EA201791336A1 - Фармацевтические составы на основе ингибиторов тропомиозин-родственных киназ (trk) - Google Patents

Фармацевтические составы на основе ингибиторов тропомиозин-родственных киназ (trk)

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Publication number
EA201791336A1
EA201791336A1 EA201791336A EA201791336A EA201791336A1 EA 201791336 A1 EA201791336 A1 EA 201791336A1 EA 201791336 A EA201791336 A EA 201791336A EA 201791336 A EA201791336 A EA 201791336A EA 201791336 A1 EA201791336 A1 EA 201791336A1
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Eurasian Patent Office
Prior art keywords
tropomyosin
trk
pharmaceutical compositions
compositions based
pharmaceutical formulations
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EA201791336A
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English (en)
Inventor
Харви Либерман
Дунлай Ян
К. Майкл Филбрук
Майкл Сантос
Крис Хо
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Джензим Корпорейшн
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Application filed by Джензим Корпорейшн filed Critical Джензим Корпорейшн
Publication of EA201791336A1 publication Critical patent/EA201791336A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

Раскрываются фармацевтические составы, содержащие ингибитор тропомиозин-родственных киназ ("Trk-ингибитор"). Фармацевтические составы содержат 3-(3-метокси-4-((4-метоксибензил)окси)бензил)-6-(1-метил-1H-пиразол-4-ил)-3H-имидазо[4,5-b]пиридин-2-амин в составах, содержащих микрокристаллическую суспензию, в его моногидратной форме, которая демонстрирует улучшенные характеристики по сравнению с ангидратной формой, и в составах с пролонгированным высвобождением. Фармацевтические составы с пролонгированным высвобождением содержат микросферы, нагруженные 3-(3-метокси-4-((4-метоксибензил)окси)бензил)-6-(1-метил-1Н-пиразол-4-ил)-3H-имидазо[4,5-b]пиридин-2-амином.
EA201791336A 2014-12-18 2015-12-17 Фармацевтические составы на основе ингибиторов тропомиозин-родственных киназ (trk) EA201791336A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462093801P 2014-12-18 2014-12-18
PCT/US2015/066396 WO2016100677A2 (en) 2014-12-18 2015-12-17 Pharmaceutical formulations of tropomyosin related kinase (trk) inhibitors

Publications (1)

Publication Number Publication Date
EA201791336A1 true EA201791336A1 (ru) 2017-10-31

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EA201791336A EA201791336A1 (ru) 2014-12-18 2015-12-17 Фармацевтические составы на основе ингибиторов тропомиозин-родственных киназ (trk)

Country Status (22)

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US (3) US10219998B2 (ru)
EP (1) EP3233057A2 (ru)
JP (1) JP6606183B2 (ru)
KR (1) KR102561692B1 (ru)
CN (2) CN110950862B (ru)
AR (1) AR103176A1 (ru)
AU (1) AU2015364557C1 (ru)
BR (1) BR112017012566B1 (ru)
CA (1) CA2970938C (ru)
CL (1) CL2017001543A1 (ru)
CO (1) CO2017007118A2 (ru)
EA (1) EA201791336A1 (ru)
IL (1) IL252901B (ru)
MA (1) MA40698A3 (ru)
MX (2) MX2017008058A (ru)
MY (1) MY195799A (ru)
NZ (1) NZ733825A (ru)
PH (1) PH12017501121A1 (ru)
SG (1) SG11201704872RA (ru)
TN (1) TN2017000234A1 (ru)
TW (2) TWI780438B (ru)
WO (1) WO2016100677A2 (ru)

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CN110950862A (zh) 2020-04-03
PH12017501121B1 (en) 2017-11-27
BR112017012566A2 (pt) 2018-01-02
PH12017501121A1 (en) 2017-11-27
WO2016100677A3 (en) 2016-08-11
MX2017008058A (es) 2017-09-28
KR20170096160A (ko) 2017-08-23
BR112017012566B1 (pt) 2024-01-30
US20180000728A1 (en) 2018-01-04
TWI780438B (zh) 2022-10-11
IL252901B (en) 2020-10-29
CA2970938C (en) 2023-04-18
AR103176A1 (es) 2017-04-19
SG11201704872RA (en) 2017-07-28
CN107231803B (zh) 2019-12-03
US11110055B2 (en) 2021-09-07
KR102561692B1 (ko) 2023-07-28
US11793749B2 (en) 2023-10-24
MX2020013015A (es) 2021-02-22
TW202104225A (zh) 2021-02-01
CO2017007118A2 (es) 2017-08-18
EP3233057A2 (en) 2017-10-25
MY195799A (en) 2023-02-21
US20220110861A1 (en) 2022-04-14
MA40698A2 (fr) 2018-10-31
AU2015364557C1 (en) 2021-11-18
AU2015364557B2 (en) 2021-04-29
TW201639837A (zh) 2016-11-16
TWI696621B (zh) 2020-06-21
JP2018503611A (ja) 2018-02-08
WO2016100677A2 (en) 2016-06-23
CN107231803A (zh) 2017-10-03
MA40698A3 (fr) 2020-01-31
US20200048222A1 (en) 2020-02-13
AU2015364557A1 (en) 2017-08-03
CN110950862B (zh) 2024-01-05
TN2017000234A1 (en) 2018-10-19
CL2017001543A1 (es) 2018-03-16
IL252901A0 (en) 2017-08-31
US10219998B2 (en) 2019-03-05
JP6606183B2 (ja) 2019-11-13

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