BR112016003288A8 - processos para sintetizar n-[(3s)-1-[4-[(3-fluorofenil)metóxi]fenil]-5-oxo-pirrolidin-3-il]acetamida cristalina, e seu intermediário - Google Patents

processos para sintetizar n-[(3s)-1-[4-[(3-fluorofenil)metóxi]fenil]-5-oxo-pirrolidin-3-il]acetamida cristalina, e seu intermediário Download PDF

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Publication number
BR112016003288A8
BR112016003288A8 BR112016003288A BR112016003288A BR112016003288A8 BR 112016003288 A8 BR112016003288 A8 BR 112016003288A8 BR 112016003288 A BR112016003288 A BR 112016003288A BR 112016003288 A BR112016003288 A BR 112016003288A BR 112016003288 A8 BR112016003288 A8 BR 112016003288A8
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BR
Brazil
Prior art keywords
crystalline
pyrrolidin
acetamide
fluorophenyl
oxo
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BR112016003288A
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English (en)
Inventor
Wirz Beat
Scalone Michelangelo
Grassmann Olaf
Meier Roland
Hildbrand Stefan
Zutter Ulrich
Schwitter Urs
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112016003288A8 publication Critical patent/BR112016003288A8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones 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 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

formas cristalinas de um derivado de pirrolidona útil no tratamento de doença de alzheimer e preparação das mesmas a presente invenção refere-se a processos para fabricar n-[(3s)-1-[4-[(3-fluorofenil)metóxi]fenil]-5-oxo-pirrolidin-3-il]acetamida cristalina. também são divulgadas formas polimórficas do referido composto, bem como compostos úteis como intermediários nos métodos da invenção.
BR112016003288A 2013-10-29 2014-10-27 processos para sintetizar n-[(3s)-1-[4-[(3-fluorofenil)metóxi]fenil]-5-oxo-pirrolidin-3-il]acetamida cristalina, e seu intermediário BR112016003288A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13190612 2013-10-29
PCT/EP2014/072934 WO2015063001A1 (en) 2013-10-29 2014-10-27 Crystalline forms of a pyrrolidone derivative useful in the treatment of alzheimer's disease and preparation thereof

Publications (1)

Publication Number Publication Date
BR112016003288A8 true BR112016003288A8 (pt) 2020-02-04

Family

ID=49485638

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016003288A BR112016003288A8 (pt) 2013-10-29 2014-10-27 processos para sintetizar n-[(3s)-1-[4-[(3-fluorofenil)metóxi]fenil]-5-oxo-pirrolidin-3-il]acetamida cristalina, e seu intermediário

Country Status (11)

Country Link
US (1) US9562009B2 (pt)
EP (1) EP3063130A1 (pt)
JP (1) JP2016535046A (pt)
KR (1) KR20160067208A (pt)
CN (1) CN105705487A (pt)
BR (1) BR112016003288A8 (pt)
CA (1) CA2920070A1 (pt)
HK (1) HK1220203A1 (pt)
MX (1) MX361764B (pt)
RU (1) RU2016118748A (pt)
WO (1) WO2015063001A1 (pt)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04342591A (ja) * 1990-07-10 1992-11-30 Nissan Chem Ind Ltd ピラノベンゾオキサジアゾール誘導体
PE20050077A1 (es) * 2002-09-20 2005-03-01 Hoffmann La Roche Derivados de 4-pirrolidino-fenil-bencil-eter
US7148362B2 (en) * 2003-09-18 2006-12-12 Hoffmann-La Roche Inc. Process for the preparation of enantiopure pyrrolidin-2-one derivatives
CA2601416C (en) * 2005-03-15 2013-07-09 F. Hoffmann-La Roche Ag Method for preparing enantiomerically pure 4-pyrrolidinophenyl benzyl ether derivatives
US7501528B2 (en) 2005-03-15 2009-03-10 Hoffmann-La Roche Inc. Method for preparing enantiomerically pure 4-pyrrolidino phenylbenzyl ether derivatives
CN103304438B (zh) * 2013-06-18 2015-12-02 山东大学 N-取代水杨酰胺类化合物、制备方法及应用

Also Published As

Publication number Publication date
JP2016535046A (ja) 2016-11-10
HK1220203A1 (zh) 2017-04-28
MX361764B (es) 2018-12-17
RU2016118748A3 (pt) 2018-06-06
CA2920070A1 (en) 2015-05-07
RU2016118748A (ru) 2017-12-05
CN105705487A (zh) 2016-06-22
US20160237032A1 (en) 2016-08-18
EP3063130A1 (en) 2016-09-07
MX2016002763A (es) 2016-05-26
WO2015063001A1 (en) 2015-05-07
US9562009B2 (en) 2017-02-07
KR20160067208A (ko) 2016-06-13

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BR112016003288A8 (pt) processos para sintetizar n-[(3s)-1-[4-[(3-fluorofenil)metóxi]fenil]-5-oxo-pirrolidin-3-il]acetamida cristalina, e seu intermediário
BR112015023591A2 (pt) processo para a preparação de 4-amino-1-((ls,4r,5s)-2-fluoro-4,5-di-hidróxi-3-hidroximetil-ciclopent-2-enii)-1h-pirimidin-2-ona

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Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

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B07D Technical examination (opinion) related to article 229 of industrial property law

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07B Technical examination (opinion): publication cancelled

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