AU2009315736B2 - Crystalline forms of fingolimod HCL - Google Patents

Crystalline forms of fingolimod HCL Download PDF

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Publication number
AU2009315736B2
AU2009315736B2 AU2009315736A AU2009315736A AU2009315736B2 AU 2009315736 B2 AU2009315736 B2 AU 2009315736B2 AU 2009315736 A AU2009315736 A AU 2009315736A AU 2009315736 A AU2009315736 A AU 2009315736A AU 2009315736 B2 AU2009315736 B2 AU 2009315736B2
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AU
Australia
Prior art keywords
weak
fty720
crystalline
salt
composition according
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Ceased
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AU2009315736A
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English (en)
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AU2009315736A1 (en
Inventor
Guido Jordine
Michael Mutz
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Novartis AG
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Novartis AG
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Publication of AU2009315736A1 publication Critical patent/AU2009315736A1/en
Priority to AU2013100530A priority Critical patent/AU2013100530B4/en
Priority to AU2013100532A priority patent/AU2013100532B4/en
Priority to AU2013100533A priority patent/AU2013100533B4/en
Priority to AU2013100531A priority patent/AU2013100531B4/en
Application granted granted Critical
Publication of AU2009315736B2 publication Critical patent/AU2009315736B2/en
Priority to AU2013263791A priority patent/AU2013263791B2/en
Priority to AU2016225785A priority patent/AU2016225785A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • 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
    • 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

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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
AU2009315736A 2008-11-11 2009-11-10 Crystalline forms of fingolimod HCL Ceased AU2009315736B2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
AU2013100530A AU2013100530B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013100532A AU2013100532B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013100533A AU2013100533B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013100531A AU2013100531B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013263791A AU2013263791B2 (en) 2008-11-11 2013-11-28 Crystalline forms of fingolimod HCL
AU2016225785A AU2016225785A1 (en) 2008-11-11 2016-09-05 Crystalline forms of fingolimod HCL

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 (5)

Application Number Title Priority Date Filing Date
AU2013100531A Division AU2013100531B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013100532A Division AU2013100532B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013100530A Division AU2013100530B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013100533A Division AU2013100533B4 (en) 2008-11-11 2013-04-12 Crystalline forms of fingolimod HCL
AU2013263791A Division AU2013263791B2 (en) 2008-11-11 2013-11-28 Crystalline forms of fingolimod HCL

Publications (2)

Publication Number Publication Date
AU2009315736A1 AU2009315736A1 (en) 2010-05-20
AU2009315736B2 true AU2009315736B2 (en) 2013-08-29

Family

ID=40521487

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009315736A Ceased AU2009315736B2 (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) 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)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103228617A (zh) * 2010-10-01 2013-07-31 斯索恩有限公司 制备盐酸芬戈莫德晶体的方法
BR112013010075A2 (pt) 2010-10-28 2017-10-24 Mapi Pharma Ltd compostos intermediários e processo para a preparação de fingolimod
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
US9216943B2 (en) 2011-04-29 2015-12-22 Dr. Reddy's Laboratories Ltd. Preparation of fingolimod and its salts
DK2739606T3 (en) 2011-05-26 2016-07-25 Jado Tech Gmbh Hydroxy-substituted amino and ammonium derivatives and their medical use
ES2731657T3 (es) * 2011-05-26 2019-11-18 Gri Bio Inc Derivados de ácido sulfónico, ácido fosfónico y ácido carboxílico que contienen amonio y su uso médico
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
EA028950B1 (ru) 2011-08-01 2018-01-31 Тева Фармасьютикал Индастриз Лтд. Способ получения фармацевтических композиций, содержащих финголимод
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
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
WO2015015254A1 (en) 2013-07-29 2015-02-05 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
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
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
TW202131921A (zh) 2019-10-31 2021-09-01 瑞士商愛杜西亞製藥有限公司 Cxcr7拮抗劑與s1p1受體調節劑之組合
US20240262783A1 (en) 2021-05-31 2024-08-08 Shanghai Bocimed Pharmaceutical Co., Ltd. Pharmaceutical salt of fingolimod, preparation method, pharmaceutical composition and use thereof
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6476004B1 (en) * 1996-07-18 2002-11-05 Mitsubishi Pharma Corporation Pharmaceutical composition

