AU2009315735B2 - Salts of fingolimod - Google Patents

Salts of fingolimod Download PDF

Info

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
Authority
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
Other languages
English (en)
Other versions
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42062355&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2009315735(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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

Links

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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (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)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Pyridine Compounds (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
EP08168862.4 2008-11-11
EP08168862 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) CN105198760A (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
US7973025B2 (en) 2005-05-26 2011-07-05 Neuron Systems, Inc. Compositions and methods of treating retinal disease
CN105198760A (zh) * 2008-11-11 2015-12-30 诺华股份有限公司 芬戈莫德的盐
US8766005B2 (en) 2009-07-24 2014-07-01 Ratiopharm Gmbh Process for producing fingolimod salts
CA2782015C (en) 2009-12-11 2020-08-25 Neuron Systems, Inc. Topical ophthalmic 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
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
AR085749A1 (es) 2011-04-01 2013-10-23 Novartis Ag Formulaciones
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
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
WO2015053879A1 (en) 2013-10-11 2015-04-16 Teikoku Pharma Usa, Inc. Sphingosine-1-phosphate receptor agonist iontophoretic devices and methods of using the same
EP3054933A4 (en) 2013-10-11 2017-03-15 Teikoku Pharma USA, Inc. Topical sphingosine-1-phosphate receptor agonist formulations and methods of using the same
EP3247341A4 (en) * 2015-01-20 2018-12-19 Handa Pharmaceuticals, Llc Stable solid fingolimod dosage forms
US9925138B2 (en) 2015-01-20 2018-03-27 Handa Pharmaceuticals, Llc Stable solid fingolimod dosage forms
CA2996183A1 (en) 2015-08-21 2017-03-02 Aldeyra Therapeutics, Inc. Deuterated compounds and uses thereof
US11129823B2 (en) 2016-05-09 2021-09-28 Aldeyra Therapeutics, Inc. Combination treatment of ocular inflammatory disorders and diseases
EP3466934B1 (en) 2016-05-31 2024-03-27 Taiho Pharmaceutical Co., Ltd. Sulfonamide compounds or salt thereof as ribonucleotide reductase inhibitors for treating cancer
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
CN111356451A (zh) 2017-10-10 2020-06-30 奥尔德拉医疗公司 炎性病症的治疗
AU2018377036B2 (en) 2017-11-29 2022-04-14 Taiho Pharmaceutical Co., Ltd. Sulfonamide compounds and use thereof
US20210261528A1 (en) * 2018-06-29 2021-08-26 Forma Therapeutics, Inc. Salts of (s)-(5-cyclobutoxy-2-methyl-6-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)-3,4-dihydroquinolin-1(2h)-yl)(cyclopropyl)methanone and solid forms thereof
CN112714762A (zh) * 2018-08-06 2021-04-27 奥尔德拉医疗公司 多晶型化合物及其用途
WO2020223685A1 (en) 2019-05-02 2020-11-05 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
WO2020223717A1 (en) 2019-05-02 2020-11-05 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
KR20220093330A (ko) 2019-10-31 2022-07-05 이도르시아 파마슈티컬스 리미티드 Cxcr7 안타고니스트와 s1p1 수용체 조절인자의 조합
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
ATE172711T1 (de) 1992-10-21 1998-11-15 Yoshitomi Pharmaceutical 2-amino-1, 3- propandiolverbindung und immunosuppressium
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)
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
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
ATE424893T1 (de) * 2001-06-08 2009-03-15 Novartis Pharma Gmbh Behandlung und vorbeugung von insulin- produzierende zelltransplantatabstossung
BR0311173A (pt) * 2002-05-16 2005-03-15 Novartis Ag Uso de agentes de ligação do receptor de edg em câncer
GB0217152D0 (en) * 2002-07-24 2002-09-04 Novartis Ag Organic compounds
CN101797241B (zh) 2003-04-08 2013-03-27 诺瓦提斯公司 包含s1p受体激动剂和糖醇的固体药物组合物
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
JP2009510112A (ja) * 2005-09-30 2009-03-12 ノバルティス アクチエンゲゼルシャフト 有機化合物の組合せ剤
WO2009100116A1 (en) * 2008-02-04 2009-08-13 Medical College Of Georgia Research Institute Oligodendrocyte precursor cell composition and methods of use
CN105198760A (zh) * 2008-11-11 2015-12-30 诺华股份有限公司 芬戈莫德的盐

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

Similar Documents

Publication Publication Date Title
AU2009315735B2 (en) Salts of fingolimod
AU2009315736B2 (en) Crystalline forms of fingolimod HCL
EP3656765B1 (en) Salts or co-crystals of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol
SG181466A1 (en) Formulations, salts and polymorphs of transnorsertraline and uses thereof
AU2013203470A1 (en) Salts of fingolimod
AU2013100531A4 (en) Crystalline forms of fingolimod HCL

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired