BR112013013134A2 - método de preparação de metaxalona, metaxalona, e, composição farmacêutica - Google Patents

método de preparação de metaxalona, metaxalona, e, composição farmacêutica

Info

Publication number
BR112013013134A2
BR112013013134A2 BR112013013134A BR112013013134A BR112013013134A2 BR 112013013134 A2 BR112013013134 A2 BR 112013013134A2 BR 112013013134 A BR112013013134 A BR 112013013134A BR 112013013134 A BR112013013134 A BR 112013013134A BR 112013013134 A2 BR112013013134 A2 BR 112013013134A2
Authority
BR
Brazil
Prior art keywords
metaxalone
solvent
tgic
pharmaceutical composition
preparation
Prior art date
Application number
BR112013013134A
Other languages
English (en)
Other versions
BR112013013134B1 (pt
Inventor
Antonello Fazio
Giovanni Battista Ciotoli
Marcello Marchetti
Mario Chiavarini
Tommaso Iacoangeli
Original Assignee
Acraf
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Acraf filed Critical Acraf
Publication of BR112013013134A2 publication Critical patent/BR112013013134A2/pt
Publication of BR112013013134B1 publication Critical patent/BR112013013134B1/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18Oxygen atoms
    • C07D263/20Oxygen atoms attached in position 2
    • C07D263/24Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/4211,3-Oxazoles, e.g. pemoline, trimethadione
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02Local antiseptics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

método de preparação de metaxalona, metaxalona, e, composição farmacêutica. a presente invenção se refere a um método de preparação de metaxalona compreendendo reação de isocianurato de triglicidila (tgic) com m-xilenol, em que a dita reação é realizada em uma mistura de solvente compreendendo um solvente polar aprótico com constante dielétrica maior ou igual a 30 e pelo menos um outro solvente selecionado do grupo compreendendo solvente apolares e solventes polares apróticos com constante dielétrica abaixo de 30 a dita mistura de solvente compreendendo de 5 a 40% em peso do dito primeiro solvente e de 95 a 60% em peso do dito segundo solvente, adicionando a tgic a uma temperatura entre 30°c e 50°c, e depois adicionando a tgic, aumentando a temperatura da solução da reação para um valor entre 80°c em um tempo entre 120 e 180 minutos a uma taxa de aumento não maior que 1,25°c por minuto. a invenção também se refere a um metaxalona com um baixo teor de impureza derivadas de reações incompletas e/ou reações laterais do método de produção.
BR112013013134-9A 2011-02-01 2012-01-17 método de preparação de metaxalona BR112013013134B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11152849.3 2011-02-01
EP11152849 2011-02-01
US201161439127P 2011-02-03 2011-02-03
US61/439,127 2011-02-03
PCT/EP2012/050609 WO2012104139A1 (en) 2011-02-01 2012-01-17 Method of preparation of metaxalone

Publications (2)

Publication Number Publication Date
BR112013013134A2 true BR112013013134A2 (pt) 2016-08-23
BR112013013134B1 BR112013013134B1 (pt) 2021-06-08

Family

ID=44115617

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013013134-9A BR112013013134B1 (pt) 2011-02-01 2012-01-17 método de preparação de metaxalona

Country Status (27)

Country Link
US (2) US20130261160A1 (pt)
EP (1) EP2670737B1 (pt)
JP (1) JP2014503564A (pt)
KR (1) KR101907599B1 (pt)
CN (1) CN103298797B (pt)
AR (1) AR084946A1 (pt)
AU (1) AU2012213666B2 (pt)
BR (1) BR112013013134B1 (pt)
CA (1) CA2817462C (pt)
CY (1) CY1118348T1 (pt)
DK (1) DK2670737T3 (pt)
EA (1) EA024417B1 (pt)
ES (1) ES2605425T3 (pt)
GE (1) GEP20156352B (pt)
HK (1) HK1191006A1 (pt)
HR (1) HRP20161660T1 (pt)
HU (1) HUE029476T2 (pt)
IL (1) IL226329A (pt)
LT (1) LT2670737T (pt)
MX (1) MX339346B (pt)
PL (1) PL2670737T3 (pt)
PT (1) PT2670737T (pt)
SG (2) SG192090A1 (pt)
SI (1) SI2670737T1 (pt)
SM (1) SMT201600415B (pt)
UA (1) UA114593C2 (pt)
WO (1) WO2012104139A1 (pt)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102181881B1 (ko) 2014-11-21 2020-11-24 삼성디스플레이 주식회사 비전 검사 장치 및 이의 감마 및 얼룩 보정 방법

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1545951A1 (de) * 1965-07-24 1970-05-14 Henkel & Cie Gmbh Verfahren zur Herstellung von substituierten Oxazolidonen
FR1487641A (fr) 1965-07-24 1967-07-07 Henkel & Cie Gmbh Procédé de préparation d'oxazolidones substituées
WO2003061552A2 (en) * 2002-01-14 2003-07-31 Sun Pharmaceutical Industries Limited Novel process for the preparation of substantially pure 5-(3,5-dimethylphenoxy)methyl-2-oxazolidinone
US6562980B1 (en) * 2002-08-19 2003-05-13 Yung Shin Pharma Ind. Co., Ltd. Method for producing 5-aryloxymethyl-2-oxazolidinones
WO2007074477A2 (en) * 2005-12-29 2007-07-05 Dabur Pharma Limited Metaxalone polymorphs
WO2008006096A1 (en) 2006-07-07 2008-01-10 Boehringer Ingelheim Chemicals, Inc. Metaxalone synthesis
CN101921241A (zh) * 2009-06-12 2010-12-22 北京京卫燕康药物研究所有限公司 具有光学活性的美他沙酮的合成

Also Published As

Publication number Publication date
UA114593C2 (uk) 2017-07-10
WO2012104139A1 (en) 2012-08-09
LT2670737T (lt) 2016-12-12
HUE029476T2 (en) 2017-02-28
KR20140000705A (ko) 2014-01-03
CN103298797A (zh) 2013-09-11
US20130261160A1 (en) 2013-10-03
MX339346B (es) 2016-05-20
EP2670737B1 (en) 2016-09-14
PT2670737T (pt) 2016-11-08
SMT201600415B (it) 2017-01-10
MX2013008426A (es) 2013-09-13
IL226329A0 (en) 2013-07-31
SG10201600357WA (en) 2016-02-26
AU2012213666A1 (en) 2013-05-30
DK2670737T3 (en) 2016-12-19
PL2670737T3 (pl) 2017-02-28
HK1191006A1 (zh) 2014-07-18
CA2817462A1 (en) 2012-08-09
KR101907599B1 (ko) 2018-10-12
EA024417B1 (ru) 2016-09-30
SG192090A1 (en) 2013-08-30
GEP20156352B (en) 2015-08-25
SI2670737T1 (sl) 2016-12-30
CA2817462C (en) 2019-03-19
ES2605425T3 (es) 2017-03-14
US20150284345A1 (en) 2015-10-08
JP2014503564A (ja) 2014-02-13
EA201390787A1 (ru) 2013-11-29
US9416116B2 (en) 2016-08-16
CY1118348T1 (el) 2017-06-28
CN103298797B (zh) 2016-04-20
HRP20161660T1 (hr) 2017-01-13
EP2670737A1 (en) 2013-12-11
BR112013013134B1 (pt) 2021-06-08
AR084946A1 (es) 2013-07-10
IL226329A (en) 2017-12-31
AU2012213666B2 (en) 2016-09-08

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06T Formal requirements before examination [chapter 6.20 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 17/01/2012, OBSERVADAS AS CONDICOES LEGAIS.