EA026144B9 - Твердофазная фармацевтическая композиция, содержащая гемифумаратную соль 1-{4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил}азетидин-3-карбоновой кислоты, и таблетка, ее содержащая - Google Patents

Твердофазная фармацевтическая композиция, содержащая гемифумаратную соль 1-{4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил}азетидин-3-карбоновой кислоты, и таблетка, ее содержащая

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Publication number
EA026144B9
EA026144B9 EA201391018A EA201391018A EA026144B9 EA 026144 B9 EA026144 B9 EA 026144B9 EA 201391018 A EA201391018 A EA 201391018A EA 201391018 A EA201391018 A EA 201391018A EA 026144 B9 EA026144 B9 EA 026144B9
Authority
EA
Eurasian Patent Office
Prior art keywords
ethyl
benzyloxyimino
azetidine
trifluoromethyl
benzyl
Prior art date
Application number
EA201391018A
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English (en)
Other versions
EA201391018A1 (ru
EA026144B1 (ru
Inventor
Филипп Буйо
Эмерик Рейно
Original Assignee
Новартис Аг
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44022942&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA026144(B9) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201391018A1 publication Critical patent/EA201391018A1/ru
Publication of EA026144B1 publication Critical patent/EA026144B1/ru
Publication of EA026144B9 publication Critical patent/EA026144B9/ru

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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

Abstract

Изобретение относится к твердофазной фармацевтической композиции, включающей один или более фармацевтически приемлемых эксципиентов и активный фармацевтический ингредиент ("API"), который представляет собой гемифумаратную соль 1-{4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил}азетидин-3-карбоновой кислоты, где API находится в смеси веществ, которая является свободной от основных соединений. Изобретение также относится к таблетке, включающей спрессованную смесь, состоящую из гемифумаратной соли 1-{4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил}азетидин-3-карбоновой кислоты, которая представлена в форме частиц, имеющих Х90 диаметр от 11 до 29 мкм, и одного или более неосновных эксципиентов. Данное изобретение обеспечивает уменьшение распада активного ингредиента и улучшение стабильности композиции и лекарственной формы.
EA201391018A 2011-01-07 2012-01-05 Твердофазная фармацевтическая композиция, содержащая гемифумаратную соль 1-{4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил}азетидин-3-карбоновой кислоты, и таблетка, ее содержащая EA026144B9 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11150431 2011-01-07
PCT/EP2012/050151 WO2012093161A1 (en) 2011-01-07 2012-01-05 Immunosuppressant formulations

Publications (3)

Publication Number Publication Date
EA201391018A1 EA201391018A1 (ru) 2013-11-29
EA026144B1 EA026144B1 (ru) 2017-03-31
EA026144B9 true EA026144B9 (ru) 2021-10-26

Family

ID=44022942

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391018A EA026144B9 (ru) 2011-01-07 2012-01-05 Твердофазная фармацевтическая композиция, содержащая гемифумаратную соль 1-{4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил}азетидин-3-карбоновой кислоты, и таблетка, ее содержащая

Country Status (34)

Country Link
US (3) US20130273161A1 (ru)
EP (2) EP3590507A1 (ru)
JP (2) JP6111202B2 (ru)
KR (2) KR101951966B1 (ru)
CN (1) CN103458877B (ru)
AR (2) AR084801A1 (ru)
AU (1) AU2012204835B2 (ru)
CA (1) CA2823616C (ru)
CL (1) CL2013001979A1 (ru)
CO (1) CO6761402A2 (ru)
CY (1) CY1122182T1 (ru)
DK (1) DK2661261T3 (ru)
EA (1) EA026144B9 (ru)
EC (1) ECSP13012812A (ru)
ES (1) ES2751920T3 (ru)
GT (1) GT201300178A (ru)
HR (1) HRP20191842T1 (ru)
HU (1) HUE045612T2 (ru)
IL (1) IL227094B (ru)
JO (1) JO3619B1 (ru)
LT (1) LT2661261T (ru)
MA (1) MA34897B1 (ru)
MX (2) MX371290B (ru)
MY (1) MY161162A (ru)
PE (1) PE20140216A1 (ru)
PL (1) PL2661261T3 (ru)
PT (1) PT2661261T (ru)
SG (1) SG191286A1 (ru)
SI (1) SI2661261T1 (ru)
TN (1) TN2013000257A1 (ru)
TW (2) TWI583380B (ru)
UA (1) UA114283C2 (ru)
WO (1) WO2012093161A1 (ru)
ZA (1) ZA201304465B (ru)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170027907A1 (en) * 2014-04-10 2017-02-02 Eric Legangneux Sip modulator immediate release dosage regimen
PT3129006T (pt) * 2014-04-10 2021-04-09 Novartis Ag Formulação imunossupressora
US20180042895A1 (en) 2015-02-26 2018-02-15 Novartis Ag Treatment of autoimmune disease in a patient receiving additionally a beta-blocker
EP4230208A1 (en) * 2015-07-03 2023-08-23 Astellas Pharma Inc. Stable pharmaceutical composition for oral administration
US11629124B2 (en) 2017-03-09 2023-04-18 Novartis Ag Solid forms comprising an oxime ether compound, compositions and methods of use thereof
JP7271517B2 (ja) 2017-09-27 2023-05-11 ノバルティス アーゲー シポニモドを含む非経口製剤
CA3073910A1 (en) 2017-09-29 2019-04-04 Novartis Ag Dosing regimen of siponimod
RU2020114751A (ru) 2017-09-29 2021-10-29 Новартис Аг Схема введения доз сипонимода
CN109908095A (zh) * 2019-04-08 2019-06-21 肇庆学院 一种西尼莫德片剂及制备方法
WO2021214717A1 (en) 2020-04-23 2021-10-28 Novartis Ag Dosing regimen for the use of siponimod for the treatment of acute respiratory distress syndrome
WO2023172508A1 (en) * 2022-03-09 2023-09-14 Isp Investments Llc Co-processed excipient composition

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU225964B1 (en) 1994-07-12 2008-01-28 Berwind Pharma Service Moisture barrier film coating composition, method, and coated form
CN100384398C (zh) * 2002-11-07 2008-04-30 日本泽托克株式会社 口腔用组合物用基质及口腔用组合物
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
AU2008310846C1 (en) * 2007-10-12 2022-10-06 Novartis Ag Compositions comprising sphingosine 1 phosphate (S1P) receptor modulators
BRPI0916968A2 (pt) * 2008-08-18 2015-11-24 Novartis Ag compostos para o tratamento de neuropatias periféricas, formulações farmacêuticas compreendendo os referidos compostos, e usos dos mesmos
RU2011129230A (ru) 2008-12-18 2013-01-27 Новартис Аг Новая полиморфная форма 1-[4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил]азетидин-3-карбоновой кислоты
UY32330A (es) * 2008-12-18 2010-07-30 Novartis Ag Novedosa forma de sal de ácido 1-(4-{1-[e-4-ciclohexil-3-trifluoro-metil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxílico, formas polimórficas, composiciones farmacéuticas conteniéndolas, procesos de preparación y aplicaciones
CN103204794A (zh) * 2008-12-18 2013-07-17 诺瓦提斯公司 新的盐
TWI472327B (zh) 2008-12-22 2015-02-11 Novartis Ag Ｓ１ｐ受體激動劑劑量療法

Also Published As

Publication number Publication date
TN2013000257A1 (en) 2014-11-10
CY1122182T1 (el) 2020-11-25
DK2661261T3 (da) 2019-10-21
LT2661261T (lt) 2019-10-25
CO6761402A2 (es) 2013-09-30
EA201391018A1 (ru) 2013-11-29
KR20140037815A (ko) 2014-03-27
AR124662A2 (es) 2023-04-19
KR101951966B1 (ko) 2019-02-25
ZA201304465B (en) 2014-02-26
JP6111202B2 (ja) 2017-04-05
JP2017141248A (ja) 2017-08-17
GT201300178A (es) 2014-12-30
EA026144B1 (ru) 2017-03-31
CA2823616A1 (en) 2012-07-12
EP2661261B1 (en) 2019-07-31
SG191286A1 (en) 2013-07-31
JP6324569B2 (ja) 2018-05-16
PE20140216A1 (es) 2014-03-01
PL2661261T3 (pl) 2020-01-31
JO3619B1 (ar) 2020-08-27
MX357304B (es) 2018-07-04
CL2013001979A1 (es) 2013-11-22
NZ612420A (en) 2015-05-29
CA2823616C (en) 2019-01-29
CN103458877A (zh) 2013-12-18
SI2661261T1 (sl) 2019-11-29
HUE045612T2 (hu) 2020-01-28
MA34897B1 (fr) 2014-02-01
TWI583380B (zh) 2017-05-21
TW201249438A (en) 2012-12-16
WO2012093161A1 (en) 2012-07-12
AU2012204835B2 (en) 2015-07-09
PT2661261T (pt) 2019-10-25
ES2751920T3 (es) 2020-04-02
TWI610672B (zh) 2018-01-11
IL227094B (en) 2019-03-31
TW201609092A (zh) 2016-03-16
EP2661261A1 (en) 2013-11-13
EP3590507A1 (en) 2020-01-08
JP2014501770A (ja) 2014-01-23
UA114283C2 (uk) 2017-05-25
BR112013017302A2 (pt) 2016-10-25
US20220064110A1 (en) 2022-03-03
MX2013007909A (es) 2013-08-29
US20200199069A1 (en) 2020-06-25
US20130273161A1 (en) 2013-10-17
MY161162A (en) 2017-04-14
ECSP13012812A (es) 2013-09-30
KR20190025727A (ko) 2019-03-11
MX371290B (es) 2020-01-24
AU2012204835A1 (en) 2013-08-01
HRP20191842T1 (hr) 2019-12-27
AR084801A1 (es) 2013-06-26
KR102166885B1 (ko) 2020-10-19
CN103458877B (zh) 2016-06-08

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