RU2543621C2 - Соли финголимода - Google Patents

Соли финголимода Download PDF

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Publication number
RU2543621C2
RU2543621C2 RU2011123365/04A RU2011123365A RU2543621C2 RU 2543621 C2 RU2543621 C2 RU 2543621C2 RU 2011123365/04 A RU2011123365/04 A RU 2011123365/04A RU 2011123365 A RU2011123365 A RU 2011123365A RU 2543621 C2 RU2543621 C2 RU 2543621C2
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Russia
Prior art keywords
salt
weak
fty720
theta
powder
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RU2011123365/04A
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English (en)
Russian (ru)
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RU2011123365A (ru
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МУТЦ Михаэль
ЙОРДИНЕ Гуидо
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Новартис Аг
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    • 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
    • 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
    • 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
    • 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

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  • 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)
RU2011123365/04A 2008-11-11 2009-11-10 Соли финголимода RU2543621C2 (ru)

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

Publications (2)

Publication Number Publication Date
RU2011123365A RU2011123365A (ru) 2012-12-20
RU2543621C2 true RU2543621C2 (ru) 2015-03-10

Family

ID=42062355

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2011123365/04A RU2543621C2 (ru) 2008-11-11 2009-11-10 Соли финголимода

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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US11634395B2 (en) 2016-05-31 2023-04-25 Taiho Pharmaceutial Co., Ltd. Sulfonamide compound or salt thereof
US12344588B2 (en) 2017-11-29 2025-07-01 Taiho Pharmaceutical Co., Ltd. Sulfonamide compounds and use thereof

Families Citing this family (25)

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AU2006249866B2 (en) 2005-05-26 2011-10-13 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
JP2012508215A (ja) * 2008-11-11 2012-04-05 ノバルティス アーゲー 有機化合物
KR20120032538A (ko) 2009-07-24 2012-04-05 라티오팜 게엠베하 핀골리모드 염의 제조 방법
CA2782015C (en) 2009-12-11 2020-08-25 Neuron Systems, Inc. Topical ophthalmic compositions and methods for the treatment of macular degeneration
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
AR085749A1 (es) 2011-04-01 2013-10-23 Novartis Ag Formulaciones
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
CN111135171B (zh) 2013-01-23 2023-09-08 奥尔德拉医疗公司 与毒性醛相关的疾病和治疗
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
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
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
WO2016118515A1 (en) 2015-01-20 2016-07-28 Handa Pharmaceuticals, Llc Stable solid fingolimod dosage forms
CN118724806A (zh) 2015-08-21 2024-10-01 奥尔德拉医疗公司 氘化化合物和其用途
CN109152774A (zh) 2016-05-09 2019-01-04 奥尔德拉医疗公司 眼部炎性病症和疾病的组合治疗
CN111356451A (zh) 2017-10-10 2020-06-30 奥尔德拉医疗公司 炎性病症的治疗
SG11202012787PA (en) * 2018-06-29 2021-01-28 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
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
CN113784954A (zh) 2019-05-02 2021-12-10 奥尔德拉医疗公司 多晶型化合物和其用途
CA3156298A1 (en) 2019-10-31 2021-05-06 Laetitia POUZOL Combination of a cxcr7 antagonist with an s1p1 receptor modulator
WO2021231792A1 (en) 2020-05-13 2021-11-18 Aldeyra Therapeutics, Inc. Pharmaceutical formulations and uses thereof
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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WO2007041368A2 (en) * 2005-09-30 2007-04-12 Novartis Ag Dpp iv inhibitor for use in the treatment of autoimmune diseases and graft rejection

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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)
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CA2707750A1 (en) 2003-04-08 2004-10-21 Novartis Ag Solid pharmaceutical compositions comprising a s1p receptor agonist and a sugar alcohol
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WO2003097028A1 (en) * 2002-05-16 2003-11-27 Novartis Ag Use of edg receptor binding agents in cancer
WO2007041368A2 (en) * 2005-09-30 2007-04-12 Novartis Ag Dpp iv inhibitor for use in the treatment of autoimmune diseases and graft rejection

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KIUCHI M; ET AL. Synthesis and Immunosuppressive Activity of 2-Substituted 2-Aminopropane-1,3-diols and 2-Aminoethanols , Journal of Medicinal Chemistry, 2000,Vol:43, Page(s):2946 - 2961 . *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11634395B2 (en) 2016-05-31 2023-04-25 Taiho Pharmaceutial 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
US12344588B2 (en) 2017-11-29 2025-07-01 Taiho Pharmaceutical Co., Ltd. Sulfonamide compounds and use thereof

Also Published As

Publication number Publication date
WO2010055027A2 (en) 2010-05-20
KR20110086142A (ko) 2011-07-27
CA2741974A1 (en) 2010-05-20
CN105198760A (zh) 2015-12-30
NZ591999A (en) 2013-06-28
JP2015178503A (ja) 2015-10-08
EP2358660A2 (en) 2011-08-24
WO2010055027A3 (en) 2010-08-19
CO6382154A2 (es) 2012-02-15
US8680146B2 (en) 2014-03-25
BRPI0921533A2 (pt) 2016-01-12
CL2011001041A1 (es) 2011-10-07
IL212073A0 (en) 2011-06-30
MX2011004924A (es) 2011-05-30
ECSP11011121A (es) 2011-07-29
MA32877B1 (fr) 2011-12-01
CN102256933A (zh) 2011-11-23
US20110218248A1 (en) 2011-09-08
US20140235722A1 (en) 2014-08-21
TN2011000187A1 (en) 2012-12-17
JP2012508215A (ja) 2012-04-05
PE20120012A1 (es) 2012-02-02
ZA201102272B (en) 2011-12-28
AU2009315735B2 (en) 2013-01-10
RU2011123365A (ru) 2012-12-20
AU2009315735A1 (en) 2010-05-20

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