EP1037620A1 - Utilisation du formoterol dans des medicaments destines au traitement des inflammations/allergies des voies aeriennes superieures - Google Patents

Utilisation du formoterol dans des medicaments destines au traitement des inflammations/allergies des voies aeriennes superieures

Info

Publication number
EP1037620A1
EP1037620A1 EP98963701A EP98963701A EP1037620A1 EP 1037620 A1 EP1037620 A1 EP 1037620A1 EP 98963701 A EP98963701 A EP 98963701A EP 98963701 A EP98963701 A EP 98963701A EP 1037620 A1 EP1037620 A1 EP 1037620A1
Authority
EP
European Patent Office
Prior art keywords
formoterol
active ingredient
inflammatory
allergic rhinitis
solvate
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.)
Withdrawn
Application number
EP98963701A
Other languages
German (de)
English (en)
Inventor
Carl Göran PERSSON
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.)
AstraZeneca AB
Original Assignee
AstraZeneca AB
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 AstraZeneca AB filed Critical AstraZeneca AB
Publication of EP1037620A1 publication Critical patent/EP1037620A1/fr
Withdrawn legal-status Critical Current

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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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

Definitions

  • the invention provides the use of formoterol in the treatment of inflammatory and allergic conditions in the upper airways of human beings.
  • Inflammatory and allergic conditions in the upper airways include conditions such as rhinitis, sinusitis and nasal polyps. Conditions such as these are conventionally treated by corticosteroid nasal sprays. The problem with using corticosteroids to treat these conditions is that it takes some time before they take effect.
  • US-A-4,975,466 to Ciba-Geigy relates to pharmaceutical preparations containing formo- terol or one of its pharmaceutically acceptable salts, especially its semifumarate, for treatment of inflammatory skin diseases.
  • the preparations are mainly used for topical, i.e. dermal, application, to the skin and/or mucous membrane, since formoterol is said to have a very pronounced antiphlogistic (dermally phlogistatic) topically anti-inflammatory, action. More specifically, the preparations are intended for external use on the outer skin, including the conjunctiva of the eyeball, the lips and the genital and anal region.
  • the present invention is directed to the use of formoterol, or pharmaceutically acceptable salts or solvates thereof for manufacturing medicaments suitable for use in the treatment of an inflammatory and or allergic condition in the upper airways of a human being.
  • the active ingredient is formoterol fumarate dihydrate.
  • an active ingredient which is formo- terol, a pharmaceutically acceptable salt or solvate of formoterol, or a solvate of such a salt in the manufacture of a medicament for use in the treatment of an inflammatory and/or allergic condition in the upper airways of a human being.
  • a method of treating a patient suffering from an inflammatory and/or allergic condition in the upper airways which comprises administering to the patient a therapeutically effective amount of the active ingredient, wherein the patient is a human being.
  • composition comp- rising the active ingredient in association with one or more pharmaceutically acceptable diluent, carrier or additive, which composition is for use in the treatment of an inflammatory and/or allergic condition in the upper airways of human beings.
