DK2563355T3 - A process for the preparation of ralfinamide-methanesulphonate or R-enantiomers thereof. - Google Patents
A process for the preparation of ralfinamide-methanesulphonate or R-enantiomers thereof. Download PDFInfo
- Publication number
- DK2563355T3 DK2563355T3 DK11714958.3T DK11714958T DK2563355T3 DK 2563355 T3 DK2563355 T3 DK 2563355T3 DK 11714958 T DK11714958 T DK 11714958T DK 2563355 T3 DK2563355 T3 DK 2563355T3
- Authority
- DK
- Denmark
- Prior art keywords
- salt
- water
- methanesulfonate
- mixture
- enantiomer
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims description 97
- 230000008569 process Effects 0.000 title claims description 42
- 238000002360 preparation method Methods 0.000 title claims description 31
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- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 123
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- 150000003839 salts Chemical class 0.000 claims description 110
- BHJIBOFHEFDSAU-LBPRGKRZSA-N ralfinamide Chemical compound C1=CC(CN[C@@H](C)C(N)=O)=CC=C1OCC1=CC=CC=C1F BHJIBOFHEFDSAU-LBPRGKRZSA-N 0.000 claims description 92
- 239000000203 mixture Substances 0.000 claims description 90
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- 239000013078 crystal Substances 0.000 claims description 72
- 239000012535 impurity Substances 0.000 claims description 72
- 239000002904 solvent Substances 0.000 claims description 69
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Diabetes (AREA)
- Hematology (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| DK2563355T3 true DK2563355T3 (en) | 2016-09-12 |
Family
ID=42634917
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK11714958.3T DK2563355T3 (en) | 2010-04-27 | 2011-04-06 | A process for the preparation of ralfinamide-methanesulphonate or R-enantiomers thereof. |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9505708B2 (OSRAM) |
| EP (1) | EP2563355B1 (OSRAM) |
| JP (3) | JP5808392B2 (OSRAM) |
| KR (1) | KR101851118B1 (OSRAM) |
| CN (2) | CN102858330B (OSRAM) |
| AR (1) | AR085171A1 (OSRAM) |
| AU (1) | AU2011246707B2 (OSRAM) |
| BR (1) | BR112012027623B1 (OSRAM) |
| CA (1) | CA2794389C (OSRAM) |
| CY (1) | CY1117879T1 (OSRAM) |
| DK (1) | DK2563355T3 (OSRAM) |
| EA (1) | EA021389B1 (OSRAM) |
| ES (1) | ES2590128T3 (OSRAM) |
| HR (1) | HRP20161077T1 (OSRAM) |
| HU (1) | HUE030504T2 (OSRAM) |
| IL (1) | IL222532A (OSRAM) |
| LT (1) | LT2563355T (OSRAM) |
| ME (1) | ME02509B (OSRAM) |
| MX (1) | MX342697B (OSRAM) |
| NZ (2) | NZ700221A (OSRAM) |
| PL (1) | PL2563355T3 (OSRAM) |
| PT (1) | PT2563355T (OSRAM) |
| RS (1) | RS55084B1 (OSRAM) |
| SI (1) | SI2563355T1 (OSRAM) |
| SM (1) | SMT201600266B (OSRAM) |
| TW (1) | TWI492919B (OSRAM) |
| WO (1) | WO2011134763A1 (OSRAM) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2563355T1 (sl) * | 2010-04-27 | 2016-10-28 | Newron Pharmaceuticals S.P.A. | Postopek za izdelavo metansulfonatnih soli ralfinamida ali njihovih R-enantiomerov |
| 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 |
Family Cites Families (18)
| 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 |
| 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 |
| BRPI0413982A (pt) | 2003-08-25 | 2006-11-07 | Newron Pharm Spa | derivados de alfa-aminoamida úteis como agentes anti-inflamatórios |
