AU2009315735B2 - Salts of fingolimod - Google Patents

Salts of fingolimod Download PDF

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Publication number
AU2009315735B2
AU2009315735B2 AU2009315735A AU2009315735A AU2009315735B2 AU 2009315735 B2 AU2009315735 B2 AU 2009315735B2 AU 2009315735 A AU2009315735 A AU 2009315735A AU 2009315735 A AU2009315735 A AU 2009315735A AU 2009315735 B2 AU2009315735 B2 AU 2009315735B2
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AU
Australia
Prior art keywords
salt
weak
theta
peaks
ray powder
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2009315735A
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English (en)
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AU2009315735A1 (en
Inventor
Guido Jordine
Michael Mutz
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
Original Assignee
Novartis AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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Application filed by Novartis AG filed Critical Novartis AG
Publication of AU2009315735A1 publication Critical patent/AU2009315735A1/en
Application granted granted Critical
Publication of AU2009315735B2 publication Critical patent/AU2009315735B2/en
Priority to AU2013203470A priority Critical patent/AU2013203470A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08—Acetic acid
    • C07C53/10—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/122—Propionic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/08—Malonic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/01—Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
    • C07C59/08—Lactic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C63/00—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/04—Monocyclic monocarboxylic acids
    • C07C63/06—Benzoic acid
    • C07C63/08—Salts thereof

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2009315735A 2008-11-11 2009-11-10 Salts of fingolimod Ceased AU2009315735B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2013203470A AU2013203470A1 (en) 2008-11-11 2013-04-10 Salts of fingolimod

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08168862 2008-11-11
EP08168862.4 2008-11-11
PCT/EP2009/064889 WO2010055027A2 (en) 2008-11-11 2009-11-10 Organic compounds

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2013203470A Division AU2013203470A1 (en) 2008-11-11 2013-04-10 Salts of fingolimod

Publications (2)

Publication Number Publication Date
AU2009315735A1 AU2009315735A1 (en) 2010-05-20
AU2009315735B2 true AU2009315735B2 (en) 2013-01-10

Family

ID=42062355

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009315735A Ceased AU2009315735B2 (en) 2008-11-11 2009-11-10 Salts of fingolimod

Country Status (20)

Country Link
US (2) US8680146B2 (enExample)
EP (1) EP2358660A2 (enExample)
JP (2) JP2012508215A (enExample)
KR (1) KR20110086142A (enExample)
CN (2) CN102256933A (enExample)
AU (1) AU2009315735B2 (enExample)
BR (1) BRPI0921533A2 (enExample)
CA (1) CA2741974A1 (enExample)
CL (1) CL2011001041A1 (enExample)
CO (1) CO6382154A2 (enExample)
EC (1) ECSP11011121A (enExample)
IL (1) IL212073A0 (enExample)
MA (1) MA32877B1 (enExample)
MX (1) MX2011004924A (enExample)
NZ (1) NZ591999A (enExample)
PE (1) PE20120012A1 (enExample)
RU (1) RU2543621C2 (enExample)
TN (1) TN2011000187A1 (enExample)
WO (1) WO2010055027A2 (enExample)
ZA (1) ZA201102272B (enExample)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2336117A1 (en) 2005-05-26 2011-06-22 Neuron Systems, Inc Heterocyclic compounds for treating retinal diseases
JP2012508215A (ja) * 2008-11-11 2012-04-05 ノバルティス アーゲー 有機化合物
EP2456752A2 (en) * 2009-07-24 2012-05-30 ratiopharm GmbH Process for producing fingolimod salts
WO2011072141A1 (en) 2009-12-11 2011-06-16 Neuron Systems, Inc. Compositions and methods for the treatment of macular degeneration
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
JO3177B1 (ar) 2011-04-01 2018-03-08 Novartis Ag تركيبات تتالف من 2-أمينو-2- [ 2- ( 4- أكتيل فينيل ) إثيل ] بروبان - 3, 1- ديول
EP2505589A1 (en) 2011-04-01 2012-10-03 Johann Wolfgang Goethe-Universität Frankfurt am Main Novel sphingolipid heterocyclic compounds as modulators of sphingolipid signaling and uses thereof
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
CA2898631C (en) 2013-01-23 2023-06-13 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
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
US10022340B2 (en) 2013-10-11 2018-07-17 Teikoku Pharma Usa, Inc. Topical sphingosine-1-phosphate receptor agonist formulations and methods of using the same
US10675254B2 (en) 2013-10-11 2020-06-09 Teikoku Seiyaku Co., Ltd. Sphingosine-1-phosphate receptor agonist iontophoretic devices and methods of using the same
CN107530301A (zh) * 2015-01-20 2018-01-02 汉达医药有限责任公司 稳定的固体芬戈莫德剂型
US9925138B2 (en) 2015-01-20 2018-03-27 Handa Pharmaceuticals, Llc Stable solid fingolimod dosage forms
CN108135907A (zh) 2015-08-21 2018-06-08 奥尔德拉医疗公司 氘化化合物和其用途
US11129823B2 (en) 2016-05-09 2021-09-28 Aldeyra Therapeutics, Inc. Combination treatment of ocular inflammatory disorders and diseases
AU2017275209C1 (en) 2016-05-31 2020-01-23 Taiho Pharmaceutical Co., Ltd. Sulfonamide compound or salt thereof
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
MX2020003425A (es) 2017-10-10 2020-07-29 Aldeyra Therapeutics Inc Tratamiento de trastornos inflamatorios.
AU2018377036B2 (en) 2017-11-29 2022-04-14 Taiho Pharmaceutical Co., Ltd. Sulfonamide compounds and use thereof
BR112020026359A2 (pt) * 2018-06-29 2021-03-30 Forma Therapeutics, Inc. Sais de (s)-(5-ciclobutóxi-2-metil-6-(1-(piperidin-4-il)-1h-pirazol-4-il)-3,4-di-hidroquinolin-1(2h)-il)(ciclopropil)metanona e formas sólidas dos mesmos
EP3833660A4 (en) * 2018-08-06 2022-05-11 Aldeyra Therapeutics, Inc. POLYMORPHIC COMPOUNDS AND THEIR USES
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
CA3137301A1 (en) 2019-05-02 2020-11-05 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
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
WO2021231792A1 (en) 2020-05-13 2021-11-18 Aldeyra Therapeutics, Inc. Pharmaceutical formulations and uses thereof
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
WO2007143081A2 (en) * 2006-06-02 2007-12-13 The Ohio State University Research Foundation Therapeutic agents for the treatment of lymphoid malignancies

