JP6796588B2 - Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物 - Google Patents

Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物 Download PDF

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Publication number
JP6796588B2
JP6796588B2 JP2017541936A JP2017541936A JP6796588B2 JP 6796588 B2 JP6796588 B2 JP 6796588B2 JP 2017541936 A JP2017541936 A JP 2017541936A JP 2017541936 A JP2017541936 A JP 2017541936A JP 6796588 B2 JP6796588 B2 JP 6796588B2
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Prior art keywords
cancer
methyl
methylethyl
ethane
pharmaceutical composition
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JP2018505193A5 (enExample
JP2018505193A (ja
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ディエゴ、フェルナンド、ドメニコ、ブロッジーニ
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Astex Therapeutics Ltd
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Astex Therapeutics Ltd
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    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K15/00—Anti-oxidant compositions; Compositions inhibiting chemical change
    • C09K15/04—Anti-oxidant compositions; Compositions inhibiting chemical change containing organic compounds
    • C09K15/20—Anti-oxidant compositions; Compositions inhibiting chemical change containing organic compounds containing nitrogen and oxygen

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Materials Engineering (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2017541936A 2015-02-10 2016-02-09 Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物 Active JP6796588B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP15154554.8 2015-02-10
EP15154554 2015-02-10
EP15188982 2015-10-08
EP15188982.1 2015-10-08
PCT/EP2016/052743 WO2016128411A1 (en) 2015-02-10 2016-02-09 Pharmaceutical compositions comprising n-(3,5-dimethoxyphenyl)-n'-(1-methylethyl)-n-[3-(1-methyl-1h-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine

Related Child Applications (1)

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JP2020189778A Division JP2021038241A (ja) 2015-02-10 2020-11-13 Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物

Publications (3)

Publication Number Publication Date
JP2018505193A JP2018505193A (ja) 2018-02-22
JP2018505193A5 JP2018505193A5 (enExample) 2019-03-22
JP6796588B2 true JP6796588B2 (ja) 2020-12-09

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JP2017541936A Active JP6796588B2 (ja) 2015-02-10 2016-02-09 Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物
JP2020189778A Pending JP2021038241A (ja) 2015-02-10 2020-11-13 Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物
JP2022172666A Active JP7550831B2 (ja) 2015-02-10 2022-10-27 Ｎ－（３，５－ジメトキシフェニル）－ｎ’－（１－メチルエチル）－ｎ－［３－（１－メチル－１ｈ－ピラゾール－４－イル）キノキサリン－６－イル］エタン－１，２－ジアミンを含んでなる医薬組成物

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JP2020189778A Pending JP2021038241A (ja) 2015-02-10 2020-11-13 Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物
JP2022172666A Active JP7550831B2 (ja) 2015-02-10 2022-10-27 Ｎ－（３，５－ジメトキシフェニル）－ｎ’－（１－メチルエチル）－ｎ－［３－（１－メチル－１ｈ－ピラゾール－４－イル）キノキサリン－６－イル］エタン－１，２－ジアミンを含んでなる医薬組成物

Country Status (32)

Country Link
US (3) US10898482B2 (enExample)
EP (2) EP3949954A1 (enExample)
JP (3) JP6796588B2 (enExample)
KR (2) KR102708049B1 (enExample)
CN (2) CN113209102A (enExample)
AU (3) AU2016218000B2 (enExample)
BR (1) BR112017017009B1 (enExample)
CA (1) CA2976356A1 (enExample)
CL (1) CL2017002022A1 (enExample)
CO (1) CO2017008862A2 (enExample)
CR (1) CR20170411A (enExample)
CY (1) CY1124432T1 (enExample)
DK (1) DK3256109T3 (enExample)
ES (1) ES2883829T3 (enExample)
HR (1) HRP20211244T1 (enExample)
HU (1) HUE056761T2 (enExample)
IL (3) IL310469B2 (enExample)
JO (2) JO3695B1 (enExample)
LT (1) LT3256109T (enExample)
MA (2) MA55571A (enExample)
MX (2) MX381504B (enExample)
MY (1) MY196599A (enExample)
NI (1) NI201700101A (enExample)
PH (2) PH12021551589A1 (enExample)
PL (1) PL3256109T3 (enExample)
RS (1) RS62221B1 (enExample)
SG (2) SG11201706472RA (enExample)
SI (1) SI3256109T1 (enExample)
SM (1) SMT202100450T1 (enExample)
TW (2) TWI719960B (enExample)
UA (1) UA123767C2 (enExample)
WO (1) WO2016128411A1 (enExample)

Cited By (1)

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JP2021038241A (ja) * 2015-02-10 2021-03-11 アステックス、セラピューティックス、リミテッドＡｓｔｅｘ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ Ｎ−（３，５−ジメトキシフェニル）−ｎ’−（１−メチルエチル）−ｎ−［３−（１−メチル−１ｈ−ピラゾール−４−イル）キノキサリン−６−イル］エタン−１，２−ジアミンを含んでなる医薬組成物

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GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
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GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
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US10736900B2 (en) 2014-03-26 2020-08-11 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
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