EA201691484A1 - Соли и твердая форма ингибитора btk - Google Patents

Соли и твердая форма ингибитора btk

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Publication number
EA201691484A1
EA201691484A1 EA201691484A EA201691484A EA201691484A1 EA 201691484 A1 EA201691484 A1 EA 201691484A1 EA 201691484 A EA201691484 A EA 201691484A EA 201691484 A EA201691484 A EA 201691484A EA 201691484 A1 EA201691484 A1 EA 201691484A1
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EA
Eurasian Patent Office
Prior art keywords
salts
compound
solid form
salt
btk inhibitor
Prior art date
Application number
EA201691484A
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English (en)
Other versions
EA033900B1 (ru
Inventor
Мохаммад Реза Масджедизаде
Стивен Гурли
Original Assignee
Принсипиа Биофарма Инк.
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Application filed by Принсипиа Биофарма Инк. filed Critical Принсипиа Биофарма Инк.
Publication of EA201691484A1 publication Critical patent/EA201691484A1/ru
Publication of EA033900B1 publication Critical patent/EA033900B1/ru

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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5395—Heterocyclic 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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
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    • 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
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    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
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    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
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    • A61K9/0043—Nose
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    • A61K9/0012—Galenical forms characterised by the site of application
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    • A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Abstract

В настоящем изобретении предложены способы получения свободного основания 2-[(3R)-3-[4-амино-3-(2-фтор-4-феноксифенил)пиразоло[3,4-d]пиримидин-1-ил]пиперидин-1-карбонил]-4-метил-4-[4-(оксетан-3-ил)пиперазин-1-ил]пент-2-еннитрила (соединение (I)), солей соединения (I) и указанных солей в твердой форме. Также в настоящем изобретении предложены фармацевтические композиции, содержащие такие соли и их твердые формы, и способы лечения рака, аутоиммунных и воспалительных заболеваний с применением соединения (I) или его фармацевтически приемлемой соли.
EA201691484A 2014-02-21 2015-02-20 СОЛЕВЫЕ И АМОРФНЫЕ ФОРМЫ 2-[(3R)-3-[4-АМИНО-3-(2-ФТОР-4-ФЕНОКСИФЕНИЛ)ПИРАЗОЛО[3,4-d]ПИРИМИДИН-1-ИЛ]ПИПЕРИДИН-1-КАРБОНИЛ]-4-МЕТИЛ-4-[4-(ОКСЕТАН-3-ИЛ)ПИПЕРАЗИН-1-ИЛ]ПЕНТ-2-ЕННИТРИЛА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ПУЗЫРЧАТКИ ОБЫКНОВЕННОЙ И ПУЗЫРЧАТКИ ЛИСТОВИДНОЙ С ИХ ПРИМЕНЕНИЕМ EA033900B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201461943262P 2014-02-21 2014-02-21
US201461946480P 2014-02-28 2014-02-28
US201462096468P 2014-12-23 2014-12-23
PCT/US2015/016963 WO2015127310A1 (en) 2014-02-21 2015-02-20 Salts and solid form of a btk inhibitor

Publications (2)

Publication Number Publication Date
EA201691484A1 true EA201691484A1 (ru) 2017-03-31
EA033900B1 EA033900B1 (ru) 2019-12-06

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EA201691484A EA033900B1 (ru) 2014-02-21 2015-02-20 СОЛЕВЫЕ И АМОРФНЫЕ ФОРМЫ 2-[(3R)-3-[4-АМИНО-3-(2-ФТОР-4-ФЕНОКСИФЕНИЛ)ПИРАЗОЛО[3,4-d]ПИРИМИДИН-1-ИЛ]ПИПЕРИДИН-1-КАРБОНИЛ]-4-МЕТИЛ-4-[4-(ОКСЕТАН-3-ИЛ)ПИПЕРАЗИН-1-ИЛ]ПЕНТ-2-ЕННИТРИЛА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ПУЗЫРЧАТКИ ОБЫКНОВЕННОЙ И ПУЗЫРЧАТКИ ЛИСТОВИДНОЙ С ИХ ПРИМЕНЕНИЕМ

Country Status (17)

Country Link
US (5) US10092569B2 (ru)
EP (2) EP3107544B1 (ru)
JP (1) JP6504548B2 (ru)
KR (2) KR20220027271A (ru)
CN (2) CN112353806A (ru)
AU (1) AU2015218713B2 (ru)
BR (1) BR112016018948B1 (ru)
CA (1) CA2939186C (ru)
EA (1) EA033900B1 (ru)
ES (1) ES2841248T3 (ru)
HK (1) HK1232155A1 (ru)
IL (2) IL247215B (ru)
MX (1) MX2016010754A (ru)
PT (1) PT3107544T (ru)
SG (2) SG11201606858RA (ru)
WO (1) WO2015127310A1 (ru)
ZA (2) ZA201605933B (ru)

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TW202308638A (zh) 2021-04-16 2023-03-01 美商普林斯匹亞生物製藥公司 藉由投予特定化合物治療藥物及疫苗誘發的免疫性血小板減少症之方法
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