  • Formoterol is an adrenoreceptor agonist which selectively stimulates ⁇ 2 -receptors, with the formula (N-[2-hydroxy-5-[l-hydroxy-2-[[2-(4-methoxyphenyl)-l-methyl-ethyl]-amino]- ethyl]-phenyl]-formamide. It has surprisingly been found to be effective in the treatment of inflammatory and allergic conditions in the upper airways of human beings. Inhaled formoterol has the advantage that it both acts rapidly, usually within minutes, and exerts a prolonged effect of up to 12 hours.
  • Suitable physiologically acceptable salts of formoterol include acid addition salts derived from inorganic and organic acids, for example the chloride, bromide, sulfate, phosphate, maleate, fumarate, tartrate, citrate, benzoate, 4-methoxybenzoate, 2- or 4-hydroxybenzoate, 4-chlorobenzoate, p-toluenesulfonate, methanesulfonate, ascorbate, acetate, succinate, lactate, glutarate, gluconate, tricarballylate, hydroxynaphthalene-carboxylate oroleate salts or solvates thereof.
  • the active ingredient is preferably formoterol fumarate, especially the dihydrate.
  • Formoterol pharmaceutically acceptable salts and solvates of formoterol, and solvates of such salts can be prepared by the methods described in US-A-5,434,304 to Astra and DE- A-2,305,092 to Yamanouchi.
  • the preferred daily dose of the active ingredient is from 5 to 250 nmol (preferably from 15 to 120 nmol).
  • the active ingredient is formoterol fumarate dihydrate the preferred daily dose is from 3 to 96 ⁇ g, more preferably from 3 to 48 ⁇ g and most preferably from 3 to 24 ⁇ g per day.
  • suitable unit doses include 3, 4.5, 6, 9 and 12 ⁇ g of formoterol fumarate dihydrate.
  • the invention provides a new and surprisingly effective treatment for inflammatory and/or allergic conditions in the upper airways of a human being.
  • the conditions treatable by the invention are preferably in the nose and paranasal sinus. They include
  • the active ingredient is used in admixture with one or more pharmaceutically acceptable additives, diluents or carriers, preferably in an amount of from 50 ⁇ g to 25 mg per dose, more preferably in an amount of from 50 ⁇ g to 10 mg, most preferably in an amount of from 100 to 4000 ⁇ g.
  • suitable diluents or carriers include lactose, dextran, mannitol and glucose.
  • lactose is used, especially as the monohydrate.
  • the active ingredient used in the invention is preferably in the form of a dry powder, more preferably a finely divided, e.g. amicronized, dry powder, e.g. having a mass median diameter of less than 10 ⁇ m, for example from 1 to 5 ⁇ m, most preferably an agglomerated micronized dry powder. Preferably at least 90% of the powder particles have a size below 15 ⁇ m.
  • the finely divided active ingredients may be in the form of an ordered mixture with one or more pharmaceutically acceptable additives, diluents or carriers.
  • An ordered mixture is the combination of a finely divided active ingre- dominant with coarse particles of a pharmaceutically acceptable additive, diluent and/or carrier.
  • the ingredients used in the invention can be obtained in these preferred forms using methods known to those skilled in the art.
  • EXAMPLE 1 10 parts of formoterol fumarate dihydrate was mixed with 990 parts of lactose mono- hydrate. The blend was micronized using a high pressure air jet mill and then conditioned using the process of EP-A-717616. The mixture was then spheronised using the process of EP-A-721331, divided into parts, each of which were filled into the storage compartment of a Turbuhaler fitted with a dosing disc such that it administered, when activated, a unit dose of 6 ⁇ g.

