CN105037188B - 用于制备拉非酰胺甲磺酸盐或其r‑对映异构体的方法 - Google Patents

用于制备拉非酰胺甲磺酸盐或其r‑对映异构体的方法 Download PDF

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CN105037188B
CN105037188B CN201510387405.XA CN201510387405A CN105037188B CN 105037188 B CN105037188 B CN 105037188B CN 201510387405 A CN201510387405 A CN 201510387405A CN 105037188 B CN105037188 B CN 105037188B
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mesylate
types
pnu
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salt
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CN105037188A (zh
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C·乔达诺
E·瓦尔德沃杰尔
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Newron Pharmaceuticals SpA
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    • 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
    • C07C237/08Carboxylic 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
    • 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)
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  • General Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • 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)
CN201510387405.XA 2010-04-27 2011-04-06 用于制备拉非酰胺甲磺酸盐或其r‑对映异构体的方法 Active CN105037188B (zh)

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EP10161207.5 2010-04-27
EP10161207 2010-04-27
CN201180020748.2A CN102858330B (zh) 2010-04-27 2011-04-06 用于制备拉非酰胺甲磺酸盐或其r-对映异构体的方法

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CN201180020748.2A Active CN102858330B (zh) 2010-04-27 2011-04-06 用于制备拉非酰胺甲磺酸盐或其r-对映异构体的方法

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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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1192199A (zh) * 1995-07-27 1998-09-02 法玛西雅厄普约翰公司 2-(4-取代)-苄基氨基-2-甲基-丙酰胺衍生物
CN1738611A (zh) * 2003-01-16 2006-02-22 纽朗制药有限公司 用作抗偏头痛剂的α-氨基酰胺衍生物
CN101018546A (zh) * 2004-09-10 2007-08-15 纽朗制药有限公司 作为钠和/或钙通道选择性调节剂的(卤代苄氨基)苄氧基-丙酰胺类
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
CN101472880A (zh) * 2006-06-19 2009-07-01 纽朗制药有限公司 生产2-[4-(3-和2-氟苄氧基)苄氨基]丙酰胺类的方法

Family Cites Families (13)

* 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
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
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
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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1192199A (zh) * 1995-07-27 1998-09-02 法玛西雅厄普约翰公司 2-(4-取代)-苄基氨基-2-甲基-丙酰胺衍生物
CN1738611A (zh) * 2003-01-16 2006-02-22 纽朗制药有限公司 用作抗偏头痛剂的α-氨基酰胺衍生物
CN101018546A (zh) * 2004-09-10 2007-08-15 纽朗制药有限公司 作为钠和/或钙通道选择性调节剂的(卤代苄氨基)苄氧基-丙酰胺类
CN101472880A (zh) * 2006-06-19 2009-07-01 纽朗制药有限公司 生产2-[4-(3-和2-氟苄氧基)苄氨基]丙酰胺类的方法
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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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
TWI492919B (zh) 2015-07-21
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
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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