2012162291A1 (en) * 2011-05-24 2012-11-29 The Wistar Institute Compositions and methods for modulating the activity of epstein-barr nuclear antigen 1
EP3102193B1 (en) * 2014-02-06 2023-01-11 Rutgers, The State University of New Jersey Antibacterial agents: n(alpha)-aroyl-n-aryl-phenylalaninamides
CN105837575B (zh) * 2015-01-13 2019-01-15 四川大学 3-乙炔基吡唑并嘧啶衍生物及其制备方法和用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015532295A (ja) * 2012-10-02 2015-11-09 エピセラピューティックス・エイ・ピー・エス ヒストン脱メチル化酵素の阻害剤
JP2016509047A (ja) * 2013-02-27 2016-03-24 エピセラピューティクス アーペーエス ヒストン脱メチル化酵素の阻害剤
JP2017512804A (ja) * 2014-03-31 2017-05-25 ギリアード サイエンシーズ， インコーポレイテッド ヒストン脱メチル化酵素の阻害剤
JP2017526675A (ja) * 2014-08-27 2017-09-14 ギリアード サイエンシーズ， インコーポレイテッド ヒストンデメチラーゼを阻害するための化合物および方法

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AU2019318046A1 (en) 2021-01-14
CA3106548A1 (en) 2020-02-13
EP3833347A4 (en) 2022-04-27
AU2019318046B2 (en) 2025-02-13
EP3833347A1 (en) 2021-06-16
WO2020033377A1 (en) 2020-02-13
US20230382865A1 (en) 2023-11-30

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