MX2011004962A - Formas cristalinas de hcl de fingolimod. - Google Patents
Formas cristalinas de hcl de fingolimod.Info
- Publication number
- MX2011004962A MX2011004962A MX2011004962A MX2011004962A MX2011004962A MX 2011004962 A MX2011004962 A MX 2011004962A MX 2011004962 A MX2011004962 A MX 2011004962A MX 2011004962 A MX2011004962 A MX 2011004962A MX 2011004962 A MX2011004962 A MX 2011004962A
- Authority
- MX
- Mexico
- Prior art keywords
- salt
- crystalline
- fty720
- ray powder
- weak
- Prior art date
Links
- 229960000556 fingolimod Drugs 0.000 title claims description 29
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- SWZTYAVBMYWFGS-UHFFFAOYSA-N fingolimod hydrochloride Chemical compound Cl.CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 SWZTYAVBMYWFGS-UHFFFAOYSA-N 0.000 claims description 27
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Classifications
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- 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
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- 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
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- 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]
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- Oncology (AREA)
- Transplantation (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)
Applications Claiming Priority (2)
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|---|---|---|---|
| EP08168865 | 2008-11-11 | ||
| PCT/EP2009/064891 WO2010055028A2 (en) | 2008-11-11 | 2009-11-10 | Organic compounds |
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| MX2011004962A true MX2011004962A (es) | 2011-05-30 |
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| PT (1) | PT2356090T (enExample) |
| RU (2) | RU2015111229A (enExample) |
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| EP2621889B1 (en) | 2010-10-01 | 2019-07-17 | Synthon BV | Process for making fingolimod hydrochloride crystals |
| CN103313964A (zh) | 2010-10-28 | 2013-09-18 | Mapi医药公司 | 用于制备芬戈莫德的中间化合物和方法 |
| WO2012071524A1 (en) | 2010-11-24 | 2012-05-31 | Ratiopharm Gmbh | Arylsulfonate salts of fingolimod and processes for preparation thereof |
| EP2646409A4 (en) * | 2010-11-25 | 2015-12-16 | Shilpa Medicare Ltd | FINGOLIMOD POLYMORPHES AND METHOD THEREFOR |
| 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 |
| EP2702034A4 (en) | 2011-04-29 | 2015-03-25 | Reddys Lab Ltd Dr | PREPARATION OF FINGOLIMOD AND ITS SALTS |
| EP2809318B1 (en) | 2011-05-26 | 2019-05-08 | GRI Bio, Inc. | Ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use |
| WO2012160188A1 (en) | 2011-05-26 | 2012-11-29 | Jado Technologies Gmbh | Hydroxy-substituted amino and ammonium derivatives and their medical use |
| DK2809648T3 (da) | 2011-05-26 | 2019-06-17 | Gri Bio Inc | Oxygenberigede amino- eller ammonium-holdige sulfonsyrederivater og disses medicinske anvendelse |
| EP2739272A1 (en) | 2011-08-01 | 2014-06-11 | Teva Pharmaceutical Industries Ltd. | Process for preparing pharmaceutical compositions comprising fingolimod |
| WO2013091704A1 (en) * | 2011-12-22 | 2013-06-27 | Synthon Bv | Pharmaceutical composition comprising fingolimod |
| CN102887829B (zh) * | 2012-09-05 | 2014-07-02 | 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 |
| NZ630290A (en) * | 2013-01-17 | 2016-09-30 | Shilpa Medicare Ltd | Process for preparation of fingolimod and its salts |
| JP6484567B2 (ja) * | 2013-03-05 | 2019-03-13 | バイオコン・リミテッドＢｉｏｃｏｎ Ｌｉｍｉｔｅｄ | ２−アミノ−１，３−プロパンジオール化合物およびその塩の製造のための方法 |
| US20160128951A1 (en) | 2013-07-29 | 2016-05-12 | Aizant Drug Research Solutions Pvt Ltd | 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 |
