CA2016089A1 - Salts of azelastine having improved solubility - Google Patents

Salts of azelastine having improved solubility

Info

Publication number
CA2016089A1
CA2016089A1 CA2016089A CA2016089A CA2016089A1 CA 2016089 A1 CA2016089 A1 CA 2016089A1 CA 2016089 A CA2016089 A CA 2016089A CA 2016089 A CA2016089 A CA 2016089A CA 2016089 A1 CA2016089 A1 CA 2016089A1
Authority
CA
Canada
Prior art keywords
azelastine
salts
improved solubility
acid
present
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.)
Granted
Application number
CA2016089A
Other languages
French (fr)
Other versions
CA2016089C (en
Inventor
Helmut Hettche
Wolfgang Morick
Reinhard Muckenschnabel
Gerhard Scheffler
Ilona Fleischhauer
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.)
Viatris Inc
Original Assignee
Individual
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
Application filed by Individual filed Critical Individual
Publication of CA2016089A1 publication Critical patent/CA2016089A1/en
Application granted granted Critical
Publication of CA2016089C publication Critical patent/CA2016089C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Cephalosporin Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention relates to salts of azelastine having improved solubility in water. The salts of the present invention are prepared by reacting azelastine with acetic acid, gluconic acid, lactic acid, or malic acid. The azelastine salts are effective in providing a cytoprotective effect.
CA002016089A 1989-05-05 1990-05-04 Salts of azelastine having improved solubility Expired - Lifetime CA2016089C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP3914859.9 1989-05-05
DE3914859 1989-05-05

Publications (2)

Publication Number Publication Date
CA2016089A1 true CA2016089A1 (en) 1990-11-05
CA2016089C CA2016089C (en) 1998-12-01

Family

ID=6380164

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002016089A Expired - Lifetime CA2016089C (en) 1989-05-05 1990-05-04 Salts of azelastine having improved solubility

Country Status (17)

Country Link
US (4) US5086050A (en)
EP (1) EP0396069B1 (en)
JP (1) JPH02295987A (en)
AT (1) ATE107643T1 (en)
AU (1) AU622022B2 (en)
CA (1) CA2016089C (en)
DD (1) DD294254A5 (en)
DE (2) DE59006184D1 (en)
DK (1) DK0396069T3 (en)
ES (1) ES2055216T3 (en)
FI (1) FI902244A0 (en)
HU (1) HU206110B (en)
IE (1) IE63662B1 (en)
NO (1) NO901985L (en)
NZ (1) NZ233546A (en)
PT (1) PT93946B (en)
YU (1) YU86390A (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5271946A (en) * 1988-04-20 1993-12-21 Asta Pharma Aktiengesellschaft Controlled release azelastine-containing pharmaceutical compositions
JPH04198180A (en) * 1990-11-28 1992-07-17 Eezai Kagaku Kk Production of benzylphthalazone derivative
US5296472A (en) * 1991-12-05 1994-03-22 Vyrex Corporation Methods for delipidation of skin and cerumen removal
JP4138910B2 (en) 1997-07-02 2008-08-27 帝國製薬株式会社 Transdermal preparation containing azelastine hydrochloride with good transdermal absorbability and low skin irritation
WO1999021565A1 (en) * 1997-10-24 1999-05-06 Cornell Research Foundation, Inc. Nutritional supplement for cerebral metabolic insufficiencies
FI982733A (en) * 1998-12-17 2000-06-18 Orion Yhtymae Oyj Soluble compositions of triphenylethylene estrogens
FI109332B (en) 1998-12-17 2002-07-15 Orion Yhtymae Oyj Soluble compositions of toremifene
GB2389530B (en) 2002-06-14 2007-01-10 Cipla Ltd Pharmaceutical compositions
US7694694B2 (en) * 2004-05-10 2010-04-13 The Aerospace Corporation Phase-change valve apparatuses
US8758816B2 (en) * 2004-11-24 2014-06-24 Meda Pharmaceuticals Inc. Compositions comprising azelastine and methods of use thereof
PT2522365T (en) 2004-11-24 2017-02-08 Meda Pharmaceuticals Inc Compositions comprising azelastine and methods of use thereof
US20070020330A1 (en) 2004-11-24 2007-01-25 Medpointe Healthcare Inc. Compositions comprising azelastine and methods of use thereof
EP2697662B1 (en) 2011-04-13 2018-06-06 Codexis, Inc. Biocatalytic process for preparing eslicarbazepine and analogs thereof
US10898493B2 (en) 2019-04-12 2021-01-26 LA PharmaTech Inc. Pharmaceutical compositions and methods for psychiatric symptoms of patients with Alzheimer's disease
US10966989B2 (en) 2019-04-12 2021-04-06 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating mental, behavioral, cognitive disorders
US10639314B1 (en) 2019-04-30 2020-05-05 LA PharmaTech Inc. Method of treating Alzheimer's disease
US11938139B2 (en) 2019-04-12 2024-03-26 LA PharmaTech Inc. Pharmaceutical compositions and methods for anxiety, depression and other psychiatric disorders
US11690849B2 (en) 2019-04-12 2023-07-04 LA PharmaTech Inc. Method of treating dementia
US11389458B2 (en) 2019-04-12 2022-07-19 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating parkinson's and huntington's disease
US11318144B2 (en) 2019-04-12 2022-05-03 LA PharmaTech Inc. Compositions and methods for treating Alzheimer's disease and Parkinson's disease
US11744833B2 (en) 2019-04-12 2023-09-05 LA PharmaTech Inc. Pharmaceutical compositions and methods for treatment of insomnia
US11351179B1 (en) 2021-08-05 2022-06-07 LA PharmaTech Inc. Pharmaceutical compositions and methods for treatment of psychiatric disorders