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention porte sur l'utilisation d'un ingrédient actif tel que le formotérol, un sel pharmaceutiquement acceptable ou un solvate de formotérol, ou un solvate d'un sel, dans la fabrication d'un médicament destiné à traiter les états inflammatoires et/ou allergiques des voies aériennes supérieures chez l'homme.
EP98963701A 1997-12-12 1998-12-10 Utilisation du formoterol dans des medicaments destines au traitement des inflammations/allergies des voies aeriennes superieures Withdrawn EP1037620A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE9704644 1997-12-12
SE9704644A SE9704644D0 (sv) 1997-12-12 1997-12-12 New use
PCT/SE1998/002278 WO1999030703A1 (fr) 1997-12-12 1998-12-10 Utilisation du formoterol dans des medicaments destines au traitement des inflammations/allergies des voies aeriennes superieures

Publications (1)

Publication Number Publication Date
EP1037620A1 true EP1037620A1 (fr) 2000-09-27

Family

ID=20409370

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98963701A Withdrawn EP1037620A1 (fr) 1997-12-12 1998-12-10 Utilisation du formoterol dans des medicaments destines au traitement des inflammations/allergies des voies aeriennes superieures

Country Status (5)

Country Link
EP (1) EP1037620A1 (fr)
JP (1) JP2002508319A (fr)
AU (1) AU1897199A (fr)
SE (1) SE9704644D0 (fr)
WO (1) WO1999030703A1 (fr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9903995D0 (sv) * 1999-11-03 1999-11-03 Astra Ab New combination
US6667344B2 (en) 2001-04-17 2003-12-23 Dey, L.P. Bronchodilating compositions and methods
US20030055026A1 (en) 2001-04-17 2003-03-20 Dey L.P. Formoterol/steroid bronchodilating compositions and methods of use thereof
KR20040081753A (ko) * 2002-02-01 2004-09-22 아스트라제네카 아베 흡입용 조성물
TW200510277A (en) 2003-05-27 2005-03-16 Theravance Inc Crystalline form of β2-adrenergic receptor agonist
TWI359675B (en) 2003-07-10 2012-03-11 Dey L P Bronchodilating β-agonist compositions
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
ES2306595B1 (es) 2007-02-09 2009-09-11 Laboratorios Almirall S.A. Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2.
ES2320961B1 (es) 2007-11-28 2010-03-17 Laboratorios Almirall, S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor adrenergico beta2.
EP2096105A1 (fr) 2008-02-28 2009-09-02 Laboratorios Almirall, S.A. Dérivés de 4-(2-amino-1-hydroxyethyl)phénol en tant qu'antagonistes du récepteur adrénergique b2
EP2228368A1 (fr) 2009-03-12 2010-09-15 Almirall, S.A. Procédé de fabrication de 5-(2-{[6-(2,2-difluoro-2-ph2nyl2thoxy)hexyl]amino}-1-hydroxy2thyl)-8-hydroxyquinolin-2(1h)-one
EP2386555A1 (fr) 2010-05-13 2011-11-16 Almirall, S.A. Nouveaux dérivés de cyclohéxylamine dotés d'activités agoniste bêta 2 adrénergique et antagoniste muscarinique m3
ITRM20110083U1 (it) 2010-05-13 2011-11-14 De La Cruz Jose Antonio Freire Piastra per la costruzione di carrelli per aeroplani
EP2578570A1 (fr) 2011-10-07 2013-04-10 Almirall, S.A. Nouveau procédé de fabrication de 5-(2-{[6-(2,2-difluoro-2-phényléthoxy)hexyl]amino}-1-hydroxyéthyl)-8-hydroxyquinolin-2(1h)-one via de nouveaux intermédiaires de synthèse
EP2592078A1 (fr) 2011-11-11 2013-05-15 Almirall, S.A. Nouveaux dérivés de cyclohéxylamine dotés d'activités agonistes bêta 2 adrénergique et antagoniste muscarinique M3
EP2592077A1 (fr) 2011-11-11 2013-05-15 Almirall, S.A. Nouveaux dérivés de cyclohéxylamine dotés d'activités agonistes bêta 2 adrénergique et antagoniste muscarinique M3
EP2641900A1 (fr) 2012-03-20 2013-09-25 Almirall, S.A. Nouvelles formes polymorphes de héminapadisylate de 5-(2-{[6-(2,2-difluoro-2-phényléthoxy) hexyl]amino}-1-(R)-hydroxyéthyl)-8-hydroxyquinolin-2(1h)-one en tant qu'agoniste du récepteur adrénergique ß2
MA38260B1 (fr) 2012-12-18 2018-04-30 Almirall Sa Nouveaux dérivés de cyclohexyl et quinuclidinyl carbamate ayant une activité d'agoniste adrénergique beta2 et une activité d'antagoniste muscarinique m3
TWI643853B (zh) 2013-02-27 2018-12-11 阿爾米雷爾有限公司 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類
TWI641373B (zh) 2013-07-25 2018-11-21 阿爾米雷爾有限公司 具有蕈毒鹼受體拮抗劑和β２腎上腺素受體促效劑二者之活性的２－胺基－１－羥乙基－８－羥基喹啉－２（１Ｈ）－酮衍生物之鹽
TW201517906A (zh) 2013-07-25 2015-05-16 Almirall Sa 含有ｍａｂａ化合物和皮質類固醇之組合
TW201617343A (zh) 2014-09-26 2016-05-16 阿爾米雷爾有限公司 具有β２腎上腺素促效劑及Ｍ３蕈毒拮抗劑活性之新穎雙環衍生物

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EE9700138A (et) * 1994-12-22 1997-12-15 Astra Aktiebolag Aerosoolravimvormid
US5668110A (en) * 1995-06-07 1997-09-16 Affymax Technologies N.V. Peptides and compounds that bind to the IL-5 receptor

Non-Patent Citations (1)

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See references of WO9930703A1 *

Also Published As

Publication number Publication date
JP2002508319A (ja) 2002-03-19
SE9704644D0 (sv) 1997-12-12
AU1897199A (en) 1999-07-05
WO1999030703A1 (fr) 1999-06-24

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