CN102858330B - 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

Info

Publication number
CN102858330B
CN102858330B CN201180020748.2A CN201180020748A CN102858330B CN 102858330 B CN102858330 B CN 102858330B CN 201180020748 A CN201180020748 A CN 201180020748A CN 102858330 B CN102858330 B CN 102858330B
Authority
CN
China
Prior art keywords
water
salt
crystalline
ralfinamide
enantiomer
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201180020748.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN102858330A (zh
Inventor
C·乔达诺
E·瓦尔德沃杰尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Newron Pharmaceuticals SpA
Original Assignee
Newron Pharmaceuticals SpA
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 Newron Pharmaceuticals SpA filed Critical Newron Pharmaceuticals SpA
Priority to CN201510387405.XA priority Critical patent/CN105037188B/zh
Publication of CN102858330A publication Critical patent/CN102858330A/zh
Application granted granted Critical
Publication of CN102858330B publication Critical patent/CN102858330B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/22—Separation; Purification; Stabilisation; Use of additives
    • C07C231/24—Separation; Purification
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Cardiology (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)
CN201180020748.2A 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 CN102858330B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510387405.XA CN105037188B (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

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510387405.XA Division CN105037188B (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

Publications (2)

Publication Number Publication Date
CN102858330A CN102858330A (zh) 2013-01-02
CN102858330B true CN102858330B (zh) 2015-07-22

Family

ID=42634917

Family Applications (2)

Application Number Title Priority Date Filing Date
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
CN201510387405.XA Active CN105037188B (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

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201510387405.XA Active CN105037188B (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

Country Status (27)

Country Link
US (2) US9505708B2 (enExample)
EP (1) EP2563355B1 (enExample)
JP (3) JP5808392B2 (enExample)
KR (1) KR101851118B1 (enExample)
CN (2) CN102858330B (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) NZ700221A (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
NZ700221A (en) * 2010-04-27 2016-04-29 Newron Pharm Spa Ralfinamide methanesulfonate salts
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
US20080096965A1 (en) * 2004-09-10 2008-04-24 Newron Pharmaceuticals S.P.A. (Halobenzyloxy) Benzylamino-Propanamides as Sodium and/or Calcium Channel Selective Modulators

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
CN1274306C (zh) 2001-09-03 2006-09-13 纽朗制药有限公司 包含加巴喷丁或其类似物和α－氨基酰胺的药物组合物及其止痛应用
EP1438956A1 (en) * 2003-01-16 2004-07-21 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful as antimigraine agents
AU2004207009A1 (en) * 2003-01-30 2004-08-12 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
IL173886A (en) 2003-08-25 2012-09-24 Newron Pharm Spa Alpha-aminoamide derivatives for treating inflammatory disorders
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
KR101593627B1 (ko) 2007-12-11 2016-02-11 뉴론 파마슈티칼즈 에스. 피. 에이. 고순도의 ２­［４­（３­ 또는 ２­플루오로벤질옥시）벤질아미노］프로판아미드의 제조방법
CA2707646C (en) 2007-12-19 2016-09-13 Newron Pharmaceuticals S.P.A. 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
NZ700221A (en) * 2010-04-27 2016-04-29 Newron Pharm Spa Ralfinamide methanesulfonate salts

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080096965A1 (en) * 2004-09-10 2008-04-24 Newron Pharmaceuticals S.P.A. (Halobenzyloxy) Benzylamino-Propanamides as Sodium and/or Calcium Channel Selective Modulators
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

Also Published As

Publication number Publication date
CN105037188A (zh) 2015-11-11
TW201139344A (en) 2011-11-16
SI2563355T1 (sl) 2016-10-28
JP2017197553A (ja) 2017-11-02
US9856207B2 (en) 2018-01-02
DK2563355T3 (en) 2016-09-12
US9505708B2 (en) 2016-11-29
IL222532A0 (en) 2012-12-31
AR085171A1 (es) 2013-09-18
MX342697B (es) 2016-10-10
KR20130094212A (ko) 2013-08-23
CA2794389C (en) 2016-08-23
NZ700221A (en) 2016-04-29
US20130039983A1 (en) 2013-02-14
MX2012012093A (es) 2012-12-17
TWI492919B (zh) 2015-07-21
WO2011134763A1 (en) 2011-11-03
EP2563355B1 (en) 2016-06-08
ES2590128T3 (es) 2016-11-18
CN105037188B (zh) 2017-06-23
EA021389B1 (ru) 2015-06-30
JP6345154B2 (ja) 2018-06-20
PL2563355T3 (pl) 2016-12-30
EA201291116A1 (ru) 2013-04-30
IL222532A (en) 2017-09-28
EP2563355A1 (en) 2013-03-06
JP6450420B2 (ja) 2019-01-09
RS55084B1 (sr) 2016-12-30
HUE030504T2 (en) 2017-05-29
AU2011246707B2 (en) 2014-11-20
BR112012027623A2 (pt) 2016-08-09
JP2015180664A (ja) 2015-10-15
BR112012027623B1 (pt) 2021-07-06
JP2013528577A (ja) 2013-07-11
SMT201600266B (it) 2016-08-31
HRP20161077T1 (hr) 2016-10-21
ME02509B (me) 2017-02-20
US20170029365A1 (en) 2017-02-02
KR101851118B1 (ko) 2018-04-23
HK1179881A1 (en) 2013-10-11
JP5808392B2 (ja) 2015-11-10
CY1117879T1 (el) 2017-05-17
CA2794389A1 (en) 2011-11-03
CN102858330A (zh) 2013-01-02
PT2563355T (pt) 2016-09-02
HK1213872A1 (zh) 2016-07-15
NZ602648A (en) 2014-10-31
LT2563355T (lt) 2016-09-26

Similar Documents

Publication Publication Date Title
JP5934204B2 (ja) Ｃ−ｍｅｔ調節剤の薬学的組成物
JP6450420B2 (ja) 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
TR201909447T4 (tr) Aramkol tuzları.
KR20090113904A (ko) （―）ｏ―데스메틸벤라팍신을 포함하는 고체 형태들 및 그들의 용도
WO2014082354A1 (zh) 西达本胺的晶型及其制备方法与应用
AU2011246707A1 (en) Process for the production of ralfinamide methanesulfonate salts or their R-enantiomers
EP2109600B1 (en) Amorphous forms of rivastigmine hydrogentartrate
HK1179881B (en) Process for the production of ralfinamide methanesulfonate salts or their r-enantiomers
HK1213872B (en) Process for the production of ralfinamide methanesulfonate salts or their r-enantiomers
US9981912B2 (en) Cocrystal of lorcaserin, preparation methods, pharmaceutical compositions and uses thereof
WO2012003413A1 (en) Novel solid forms of tacedinaline
JP2025502480A (ja) イソクロマン－イミダゾール構造のアルファ－２ａアドレナリン受容体アゴニストの新規な硫酸塩形
EP3941588A1 (en) Co-crystal forms of selinexor
HK40017692B (en) Polymorphic forms of rad1901-2hcl
KR20180029401A (ko) 텔미사르탄을 포함하는 고체 분산체 및 이의 제조방법

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1179881

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1179881

Country of ref document: HK