CN109563088B - MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途 - Google Patents

MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途 Download PDF

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CN109563088B
CN109563088B CN201780049835.8A CN201780049835A CN109563088B CN 109563088 B CN109563088 B CN 109563088B CN 201780049835 A CN201780049835 A CN 201780049835A CN 109563088 B CN109563088 B CN 109563088B
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cancer
disease
pi3k
mek
tumors
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CN109563088A (zh
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布莱恩·D·罗斯
马尔奇安·范·杜特
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University of Michigan Ann Arbor
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K41/00Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
    • A61K41/0057Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
CN201780049835.8A 2016-07-06 2017-07-06 MEK/PI3K和mTOR/MEK/PI3K的多功能抑制剂和治疗用途 Active CN109563088B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662359001P 2016-07-06 2016-07-06
US62/359,001 2016-07-06
US201762454163P 2017-02-03 2017-02-03
US62/454,163 2017-02-03
PCT/US2017/040866 WO2018009638A1 (en) 2016-07-06 2017-07-06 MULTIFUNCTIONAL INHIBITORS OF MEK/PI3K AND mTOR/MEK/PI3K BIOLOGICAL PATHWAYS AND THERAPEUTIC METHODS USING THE SAME

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CN109563088A CN109563088A (zh) 2019-04-02
CN109563088B true CN109563088B (zh) 2022-10-11

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US (1) US10919877B2 (https=)
EP (2) EP4086250B1 (https=)
JP (2) JP2019519593A (https=)
CN (1) CN109563088B (https=)
AU (2) AU2017291838B2 (https=)
CA (1) CA3029875C (https=)
ES (2) ES3002745T3 (https=)
WO (1) WO2018009638A1 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018316175B2 (en) 2017-08-11 2023-02-23 The Regents Of The University Of Michigan Inhibitors of MEK/PI3K, JAK/MEK, JAK/PI3K/mTOR and MEK/PI3K3k/mTOR biological pathways and methods for improving lymphatic uptake, bioavailability, and solubility of therapeutic compounds
CN112143700B (zh) * 2019-06-26 2024-07-19 上海细胞治疗集团股份有限公司 制备过表达外源基因的免疫效应细胞的方法
CN117396470A (zh) * 2021-04-09 2024-01-12 巴塞尔大学 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物
EP4320115A1 (en) * 2021-04-09 2024-02-14 Universität Basel Triazine derivative as reversible and irreversible covalent inhibitors of pi3k
WO2023170107A1 (en) 2022-03-07 2023-09-14 Centre Hospitalier Universitaire Vaudois (Chuv) Pi3k/akt/mtor inhibitor for improving the cellular uptake of a radiopharmaceutical
JP2023180347A (ja) * 2022-06-09 2023-12-21 国立大学法人金沢大学 ハイブリッド型化合物又はその塩
WO2025072796A1 (en) * 2023-09-27 2025-04-03 Totus Medicines Inc. Pharmaceutical compositions and methods of use thereof

Citations (4)

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WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
CN103748099A (zh) * 2011-05-19 2014-04-23 西班牙国家癌症研究中心 作为蛋白激酶抑制剂的大环化合物
CN105283454A (zh) * 2013-04-12 2016-01-27 阿萨纳生物科技有限责任公司 作为ras/raf/mek/erk和pi3k/akt/pten/mtor通路双重抑制剂的喹唑啉和氮杂喹唑啉
CN105358156A (zh) * 2013-03-13 2016-02-24 密执安大学评议会 双重mek/pi3k抑制剂和使用其的治疗方法

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DZ3401A1 (fr) 2000-07-19 2002-01-24 Warner Lambert Co Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques
TW200505834A (en) 2003-03-18 2005-02-16 Sankyo Co Sulfamide derivative and the pharmaceutical composition thereof
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
AR059339A1 (es) 2006-02-09 2008-03-26 Chugai Pharmaceutical Co Ltd Derivados de la cumarina para trastornos proliferativos de celulas, composicion farmaceutica y agente terapeutico que los contiene
DK2074122T5 (da) 2006-09-15 2014-03-17 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer
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CN103748099A (zh) * 2011-05-19 2014-04-23 西班牙国家癌症研究中心 作为蛋白激酶抑制剂的大环化合物
CN105358156A (zh) * 2013-03-13 2016-02-24 密执安大学评议会 双重mek/pi3k抑制剂和使用其的治疗方法
CN105283454A (zh) * 2013-04-12 2016-01-27 阿萨纳生物科技有限责任公司 作为ras/raf/mek/erk和pi3k/akt/pten/mtor通路双重抑制剂的喹唑啉和氮杂喹唑啉

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"Phospshoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Discovery and Structure Activity Relationships of a Series of Quinoline and Quinoxaline Derivatives";Nobuko Nishimura,et al.;《Journal of medicinal chemistry》;20110525;第54卷;第4735-4751页 *
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Publication number Publication date
ES3002745T3 (en) 2025-03-07
EP4086250B1 (en) 2024-12-11
EP4086250A3 (en) 2023-03-22
JP7475062B2 (ja) 2024-04-26
JP2019519593A (ja) 2019-07-11
CA3029875A1 (en) 2018-01-11
CN109563088A (zh) 2019-04-02
CA3029875C (en) 2023-12-19
EP4086250C0 (en) 2024-12-11
JP2022019812A (ja) 2022-01-27
EP3481822A1 (en) 2019-05-15
AU2017291838B2 (en) 2021-01-28
AU2017291838A1 (en) 2019-01-17
US10919877B2 (en) 2021-02-16
AU2021202619A1 (en) 2021-05-27
WO2018009638A1 (en) 2018-01-11
EP4086250A2 (en) 2022-11-09
AU2021202619B2 (en) 2022-03-10
ES2922898T3 (es) 2022-09-21
EP3481822B1 (en) 2022-06-22
US20190224207A1 (en) 2019-07-25

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