JP7187023B6 - オキサビシクロヘプタンプロドラッグ - Google Patents

オキサビシクロヘプタンプロドラッグ Download PDF

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JP7187023B6
JP7187023B6 JP2018511344A JP2018511344A JP7187023B6 JP 7187023 B6 JP7187023 B6 JP 7187023B6 JP 2018511344 A JP2018511344 A JP 2018511344A JP 2018511344 A JP2018511344 A JP 2018511344A JP 7187023 B6 JP7187023 B6 JP 7187023B6
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alkyl
aryl
alkenyl
alkynyl
heteroaryl
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JP7187023B2 (ja
JP2018515614A5 (https=
JP2018515614A (ja
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コバック、ジョン・エス．
ボルクマン、ロバート
マルファト、アンソニー
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リクスト・バイオテクノロジー，インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C07H15/252—Naphthacene radicals, e.g. daunomycins, adriamycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2018511344A 2015-05-15 2016-05-12 オキサビシクロヘプタンプロドラッグ Active JP7187023B6 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562162501P 2015-05-15 2015-05-15
US62/162,501 2015-05-15
PCT/US2016/032123 WO2016186963A1 (en) 2015-05-15 2016-05-12 Oxabicycloheptane prodrugs

Related Child Applications (1)

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JP2020105369A Division JP2020180130A (ja) 2015-05-15 2020-06-18 オキサビシクロヘプタンプロドラッグ

Publications (4)

Publication Number Publication Date
JP2018515614A JP2018515614A (ja) 2018-06-14
JP2018515614A5 JP2018515614A5 (https=) 2019-06-06
JP7187023B2 JP7187023B2 (ja) 2022-12-12
JP7187023B6 true JP7187023B6 (ja) 2023-01-05

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JP2018511344A Active JP7187023B6 (ja) 2015-05-15 2016-05-12 オキサビシクロヘプタンプロドラッグ
JP2020105369A Pending JP2020180130A (ja) 2015-05-15 2020-06-18 オキサビシクロヘプタンプロドラッグ
JP2023064829A Pending JP2023100645A (ja) 2015-05-15 2023-04-12 オキサビシクロヘプタンプロドラッグ

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JP2020105369A Pending JP2020180130A (ja) 2015-05-15 2020-06-18 オキサビシクロヘプタンプロドラッグ
JP2023064829A Pending JP2023100645A (ja) 2015-05-15 2023-04-12 オキサビシクロヘプタンプロドラッグ

Country Status (12)

Country Link
US (5) US9988394B2 (https=)
EP (2) EP3736275B1 (https=)
JP (3) JP7187023B6 (https=)
CN (2) CN107708686B (https=)
AU (1) AU2016263079B2 (https=)
DK (1) DK3294287T3 (https=)
ES (2) ES2985668T3 (https=)
HU (1) HUE050177T2 (https=)
IL (2) IL255516B (https=)
MX (2) MX386975B (https=)
TW (2) TWI757720B (https=)
WO (1) WO2016186963A1 (https=)

Families Citing this family (8)

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CA2877167A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of diabetes
EP2983661B1 (en) 2013-04-09 2024-05-29 Lixte Biotechnology, Inc. Formulations of oxabicycloheptanes and oxabicycloheptenes
US10071094B2 (en) 2014-07-24 2018-09-11 H. Lee Moffitt Cancer Center And Research Institute, Inc. Protein phosphatase 2A inhibitors for treating myelodysplastic syndromes
US10118890B2 (en) 2014-10-10 2018-11-06 The Research Foundation For The State University Of New York Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration
AU2016219853B2 (en) 2015-02-19 2019-05-16 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of depressive and stress disorders
DK3294287T3 (da) * 2015-05-15 2020-06-08 Lixte Biotechnology Inc Oxabicycloheptan-prodrugs
MX2019006694A (es) 2016-12-08 2019-08-21 Lixte Biotechnology Inc Oxabicicloheptanos para la modulacion de la respuesta inmunitaria.
CN118791500B (zh) * 2024-06-17 2025-11-21 中国药科大学 7-氧杂双环[2.2.1]庚烷-2,3-二羧酸类衍生物及其制备方法和应用

