RU2019132074A - Новая аморфная дисперсия (5-{ 5-[n'-(2-хлор-6-метилбензоил)гидразинокарбонил]-2-метил-фенилэтинил} -пиридин-2-ил)амида циклопропанкарбоновой кислоты - Google Patents

Новая аморфная дисперсия (5-{ 5-[n'-(2-хлор-6-метилбензоил)гидразинокарбонил]-2-метил-фенилэтинил} -пиридин-2-ил)амида циклопропанкарбоновой кислоты Download PDF

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RU2019132074A
RU2019132074A RU2019132074A RU2019132074A RU2019132074A RU 2019132074 A RU2019132074 A RU 2019132074A RU 2019132074 A RU2019132074 A RU 2019132074A RU 2019132074 A RU2019132074 A RU 2019132074A RU 2019132074 A RU2019132074 A RU 2019132074A
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dosage form
amorphous dispersion
solid dosage
oral solid
hydrazinocarbonyl
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RU2019132074A3 (ru
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Яшорадж ЗАЛА
Брамхананд ХАНАМАННАВАР
Нитин ДХАРМАДХИКАРИ
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Сан Фарма Эдвансд Рисёч Компани Лимитед
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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
    • A61K31/435—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
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    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
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    • A—HUMAN NECESSITIES
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    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
    • C07D213/16—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/76—Nitrogen atoms to which a second hetero atom is attached
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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

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  • Engineering & Computer Science (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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Claims (8)

1. Пероральная твердая лекарственная форма, содержащая смесь соединения Формулы I
Figure 00000001
и плавкого полимерного носителя; и,
возможно, фармацевтически приемлемые эксципиенты, где данная смесь представляет собой аморфную дисперсию.
2. Пероральная твердая лекарственная форма по п. 1, в которой плавкий полимерный носитель представляет собой привитой сополимер поливинилкапролактама-поливинилацетата-полиэтиленгликоля.
3. Пероральная твердая лекарственная форма по п. 2, в которой аморфная дисперсия находится в размельченной форме, где все частицы имеют размер менее 500 микрометров.
4. Пероральная твердая лекарственная форма по п. 1, в которой массовое отношение плавкого полимерного носителя к соединению Формулы I составляет примерно 7:1.
5. Пероральная твердая лекарственная форма по п. 3, где данная лекарственная форма представляет собой капсулу, заполненную аморфной дисперсией и фармацевтически приемлемым эксципиентом.
RU2019132074A 2017-03-15 2018-03-15 Новая аморфная дисперсия (5-{ 5-[n'-(2-хлор-6-метилбензоил)гидразинокарбонил]-2-метил-фенилэтинил} -пиридин-2-ил)амида циклопропанкарбоновой кислоты RU2768887C2 (ru)

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IN201721005409 2017-03-15
IN201721005409 2017-03-15
PCT/IN2018/050147 WO2018167803A1 (en) 2017-03-15 2018-03-15 Novel amorphous dispersion of cyclopropanecarboxylic acid (5-{5-[ n'-(2-chloro-6-methylbenzoyl) hydrazinocarbonyl] -2-methyl-phenylethynyl}-pyridin-2-yl) amide

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KR20090018104A (ko) * 2006-05-08 2009-02-19 어리어드 파마슈티칼스, 인코포레이티드 아세틸렌계 헤테로아릴 화합물
JP2010509289A (ja) * 2006-11-09 2010-03-25 アボット ゲーエムベーハー ウント コンパニー カーゲー チロシンキナーゼ阻害剤の経口投与用薬学的剤形
AU2010208480A1 (en) * 2009-02-02 2011-07-28 Msd K.K. Inhibitors of Akt activity
JP5868414B2 (ja) * 2010-11-08 2016-02-24 カディラ ファーマシューティカルズ リミテッド タキソイドの医薬組成物
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RU2768887C2 (ru) 2022-03-25
WO2018167803A1 (en) 2018-09-20
JP7234128B2 (ja) 2023-03-07
MA47798A (fr) 2020-01-22
RU2019132074A3 (ru) 2021-07-13
JP2020510064A (ja) 2020-04-02
EP3596049A1 (en) 2020-01-22
EP3596049A4 (en) 2021-01-13
CN110506036A (zh) 2019-11-26
WO2018167803A9 (en) 2019-02-28
AU2018235447B2 (en) 2021-12-09
US20210113470A1 (en) 2021-04-22

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