EA201070719A1 - Способ получения 2-[4-(3- или 2-фторбензилокси)бензиламино]пропанамидов с высокой степенью чистоты - Google Patents

Способ получения 2-[4-(3- или 2-фторбензилокси)бензиламино]пропанамидов с высокой степенью чистоты

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Publication number
EA201070719A1
EA201070719A1 EA201070719A EA201070719A EA201070719A1 EA 201070719 A1 EA201070719 A1 EA 201070719A1 EA 201070719 A EA201070719 A EA 201070719A EA 201070719 A EA201070719 A EA 201070719A EA 201070719 A1 EA201070719 A1 EA 201070719A1
Authority
EA
Eurasian Patent Office
Prior art keywords
propanamides
benzylamino
purity
high degree
obtaining
Prior art date
Application number
EA201070719A
Other languages
English (en)
Other versions
EA019898B1 (ru
Inventor
Елена Барбанти
Лаура Фаравелли
Патрисия Сальвати
Ренато Каневотти
Франческо Понзини
Original Assignee
Ньюрон Фармасьютикалс С.П.А.
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 Ньюрон Фармасьютикалс С.П.А. filed Critical Ньюрон Фармасьютикалс С.П.А.
Publication of EA201070719A1 publication Critical patent/EA201070719A1/ru
Publication of EA019898B1 publication Critical patent/EA019898B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/02Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups
    • C07C251/24Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/22Separation; Purification; Stabilisation; Use of additives
    • C07C231/24Separation; Purification

Abstract

Способ получения терапевтически активных 2-[4-(3- и 2-(фторбензилокси)бензиламино]пропанамидов и их солей с фармацевтически приемлемыми кислотами с высокой степенью чистоты, в частности с содержанием примесей дибензиловых производных менее 0,03, предпочтительно менее 0,01 мас.%. Способ осуществляют, подвергая промежуточные основания Шиффа 2-[4-(3- и 2-фторбензилокси)бензилиденамино]пропанамидов реакции восстановления восстановителем, выбранным из боргидрида натрия и боргидрида калия в соответствующем количестве органического растворителя, выбранного из низших (C-C)-алканолов, обеспечивая образование и присутствие в ходе значительной части реакции восстановления суспензии основания Шиффа в насыщенном растворе основания Шиффа в том же органическом растворителе.
EA201070719A 2007-12-11 2008-12-01 Способ получения 2-[4-(3- или 2-фторбензилокси)бензиламино]пропанамидов с высокой степенью чистоты EA019898B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07023937 2007-12-11
PCT/EP2008/066559 WO2009074478A1 (en) 2007-12-11 2008-12-01 Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree

Publications (2)

Publication Number Publication Date
EA201070719A1 true EA201070719A1 (ru) 2010-12-30
EA019898B1 EA019898B1 (ru) 2014-07-30

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
EA201400105A EA030250B1 (ru) 2007-12-11 2008-12-01 Применение 2-[4-(3- или 2-фторбензилокси)бензиламино]пропанамидов с высокой степенью чистоты и содержащие их фармацевтические композиции
EA201070719A EA019898B1 (ru) 2007-12-11 2008-12-01 Способ получения 2-[4-(3- или 2-фторбензилокси)бензиламино]пропанамидов с высокой степенью чистоты

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201400105A EA030250B1 (ru) 2007-12-11 2008-12-01 Применение 2-[4-(3- или 2-фторбензилокси)бензиламино]пропанамидов с высокой степенью чистоты и содержащие их фармацевтические композиции

Country Status (27)

Country Link
US (2) US8530701B2 (ru)
EP (2) EP2229351B1 (ru)
JP (2) JP5460613B2 (ru)
KR (2) KR101709498B1 (ru)
CN (2) CN101896456B (ru)
AR (1) AR071267A1 (ru)
AU (1) AU2008334778B2 (ru)
BR (1) BRPI0820657A2 (ru)
CA (2) CA2706789C (ru)
CY (1) CY1119991T1 (ru)
DK (1) DK2229351T3 (ru)
EA (2) EA030250B1 (ru)
ES (2) ES2837000T3 (ru)
HK (2) HK1145673A1 (ru)
HR (1) HRP20180210T1 (ru)
HU (1) HUE036232T2 (ru)
IL (1) IL205872A (ru)
LT (1) LT2229351T (ru)
MX (1) MX2010006278A (ru)
NO (1) NO2229351T3 (ru)
NZ (1) NZ585806A (ru)
PL (1) PL2229351T3 (ru)
PT (1) PT2229351T (ru)
RS (1) RS56803B1 (ru)
SI (1) SI2229351T1 (ru)
TW (1) TWI429425B (ru)
WO (1) WO2009074478A1 (ru)

