WO1995022324A1 - Traitement des cephalees migraineuses et formulations - Google Patents

Traitement des cephalees migraineuses et formulations Download PDF

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Publication number
WO1995022324A1
WO1995022324A1 PCT/US1994/001741 US9401741W WO9522324A1 WO 1995022324 A1 WO1995022324 A1 WO 1995022324A1 US 9401741 W US9401741 W US 9401741W WO 9522324 A1 WO9522324 A1 WO 9522324A1
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
pharmaceutically acceptable
migraine headaches
compound
formulations
Prior art date
Application number
PCT/US1994/001741
Other languages
English (en)
Inventor
Walter Pinsker
Original Assignee
Walter Pinsker
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 Walter Pinsker filed Critical Walter Pinsker
Priority to US08/693,158 priority Critical patent/US5753712A/en
Priority to PCT/US1994/001741 priority patent/WO1995022324A1/fr
Publication of WO1995022324A1 publication Critical patent/WO1995022324A1/fr

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
    • A61K31/33—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone

Definitions

  • Bupropion hydrochloride is the generic name for m-chloro- ⁇ -t-butylaminoproxinphenone which is used under the trademark WELLBUTRIN® in the United States of America for the treatment of depressions.
  • WELLBUTRIN® the trademark of WELLBUTRIN® in the United States of America for the treatment of depressions.
  • the neurochemical mechanism of the antidepressant effect of bupropion is not known.
  • bupropion hydrochloride is effective in treating migraine headaches in humans. It is effective when administered alone or together with caffeine, e.g., with one or two cups of coffee.
  • the compound of formula (I) (the active ingredient) or the pharmaceutically acceptable acid addition salt thereof is preferably administered in unit dosage form to the human being treated.
  • a pharmaceutical composition containing a compound of formula (I), or a pharmaceutically acceptable salt thereof may be presented in discrete units such as tablets, capsules, ampules or suppositories, each containing an effective amount of the compound or salt for treatment of migraine.
  • the preferred unit dosage of a compound of formula (I) as the hydrochloride salt thereof for oral administration is about 10 mg to 450 mg, preferably 50 mg to 300 mg, and the most preferred unit dosage of 100 to 200 mg optionally given in divided doses. Treatment is preferably initiated at the first (prodromal) symptom of a migraine.
  • the compound of formula (I) may also be administered prophylactically, e.g., at a preferred dose of 100 mg per day, especially for patients suffering frequent migraines.
  • a compound of formula (I) or pharmaceutically acceptable salts thereof may be presented as an oral unit preparation (for example as a cachet, tablet or capsule) containing one or more pharmaceutically acceptable carriers which may take the form of solid diluents such as lactose, cornstarch, micronized silica gel as well as other excipients known in the art.
  • the pharmaceutical composition of this invention may include one or more of additional ingredients e.g., pharmaceutically acceptable carriers such as diluents, buffers, flavouring agents, binders, surface active agents, thickeners, lubricants, preservatives, and the like.
  • pharmaceutically acceptable carriers such as diluents, buffers, flavouring agents, binders, surface active agents, thickeners, lubricants, preservatives, and the like.
  • the formulations may be prepared by admixture of the ingredients, and, if necessary, shaping the resulting mass, and filling into suitable containers.
  • a preferred pharmaceutical formulation comprises bupropion hydrochloride (100 mg) and caffeine (200 mg) and a pharmaceutically acceptable carrier therefor.
  • the compound used in this invention is preferably presented for use as a pharmaceutically acceptable acid addition salt.
  • examples of some of the pharmaceutically acceptable salts which can be utilized are salts of the following acids: hydrochloric, sulfuric, phosphoric and toluenesulphonic.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un procédé de traitement des céphalées migraineuses. Il consiste à administrer, à l'individu en manifestant le besoin, le composé de la formule générale (1) ou l'un de ses sels d'addition d'acide pharmaceutiquement acceptables, en une dose non toxique et thérapeutiquement efficace (calculée comme dose de base).
PCT/US1994/001741 1994-02-18 1994-02-18 Traitement des cephalees migraineuses et formulations WO1995022324A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US08/693,158 US5753712A (en) 1994-02-18 1994-02-18 Treatment of migraine headaches and formulations
PCT/US1994/001741 WO1995022324A1 (fr) 1994-02-18 1994-02-18 Traitement des cephalees migraineuses et formulations

