KR101851118B1 - 랄핀아미드 메탄설포네이트 염들 또는 이들의 ｒ―에난티오머들의 제조 방법 - Google Patents

랄핀아미드 메탄설포네이트 염들 또는 이들의 ｒ―에난티오머들의 제조 방법 Download PDF

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KR101851118B1
KR101851118B1 KR1020127030931A KR20127030931A KR101851118B1 KR 101851118 B1 KR101851118 B1 KR 101851118B1 KR 1020127030931 A KR1020127030931 A KR 1020127030931A KR 20127030931 A KR20127030931 A KR 20127030931A KR 101851118 B1 KR101851118 B1 KR 101851118B1
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salt
crystalline
water
methanesulfonate
mixture
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KR20130094212A (ko
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클라우디오 지오르다노
에르빈 발트포겔
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뉴론 파마슈티칼즈 에스. 피. 에이.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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 the carbon skeleton being acyclic and saturated
    • C07C237/08—Carboxylic 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 the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/22—Separation; Purification; Stabilisation; Use of additives
    • C07C231/24—Separation; Purification
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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 the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic 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 the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group

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  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
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  • Cardiology (AREA)
  • Hematology (AREA)
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  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020127030931A 2010-04-27 2011-04-06 랄핀아미드 메탄설포네이트 염들 또는 이들의 ｒ―에난티오머들의 제조 방법 Active KR101851118B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10161207 2010-04-27
EP10161207.5 2010-04-27
PCT/EP2011/055309 WO2011134763A1 (en) 2010-04-27 2011-04-06 Process for the production of ralfinamide methanesulfonate salts or their r-enantiomers

Publications (2)

Publication Number Publication Date
KR20130094212A KR20130094212A (ko) 2013-08-23
KR101851118B1 true KR101851118B1 (ko) 2018-04-23

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US (2) US9505708B2 (https=)
EP (1) EP2563355B1 (https=)
JP (3) JP5808392B2 (https=)
KR (1) KR101851118B1 (https=)
CN (2) CN102858330B (https=)
AR (1) AR085171A1 (https=)
AU (1) AU2011246707B2 (https=)
BR (1) BR112012027623B1 (https=)
CA (1) CA2794389C (https=)
CY (1) CY1117879T1 (https=)
DK (1) DK2563355T3 (https=)
EA (1) EA021389B1 (https=)
ES (1) ES2590128T3 (https=)
HR (1) HRP20161077T1 (https=)
HU (1) HUE030504T2 (https=)
IL (1) IL222532A (https=)
LT (1) LT2563355T (https=)
ME (1) ME02509B (https=)
MX (1) MX342697B (https=)
NZ (2) NZ602648A (https=)
PL (1) PL2563355T3 (https=)
PT (1) PT2563355T (https=)
RS (1) RS55084B1 (https=)
SI (1) SI2563355T1 (https=)
SM (1) SMT201600266B (https=)
TW (1) TWI492919B (https=)
WO (1) WO2011134763A1 (https=)

Families Citing this family (5)

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JP5808392B2 (ja) * 2010-04-27 2015-11-10 ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー ラルフィナミドメタンスルホネート塩またはそのｒ−エナンチオマーの製造方法
CN103804341B (zh) * 2012-11-13 2018-04-10 中国人民解放军军事医学科学院毒物药物研究所 酰胺衍生物及其医药用途
CN104761531B (zh) * 2014-01-03 2017-12-01 中国人民解放军军事医学科学院毒物药物研究所 镇痛活性化合物及其医药用途
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
CN115368310B (zh) * 2021-05-18 2025-06-27 奥库菲尔医药公司 合成甲磺酸酚妥拉明的方法

Citations (1)