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0627406B1 (en) * 1992-10-21 1998-10-28 Yoshitomi Pharmaceutical Industries, Ltd. 2-amino-1,3-propanediol compound and immunosuppressant
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
ATE288414T1 (de) * 1998-11-11 2005-02-15 Novartis Pharma Gmbh Herstellung von 2-amino-2(2-(4- alkylphenyl)äthyl)propan-1,3-diolen
PT1031347E (pt) * 1999-01-27 2002-09-30 Idea Ag Transporte/imunizacao transnasal com veiculos muitissimo adaptaveis
KR100659007B1 (ko) * 1999-02-10 2007-02-28 미츠비시 웰파마 가부시키가이샤 아미드 화합물 및 그 의약으로서의 용도
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
NZ529044A (en) * 2001-06-08 2008-03-28 Novartis Ag Treatment or prophylaxis of insulin-producing cell graft rejection
US20030144712A1 (en) * 2001-12-20 2003-07-31 Jackson Streeter, M.D. Methods for overcoming organ transplant rejection
CA2483594C (en) * 2002-05-16 2011-02-15 Novartis Ag Use of edg receptor binding agents in cancer
GB0217152D0 (en) * 2002-07-24 2002-09-04 Novartis Ag Organic compounds
DE202004021680U1 (de) * 2003-04-08 2010-04-22 Novartis Ag Feste pharmazeutische Zusammensetzung
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
WO2007143081A2 (en) * 2006-06-02 2007-12-13 The Ohio State University Research Foundation Therapeutic agents for the treatment of lymphoid malignancies
SI3103448T1 (sl) * 2006-09-26 2019-11-29 Novartis Ag Farmacevtski sestavek, ki vsebuje modulator S1P
KR20180017232A (ko) * 2008-06-20 2018-02-20 노파르티스 아게 다발성 경화증을 치료하기 위한 소아용 조성물
CN103228617A (zh) 2010-10-01 2013-07-31 斯索恩有限公司 制备盐酸芬戈莫德晶体的方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6476004B1 (en) * 1996-07-18 2002-11-05 Mitsubishi Pharma Corporation Pharmaceutical composition

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KIUCHI, M. ET AL., "Synthesis and Immunosuppressive Activity of 2-Substituted 2-Aminopropane-1,3-diols and 2-Aminoethanols", 2000, J. Med. Chem., vol 43, pages 2946-2961. *

Also Published As

Publication number Publication date
JP2012508216A (ja) 2012-04-05
EP2356090B1 (en) 2017-07-05
CA2743232A1 (en) 2010-05-20
MX2011004962A (es) 2011-05-30
AU2009315736A1 (en) 2010-05-20
BRPI0921826A2 (pt) 2016-01-12
CA2743232C (en) 2015-12-29
WO2010055028A2 (en) 2010-05-20
CN104788325A (zh) 2015-07-22
RU2015111229A3 (enExample) 2018-11-08
PT2356090T (pt) 2017-10-16
JP2014139179A (ja) 2014-07-31
US20140051766A1 (en) 2014-02-20
WO2010055028A3 (en) 2010-07-08
US20110229501A1 (en) 2011-09-22
PL2356090T3 (pl) 2017-12-29
RU2549899C2 (ru) 2015-05-10
RU2011123371A (ru) 2012-12-20
JP2018035160A (ja) 2018-03-08
RU2015111229A (ru) 2015-11-20
KR20130109254A (ko) 2013-10-07
EP2356090A2 (en) 2011-08-17
US8530522B2 (en) 2013-09-10
KR20110069156A (ko) 2011-06-22
CN102209705A (zh) 2011-10-05
KR101393994B1 (ko) 2014-05-14
ES2643161T3 (es) 2017-11-21
CN107233336A (zh) 2017-10-10
JP2016028056A (ja) 2016-02-25

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
GD Licence registered

Name of requester: NOVARTIS PHARMACEUTICALS AUSTRALIA PTY LIMITED

MK14 Patent ceased section 143(a) (annual fees not paid) or expired