| 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 |
| KR101277520B1 (ko) * | 2004-09-10 | 2013-06-21 | 뉴론 파마슈티칼즈 에스. 피. 에이. | （할로벤질옥시）벤질아미노－프로판아미드를 포함하는 선택적 나트륨 및／또는 칼슘 채널 조절제로서 유용한 약제학적 조성물 |
| EP1870097A1 (en) | 2006-06-15 | 2007-12-26 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of cognitive disorders |
| JP5240476B2 (ja) | 2006-06-19 | 2013-07-17 | ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー | ２−［４−（３−及び２−フルオロベンジルオキシ）ベンジルアミノ］プロパンアミドの製造方法 |
| 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 |
| DK2229351T3 (en) * | 2007-12-11 | 2018-01-22 | Newron Pharm Spa | PROCEDURE FOR THE PREPARATION OF 2- [4- (3- OR 2-FLUORBENZYLOXY) BENZYLAMINO] PROPANAMIDS WITH HIGH PURITY |
| JP5736175B2 (ja) | 2007-12-19 | 2015-06-17 | ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー | 精神障害の治療に有用なα−アミノアミド誘導体 |
| 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 |
| SI2563355T1 (sl) * | 2010-04-27 | 2016-10-28 | Newron Pharmaceuticals S.P.A. | Postopek za izdelavo metansulfonatnih soli ralfinamida ali njihovih R-enantiomerov |
-
2011
- 2011-04-06 SI SI201130927A patent/SI2563355T1/sl unknown
- 2011-04-06 WO PCT/EP2011/055309 patent/WO2011134763A1/en not_active Ceased
- 2011-04-06 US US13/643,716 patent/US9505708B2/en active Active
- 2011-04-06 ES ES11714958.3T patent/ES2590128T3/es active Active
- 2011-04-06 PL PL11714958.3T patent/PL2563355T3/pl unknown
- 2011-04-06 CN CN201180020748.2A patent/CN102858330B/zh active Active
- 2011-04-06 EP EP11714958.3A patent/EP2563355B1/en active Active
- 2011-04-06 BR BR112012027623-9A patent/BR112012027623B1/pt active IP Right Grant
- 2011-04-06 HR HRP20161077TT patent/HRP20161077T1/hr unknown
- 2011-04-06 NZ NZ700221A patent/NZ700221A/en unknown
- 2011-04-06 PT PT117149583T patent/PT2563355T/pt unknown
- 2011-04-06 DK DK11714958.3T patent/DK2563355T3/en active
- 2011-04-06 LT LTEP11714958.3T patent/LT2563355T/lt unknown
- 2011-04-06 EA EA201291116A patent/EA021389B1/ru unknown
- 2011-04-06 AU AU2011246707A patent/AU2011246707B2/en active Active
- 2011-04-06 RS RS20160665A patent/RS55084B1/sr unknown
- 2011-04-06 MX MX2012012093A patent/MX342697B/es active IP Right Grant
- 2011-04-06 HU HUE11714958A patent/HUE030504T2/en unknown
- 2011-04-06 NZ NZ602648A patent/NZ602648A/en unknown
- 2011-04-06 JP JP2013506566A patent/JP5808392B2/ja active Active
- 2011-04-06 CN CN201510387405.XA patent/CN105037188B/zh active Active
- 2011-04-06 CA CA2794389A patent/CA2794389C/en active Active
- 2011-04-06 ME MEP-2016-169A patent/ME02509B/me unknown
- 2011-04-06 KR KR1020127030931A patent/KR101851118B1/ko active Active
- 2011-04-18 TW TW100113339A patent/TWI492919B/zh active
- 2011-04-25 AR ARP110101401A patent/AR085171A1/es not_active Application Discontinuation
-
2012
- 2012-10-18 IL IL222532A patent/IL222532A/en active IP Right Grant
-
2015
- 2015-05-22 JP JP2015104930A patent/JP6345154B2/ja active Active
-
2016
- 2016-08-05 SM SM201600266T patent/SMT201600266B/it unknown
- 2016-08-10 CY CY20161100786T patent/CY1117879T1/el unknown
- 2016-10-12 US US15/291,202 patent/US9856207B2/en active Active
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2017
- 2017-05-30 JP JP2017106571A patent/JP6450420B2/ja active Active
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