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH572914A5 (en) * 1971-01-22 1976-02-27 Asta Werke Ag Chem Fab
US3813384A (en) * 1972-01-17 1974-05-28 Asta Werke Ag Chem Fab Basically substituted benzyl phthalazone derivatives,acid salts thereof and process for the production thereof
DE3575135D1 (en) * 1984-09-14 1990-02-08 Asta Pharma Ag SUBSTITUTED BENZYLPHTHALAZINONE DERIVATIVES.
ATE60598T1 (en) * 1985-11-11 1991-02-15 Asta Pharma Ag 4-BENZYL-1-(2H)-PHTHALAZINONE DERIVATIVES.
JPH0667844B2 (en) * 1987-03-06 1994-08-31 エーザイ株式会社 Treatment / prevention agent for ischemic heart disease
EP0289939A1 (en) * 1987-05-08 1988-11-09 ASTA Pharma AG 4-Benzyl-1-(2H)-phthalazinone-derivatives with an aminoacid residue
DE3850044D1 (en) * 1987-11-13 1994-07-14 Asta Medica Ag Azelastine embonate, process for its preparation and pharmaceutical preparations containing azelastine embonate as active ingredient.
US5232919A (en) * 1987-11-13 1993-08-03 Asta Pharma Aktiengesellschaft Azelastine embonate and compositions which contain it
IE64051B1 (en) * 1987-11-13 1995-06-28 Asta Medica Ag Azelastine embonate process for its preparation and pharmaceutical preparations which contain azelastine embonate as active substance
JP2794021B2 (en) * 1988-11-02 1998-09-03 エーザイ株式会社 Transdermal preparation containing azelastine or its salts

Also Published As

Publication number Publication date
YU86390A (en) 1992-05-28
JPH02295987A (en) 1990-12-06
DD294254A5 (en) 1991-09-26
FI902244A0 (en) 1990-05-04
HUT53901A (en) 1990-12-28
ATE107643T1 (en) 1994-07-15
DE4013696A1 (en) 1990-11-08
HU902678D0 (en) 1990-09-28
US5859003A (en) 1999-01-12
US5086050A (en) 1992-02-04
EP0396069A1 (en) 1990-11-07
US5998403A (en) 1999-12-07
NO901985L (en) 1990-11-06
AU5473690A (en) 1990-11-08
DK0396069T3 (en) 1994-07-25
AU622022B2 (en) 1992-03-26
NO901985D0 (en) 1990-05-04
DE59006184D1 (en) 1994-07-28
ES2055216T3 (en) 1994-08-16
US6017909A (en) 2000-01-25
EP0396069B1 (en) 1994-06-22
PT93946B (en) 1996-11-29
IE63662B1 (en) 1995-05-31
CA2016089C (en) 1998-12-01
IE901639L (en) 1990-11-05
PT93946A (en) 1991-01-08
NZ233546A (en) 1991-09-25
HU206110B (en) 1992-08-28

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Legal Events

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EEER Examination request
MKEX Expiry