CN102209705A - 芬戈莫德盐酸盐的结晶形式 - Google Patents
芬戈莫德盐酸盐的结晶形式 Download PDFInfo
- Publication number
- CN102209705A CN102209705A CN200980144998XA CN200980144998A CN102209705A CN 102209705 A CN102209705 A CN 102209705A CN 200980144998X A CN200980144998X A CN 200980144998XA CN 200980144998 A CN200980144998 A CN 200980144998A CN 102209705 A CN102209705 A CN 102209705A
- Authority
- CN
- China
- Prior art keywords
- salt
- fty720
- peak
- weak
- ray powder
- 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.)
- Pending
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Classifications
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/02—Local antiseptics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
- C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510141353.8A CN104788325A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
| CN201710377640.8A CN107233336A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08168865 | 2008-11-11 | ||
| EP08168865.7 | 2008-11-11 | ||
| PCT/EP2009/064891 WO2010055028A2 (en) | 2008-11-11 | 2009-11-10 | Organic compounds |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710377640.8A Division CN107233336A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
| CN201510141353.8A Division CN104788325A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102209705A true CN102209705A (zh) | 2011-10-05 |
Family
ID=40521487
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980144998XA Pending CN102209705A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德盐酸盐的结晶形式 |
| CN201510141353.8A Pending CN104788325A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
| CN201710377640.8A Pending CN107233336A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510141353.8A Pending CN104788325A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
| CN201710377640.8A Pending CN107233336A (zh) | 2008-11-11 | 2009-11-10 | 芬戈莫德的结晶形式 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8530522B2 (https=) |
| EP (1) | EP2356090B1 (https=) |
| JP (4) | JP2012508216A (https=) |
| KR (2) | KR20130109254A (https=) |
| CN (3) | CN102209705A (https=) |
| AU (1) | AU2009315736B2 (https=) |
| BR (1) | BRPI0921826A2 (https=) |
| CA (1) | CA2743232C (https=) |
| ES (1) | ES2643161T3 (https=) |
| MX (1) | MX2011004962A (https=) |
| PL (1) | PL2356090T3 (https=) |
| PT (1) | PT2356090T (https=) |
| RU (2) | RU2549899C2 (https=) |
| WO (1) | WO2010055028A2 (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014036865A1 (zh) * | 2012-09-05 | 2014-03-13 | 中国科学院上海药物研究所 | 芬戈莫德粘酸盐及其晶体的制备方法和用途 |
| CN106667981A (zh) * | 2017-01-16 | 2017-05-17 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗药物性肝损伤药物中的应用 |
| CN106860440A (zh) * | 2017-01-16 | 2017-06-20 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗系统性红斑狼疮脑病药物中的应用 |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012041358A1 (en) | 2010-10-01 | 2012-04-05 | Synthon B.V. | Process for making fingolimod hydrochloride crystals |
| EP2632889B1 (en) | 2010-10-28 | 2018-08-29 | Mapi Pharma Limited | Intermediate compounds and process for the preparation of fingolimod |
