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 | 2006-06-19 | ||
| EP06012565.5 | 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) | EP2029524B1 (enExample) |
| JP (2) | JP5240476B2 (enExample) |
| KR (2) | KR101491541B1 (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) | EA025326B1 (enExample) |
| ES (2) | ES2602069T3 (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) | NZ572798A (enExample) |
| PL (2) | PL2029524T3 (enExample) |
| PT (2) | PT2029524E (enExample) |
| RS (2) | RS55464B1 (enExample) |
| SI (2) | SI2029524T1 (enExample) |
| TW (2) | TWI393700B (enExample) |
| WO (1) | WO2007147491A1 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070276046A1 (en) * | 2003-08-25 | 2007-11-29 | Patricia Salvati | Alpha-Aminoamide Derivatives Useful as Anti-Inflammatory Agents |
| KR101491541B1 (ko) * | 2006-06-19 | 2015-02-09 | 뉴론 파마슈티칼즈 에스. 피. 에이. | 2-［4-(3- 및 2-플루오로벤질옥시)벤질아미노)프로판 아미드의 제조방법 |
| EP3257842B1 (en) * | 2007-12-11 | 2020-11-18 | Newron Pharmaceuticals S.p.A. | Therapeutic use of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree |
| 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 |
| LT2563355T (lt) * | 2010-04-27 | 2016-09-26 | Newron Pharmaceuticals S.P.A. | Ralfinamido metansulfonato druskų arba jų r-enentiomerų gavimo būdas |
| KR20150090100A (ko) | 2012-12-03 | 2015-08-05 | 에프. 호프만-라 로슈 아게 | 스테아로일-CoA 불포화화효소 1(에스씨디 1)의 억제제로서의 치환된 이속사졸 아마이드 화합물 |
| US9475757B2 (en) | 2013-05-03 | 2016-10-25 | Council Of Scientific & Industrial Research | 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 |
| 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 |
| 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 |
| 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 |
| CN117923998A (zh) * | 2022-10-24 | 2024-04-26 | 中国石油化工股份有限公司 | 苯甲醛及其衍生物的制备方法 |
| 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 |
| EP4750446A1 (en) | 2023-07-25 | 2026-06-03 | 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 |
| JP2003529589A (ja) | 2000-03-31 | 2003-10-07 | ユーロ−セルティック エス． ア． | アミノピリジンならびにこれらの鎮痙薬およびナトリウムチャンネル遮断薬としての使用 |
| 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 |
| AU2004207010A1 (en) * | 2003-01-30 | 2004-08-12 | Dynogen Pharmaceuticals, Inc. | Methods of treating lower urinary tract disorders using sodium channel modulators |
| CA2514574A1 (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 |
| US20070276046A1 (en) | 2003-08-25 | 2007-11-29 | Patricia Salvati | 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 |
| RS51411B (sr) | 2004-09-10 | 2011-02-28 | Newron Pharmaceuticals S.P.A. | Upotreba (r)-(halobenziloksi) benzilamino-propanamida kao selektivnih modulatora natrijumovih i/ili kalcijumovih kanala |
| EP1870097A1 (en) | 2006-06-15 | 2007-12-26 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of cognitive disorders |
| KR101491541B1 (ko) * | 2006-06-19 | 2015-02-09 | 뉴론 파마슈티칼즈 에스. 피. 에이. | 2-［4-(3- 및 2-플루오로벤질옥시)벤질아미노)프로판 아미드의 제조방법 |
| EP3257842B1 (en) | 2007-12-11 | 2020-11-18 | Newron Pharmaceuticals S.p.A. | Therapeutic use of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree |
| CN101903021B (zh) | 2007-12-19 | 2012-11-14 | 纽朗制药有限公司 | 用于治疗精神病的α-氨基酰胺衍生物 |
-
2007
- 2007-06-08 KR KR20147003965A patent/KR101491541B1/ko active Active
- 2007-06-08 PL PL07764601T patent/PL2029524T3/pl unknown
- 2007-06-08 NZ NZ572798A patent/NZ572798A/en 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 EA EA201101308A patent/EA025326B1/ru unknown
- 2007-06-08 EA EA200970028A patent/EA017123B1/ru unknown
- 2007-06-08 CN CN2007800228798A patent/CN101472880B/zh not_active Ceased
- 2007-06-08 PT PT07764601T patent/PT2029524E/pt unknown
- 2007-06-08 PL PL12163085T patent/PL2474521T3/pl unknown
- 2007-06-08 JP JP2009515731A patent/JP5240476B2/ja active Active
- 2007-06-08 EP EP07764601.6A patent/EP2029524B1/en active Active
- 2007-06-08 MX MX2008015704A patent/MX2008015704A/es active IP Right Grant
- 2007-06-08 AU AU2007263328A patent/AU2007263328C1/en active Active
- 2007-06-08 EP EP12163085.9A patent/EP2474521B1/en active Active
- 2007-06-08 BR BRPI0712936A patent/BRPI0712936B8/pt active IP Right Grant
- 2007-06-08 RS RS20160965A patent/RS55464B1/sr unknown
- 2007-06-08 NZ NZ595737A patent/NZ595737A/xx unknown
- 2007-06-08 DK DK07764601.6T patent/DK2029524T3/da active
- 2007-06-08 MX MX2012005094A patent/MX342698B/es unknown
- 2007-06-08 SI SI200731603T patent/SI2029524T1/sl unknown
- 2007-06-08 ES ES07764601.6T patent/ES2527437T3/es active Active
- 2007-06-08 RS RS20150114A patent/RS53824B1/sr unknown
- 2007-06-08 CA CA2653012A patent/CA2653012C/en active Active
- 2007-06-08 CN CN201310142245.3A patent/CN103284984B/zh active Active
- 2007-06-08 HU HUE12163085A patent/HUE030233T2/en unknown
- 2007-06-08 PT PT121630859T patent/PT2474521T/pt unknown
- 2007-06-08 KR KR1020097001124A patent/KR101410291B1/ko active Active
- 2007-06-08 SI SI200731854A patent/SI2474521T1/sl unknown
- 2007-06-08 LT LTEP12163085.9T patent/LT2474521T/lt unknown
- 2007-06-08 DK DK12163085.9T patent/DK2474521T3/en active
- 2007-06-08 HR HRP20150136TT patent/HRP20150136T1/hr unknown
- 2007-06-15 TW TW096121879A patent/TWI393700B/zh active
- 2007-06-15 TW TW101148004A patent/TWI412512B/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
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2011
- 2011-11-03 US US13/288,891 patent/US8278485B2/en active Active
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2013
- 2013-01-10 JP JP2013002429A patent/JP5795342B2/ja active Active
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2015
- 2015-01-23 CY CY20151100072T patent/CY1115951T1/el unknown
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2016
- 2016-10-18 CY CY20161101038T patent/CY1118113T1/el unknown
- 2016-11-03 HR HRP20161456TT patent/HRP20161456T1/hr unknown
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2017
- 2017-11-30 NO NO20171916A patent/NO342644B1/no unknown
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