JP2016538281A - 血液脳関門を通過するタンパク質ホスファターゼ阻害剤 - Google Patents

血液脳関門を通過するタンパク質ホスファターゼ阻害剤 Download PDF

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JP2016538281A
JP2016538281A JP2016530111A JP2016530111A JP2016538281A JP 2016538281 A JP2016538281 A JP 2016538281A JP 2016530111 A JP2016530111 A JP 2016530111A JP 2016530111 A JP2016530111 A JP 2016530111A JP 2016538281 A JP2016538281 A JP 2016538281A
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alkyl
alkenyl
alkynyl
compound
cancer
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JP2016538281A5 (enExample
Inventor
コバッチ、ジョン・エス．
ジョンソン、フランシス
サムドララ、ラマクリシュナ
グプタ、ラメシュ・シー．
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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
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a 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
    • A61K31/395—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016530111A 2013-11-15 2014-11-14 血液脳関門を通過するタンパク質ホスファターゼ阻害剤 Pending JP2016538281A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361904821P 2013-11-15 2013-11-15
US61/904,821 2013-11-15
PCT/US2014/065669 WO2015073802A1 (en) 2013-11-15 2014-11-14 Protein phosphatase inhibitors that cross the blood brain barrier

Publications (2)

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JP2016538281A true JP2016538281A (ja) 2016-12-08
JP2016538281A5 JP2016538281A5 (enExample) 2018-01-11

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JP2016530111A Pending JP2016538281A (ja) 2013-11-15 2014-11-14 血液脳関門を通過するタンパク質ホスファターゼ阻害剤

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Country Link
US (1) US20160264593A1 (enExample)
EP (1) EP3068398A4 (enExample)
JP (1) JP2016538281A (enExample)
WO (1) WO2015073802A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024504586A (ja) * 2021-01-19 2024-02-01 リクスト・バイオテクノロジー，インコーポレイテッド 小細胞肺がんの処置のためのオキサビシクロヘプタン

Families Citing this family (12)

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WO2010147612A1 (en) 2009-06-18 2010-12-23 Lixte Biotechnology, Inc. Methods of modulating cell regulation by inhibiting p53
CA2877167A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of diabetes
CA2909160C (en) 2013-04-09 2021-05-25 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
WO2016057931A1 (en) 2014-10-10 2016-04-14 The Research Foundation For The State University Of New York Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration
US9359373B1 (en) * 2014-11-21 2016-06-07 Taipei Veterans General Hospital Lipophilic N-substituted norcantharimide derivatives and uses thereof
AU2016219853B2 (en) 2015-02-19 2019-05-16 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of depressive and stress disorders
EP3736275B1 (en) * 2015-05-15 2024-07-03 Lixte Biotechnology, Inc. Oxabicycloheptane prodrugs for use in treating cancer
CN106083877A (zh) * 2016-06-21 2016-11-09 遵义医学院附属医院 不饱和去甲斑蝥素甲酯钡盐及其抗肿瘤应用
CN106117236A (zh) * 2016-06-21 2016-11-16 遵义医学院附属医院 不饱和去甲斑蝥素苄酯钡盐及其抗肿瘤应用
JP7246309B2 (ja) 2016-12-08 2023-03-27 リクスト・バイオテクノロジー，インコーポレイテッド 免疫応答を調節するためのオキサビシクロヘプタン
WO2024097784A2 (en) * 2022-11-03 2024-05-10 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for treating refractory cancers

Citations (4)

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US20050136065A1 (en) * 2003-03-28 2005-06-23 Chiron Corporation Use of small molecule compounds for immunopotentiation
US20100029683A1 (en) * 2008-08-01 2010-02-04 Kovach John S Methods for regulating cell mitosis by inhibiting serine/threonine phosphateses
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
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

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US5206386A (en) * 1991-03-20 1993-04-27 Isp Investments Inc. Controlled release N-substituted pyrrolidone esters and process for the use thereof
US20080267947A1 (en) * 2006-09-07 2008-10-30 Cirrito Thomas P Cancer therapy with cantharidin and cantharidin analogs

Patent Citations (4)

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US20050136065A1 (en) * 2003-03-28 2005-06-23 Chiron Corporation Use of small molecule compounds for immunopotentiation
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

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, VOL.7(19), P.2513-2518, JPN6018034411, ISSN: 0003872402 *
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024504586A (ja) * 2021-01-19 2024-02-01 リクスト・バイオテクノロジー，インコーポレイテッド 小細胞肺がんの処置のためのオキサビシクロヘプタン

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EP3068398A1 (en) 2016-09-21
US20160264593A1 (en) 2016-09-15
WO2015073802A1 (en) 2015-05-21
EP3068398A4 (en) 2017-11-15

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