| 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 |
| 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 |
| 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 |
| WO2021084068A1 (en) | 2019-10-31 | 2021-05-06 | Idorsia Pharmaceuticals Ltd | Combination of a cxcr7 antagonist with an s1p1 receptor modulator |
| EP4353709A4 (en) | 2021-05-31 | 2026-02-18 | Shanghai Yonsun Biotechnology Co Ltd | FINGOLIMOD PHARMACEUTICAL SALT, ITS PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION, CONTAINER AND ASSOCIATED USES |
| 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 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994008943A1 (fr) | 1992-10-21 | 1994-04-28 | Yoshitomi Pharmaceutical Industries, Ltd. | Compose 2-amino-1,3-propanediol et immunosuppresseur |
| US6476004B1 (en) | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| 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 |
| ES2237970T3 (es) * | 1998-11-11 | 2005-08-01 | Novartis Ag | Produccion de 2-amino-2-(2-(4-alquil c2-20-fenil)etil)propano-1,3-dioles. |
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| US7015218B1 (en) * | 1999-02-10 | 2006-03-21 | Mitsubishi Pharma Corporation | Amide compounds and medicinal use thereof |
| 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 |
| JP4476623B2 (ja) * | 2001-06-08 | 2010-06-09 | ノバルティス アーゲー | インスリン産生細胞移植片拒絶の処置または予防 |
| US20030144712A1 (en) * | 2001-12-20 | 2003-07-31 | Jackson Streeter, M.D. | Methods for overcoming organ transplant rejection |
| NZ560662A (en) * | 2002-05-16 | 2009-09-25 | Novartis Ag | Use of EDG receptor binding agents in cancer |
| GB0217152D0 (en) * | 2002-07-24 | 2002-09-04 | Novartis Ag | Organic compounds |
| BRPI0409250B8 (pt) * | 2003-04-08 | 2022-01-18 | Mitsubishi Pharma Corp | Composições farmacêuticas sólidas compreendendo um agonista receptor de s1p e um álcool do açúcar |
| 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 |
| EP2046315B1 (en) * | 2006-06-02 | 2013-04-10 | The Ohio State University Research Foundation | Therapeutic agents for the treatment of mantle cell lymphoma |
| PT3103448T (pt) * | 2006-09-26 | 2019-07-12 | Novartis Ag | Composições farmacêuticas que compreendem um modulador de s1p |
| CN104800196A (zh) * | 2008-06-20 | 2015-07-29 | 诺华股份有限公司 | 用于治疗多发性硬化的儿科组合物 |
| EP2621889B1 (en) | 2010-10-01 | 2019-07-17 | Synthon BV | Process for making fingolimod hydrochloride crystals |
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| JP2016028056A (ja) | 2016-02-25 |
| KR20130109254A (ko) | 2013-10-07 |
| RU2549899C2 (ru) | 2015-05-10 |
| RU2015111229A3 (enExample) | 2018-11-08 |
| US8530522B2 (en) | 2013-09-10 |
| KR20110069156A (ko) | 2011-06-22 |
| US20110229501A1 (en) | 2011-09-22 |
| BRPI0921826A2 (pt) | 2016-01-12 |
| US20140051766A1 (en) | 2014-02-20 |
| WO2010055028A3 (en) | 2010-07-08 |
| AU2009315736A1 (en) | 2010-05-20 |
| JP2018035160A (ja) | 2018-03-08 |
| PT2356090T (pt) | 2017-10-16 |
| WO2010055028A2 (en) | 2010-05-20 |
| KR101393994B1 (ko) | 2014-05-14 |
| CN104788325A (zh) | 2015-07-22 |
| CA2743232A1 (en) | 2010-05-20 |
| CN102209705A (zh) | 2011-10-05 |
| PL2356090T3 (pl) | 2017-12-29 |
| JP2014139179A (ja) | 2014-07-31 |
| JP2012508216A (ja) | 2012-04-05 |
| CA2743232C (en) | 2015-12-29 |
| RU2015111229A (ru) | 2015-11-20 |
| RU2011123371A (ru) | 2012-12-20 |
| EP2356090A2 (en) | 2011-08-17 |
| AU2009315736B2 (en) | 2013-08-29 |
| CN107233336A (zh) | 2017-10-10 |
| ES2643161T3 (es) | 2017-11-21 |
| EP2356090B1 (en) | 2017-07-05 |
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