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1994/001741 WO1995022324A1 (fr) 1994-02-18 1994-02-18 Traitement des cephalees migraineuses et formulations

Publications (1)

Publication Number Publication Date
WO1995022324A1 true WO1995022324A1 (fr) 1995-08-24

Family

ID=22242285

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1994/001741 WO1995022324A1 (fr) 1994-02-18 1994-02-18 Traitement des cephalees migraineuses et formulations

Country Status (1)

Country Link
WO (1) WO1995022324A1 (fr)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6110973A (en) * 1998-01-29 2000-08-29 Sepracor Methods for treating obesity and weight gain using optically pure (-)-bupropion
US6280763B1 (en) 1999-05-10 2001-08-28 Pierce Management, Llc Apparatus and method for transdermal delivery of bupropion
US6337328B1 (en) 1999-03-01 2002-01-08 Sepracor, Inc. Bupropion metabolites and methods of use
US6342496B1 (en) 1999-03-01 2002-01-29 Sepracor Inc. Bupropion metabolites and methods of use
US6458374B1 (en) 1998-01-29 2002-10-01 Sepracor, Inc. Methods and compositions for treating chronic disorders using optically pure (+)-bupropion
US6734213B2 (en) 1999-01-20 2004-05-11 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US6855820B2 (en) 1999-01-20 2005-02-15 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US6998400B2 (en) 1998-01-22 2006-02-14 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US7098206B2 (en) 1998-01-21 2006-08-29 Smithkline Beecham Corporation Pharmaceutically active morpholinol

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3819706A (en) * 1969-12-04 1974-06-25 Burroughs Wellcome Co Meta chloro substituted-alpha-butylamino-propiophenones
US3885046A (en) * 1969-12-04 1975-05-20 Burroughs Wellcome Co Meta chloro or fluoro substituted alpha-T-butylaminopropionphenones in the treatment of depression

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3819706A (en) * 1969-12-04 1974-06-25 Burroughs Wellcome Co Meta chloro substituted-alpha-butylamino-propiophenones
US3885046A (en) * 1969-12-04 1975-05-20 Burroughs Wellcome Co Meta chloro or fluoro substituted alpha-T-butylaminopropionphenones in the treatment of depression

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7098206B2 (en) 1998-01-21 2006-08-29 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US6998400B2 (en) 1998-01-22 2006-02-14 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US6495605B2 (en) 1998-01-29 2002-12-17 Sepracor Inc. Methods and compositions for aiding in smoking cessation and for treating pain and other disorders using optically pure (+)-bupropion
US6277887B1 (en) 1998-01-29 2001-08-21 Sepracor, Inc. Methods for treating Parkinson's disease using optically pure (−)-bupropion
US6110973A (en) * 1998-01-29 2000-08-29 Sepracor Methods for treating obesity and weight gain using optically pure (-)-bupropion
US6369113B2 (en) 1998-01-29 2002-04-09 Sepracor, Inc. Method for treating depression using optically pure (−)-bupropion
US6451860B1 (en) 1998-01-29 2002-09-17 Sepracor, Inc. Methods for treating depression and other disorders using optically pure (−)-bupropion
US6458374B1 (en) 1998-01-29 2002-10-01 Sepracor, Inc. Methods and compositions for treating chronic disorders using optically pure (+)-bupropion
US6734213B2 (en) 1999-01-20 2004-05-11 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US6855820B2 (en) 1999-01-20 2005-02-15 Smithkline Beecham Corporation Pharmaceutically active morpholinol
US6342496B1 (en) 1999-03-01 2002-01-29 Sepracor Inc. Bupropion metabolites and methods of use
US6337328B1 (en) 1999-03-01 2002-01-08 Sepracor, Inc. Bupropion metabolites and methods of use
US6280763B1 (en) 1999-05-10 2001-08-28 Pierce Management, Llc Apparatus and method for transdermal delivery of bupropion

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