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WO2003045898A1 (en) 2001-11-23 2003-06-05 Eli Lilly And Company Prodrugs of excitatory amino acids
US20100029683A1 (en) 2008-08-01 2010-02-04 Kovach John S Methods for regulating cell mitosis by inhibiting serine/threonine phosphateses
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WO2001062242A1 (en) 2000-02-24 2001-08-30 Biocryst Pharmaceuticals, Inc. Prodrugs of substituted cyclopentane and cyclopentene compounds useful as neuraminidase inhibitors
WO2003045898A1 (en) 2001-11-23 2003-06-05 Eli Lilly And Company Prodrugs of excitatory amino acids
JP2010518081A (ja) 2007-02-06 2010-05-27 リクスト・バイオテクノロジー・ホールディングス，インコーポレイテッド オキサビシクロヘプタンおよびオキサビシクロヘプテン、それらの製造および使用
US20100029683A1 (en) 2008-08-01 2010-02-04 Kovach John S Methods for regulating cell mitosis by inhibiting serine/threonine phosphateses
JP2011529883A (ja) 2008-08-01 2011-12-15 リクスト・バイオテクノロジー，インコーポレイテッド オキサビシクロヘプタンおよびオキサビシクロヘプテン、その調製並びに使用
WO2011132171A1 (en) 2010-04-23 2011-10-27 Piramal Life Sciences Limited Nitric oxide releasing prodrugs of therapeutic agents
WO2013180271A1 (ja) 2012-06-01 2013-12-05 大正製薬株式会社 含フッ素アミノ酸のプロドラッグ
WO2014005084A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of diabetes
WO2014005080A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of reperfusion injury
WO2014168941A1 (en) 2013-04-09 2014-10-16 Lixte Biotechnology, Inc. Formulations of oxabicycloheptanes and oxabicycloheptenes
JP2020180130A (ja) 2015-05-15 2020-11-05 リクスト・バイオテクノロジー，インコーポレイテッド オキサビシクロヘプタンプロドラッグ

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Title
Ｄｒｕｇｓ ｏｆ ｔｈｅ Ｆｕｔｕｒｅ １９９１、１６（５）、ｐｐ．４４３－４５８
ＮＡＴＵＲＥ ＲＥＶＩＥＷＳ．ＤＲＵＧ ＤＩＳＣＯＶＥＲＹ、（２００８）、Ｖｏｌ．７、ｐｐ．２５５－２７０

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AU2016263079A1 (en) 2017-12-07
MX2017014549A (es) 2018-09-11
IL255516B (en) 2020-02-27
IL272027A (en) 2020-02-27
HUE050177T2 (hu) 2020-11-30
EP3736275A1 (en) 2020-11-11
JP2023100645A (ja) 2023-07-19
IL272027B (en) 2021-10-31
US11866444B2 (en) 2024-01-09
JP7187023B2 (ja) 2022-12-12
TWI693226B (zh) 2020-05-11
TW201713667A (zh) 2017-04-16
US11236102B2 (en) 2022-02-01
ES2985668T3 (es) 2024-11-06
TW202043237A (zh) 2020-12-01
IL255516A (en) 2018-01-31
US10618908B2 (en) 2020-04-14
EP3294287A1 (en) 2018-03-21
CN107708686B (zh) 2021-02-19
WO2016186963A1 (en) 2016-11-24
US9988394B2 (en) 2018-06-05
ES2795950T3 (es) 2020-11-25
US20200325151A1 (en) 2020-10-15
EP3736275C0 (en) 2024-07-03
TWI757720B (zh) 2022-03-11
US20190359627A1 (en) 2019-11-28
DK3294287T3 (da) 2020-06-08
MX386975B (es) 2025-03-19
AU2016263079B2 (en) 2019-08-15
JP2020180130A (ja) 2020-11-05
MX2021012440A (es) 2022-06-28
EP3736275B1 (en) 2024-07-03
EP3294287A4 (en) 2018-10-31
HK1247576A1 (en) 2018-09-28
US20180244690A1 (en) 2018-08-30
US20160333024A1 (en) 2016-11-17
CN107708686A (zh) 2018-02-16
CA2986104A1 (en) 2016-11-24
MX393461B (es) 2025-03-24
JP2018515614A (ja) 2018-06-14
US10364252B2 (en) 2019-07-30
EP3294287B1 (en) 2020-04-08
US20220235066A1 (en) 2022-07-28
CN113150030A (zh) 2021-07-23

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