JP2013139446A5 - - Google Patents
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- Publication number
- JP2013139446A5 JP2013139446A5 JP2013002429A JP2013002429A JP2013139446A5 JP 2013139446 A5 JP2013139446 A5 JP 2013139446A5 JP 2013002429 A JP2013002429 A JP 2013002429A JP 2013002429 A JP2013002429 A JP 2013002429A JP 2013139446 A5 JP2013139446 A5 JP 2013139446A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- pharmaceutically acceptable
- acceptable acid
- ralfinamide
- less
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 20
- 239000002253 acid Substances 0.000 claims 19
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 18
- 229940098779 methanesulfonic acid Drugs 0.000 claims 9
- 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 9
- 239000012535 impurity Substances 0.000 claims 8
- NEMGRZFTLSKBAP-LBPRGKRZSA-N safinamide Chemical compound C1=CC(CN[C@@H](C)C(N)=O)=CC=C1OCC1=CC=CC(F)=C1 NEMGRZFTLSKBAP-LBPRGKRZSA-N 0.000 claims 8
- 229950002652 safinamide Drugs 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 102000006378 Catechol O-methyltransferase Human genes 0.000 claims 4
- 108020002739 Catechol O-methyltransferase Proteins 0.000 claims 4
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical group OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 3
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 108010052832 Cytochromes Proteins 0.000 claims 2
- 102000018832 Cytochromes Human genes 0.000 claims 2
- 101001047090 Homo sapiens Potassium voltage-gated channel subfamily H member 2 Proteins 0.000 claims 2
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 229960002870 gabapentin Drugs 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 229960004502 levodopa Drugs 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 229960001233 pregabalin Drugs 0.000 claims 2
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims 2
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 2
- -1 2-fluorobenzyloxy Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 108010026925 Cytochrome P-450 CYP2C19 Proteins 0.000 claims 1
- 108010000543 Cytochrome P-450 CYP2C9 Proteins 0.000 claims 1
- 108010001237 Cytochrome P-450 CYP2D6 Proteins 0.000 claims 1
- 108010081668 Cytochrome P-450 CYP3A Proteins 0.000 claims 1
- 102100029363 Cytochrome P450 2C19 Human genes 0.000 claims 1
- 102100029358 Cytochrome P450 2C9 Human genes 0.000 claims 1
- 102100021704 Cytochrome P450 2D6 Human genes 0.000 claims 1
- 102100039205 Cytochrome P450 3A4 Human genes 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 229940052760 dopamine agonists Drugs 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06012565.5 | 2006-06-19 | ||
| EP06012565 | 2006-06-19 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009515731A Division JP5240476B2 (ja) | 2006-06-19 | 2007-06-08 | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013139446A JP2013139446A (ja) | 2013-07-18 |
| JP2013139446A5 true JP2013139446A5 (enExample) | 2014-02-13 |
| JP5795342B2 JP5795342B2 (ja) | 2015-10-14 |
Family
ID=37101658
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009515731A Active JP5240476B2 (ja) | 2006-06-19 | 2007-06-08 | 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 |
