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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CA
Canada
Prior art keywords
weak
fty720
crystalline
composition
hydrate
Prior art date
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Active
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CA2743232A
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English (en)
French (fr)
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CA2743232A1 (en
Inventor
Michael Mutz
Guido Jordine
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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Novartis AG
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Publication date
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Publication of CA2743232A1 publication Critical patent/CA2743232A1/en
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Publication of CA2743232C publication Critical patent/CA2743232C/en
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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)
  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • 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)
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
EP08168865.7 2008-11-11
EP08168865 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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PT2621889T (pt) * 2010-10-01 2019-10-30 Synthon Bv Processo para produzir cristais de cloridrato de fingolimod
US8735627B2 (en) 2010-10-28 2014-05-27 Mapi Pharma Ltd. 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
EP2702034A4 (en) 2011-04-29 2015-03-25 Reddys Lab Ltd Dr PREPARATION OF FINGOLIMOD AND ITS SALTS
WO2012160188A1 (en) 2011-05-26 2012-11-29 Jado Technologies Gmbh Hydroxy-substituted amino and ammonium derivatives and their medical use
DK3610868T3 (da) 2011-05-26 2025-03-31 Gri Bio Inc Amino- eller ammoniumholdige sulfonsyrederivater og medicinsk anvendelse deraf
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
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
NZ630290A (en) * 2013-01-17 2016-09-30 Shilpa Medicare Ltd Process for preparation of fingolimod and its salts
AU2014224237B2 (en) * 2013-03-05 2017-07-20 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
WO2016118515A1 (en) 2015-01-20 2016-07-28 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
CA3156298A1 (en) 2019-10-31 2021-05-06 Laetitia POUZOL Combination of a cxcr7 antagonist with an s1p1 receptor modulator
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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KR0155015B1 (ko) 1992-10-21 1998-12-01 고우야 마사시 2-아미노-1,3-프로판디올 화합물 및 면역 억제제
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
WO2000027798A1 (en) * 1998-11-11 2000-05-18 Novartis Ag Production of 2-amino-2-[2-(4-c2-20-alkyl-phenyl)ethyl]propane-1,3-diols
EP1031347B1 (en) * 1999-01-27 2002-04-17 Idea Ag Transnasal transport/immunisation with highly adaptable carriers
DE60017115T2 (de) * 1999-02-10 2005-12-08 Mitsubishi Pharma Corp. Amid-derivate und deren medizinische verwendung
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
ES2322442T3 (es) * 2001-06-08 2009-06-22 Novartis Ag Tratamiento o profilaxis del rechazo de injertos de celulas productoras de insulina.
US20030144712A1 (en) * 2001-12-20 2003-07-31 Jackson Streeter, M.D. Methods for overcoming organ transplant rejection
JP5227492B2 (ja) * 2002-05-16 2013-07-03 ノバルティス アーゲー 癌におけるｅｄｇレセプター結合剤の使用
GB0217152D0 (en) * 2002-07-24 2002-09-04 Novartis Ag Organic compounds
CA2707750A1 (en) * 2003-04-08 2004-10-21 Novartis Ag Solid pharmaceutical compositions comprising a s1p receptor agonist and a 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
EP1940388A2 (en) * 2005-09-30 2008-07-09 Novartis AG Dpp iv inhibtor 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
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
RU2487703C2 (ru) * 2006-09-26 2013-07-20 Новартис Аг Фармацевтические композиции, включающие модулятор s1р
WO2009155475A1 (en) * 2008-06-20 2009-12-23 Novartis Ag Paediatric compositions for treating1 multiple sclerosis
PT2621889T (pt) 2010-10-01 2019-10-30 Synthon Bv Processo para produzir cristais de cloridrato de fingolimod

Also Published As

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

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Effective date: 20250512