TWI492919B - 實質上不含具有基因毒性作用雜質之羅芬醯胺(ralfinamide)鹽類的製造方法 - Google Patents

實質上不含具有基因毒性作用雜質之羅芬醯胺(ralfinamide)鹽類的製造方法 Download PDF

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Publication number
TWI492919B
TWI492919B TW100113339A TW100113339A TWI492919B TW I492919 B TWI492919 B TW I492919B TW 100113339 A TW100113339 A TW 100113339A TW 100113339 A TW100113339 A TW 100113339A TW I492919 B TWI492919 B TW I492919B
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Taiwan
Prior art keywords
water
mixture
salt
methanesulfonate
crystalline
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TW100113339A
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English (en)
Chinese (zh)
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TW201139344A (en
Inventor
Claudio Giordano
Erwin Waldvogel
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Newron Pharm Spa
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Publication of TW201139344A publication Critical patent/TW201139344A/zh
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Publication of TWI492919B publication Critical patent/TWI492919B/zh

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    • 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
    • C07C237/04Carboxylic 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
    • C07C237/08Carboxylic 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
    • 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
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/04Centrally 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • C07C231/22Separation; Purification; Stabilisation; Use of additives
    • C07C231/24Separation; Purification
    • 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
    • C07C237/04Carboxylic 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
    • C07C237/06Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (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)
TW100113339A 2010-04-27 2011-04-18 實質上不含具有基因毒性作用雜質之羅芬醯胺(ralfinamide)鹽類的製造方法 TWI492919B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10161207 2010-04-27

Publications (2)

Publication Number Publication Date
TW201139344A TW201139344A (en) 2011-11-16
TWI492919B true TWI492919B (zh) 2015-07-21

Family

ID=42634917

Family Applications (1)

Application Number Title Priority Date Filing Date
TW100113339A TWI492919B (zh) 2010-04-27 2011-04-18 實質上不含具有基因毒性作用雜質之羅芬醯胺(ralfinamide)鹽類的製造方法

Country Status (27)

Country Link
US (2) US9505708B2 (enExample)
EP (1) EP2563355B1 (enExample)
JP (3) JP5808392B2 (enExample)
KR (1) KR101851118B1 (enExample)
CN (2) CN105037188B (enExample)
AR (1) AR085171A1 (enExample)
AU (1) AU2011246707B2 (enExample)
BR (1) BR112012027623B1 (enExample)
CA (1) CA2794389C (enExample)
CY (1) CY1117879T1 (enExample)
DK (1) DK2563355T3 (enExample)
EA (1) EA021389B1 (enExample)
ES (1) ES2590128T3 (enExample)
HR (1) HRP20161077T1 (enExample)
HU (1) HUE030504T2 (enExample)
IL (1) IL222532A (enExample)
LT (1) LT2563355T (enExample)
ME (1) ME02509B (enExample)
MX (1) MX342697B (enExample)
NZ (2) NZ602648A (enExample)
PL (1) PL2563355T3 (enExample)
PT (1) PT2563355T (enExample)
RS (1) RS55084B1 (enExample)
SI (1) SI2563355T1 (enExample)
SM (1) SMT201600266B (enExample)
TW (1) TWI492919B (enExample)
WO (1) WO2011134763A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2794389C (en) * 2010-04-27 2016-08-23 Newron Pharmaceuticals S.P.A. Process for the production of ralfinamide methanesulfonate salts or their r-enantiomers
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007147491A1 (en) * 2006-06-19 2007-12-27 Newron Pharmaceuticals S.P.A. Process for the production of 2- [4 - ( 3- and 2-flu0r0benzyl0xy) benzylamin0] propan amides
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

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
PT1423168E (pt) 2001-09-03 2006-05-31 Newron Pharm Spa Composicao farmaceutica que compreende gabapentina ou um seu analogo e uma x-aminoamida e a sua utilizacao como analgesico
EP1438956A1 (en) * 2003-01-16 2004-07-21 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful as antimigraine agents
EP1596844A2 (en) * 2003-01-30 2005-11-23 Dynogen Pharmaceuticals Inc. Use of sodium channel modulators for treating gastrointestinal tract disorders
AR044007A1 (es) 2003-04-11 2005-08-24 Newron Pharmaceuticals Inc Metodos para el tratamiento de la enfermedad de parkinson
US20070276046A1 (en) 2003-08-25 2007-11-29 Patricia Salvati 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
DK1809271T5 (da) 2004-09-10 2010-12-06 Newron Pharm Spa Anvendelse af (R)-(halogenbenzyloxy)benzylaminopropanamider som natrium- og/eller calciumkanalselektive modulatorer
EP1870097A1 (en) 2006-06-15 2007-12-26 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful in the treatment of cognitive disorders
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
NZ586182A (en) 2007-12-19 2012-02-24 Newron Pharm Spa Alpha-aminoamide derivatives useful in the treatment of psychiatric disorders
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
CA2794389C (en) * 2010-04-27 2016-08-23 Newron Pharmaceuticals S.P.A. Process for the production of ralfinamide methanesulfonate salts or their r-enantiomers

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007147491A1 (en) * 2006-06-19 2007-12-27 Newron Pharmaceuticals S.P.A. Process for the production of 2- [4 - ( 3- and 2-flu0r0benzyl0xy) benzylamin0] propan amides
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

Also Published As

Publication number Publication date
KR101851118B1 (ko) 2018-04-23
JP6450420B2 (ja) 2019-01-09
EP2563355B1 (en) 2016-06-08
IL222532A0 (en) 2012-12-31
ES2590128T3 (es) 2016-11-18
US20170029365A1 (en) 2017-02-02
US9856207B2 (en) 2018-01-02
SI2563355T1 (sl) 2016-10-28
AU2011246707B2 (en) 2014-11-20
JP2013528577A (ja) 2013-07-11
BR112012027623A2 (pt) 2016-08-09
HK1213872A1 (zh) 2016-07-15
CA2794389C (en) 2016-08-23
HUE030504T2 (en) 2017-05-29
HRP20161077T1 (hr) 2016-10-21
EA201291116A1 (ru) 2013-04-30
PT2563355T (pt) 2016-09-02
DK2563355T3 (en) 2016-09-12
US9505708B2 (en) 2016-11-29
CN102858330A (zh) 2013-01-02
US20130039983A1 (en) 2013-02-14
MX2012012093A (es) 2012-12-17
EP2563355A1 (en) 2013-03-06
EA021389B1 (ru) 2015-06-30
CN105037188A (zh) 2015-11-11
CA2794389A1 (en) 2011-11-03
NZ700221A (en) 2016-04-29
JP2017197553A (ja) 2017-11-02
JP5808392B2 (ja) 2015-11-10
LT2563355T (lt) 2016-09-26
AR085171A1 (es) 2013-09-18
JP6345154B2 (ja) 2018-06-20
HK1179881A1 (en) 2013-10-11
SMT201600266B (it) 2016-08-31
MX342697B (es) 2016-10-10
JP2015180664A (ja) 2015-10-15
CN105037188B (zh) 2017-06-23
PL2563355T3 (pl) 2016-12-30
ME02509B (me) 2017-02-20
NZ602648A (en) 2014-10-31
KR20130094212A (ko) 2013-08-23
WO2011134763A1 (en) 2011-11-03
IL222532A (en) 2017-09-28
CY1117879T1 (el) 2017-05-17
TW201139344A (en) 2011-11-16
BR112012027623B1 (pt) 2021-07-06
CN102858330B (zh) 2015-07-22
RS55084B1 (sr) 2016-12-30

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