| WO2012071524A1 (en) | 2010-11-24 | 2012-05-31 | Ratiopharm Gmbh | Arylsulfonate salts of fingolimod and processes for preparation thereof |
| WO2012070059A1 (en) * | 2010-11-25 | 2012-05-31 | Shilpa Medicare Limited | Fingolimod polymorphs and their processes |
| WO2012089238A1 (en) | 2010-12-28 | 2012-07-05 | Synthon Bv | Process for making fingolimod hydrochloride crystals |
| WO2012097330A2 (en) * | 2011-01-14 | 2012-07-19 | University Of Washington | Compositions and methods for treating degenerative muscle conditions |
| US9216943B2 (en) | 2011-04-29 | 2015-12-22 | Dr. Reddy's Laboratories Ltd. | Preparation of fingolimod and its salts |
| DK2809318T3 (da) | 2011-05-26 | 2019-07-22 | Gri Bio Inc | Ammoniumholdige sulfonsyre-, phosphonsyre- og carboxylsyrederivater og disses medicinske anvendelse |
| WO2012160186A1 (en) | 2011-05-26 | 2012-11-29 | Jado Technologies Gmbh | Oxygenated amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use |
| DK2739606T3 (en) | 2011-05-26 | 2016-07-25 | Jado Tech Gmbh | Hydroxy-substituted amino and ammonium derivatives and their medical use |
| US9186333B2 (en) | 2011-08-01 | 2015-11-17 | Teva Pharmaceutical Industries Ltd. | Process for preparing pharmaceutical compositions of fingolimod |
| WO2013091704A1 (en) * | 2011-12-22 | 2013-06-27 | Synthon Bv | Pharmaceutical composition comprising fingolimod |
| AU2014206588A1 (en) * | 2013-01-17 | 2015-07-23 | Shilpa Medicare Limited | Process for preparation of Fingolimod and its salts |
| US9815772B2 (en) * | 2013-03-05 | 2017-11-14 | Biocon Limited | Process for the preparation of 2-amino-1,3-propane diol compounds and salts thereof |
| EP3027174B1 (en) | 2013-07-29 | 2019-07-24 | Aizant Drug Research Solutions Private Limited | Pharmaceutical compositions of fingolimod |
| WO2016042493A1 (en) * | 2014-09-19 | 2016-03-24 | Aizant Drug Research Pvt. Ltd | Pharmaceutical compositions of fingolimod |
| US9925138B2 (en) | 2015-01-20 | 2018-03-27 | Handa Pharmaceuticals, Llc | Stable solid fingolimod dosage forms |
| RU2627691C1 (ru) * | 2016-07-06 | 2017-08-10 | Олег Ростиславович Михайлов | Кристаллическая η-модификация 2-амино-2-(2-(4-октилфенил)этил)пропан-1,3-диол гидрохлорида, способ её получения и фармацевтическая композиция на её основе |
| GR1009654B (el) | 2018-08-31 | 2019-11-18 | Φαρματεν Α.Β.Ε.Ε. | Φαρμακευτικο σκευασμα που περιλαμβανει εναν ανοσοτροποποιητικο παραγοντα και μεθοδος για την παρασκευη αυτου |
| WO2020245775A1 (en) * | 2019-06-05 | 2020-12-10 | Biocon Limited | Crystalline forms of 2-amino-2-(2-(4-octylphenyl) ethyl) propane-1,3-diol |
| JP7749552B2 (ja) | 2019-10-31 | 2025-10-06 | イドルシア・ファーマシューティカルズ・リミテッド | Cxcr7アンタゴニストのs1p1受容体調節剤との合剤 |
| CN115477590B (zh) | 2021-05-31 | 2023-12-12 | 上海云晟研新生物科技有限公司 | 芬戈莫德药用盐、制备方法、含其的药物组合物及应用 |
| EP4212156A1 (en) | 2022-01-13 | 2023-07-19 | Abivax | Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a s1p receptor modulator |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5604229A (en) * | 1992-10-21 | 1997-02-18 | Yoshitomi Pharmaceutical Industries, Ltd. | 2-amino-1,3-propanediol compound and immunosuppressant |
| CN1344155A (zh) * | 1999-01-27 | 2002-04-10 | 概念股份公司 | 用高适应性的载体经鼻输送/免疫接种 |
