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WO2008138968A4 - Dosage form comprising 10-[(3s)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10h-phenothiazine, provided in a form suitable for oral administration of a daily dose of 1 mg to 3 mg - Google Patents

Dosage form comprising 10-[(3s)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10h-phenothiazine, provided in a form suitable for oral administration of a daily dose of 1 mg to 3 mg Download PDF

Info

Publication number
WO2008138968A4
WO2008138968A4 PCT/EP2008/055971 EP2008055971W WO2008138968A4 WO 2008138968 A4 WO2008138968 A4 WO 2008138968A4 EP 2008055971 W EP2008055971 W EP 2008055971W WO 2008138968 A4 WO2008138968 A4 WO 2008138968A4
Authority
WO
WIPO (PCT)
Prior art keywords
dosage form
drug
azabicyclo
ylmethyl
oct
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
PCT/EP2008/055971
Other languages
French (fr)
Other versions
WO2008138968A2 (en
WO2008138968A3 (en
Inventor
Thierry Clerc
Alain Delarue
Christophe Przybylski
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.)
Pierre Fabre Medicament SA
Original Assignee
Pierre Fabre Medicament SA
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 Pierre Fabre Medicament SA filed Critical Pierre Fabre Medicament SA
Publication of WO2008138968A2 publication Critical patent/WO2008138968A2/en
Publication of WO2008138968A3 publication Critical patent/WO2008138968A3/en
Publication of WO2008138968A4 publication Critical patent/WO2008138968A4/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention relates to a dosage form comprising 10-[(3S)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine, or at least one pharmaceutically acceptable salt of same, characterized in that it provides in a suitable form for oral administration a daily dose of 1mg to 3 mg, and to the use of same to prepare a drug to prevent and/or treat allergic disorders, most notably allergic rhinitis.

Claims

AMENDED CLAIMS (received by the International Bureau on 15 May 2009)
1. A dosage form comprising a mixture of (R)- and (S) -enantioπiers of 10- [ 1-azabicyclo [2.2.2 ] oct-3- ylmethyl] -10#-phenothiazine containing between 95% and 100% by weight of the (S ) -enantiomer, preferably between 99% and 100% by weight of the (S) -enantiomer, or at least one pharmaceutically acceptable salt of same, characterized in that it provides in a suitable form for oral administration a daily dose of 1 mg to 3 mg.
2. The dosage form according to claim 1, characterized in that it provides in a suitable form for oral administration a daily dose of 1.5 mg to 2.5 mg .
3. The dosage form according to claim 1, characterized in that it is provided as a daily dosage unit comprising 1 mg to 3 mg of said mixture of enantiomers, or at least one pharmaceutically acceptable salt of same.
4. The dosage form according to claim 3, characterized in that said daily dosage unit comprises
1.5 mg to 2.5 mg of said mixture of enantiomers, or at least one pharmaceutically acceptable salt of same.
5. The dosage form according to any of the preceding claims, characterized in that it is provided in the form of a tablet, gelatin capsule, syrup, suspension or solution.
6. The dosage form according to any of the preceding claims, characterized in that said mixture of enantiomers of 10- [ 1-azabicyclo [2.2.2 ] oct-3-ylmethyl] - lOH-phenothiazine is essentially pure (S) -enantioraer .
7. Use of 10- [ (3S)-l-azabicyclo[2.2.2]oct-3- ylmethyl] -lOH-phenothiazine, or at least one pharmaceutically acceptable salt of same, to prepare a drug provided in a dosage form suitable for oral administration of a daily dose of 1 mg to 3 mg to prevent and/or treat allergic disorders.
8. Use according to claim 7, characterized in that said allergic disorders are allergic rhinitis.
9. Use according to claim 7, characterized in that said allergic disorders are allergic conjunctivitis.
10. Use according to any of claims 7 to 9, characterized in that said drug is provided in a dosage form suitable for oral administration of a daily dose of 1.5 mg to 2.5 mg.
11. Use according to any of claims 7 to 10, characterized in that said drug is provided as a daily dosage unit comprising 1 mg to 3 mg of 10- [ (3S)-I- azabicyclo [2.2.2] oct-3-ylmethyl] -10H- phenothiazine, or at least one pharmaceutically acceptable salt of same.
12. Use according to claim 9, characterized in that said drug is provided as a daily dosage unit comprising 1.5 mg to 2.5 mg of 10- [ (3S)-I- azabicyclo [2.2.2] oct-3-ylmethyl] -lOH-phenothiazine, or at least one pharmaceutically acceptable salt of same.
13. Use according to any of claims 7 to 12, characterized in that said drug is to prevent and/or treat dermatological symptoms caused by a release of histamine or by an abnormally high level of IgE, such as chronic idiopathic urticaria.
14. Use according to any of claims 7 to 13, characterized in that said drug minimizes the appearance of adverse effects, such as sedative effects .
15. Use according to any of claims 7 to 14, characterized in that said drug is used in combination with another active ingredient selected among antihistamines, lipoxygenase inhibitors, anti- inflammatories, inhibitors of pro-inflammatory cytokine release, leukotriene receptor antagonists, or compounds that control the release of mediators from mast cells, such as leukotrienes, prostaglandins, thromboxane A2 or platelet-activating factor.
PCT/EP2008/055971 2007-05-15 2008-05-15 Dosage form comprising 10-[(3s)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10h-phenothiazine, provided in a form suitable for oral administration of a daily dose of 1 mg to 3 mg Ceased WO2008138968A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0755075 2007-05-15
FR0755075A FR2916142A1 (en) 2007-05-15 2007-05-15 PHARMACEUTICAL FORM COMPRISING (10 - [(3S) -1-AZABICYCLO [2.2.2] OCT-3-YLMETHYL] -10H-PHENOTHIAZINE PRESENTING IN AN APPROPRIATE FORM FOR ADMINISTRATION OF A DAILY DOSE UNDER BETWEEN 1 AND 3 MG