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EP2229351B1 (en) * 2007-12-11 2017-11-08 Newron Pharmaceuticals S.p.A. Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree
EP2314569A1 (en) * 2009-10-22 2011-04-27 Merck Patent GmbH Novel polymorphic forms of (S)-2-[4-(3-Fluoro-benzyloxy)-benzylamino]-propionamide mesylate salt and processes of manufacturing thereof
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WO2015102390A1 (ko) * 2013-12-30 2015-07-09 이화여자대학교 산학협력단 신규한 아미드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 통증의 예방 또는 치료용 약학적 조성물
CN104292128A (zh) * 2014-07-01 2015-01-21 南京正科制药有限公司 一种沙芬酰胺晶型a
CN105017060B (zh) * 2015-07-03 2017-06-16 南京正大天晴制药有限公司 一种沙芬酰胺新晶型及其制备方法
CN106365966A (zh) * 2015-07-24 2017-02-01 上海医药集团股份有限公司 一种苄基芳基醚的制备方法
CN105061245A (zh) * 2015-08-25 2015-11-18 成都维恒医药科技有限公司 一种高纯度沙芬酰胺的制备方法
CN106565521B (zh) * 2016-08-24 2019-03-08 浙江美诺华药物化学有限公司 (s)-2-[3-(3-氟苄基)-4-(3-氟苄氧基)苄氨基]丙酰胺及其盐的制备方法
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CN106596828B (zh) * 2016-12-15 2018-09-25 扬子江药业集团有限公司 一种甲磺酸沙芬酰胺有关物质的检测方法
WO2019167085A1 (en) * 2018-03-01 2019-09-06 Msn Laboratories Private Limited, R&D Center Process for the preparation of (s)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino propanamide methanesulfonate
WO2020136671A1 (en) * 2018-12-27 2020-07-02 Natco Pharma Limited Improved process for the preparation of lapatinib base and it's anhydrous ditosylate salt
EP3725768A1 (en) * 2019-04-17 2020-10-21 Newron Pharmaceuticals S.p.A. Process for the production of substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives
US11111208B2 (en) * 2019-06-17 2021-09-07 RK Pharma Solutions LLC Process for the preparation of safinamide mesylate intermediate
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CN113444010B (zh) * 2020-03-28 2023-09-05 南京正大天晴制药有限公司 一种沙芬酰胺有关物质的制备方法
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EP2229351B1 (en) * 2007-12-11 2017-11-08 Newron Pharmaceuticals S.p.A. Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree

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Publication number Publication date
CN104523668A (zh) 2015-04-22
IL205872A (en) 2015-06-30
JP6023727B2 (ja) 2016-11-09
EA201400105A1 (ru) 2014-05-30
JP2011506375A (ja) 2011-03-03
KR101593627B1 (ko) 2016-02-11
AU2008334778B2 (en) 2013-05-23
BRPI0820657A2 (pt) 2015-06-16
US20100324141A1 (en) 2010-12-23
EP3257842A1 (en) 2017-12-20
ES2837000T3 (es) 2021-06-29
CN101896456B (zh) 2014-10-22
WO2009074478A1 (en) 2009-06-18
RS56803B1 (sr) 2018-04-30
CA2706789C (en) 2016-09-06
AU2008334778A2 (en) 2010-07-08
EP2229351B1 (en) 2017-11-08
JP2014159407A (ja) 2014-09-04
HRP20180210T1 (hr) 2018-03-09
HK1204960A1 (en) 2015-12-11
TW200932209A (en) 2009-08-01
US8530701B2 (en) 2013-09-10
HK1145673A1 (en) 2011-04-29
EP3257842B1 (en) 2020-11-18
LT2229351T (lt) 2018-01-25
PL2229351T3 (pl) 2018-04-30
KR20100103571A (ko) 2010-09-27
JP5460613B2 (ja) 2014-04-02
CA2936209C (en) 2020-02-11
AU2008334778A1 (en) 2009-06-18
SI2229351T1 (en) 2018-02-28
DK2229351T3 (en) 2018-01-22
IL205872A0 (en) 2010-11-30
NO2229351T3 (ru) 2018-04-07
US8846763B2 (en) 2014-09-30
AR071267A1 (es) 2010-06-09
EA019898B1 (ru) 2014-07-30
EA030250B1 (ru) 2018-07-31
NZ585806A (en) 2011-09-30
US20140051758A1 (en) 2014-02-20
HUE036232T2 (hu) 2018-06-28
TWI429425B (zh) 2014-03-11
CN101896456A (zh) 2010-11-24
ES2655706T3 (es) 2018-02-21
EP2229351A1 (en) 2010-09-22
PT2229351T (pt) 2018-01-19
KR101709498B1 (ko) 2017-02-23
CN104523668B (zh) 2020-06-09
CA2936209A1 (en) 2009-06-18
KR20160017140A (ko) 2016-02-15
CY1119991T1 (el) 2018-12-12
MX2010006278A (es) 2010-08-31
CA2706789A1 (en) 2009-06-18

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