| CN1346348A (zh) * | 1999-02-10 | 2002-04-24 | 卫福有限公司 | 酰胺化合物及其药物用途 |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| WO2004089341A1 (en) * | 2003-04-08 | 2004-10-21 | Novartis Ag | Organic compounds |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4079505B2 (ja) * | 1998-04-28 | 2008-04-23 | 田辺三菱製薬株式会社 | 2−アミノ−2−[2−(4−オクチルフェニル)エチル]プロパン−1,3−ジオールの新規な製造法 |
| DK1129066T3 (da) * | 1998-11-11 | 2005-03-29 | Novartis Ag | Fremstilling af 2-amino-2-[2-(C2-20alkylphenyl)ethyl]propan-1,3-dioler |
| CN1144779C (zh) * | 1999-03-11 | 2004-04-07 | 杭州中美华东制药有限公司 | 制备2-[2-(4-烷基苯基)-乙基]-2-氨基-丙二醇的方法以及其中制得的中间产物 |
| BR0209319A (pt) * | 2001-06-08 | 2004-07-20 | Novartis Ag | Tratamento ou profilaxia de rejeição de enxerto de célula produtora de insulina |
| US20030144712A1 (en) * | 2001-12-20 | 2003-07-31 | Jackson Streeter, M.D. | Methods for overcoming organ transplant rejection |
| PT1505959E (pt) * | 2002-05-16 | 2009-02-05 | Novartis Ag | Utilização de agentes de ligação do receptor edg em cancro |
| GB0217152D0 (en) * | 2002-07-24 | 2002-09-04 | Novartis Ag | Organic compounds |
| CN1212308C (zh) * | 2003-07-24 | 2005-07-27 | 漆又毛 | 2-氨基-2-(2-(4-辛基苯基)乙基)-1,3-丙二醇盐酸盐的制备方法 |
| CN1241903C (zh) * | 2003-10-14 | 2006-02-15 | 马启明 | 制备2-对辛基苯乙基-2-氨基丙二醇的方法 |
| TWI418350B (zh) * | 2005-06-24 | 2013-12-11 | Sankyo Co | 含有ppar調節劑之醫藥組成物的用途 |
| CA2623826A1 (en) * | 2005-09-30 | 2007-04-12 | Novartis Ag | Dpp iv inhibitor for use in the treatment of autoimmune diseases and graft rejection |
| CN1310869C (zh) * | 2005-11-22 | 2007-04-18 | 江苏吴中苏药医药开发有限责任公司 | 2-氨基-2-[2-(4-烷基苯基)乙基]-1,3-丙二醇的制备方法 |
| CN100548968C (zh) * | 2006-03-01 | 2009-10-14 | 徐州师范大学 | 一种制备2-对辛基苯乙基-2-氨基丙二醇盐酸盐的方法 |
| WO2007143081A2 (en) * | 2006-06-02 | 2007-12-13 | The Ohio State University Research Foundation | Therapeutic agents for the treatment of lymphoid malignancies |
| HUE046441T2 (hu) * | 2006-09-26 | 2020-02-28 | Novartis Ag | S1P modulátort tartalmazó gyógyászati készítmények |
| JP2011525189A (ja) * | 2008-06-20 | 2011-09-15 | ノバルティス アーゲー | 多発性硬化症を治療するための小児科の組成物 |
| WO2012041358A1 (en) | 2010-10-01 | 2012-04-05 | Synthon B.V. | Process for making fingolimod hydrochloride crystals |
-
2009
- 2009-11-10 PT PT97483507T patent/PT2356090T/pt unknown
- 2009-11-10 EP EP09748350.7A patent/EP2356090B1/en active Active
- 2009-11-10 KR KR1020137024001A patent/KR20130109254A/ko not_active Withdrawn
- 2009-11-10 WO PCT/EP2009/064891 patent/WO2010055028A2/en not_active Ceased
- 2009-11-10 KR KR1020117010560A patent/KR101393994B1/ko not_active Expired - Fee Related
- 2009-11-10 CN CN200980144998XA patent/CN102209705A/zh active Pending
- 2009-11-10 BR BRPI0921826A patent/BRPI0921826A2/pt not_active Application Discontinuation
- 2009-11-10 MX MX2011004962A patent/MX2011004962A/es active IP Right Grant
- 2009-11-10 ES ES09748350.7T patent/ES2643161T3/es active Active
- 2009-11-10 CA CA2743232A patent/CA2743232C/en active Active
- 2009-11-10 CN CN201510141353.8A patent/CN104788325A/zh active Pending
- 2009-11-10 PL PL09748350T patent/PL2356090T3/pl unknown
- 2009-11-10 US US13/128,825 patent/US8530522B2/en not_active Expired - Fee Related