Family Cites Families (14)

* 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
ECSP951461A (es) 1995-06-07 1998-04-07 SINTESIS DE 3- {4-(2- AMINOETOXI) BENZOIL]-2-ARIL-6- HIDROXIBENZO {b] TIOFENOS (CASO X- 9295B)
ECSP972265A (es) 1997-09-23 1998-11-30 Dihidrato de d-olanzapina
FR2785607B1 (fr) 1998-11-09 2001-02-09 Rhodia Chimie Sa Procede de preparation de tris(ether-amine)
ATE288414T1 (de) * 1998-11-11 2005-02-15 Novartis Pharma Gmbh Herstellung von 2-amino-2(2-(4- alkylphenyl)äthyl)propan-1,3-diolen
JP4627356B2 (ja) * 1999-06-30 2011-02-09 昭 松森 ウイルス性心筋炎の予防または治療薬剤
NZ529044A (en) * 2001-06-08 2008-03-28 Novartis Ag Treatment or prophylaxis of insulin-producing cell graft 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
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
RU2008116578A (ru) * 2005-09-30 2009-11-10 Новартис АГ (CH) Применение ингибиторов dpp-iv для лечения аутоиммунных заболеваний и отторжения трансплантата
US7985586B2 (en) * 2008-02-04 2011-07-26 Georgia Health Sciences University Oligodendrocyte precursor cell composition and methods of use
JP2012508215A (ja) * 2008-11-11 2012-04-05 ノバルティス アーゲー 有機化合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007143081A2 (en) * 2006-06-02 2007-12-13 The Ohio State University Research Foundation Therapeutic agents for the treatment of lymphoid malignancies

Also Published As

Publication number Publication date
CN102256933A (zh) 2011-11-23
ZA201102272B (en) 2011-12-28
JP2012508215A (ja) 2012-04-05
US20110218248A1 (en) 2011-09-08
CL2011001041A1 (es) 2011-10-07
RU2011123365A (ru) 2012-12-20
TN2011000187A1 (en) 2012-12-17
WO2010055027A2 (en) 2010-05-20
AU2009315735A1 (en) 2010-05-20
RU2543621C2 (ru) 2015-03-10
MA32877B1 (fr) 2011-12-01
ECSP11011121A (es) 2011-07-29
CO6382154A2 (es) 2012-02-15
NZ591999A (en) 2013-06-28
US8680146B2 (en) 2014-03-25
BRPI0921533A2 (pt) 2016-01-12
US20140235722A1 (en) 2014-08-21
PE20120012A1 (es) 2012-02-02
CN105198760A (zh) 2015-12-30
KR20110086142A (ko) 2011-07-27
IL212073A0 (en) 2011-06-30
CA2741974A1 (en) 2010-05-20
WO2010055027A3 (en) 2010-08-19
MX2011004924A (es) 2011-05-30
EP2358660A2 (en) 2011-08-24
JP2015178503A (ja) 2015-10-08

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