Publications (3)

Publication Number Publication Date
WO2008138968A2 WO2008138968A2 (en) 2008-11-20
WO2008138968A3 WO2008138968A3 (en) 2009-05-22
WO2008138968A4 true WO2008138968A4 (en) 2009-07-02

Family

ID=38752476

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/055971 Ceased WO2008138968A2 (en) 2007-05-15 2008-05-15 Dosage form comprising 10-[(3s)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10h-phenothiazine, provided in a form suitable for oral administration of a daily dose of 1 mg to 3 mg

Country Status (4)

Country Link
AR (1) AR066587A1 (en)
FR (1) FR2916142A1 (en)
TW (1) TW200906417A (en)
WO (1) WO2008138968A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019099995A1 (en) * 2017-11-17 2019-05-23 Neurana Pharmaceuticals, Inc. Methods of administering tolperisone

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2522660A1 (en) * 1982-03-05 1983-09-09 Pharmuka Lab MEQUITAZINE LEVOGYER ISOMER, PROCESS FOR PREPARING THE SAME AND MEDICAMENTS CONTAINING THE SAME
JPH07188040A (en) * 1993-12-27 1995-07-25 Taisho Pharmaceut Co Ltd Composition for treating rhinitis
FR2772029B1 (en) * 1997-12-08 2000-02-25 Pf Medicament PROCESS FOR THE PREPARATION OF MEQUITAZINE AND NOVEL SYNTHESIS INTERMEDIATE
JP2000191536A (en) * 1998-10-20 2000-07-11 Taisho Pharmaceut Co Ltd Oral solid preparation containing mequitazine
WO2005037245A2 (en) * 2003-10-21 2005-04-28 Direct-Haler A/S A multiple route medication for the treatment of rhinitis and asthma
JP2006096749A (en) * 2004-08-31 2006-04-13 Takeda Chem Ind Ltd Medicine composition for common cold
FR2896690B1 (en) * 2006-01-30 2008-05-02 Pierre Fabre Medicament Sa USE OF MEQUITAZINE ENANTIOMER (S) FOR THE PREPARATION OF A MEDICINAL PRODUCT WHILE LIMITING GENOMIC TOXICITY

Also Published As

Publication number Publication date
AR066587A1 (en) 2009-09-02
TW200906417A (en) 2009-02-16
WO2008138968A2 (en) 2008-11-20
WO2008138968A3 (en) 2009-05-22
FR2916142A1 (en) 2008-11-21

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