| JP2013002429A Active JP5795342B2 (ja) | 2006-06-19 | 2013-01-10 | 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 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009515731A Active JP5240476B2 (ja) | 2006-06-19 | 2007-06-08 | 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 |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US8076515B2 (enExample) |
| EP (2) | EP2474521B1 (enExample) |
| JP (2) | JP5240476B2 (enExample) |
| KR (2) | KR101410291B1 (enExample) |
| CN (2) | CN101472880B (enExample) |
| AR (1) | AR061510A1 (enExample) |
| AU (1) | AU2007263328C1 (enExample) |
| BR (1) | BRPI0712936B8 (enExample) |
| CA (1) | CA2653012C (enExample) |
| CY (2) | CY1115951T1 (enExample) |
| DK (2) | DK2029524T3 (enExample) |
| EA (2) | EA017123B1 (enExample) |
| ES (2) | ES2527437T3 (enExample) |
| HR (2) | HRP20150136T1 (enExample) |
| HU (1) | HUE030233T2 (enExample) |
| IL (1) | IL195294A (enExample) |
| LT (1) | LT2474521T (enExample) |
| MX (2) | MX2008015704A (enExample) |
| NO (2) | NO342018B1 (enExample) |
| NZ (2) | NZ595737A (enExample) |
| PL (2) | PL2029524T3 (enExample) |
| PT (2) | PT2029524E (enExample) |
| RS (2) | RS53824B1 (enExample) |
| SI (2) | SI2029524T1 (enExample) |
| TW (2) | TWI412512B (enExample) |
| WO (1) | WO2007147491A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005018627A1 (en) * | 2003-08-25 | 2005-03-03 | Newron Pharmaceuticals, Spa | Alpha-aminoamide derivatives useful as anti-inflammatory agents |
| EA017123B1 (ru) * | 2006-06-19 | 2012-10-30 | Ньюрон Фармасьютикалс С.П.А. | Способ получения 2-[4-(3- и 2-фторбензилокси)бензиламино]пропанамидов |
| KR101709498B1 (ko) * | 2007-12-11 | 2017-02-23 | 뉴론 파마슈티칼즈 에스. 피. 에이. | 고순도의 ２［４（３ 또는 ２플루오로벤질옥시）벤질아미노］프로판아미드의 제조방법 |
| EP2314569A1 (en) | 2009-10-22 | 2011-04-27 | Merck Patent GmbH | Novel polymorphic forms of (S)-2-[4-(3-Fluoro-benzyloxy)-benzylamino]-propionamide mesylate salt and processes of manufacturing thereof |
| 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 |
| BR112015007312A2 (pt) | 2012-12-03 | 2017-08-08 | Hoffmann La Roche | composto, composição farmacêutica, utilização de um composto, método para o tratamento de câncer e invenção |
| WO2014178083A1 (en) | 2013-05-03 | 2014-11-06 | Council Of Scientific & Industrial Research | An improved synthesis of anti-parkinson agent |
| 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 |
| JP6466109B2 (ja) * | 2014-09-09 | 2019-02-06 | 東ソー・ファインケム株式会社 | ２−ベンジルオキシ−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法 |
| CN105017060B (zh) * | 2015-07-03 | 2017-06-16 | 南京正大天晴制药有限公司 | 一种沙芬酰胺新晶型及其制备方法 |
| CN106365966A (zh) * | 2015-07-24 | 2017-02-01 | 上海医药集团股份有限公司 | 一种苄基芳基醚的制备方法 |
| CN105061245A (zh) * | 2015-08-25 | 2015-11-18 | 成都维恒医药科技有限公司 | 一种高纯度沙芬酰胺的制备方法 |
| CN106220525A (zh) * | 2016-07-31 | 2016-12-14 | 合肥远志医药科技开发有限公司 | 一种工业化沙芬酰胺甲磺酸盐的制备方法 |
| CN106336363B (zh) * | 2016-08-22 | 2018-10-30 | 上海医药集团股份有限公司 | 一种沙芬酰胺甲磺酸盐晶型c及其制备方法 |
| CN106565521B (zh) * | 2016-08-24 | 2019-03-08 | 浙江美诺华药物化学有限公司 | (s)-2-[3-(3-氟苄基)-4-(3-氟苄氧基)苄氨基]丙酰胺及其盐的制备方法 |
