CA2743232C - Crystalline forms of fingolimod hcl - Google Patents

Crystalline forms of fingolimod hcl Download PDF

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Publication number
CA2743232C
CA2743232C CA2743232A CA2743232A CA2743232C CA 2743232 C CA2743232 C CA 2743232C CA 2743232 A CA2743232 A CA 2743232A CA 2743232 A CA2743232 A CA 2743232A CA 2743232 C CA2743232 C CA 2743232C
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Canada
Prior art keywords
weak
fty720
crystalline
composition
hydrate
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CA2743232A
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English (en)
French (fr)
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CA2743232A1 (en
Inventor
Michael Mutz
Guido Jordine
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Novartis AG
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Novartis AG
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Publication of CA2743232A1 publication Critical patent/CA2743232A1/en
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02Local antiseptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02Compounds 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
    • C07C215/22Compounds 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
    • C07C215/28Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)
CA2743232A 2008-11-11 2009-11-10 Crystalline forms of fingolimod hcl Active CA2743232C (en)

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

Publications (2)

Publication Number Publication Date
CA2743232A1 CA2743232A1 (en) 2010-05-20
CA2743232C true CA2743232C (en) 2015-12-29

Family

ID=40521487

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2743232A Active CA2743232C (en) 2008-11-11 2009-11-10 Crystalline forms of fingolimod hcl

Country Status (14)

Country Link
US (2) US8530522B2 (enExample)
EP (1) EP2356090B1 (enExample)
JP (4) JP2012508216A (enExample)
KR (2) KR101393994B1 (enExample)
CN (3) CN104788325A (enExample)
AU (1) AU2009315736B2 (enExample)
BR (1) BRPI0921826A2 (enExample)
CA (1) CA2743232C (enExample)
ES (1) ES2643161T3 (enExample)
MX (1) MX2011004962A (enExample)
PL (1) PL2356090T3 (enExample)
PT (1) PT2356090T (enExample)
RU (2) RU2015111229A (enExample)
WO (1) WO2010055028A2 (enExample)

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ES2746939T3 (es) * 2010-10-01 2020-03-09 Synthon Bv Procedimiento para la preparación de cristales de clorhidrato de fingolimod
PL2632889T3 (pl) 2010-10-28 2019-04-30 Mapi Pharma Ltd Związki pośrednie i sposób wytwarzania fingolimodu
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
ES2746016T3 (es) 2010-12-28 2020-03-04 Synthon Bv Procedimiento para la preparación de cristales de clorhidrato de fingolimod
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
US9751834B2 (en) 2011-05-26 2017-09-05 Gri Bio, Inc. 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
EP3610868B1 (en) 2011-05-26 2025-02-19 GRI Bio, Inc. Amino- or ammonium-containing sulfonic acid derivatives and their medical use
WO2013019872A1 (en) 2011-08-01 2013-02-07 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
EP2945927A4 (en) * 2013-01-17 2017-01-18 Shilpa Medicare Limited Process for preparation of fingolimod and its salts
EP2964210B1 (en) * 2013-03-05 2023-10-04 Biocon Limited A 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
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
MX2022005014A (es) 2019-10-31 2022-05-16 Idorsia Pharmaceuticals Ltd Combinacion de un antagonista de cxcr7 con un modulador del receptor s1p1.
JP2024521882A (ja) 2021-05-31 2024-06-04 上海雲晟研新生物科技有限公司 フィンゴリモド薬用塩、製造方法、それを含む医薬組成物及び使用
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

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JP2579602B2 (ja) 1992-10-21 1997-02-05 吉富製薬株式会社 2−アミノ−1,3−プロパンジオール化合物および免疫抑制剤
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
ES2644413T3 (es) * 1998-11-11 2017-11-28 Novartis Ag Producción de 2-amino-2-[2-(4-alquil-fenil)etil]propano-1,3-dioles
PT1031347E (pt) * 1999-01-27 2002-09-30 Idea Ag Transporte/imunizacao transnasal com veiculos muitissimo adaptaveis
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
RU2003136730A (ru) * 2001-06-08 2005-05-20 Новартис АГ (CH) Лечение или профилактика отторжения инсулин-продуцирующего клеточного трансплантата
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
NZ592339A (en) * 2003-04-08 2012-09-28 Novartis Ag Solid pharmaceutical compositions of S1P receptor agonist with sugar alcohol
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
RU2008116578A (ru) * 2005-09-30 2009-11-10 Новартис АГ (CH) Применение ингибиторов dpp-iv для лечения аутоиммунных заболеваний и отторжения трансплантата
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
ES2414205T3 (es) * 2006-06-02 2013-07-18 The Ohio State University Research Foundation Agentes terapéuticos para el tratamiento de linfoma de células del manto
KR101686369B1 (ko) * 2006-09-26 2016-12-13 노파르티스 아게 S1p 조정제를 포함하는 제약 조성물
KR20170081755A (ko) * 2008-06-20 2017-07-12 노파르티스 아게 다발성 경화증을 치료하기 위한 소아용 조성물
ES2746939T3 (es) 2010-10-01 2020-03-09 Synthon Bv Procedimiento para la preparación de cristales de clorhidrato de fingolimod

Also Published As

Publication number Publication date
JP2014139179A (ja) 2014-07-31
KR20110069156A (ko) 2011-06-22
EP2356090A2 (en) 2011-08-17
JP2012508216A (ja) 2012-04-05
AU2009315736A1 (en) 2010-05-20
RU2549899C2 (ru) 2015-05-10
KR20130109254A (ko) 2013-10-07
KR101393994B1 (ko) 2014-05-14
RU2011123371A (ru) 2012-12-20
US20140051766A1 (en) 2014-02-20
PT2356090T (pt) 2017-10-16
WO2010055028A2 (en) 2010-05-20
US20110229501A1 (en) 2011-09-22
CA2743232A1 (en) 2010-05-20
PL2356090T3 (pl) 2017-12-29
EP2356090B1 (en) 2017-07-05
RU2015111229A3 (enExample) 2018-11-08
ES2643161T3 (es) 2017-11-21
US8530522B2 (en) 2013-09-10
JP2016028056A (ja) 2016-02-25
WO2010055028A3 (en) 2010-07-08
AU2009315736B2 (en) 2013-08-29
RU2015111229A (ru) 2015-11-20
CN102209705A (zh) 2011-10-05
CN104788325A (zh) 2015-07-22
BRPI0921826A2 (pt) 2016-01-12
JP2018035160A (ja) 2018-03-08
CN107233336A (zh) 2017-10-10
MX2011004962A (es) 2011-05-30

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