CN106572989B - 用于治疗骨髓增生异常综合征的蛋白磷酸酶2a抑制剂 - Google Patents

用于治疗骨髓增生异常综合征的蛋白磷酸酶2a抑制剂 Download PDF

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CN106572989B
CN106572989B CN201580041767.1A CN201580041767A CN106572989B CN 106572989 B CN106572989 B CN 106572989B CN 201580041767 A CN201580041767 A CN 201580041767A CN 106572989 B CN106572989 B CN 106572989B
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mds
alkyl
substituted
alkenyl
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CN106572989A (zh
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艾伦·F·利斯特
大卫·A·萨尔曼
约翰·S·科瓦奇
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Moffitt Cancer Center
Lixte Biotechnology Inc
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Lixte Biotechnology Inc
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    • 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
    • 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
    • A61K31/435—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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics

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  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580041767.1A 2014-07-24 2015-07-23 用于治疗骨髓增生异常综合征的蛋白磷酸酶2a抑制剂 Expired - Fee Related CN106572989B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462028729P 2014-07-24 2014-07-24
US62/028,729 2014-07-24
US201462029327P 2014-07-25 2014-07-25
US62/029,327 2014-07-25
PCT/US2015/041714 WO2016014783A1 (en) 2014-07-24 2015-07-23 Protein phosphatase 2a inhibitors for treating myelodysplastic syndromes

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CN106572989A CN106572989A (zh) 2017-04-19
CN106572989B true CN106572989B (zh) 2021-08-27

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US (3) US10071094B2 (enExample)
EP (1) EP3171870B1 (enExample)
JP (2) JP6453441B2 (enExample)
CN (1) CN106572989B (enExample)
WO (2) WO2016014778A1 (enExample)

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EP2867239A4 (en) 2012-06-29 2015-12-23 Lixte Biotechnology Inc OXABICYCLOHEPTANES AND OXABICYCLOHEPTENES FOR THE TREATMENT OF DIABETES
KR20160004299A (ko) 2013-04-09 2016-01-12 릭스트 바이오테크놀로지, 인코포레이티드 옥사바이시클로헵탄류 및 옥사바이시클로헵텐류의 제형
WO2016014778A1 (en) 2014-07-24 2016-01-28 H. Lee Moffitt Cancer Center And Research Institute, Inc. Protein phosphatase 2a inhibitors for treating myelodysplastic syndromes
MX382044B (es) 2015-02-19 2025-03-13 Lixte Biotechnology Inc Oxabicicloheptanos y oxabicicloheptenos para el tratamiento de trastornos depresivos y de estrés.
JP7187023B6 (ja) 2015-05-15 2023-01-05 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
EP3407887B1 (en) * 2016-01-27 2021-09-01 Lixte Biotechnology, Inc. Clinical regimen for treating myelodysplastic syndrome with phosphatase inhibitor
AU2017370731B2 (en) 2016-12-08 2022-06-02 Lixte Biotechnology, Inc. Oxabicycloheptanes for modulation of immune response
CN113694071B (zh) * 2021-08-31 2025-08-15 上海交通大学医学院附属瑞金医院 清除和/或溶解衰老细胞和/或抑制细胞衰老的化合物用于治疗精神障碍

Citations (1)

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US20170209434A1 (en) 2017-07-27
WO2016014778A1 (en) 2016-01-28
JP6453441B2 (ja) 2019-01-16
US20190046525A1 (en) 2019-02-14
US10434100B2 (en) 2019-10-08
US20170340628A1 (en) 2017-11-30
JP2019069969A (ja) 2019-05-09
EP3171870B1 (en) 2021-10-20
EP3171870A1 (en) 2017-05-31
US10071094B2 (en) 2018-09-11
JP2017523178A (ja) 2017-08-17
EP3171870A4 (en) 2017-12-27
CN106572989A (zh) 2017-04-19
WO2016014783A1 (en) 2016-01-28
JP6862404B2 (ja) 2021-04-21

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