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

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

Info

Publication number
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
Authority
KR
South Korea
Prior art keywords
salt
crystalline
water
methanesulfonate
mixture
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
KR1020127030931A
Other languages
English (en)
Korean (ko)
Other versions
KR20130094212A (ko
Inventor
클라우디오 지오르다노
에르빈 발트포겔
Original Assignee
뉴론 파마슈티칼즈 에스. 피. 에이.
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 뉴론 파마슈티칼즈 에스. 피. 에이. filed Critical 뉴론 파마슈티칼즈 에스. 피. 에이.
Publication of KR20130094212A publication Critical patent/KR20130094212A/ko
Application granted granted Critical
Publication of KR101851118B1 publication Critical patent/KR101851118B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/22Separation; Purification; Stabilisation; Use of additives
    • C07C231/24Separation; Purification
    • 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

Landscapes

  • 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)
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
EP10161207.5 2010-04-27
EP10161207 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

Family

ID=42634917

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127030931A Active KR101851118B1 (ko) 2010-04-27 2011-04-06 랄핀아미드 메탄설포네이트 염들 또는 이들의 r―에난티오머들의 제조 방법

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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (17)

* 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
EP2029524B1 (en) * 2006-06-19 2014-11-26 Newron Pharmaceuticals S.p.A. Process for the production of 2- [4 - ( 3- and 2-fluorobenzyloxy) benzylamino] propan amides
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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

Similar Documents

Publication Publication Date Title
JP6028016B2 (ja) リナグリプチンベンゾエートの多形体
JP5934204B2 (ja) C−met調節剤の薬学的組成物
KR101851118B1 (ko) 랄핀아미드 메탄설포네이트 염들 또는 이들의 r―에난티오머들의 제조 방법
JP2023027066A (ja) オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途
AU2011246707A1 (en) Process for the production of ralfinamide methanesulfonate salts or their R-enantiomers
US9708301B2 (en) Crystalline forms of afatinib monomaleate, preparation methods and pharmaceutical compositions thereof
WO2011095985A2 (en) Rasagiline salts and processes for the preparation thereof
CN120826397A (zh) 嘧啶三唑化合物的固体及共晶体形式
HK1213872B (en) Process for the production of ralfinamide methanesulfonate salts or their r-enantiomers
TW202245790A (zh) Gaba-a正向異位調節劑的半檸檬酸鹽及其結晶型
HK1179881B (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
CA3080657A1 (en) Crystalline salt of a tricyclic poly(adp-ribose) polymerase inhibitor
KR20180029401A (ko) 텔미사르탄을 포함하는 고체 분산체 및 이의 제조방법

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20121126

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20160404

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20170816

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20180201

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20180417

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20180418

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20210406

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20230405

Start annual number: 6

End annual number: 6