- 2009-11-10 RU RU2011123371/04A patent/RU2549899C2/ru active
- 2009-11-10 RU RU2015111229/04A patent/RU2015111229A/ru not_active Application Discontinuation
- 2009-11-10 AU AU2009315736A patent/AU2009315736B2/en not_active Ceased
- 2009-11-10 CN CN201710377640.8A patent/CN107233336A/zh active Pending
- 2009-11-10 JP JP2011535130A patent/JP2012508216A/ja not_active Withdrawn
-
2013
- 2013-08-12 US US13/964,817 patent/US20140051766A1/en not_active Abandoned
-
2014
- 2014-02-06 JP JP2014020950A patent/JP2014139179A/ja not_active Withdrawn
-
2015
- 2015-09-03 JP JP2015173474A patent/JP2016028056A/ja not_active Withdrawn
-
2017
- 2017-09-07 JP JP2017172276A patent/JP2018035160A/ja active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5604229A (en) * | 1992-10-21 | 1997-02-18 | Yoshitomi Pharmaceutical Industries, Ltd. | 2-amino-1,3-propanediol compound and immunosuppressant |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| CN1344155A (zh) * | 1999-01-27 | 2002-04-10 | 概念股份公司 | 用高适应性的载体经鼻输送/免疫接种 |
| CN1346348A (zh) * | 1999-02-10 | 2002-04-24 | 卫福有限公司 | 酰胺化合物及其药物用途 |
| WO2004089341A1 (en) * | 2003-04-08 | 2004-10-21 | Novartis Ag | Organic compounds |
Non-Patent Citations (2)
| Title |
|---|
| MASATOSHI KIUCHI等: "Synthesis and Immunosuppressive Activity of 2-Substituted 2-Aminopropane-1,3-diols and 2-Aminoethanols", 《JOURNAL OF MEDICINAL CHEMISTRY》 * |
| 王迷娟: "芬戈莫德(fingolimode)", 《中国新药杂志》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014036865A1 (zh) * | 2012-09-05 | 2014-03-13 | 中国科学院上海药物研究所 | 芬戈莫德粘酸盐及其晶体的制备方法和用途 |
| CN106667981A (zh) * | 2017-01-16 | 2017-05-17 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗药物性肝损伤药物中的应用 |
| CN106860440A (zh) * | 2017-01-16 | 2017-06-20 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗系统性红斑狼疮脑病药物中的应用 |
| CN106667981B (zh) * | 2017-01-16 | 2019-05-14 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗药物性肝损伤药物中的应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2014139179A (ja) | 2014-07-31 |
| US20140051766A1 (en) | 2014-02-20 |
| RU2015111229A (ru) | 2015-11-20 |
| CN104788325A (zh) | 2015-07-22 |
| EP2356090A2 (en) | 2011-08-17 |
| US20110229501A1 (en) | 2011-09-22 |
| BRPI0921826A2 (pt) | 2016-01-12 |
| US8530522B2 (en) | 2013-09-10 |
| MX2011004962A (es) | 2011-05-30 |
| RU2549899C2 (ru) | 2015-05-10 |
| KR20110069156A (ko) | 2011-06-22 |
| CA2743232C (en) | 2015-12-29 |
| WO2010055028A2 (en) | 2010-05-20 |
| EP2356090B1 (en) | 2017-07-05 |
| KR20130109254A (ko) | 2013-10-07 |
| RU2015111229A3 (https=) | 2018-11-08 |
| JP2018035160A (ja) | 2018-03-08 |
| WO2010055028A3 (en) | 2010-07-08 |
| ES2643161T3 (es) | 2017-11-21 |
| PL2356090T3 (pl) | 2017-12-29 |
| JP2012508216A (ja) | 2012-04-05 |
| RU2011123371A (ru) | 2012-12-20 |
| JP2016028056A (ja) | 2016-02-25 |
| PT2356090T (pt) | 2017-10-16 |
| AU2009315736A1 (en) | 2010-05-20 |
| KR101393994B1 (ko) | 2014-05-14 |
| CN107233336A (zh) | 2017-10-10 |
| AU2009315736B2 (en) | 2013-08-29 |
| CA2743232A1 (en) | 2010-05-20 |
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| AU2013100532B4 (en) | Crystalline forms of fingolimod HCL | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20111005 |