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IL94466A (en) 1989-05-25 1995-01-24 Erba Carlo Spa Pharmaceutical preparations containing the history of A-amino carboxamide N-phenylalkyl are converted into such new compounds and their preparation
GB9515412D0 (en) * 1995-07-27 1995-09-27 Pharmacia Spa 2-(4-substituted)-benzylamino-2-methyl-propanamide derivatives
GB9727523D0 (en) 1997-12-31 1998-02-25 Pharmacia & Upjohn Spa Alpha-aminoamide derivatives useful as analgesic agents
IL160523A0 (en) 2001-09-03 2004-07-25 Newron Pharm Spa PHARMACEUTICAL COMPOSITION COMPRISING GABAPENTIN OR AN ANALOGUE THEREOF AND AN alpha-AMINOAMIDE AND ITS ANALGESIC USE
EP1438956A1 (en) 2003-01-16 2004-07-21 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful as antimigraine agents
US20040213842A1 (en) * 2003-01-30 2004-10-28 Dynogen Pharmaceuticals, Inc. Methods of treating gastrointestinal tract disorders using sodium channel modulators
AR044007A1 (es) 2003-04-11 2005-08-24 Newron Pharmaceuticals Inc Metodos para el tratamiento de la enfermedad de parkinson
AU2004266494B2 (en) 2003-08-25 2010-04-08 Newron Pharmaceuticals, Spa Alpha-aminoamide derivatives useful as anti-inflammatory agents
EP1557166A1 (en) 2004-01-21 2005-07-27 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful in the treatment of lower urinary tract disorders
EP1588704A1 (en) 2004-04-22 2005-10-26 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful in the treatment of restless legs syndrome and addictive disorders
ATE471147T1 (de) * 2004-09-10 2010-07-15 Newron Pharm Spa Verwendung von (r)-(halogenbenzyloxy)-benzylamino-propanamiden als natrium- und/oder calciumkanal- selektive modulatoren
EP1870097A1 (en) 2006-06-15 2007-12-26 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful in the treatment of cognitive disorders
HUE030233T2 (en) * 2006-06-19 2017-04-28 Newron Pharm Spa High purity 2- [4- (3- and 2-fluorobenzyloxy) benzylamino] propanamides for use as medicaments and pharmaceutical compositions containing them
JP5315674B2 (ja) * 2007-11-19 2013-10-16 セントラル硝子株式会社 非水電池用電解液及びこれを用いた非水電池
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WO2009109334A1 (en) 2008-03-07 2009-09-11 Newron Pharmaceuticals S.P.A. (s)-(+)-2-[4-fluorbenzyloxy)benzylamino]propanamide for use in the treatment of mixed or combined pain
JP5808392B2 (ja) * 2010-04-27 2015-11-10 ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー ラルフィナミドメタンスルホネート塩またはそのｒ−エナンチオマーの製造方法

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WO2009074478A1 (en) * 2007-12-11 2009-06-18 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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US9856207B2 (en) 2018-01-02
DK2563355T3 (en) 2016-09-12
CA2794389A1 (en) 2011-11-03
BR112012027623B1 (pt) 2021-07-06
CA2794389C (en) 2016-08-23
CN105037188A (zh) 2015-11-11
EA021389B1 (ru) 2015-06-30
CY1117879T1 (el) 2017-05-17
JP2017197553A (ja) 2017-11-02
HUE030504T2 (en) 2017-05-29
MX2012012093A (es) 2012-12-17
ES2590128T3 (es) 2016-11-18
TWI492919B (zh) 2015-07-21
US20170029365A1 (en) 2017-02-02
WO2011134763A1 (en) 2011-11-03
TW201139344A (en) 2011-11-16
CN105037188B (zh) 2017-06-23
CN102858330A (zh) 2013-01-02
JP6450420B2 (ja) 2019-01-09
JP2013528577A (ja) 2013-07-11
JP2015180664A (ja) 2015-10-15
EP2563355A1 (en) 2013-03-06
MX342697B (es) 2016-10-10
JP6345154B2 (ja) 2018-06-20
LT2563355T (lt) 2016-09-26
US20130039983A1 (en) 2013-02-14
SMT201600266B (it) 2016-08-31
EP2563355B1 (en) 2016-06-08
BR112012027623A2 (pt) 2016-08-09
AU2011246707B2 (en) 2014-11-20
SI2563355T1 (sl) 2016-10-28
HRP20161077T1 (hr) 2016-10-21
RS55084B1 (sr) 2016-12-30
HK1213872A1 (zh) 2016-07-15
NZ602648A (en) 2014-10-31
PL2563355T3 (pl) 2016-12-30
EA201291116A1 (ru) 2013-04-30
CN102858330B (zh) 2015-07-22
PT2563355T (pt) 2016-09-02
ME02509B (me) 2017-02-20
JP5808392B2 (ja) 2015-11-10
IL222532A0 (en) 2012-12-31
AR085171A1 (es) 2013-09-18
IL222532A (en) 2017-09-28
KR20130094212A (ko) 2013-08-23
NZ700221A (en) 2016-04-29
US9505708B2 (en) 2016-11-29
HK1179881A1 (en) 2013-10-11

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