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
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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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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)
  • 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)
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) KR20130109254A (enExample)
CN (3) CN102209705A (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) RU2549899C2 (enExample)
WO (1) WO2010055028A2 (enExample)

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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
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
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
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
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

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Publication number Priority date Publication date Assignee Title
DE69321823T2 (de) 1992-10-21 1999-06-02 Taito Co., Ltd., Tokio/Tokyo 2-amino-1, 3- propandiolverbindung und immunosuppressium
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
DK1129066T3 (da) * 1998-11-11 2005-03-29 Novartis Ag Fremstilling af 2-amino-2-[2-(C2-20alkylphenyl)ethyl]propan-1,3-dioler
SI1031347T1 (en) * 1999-01-27 2002-10-31 Idea Ag Transnasal transport/immunisation with highly adaptable carriers
MXPA01008142A (es) * 1999-02-10 2003-07-21 Welfide Corp Compuestos de amida, y uso medicinal de los mismos.
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
PE20130200A1 (es) * 2003-04-08 2013-03-09 Novartis Ag Composicion farmaceutica que contiene un agonista del receptor s1p y un alcohol de azucar
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

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
WO2010055028A2 (en) 2010-05-20
EP2356090B1 (en) 2017-07-05
KR20130109254A (ko) 2013-10-07
RU2015111229A3 (enExample) 2018-11-08
JP2018035160A (ja) 2018-03-08
WO2010055028A3 (en) 2010-07-08
CN102209705A (zh) 2011-10-05
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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Effective date: 20250512