CN107708686B - 氧杂二环庚烷前药 - Google Patents

氧杂二环庚烷前药 Download PDF

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Publication number
CN107708686B
CN107708686B CN201680032555.1A CN201680032555A CN107708686B CN 107708686 B CN107708686 B CN 107708686B CN 201680032555 A CN201680032555 A CN 201680032555A CN 107708686 B CN107708686 B CN 107708686B
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alkyl
compound
alkenyl
cancer
liver
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Chinese (zh)
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CN107708686A (zh
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约翰·S·科瓦奇
罗伯特·福尔克曼
安东尼·玛法特
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Lixte Biotechnology Inc
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    • 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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (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)
CN201680032555.1A 2015-05-15 2016-05-12 氧杂二环庚烷前药 Expired - Fee Related CN107708686B (zh)

Priority Applications (1)

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CN202110080437.0A CN113150030A (zh) 2015-05-15 2016-05-12 氧杂二环庚烷前药

Applications Claiming Priority (3)

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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

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CN202110080437.0A Division CN113150030A (zh) 2015-05-15 2016-05-12 氧杂二环庚烷前药

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CN107708686A CN107708686A (zh) 2018-02-16
CN107708686B true CN107708686B (zh) 2021-02-19

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US (5) US9988394B2 (cg-RX-API-DMAC7.html)
EP (2) EP3294287B1 (cg-RX-API-DMAC7.html)
JP (3) JP7187023B6 (cg-RX-API-DMAC7.html)
CN (2) CN107708686B (cg-RX-API-DMAC7.html)
AU (1) AU2016263079B2 (cg-RX-API-DMAC7.html)
DK (1) DK3294287T3 (cg-RX-API-DMAC7.html)
ES (2) ES2795950T3 (cg-RX-API-DMAC7.html)
HU (1) HUE050177T2 (cg-RX-API-DMAC7.html)
IL (2) IL255516B (cg-RX-API-DMAC7.html)
MX (2) MX386975B (cg-RX-API-DMAC7.html)
TW (2) TWI693226B (cg-RX-API-DMAC7.html)
WO (1) WO2016186963A1 (cg-RX-API-DMAC7.html)

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CA2877167A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of diabetes
JP2016516772A (ja) 2013-04-09 2016-06-09 リクスト・バイオテクノロジー，インコーポレイテッド オキサシクロヘプタン及びオキサビシクロヘプテンの配合物
JP6453441B2 (ja) 2014-07-24 2019-01-16 エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド 骨髄異形成症候群を治療するためのタンパク質ホスファターゼ２ａ阻害剤
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
MX382044B (es) 2015-02-19 2025-03-13 Lixte Biotechnology Inc Oxabicicloheptanos y oxabicicloheptenos para el tratamiento de trastornos depresivos y de estrés.
EP3294287B1 (en) 2015-05-15 2020-04-08 Lixte Biotechnology, Inc. Oxabicycloheptane prodrugs
BR112019011627A2 (pt) 2016-12-08 2019-11-12 Lixte Biotechnology Inc oxabiciclo-heptanos para modulação da resposta imunológica

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US20200325151A1 (en) 2020-10-15
EP3294287A4 (en) 2018-10-31
US10364252B2 (en) 2019-07-30
WO2016186963A1 (en) 2016-11-24
MX2017014549A (es) 2018-09-11
JP2020180130A (ja) 2020-11-05
JP7187023B6 (ja) 2023-01-05
CN107708686A (zh) 2018-02-16
EP3294287A1 (en) 2018-03-21
ES2985668T3 (es) 2024-11-06
DK3294287T3 (da) 2020-06-08
US9988394B2 (en) 2018-06-05
US11866444B2 (en) 2024-01-09
TW201713667A (zh) 2017-04-16
TWI757720B (zh) 2022-03-11
US20190359627A1 (en) 2019-11-28
JP7187023B2 (ja) 2022-12-12
CA2986104A1 (en) 2016-11-24
HK1247576A1 (en) 2018-09-28
US20220235066A1 (en) 2022-07-28
EP3736275B1 (en) 2024-07-03
CN113150030A (zh) 2021-07-23
IL255516A (en) 2018-01-31
US20160333024A1 (en) 2016-11-17
TW202043237A (zh) 2020-12-01
EP3294287B1 (en) 2020-04-08
IL272027B (en) 2021-10-31
US20180244690A1 (en) 2018-08-30
MX2021012440A (es) 2022-06-28
US11236102B2 (en) 2022-02-01
IL272027A (en) 2020-02-27
TWI693226B (zh) 2020-05-11
AU2016263079B2 (en) 2019-08-15
EP3736275A1 (en) 2020-11-11
JP2023100645A (ja) 2023-07-19
MX393461B (es) 2025-03-24
AU2016263079A1 (en) 2017-12-07
IL255516B (en) 2020-02-27
EP3736275C0 (en) 2024-07-03
ES2795950T3 (es) 2020-11-25
US10618908B2 (en) 2020-04-14
MX386975B (es) 2025-03-19
HUE050177T2 (hu) 2020-11-30
JP2018515614A (ja) 2018-06-14

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