| CN106596828B (zh) * | 2016-12-15 | 2018-09-25 | 扬子江药业集团有限公司 | 一种甲磺酸沙芬酰胺有关物质的检测方法 |
| CN107271600B (zh) * | 2017-07-28 | 2019-01-25 | 成都百裕制药股份有限公司 | 一种4-(3-氟苄氧基)苯甲醛中异构体杂质含量的检测方法 |
| CN107759487A (zh) * | 2017-11-23 | 2018-03-06 | 江苏恒盛药业有限公司 | 一种沙芬酰胺盐酸盐及其一种晶型以及制备方法 |
| CN107857713A (zh) * | 2017-11-23 | 2018-03-30 | 江苏恒盛药业有限公司 | 一种沙芬酰胺氢溴酸盐及其一种晶型 |
| WO2019167085A1 (en) * | 2018-03-01 | 2019-09-06 | Msn Laboratories Private Limited, R&D Center | Process for the preparation of (s)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino propanamide methanesulfonate |
| US11111208B2 (en) | 2019-06-17 | 2021-09-07 | RK Pharma Solutions LLC | Process for the preparation of safinamide mesylate intermediate |
| US11225457B2 (en) | 2019-08-06 | 2022-01-18 | Medichem, S.A. | Process for preparing safinamide |
| CN111122736B (zh) * | 2019-12-30 | 2021-03-12 | 北京鑫开元医药科技有限公司海南分公司 | 一种用于检测布瓦西坦中间体中对映异构体的方法 |
| CN113214097B (zh) * | 2020-01-21 | 2022-08-30 | 厦门大学 | 治疗阿尔茨海默病的化合物 |
| CN112028754A (zh) * | 2020-06-17 | 2020-12-04 | 浙江美诺华药物化学有限公司 | 一种甲磺酸沙芬酰胺中间体的制备方法 |
| CN114088830B (zh) * | 2021-11-10 | 2022-09-23 | 石家庄四药有限公司 | 一种4-(3-氟苄氧基)苯甲醛中异构体的检测方法 |
| CN116008439B (zh) * | 2023-02-20 | 2023-10-27 | 山东绿叶制药有限公司 | 一种检测2,6-二氧杂螺[4,5]癸烷类化合物或其盐中杂质的方法 |
| WO2025022300A1 (en) | 2023-07-25 | 2025-01-30 | Intas Pharmaceuticals Ltd. | An orodispersible pharmaceutical solid dosage form of safinamide |
Family Cites Families (19)
| 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 |
| EP0974351A3 (en) * | 1998-04-24 | 2000-12-13 | Jouveinal | Medicament for preventing and treating gastrointestinal damage |
| CA2403991A1 (en) | 2000-03-31 | 2001-10-11 | Euro-Celtique S.A. | Aminopyridines and their use as anticonvulsants and sodium channel blockers |
| JP4350508B2 (ja) | 2001-09-03 | 2009-10-21 | ニユーロン・フアーマシユーテイカルズ・エツセ・ピー・アー | ガバペンチンまたはその類似体とα−アミノアミドとを含む薬剤組成物およびその鎮痛用途 |
| EP1438956A1 (en) | 2003-01-16 | 2004-07-21 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful as antimigraine agents |
| WO2004066990A2 (en) * | 2003-01-30 | 2004-08-12 | Dynogen Pharmaceuticals, Inc. | Methods of treating lower urinary tract disorders using sodium channel modulators |
| WO2004066987A2 (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 |
| TW200507850A (en) * | 2003-07-25 | 2005-03-01 | Kyowa Hakko Kogyo Kk | Pharmaceutical composition |
| WO2005018627A1 (en) | 2003-08-25 | 2005-03-03 | Newron Pharmaceuticals, Spa | Alpha-aminoamide derivatives useful as anti-inflammatory agents |
| EP1524267A1 (en) | 2003-10-15 | 2005-04-20 | Newron Pharmaceuticals S.p.A. | Substituted benzylaminoalkylene heterocycles |
| 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 |
| SI1809271T1 (sl) | 2004-09-10 | 2010-10-29 | Newron Pharm Spa | Uporaba (R)-(halobenziloksi) benzilamino propanamidov kot selektivnih modulatorjev natrijevih in/ali kalcijevih kanalov |
| EP1870097A1 (en) | 2006-06-15 | 2007-12-26 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of cognitive disorders |
| EA017123B1 (ru) * | 2006-06-19 | 2012-10-30 | Ньюрон Фармасьютикалс С.П.А. | Способ получения 2-[4-(3- и 2-фторбензилокси)бензиламино]пропанамидов |
| KR101709498B1 (ko) | 2007-12-11 | 2017-02-23 | 뉴론 파마슈티칼즈 에스. 피. 에이. | 고순도의 ２［４（３ 또는 ２플루오로벤질옥시）벤질아미노］프로판아미드의 제조방법 |
| BRPI0821026A2 (pt) | 2007-12-19 | 2015-06-16 | Newron Pharmaceutical S P A | Derivados de alfa-minoamidas úteis no tratamento de transtornos psiquiátricos |
-
2007
- 2007-06-08 EA EA200970028A patent/EA017123B1/ru unknown
- 2007-06-08 ES ES07764601.6T patent/ES2527437T3/es active Active
- 2007-06-08 AU AU2007263328A patent/AU2007263328C1/en active Active
- 2007-06-08 SI SI200731603T patent/SI2029524T1/sl unknown
- 2007-06-08 ES ES12163085.9T patent/ES2602069T3/es active Active
- 2007-06-08 WO PCT/EP2007/005105 patent/WO2007147491A1/en not_active Ceased
- 2007-06-08 NZ NZ595737A patent/NZ595737A/xx unknown
- 2007-06-08 BR BRPI0712936A patent/BRPI0712936B8/pt active IP Right Grant
- 2007-06-08 KR KR1020097001124A patent/KR101410291B1/ko active Active
- 2007-06-08 EP EP12163085.9A patent/EP2474521B1/en active Active
- 2007-06-08 MX MX2008015704A patent/MX2008015704A/es active IP Right Grant
- 2007-06-08 KR KR20147003965A patent/KR101491541B1/ko active Active
- 2007-06-08 EA EA201101308A patent/EA025326B1/ru unknown
- 2007-06-08 PT PT07764601T patent/PT2029524E/pt unknown
- 2007-06-08 DK DK07764601.6T patent/DK2029524T3/da active
- 2007-06-08 JP JP2009515731A patent/JP5240476B2/ja active Active
- 2007-06-08 RS RS20150114A patent/RS53824B1/sr unknown
- 2007-06-08 EP EP07764601.6A patent/EP2029524B1/en active Active
- 2007-06-08 MX MX2012005094A patent/MX342698B/es unknown
- 2007-06-08 LT LTEP12163085.9T patent/LT2474521T/lt unknown
- 2007-06-08 PL PL07764601T patent/PL2029524T3/pl unknown
- 2007-06-08 HU HUE12163085A patent/HUE030233T2/en unknown
- 2007-06-08 RS RS20160965A patent/RS55464B1/sr unknown
- 2007-06-08 CN CN2007800228798A patent/CN101472880B/zh not_active Ceased
- 2007-06-08 DK DK12163085.9T patent/DK2474521T3/en active
- 2007-06-08 CN CN201310142245.3A patent/CN103284984B/zh active Active
- 2007-06-08 HR HRP20150136TT patent/HRP20150136T1/hr unknown
- 2007-06-08 NZ NZ572798A patent/NZ572798A/en unknown
- 2007-06-08 PT PT121630859T patent/PT2474521T/pt unknown
- 2007-06-08 CA CA2653012A patent/CA2653012C/en active Active
- 2007-06-08 SI SI200731854A patent/SI2474521T1/sl unknown
- 2007-06-08 PL PL12163085T patent/PL2474521T3/pl unknown
- 2007-06-15 TW TW101148004A patent/TWI412512B/zh active
- 2007-06-15 TW TW096121879A patent/TWI393700B/zh active
- 2007-06-19 AR ARP070102674A patent/AR061510A1/es active IP Right Grant
-
2008
- 2008-11-13 IL IL195294A patent/IL195294A/en active Protection Beyond IP Right Term
- 2008-12-18 US US12/338,825 patent/US8076515B2/en active Active
-
2009
- 2009-01-14 NO NO20090231A patent/NO342018B1/no unknown
-
2011
- 2011-11-03 US US13/288,891 patent/US8278485B2/en active Active
-
2013
- 2013-01-10 JP JP2013002429A patent/JP5795342B2/ja active Active
-
2015
- 2015-01-23 CY CY20151100072T patent/CY1115951T1/el unknown
-
2016
- 2016-10-18 CY CY20161101038T patent/CY1118113T1/el unknown
- 2016-11-03 HR HRP20161456TT patent/HRP20161456T1/hr unknown
-
2017
- 2017-11-30 NO NO20171916A patent/NO342644B1/no unknown
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