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WO1998056379A1 - Compositions et procedes de traitement des glaucomes - Google Patents

Compositions et procedes de traitement des glaucomes Download PDF

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Publication number
WO1998056379A1
WO1998056379A1 PCT/US1998/010779 US9810779W WO9856379A1 WO 1998056379 A1 WO1998056379 A1 WO 1998056379A1 US 9810779 W US9810779 W US 9810779W WO 9856379 A1 WO9856379 A1 WO 9856379A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
concentration
glaucoma
compositions
administered
Prior art date
Application number
PCT/US1998/010779
Other languages
English (en)
Inventor
Billie M. York
Original Assignee
Alcon Laboratories, Inc.
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 Alcon Laboratories, Inc. filed Critical Alcon Laboratories, Inc.
Priority to AU77998/98A priority Critical patent/AU7799898A/en
Publication of WO1998056379A1 publication Critical patent/WO1998056379A1/fr

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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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine

Definitions

  • the invention is directed to the use of a reversible cholinesterase inhibitor to lower and control the elevated intraocular pressure (IOP) associated with primary open angle glaucoma or ocular hypertension.
  • IOP intraocular pressure
  • the reversible cholinesterase inhibitor can also be used in closed angle glaucoma because it induces miosis which reduces angle crowding.
  • U.S. Patent No. 4,895,841 is directed to certain cyclic amine compounds and their pharmaceutical use, in particular, for the treatment of senile dementia.
  • the compounds are acetylcholinesterase inhibitors.
  • the patent discloses the compound, l-benzyl-4-[(5,6- dimethoxy-l-indanon-2yl)methyl]piperidine, also known as E 2020.
  • U.S. Patent No. 5,100,901 and European Patent Application Nos. 0 579 263 Al and 0 296 560 A2 also disclose the compound and are related applications. None of the patents or applications disclose the compounds for use in lowering elevated IOP or treating glaucoma or ocular hypertension.
  • Cholinesterase inhibitors have been used to lower IOP, for example, echothiophate iodide (Phospholine Iodide ® , Wyeth Ayerst) and demecarium bromide (Humorsol ® , Merck and Co., Inc.). Both of these compounds are strong, or long acting, cholinesterase inhibitors which, although effective in lowering IOP, cause significant side effects, such as miosis, nearsightedness, and brow ache.
  • echothiophate iodide Phospholine Iodide ® , Wyeth Ayerst
  • demecarium bromide Humorsol ® , Merck and Co., Inc.
  • the compound, l-benzyl-4-[(5,6-dimethoxy-l-indanon-2yl)methyl]piperidine is a reversible cholinesterase inhibitor and is effective in lowering IOP, but without the severe side effects associated with prior cholinesterase inhibitors.
  • This invention is directed to compositions of E2020 and its isomers and methods for its use in lowering and controlling the elevated IOP associated with glaucoma and ocular hypertension.
  • the present invention is directed to using l-benzyl-4-[(5,6-dimethoxy-l-indanon- 2yl)methyl]piperidine (E 2020), and its stereo and optical isomers, hereinafter "Compound,” to lower and control the elevated IOP associated with glaucoma or ocular hypertension.
  • E 2020 l-benzyl-4-[(5,6-dimethoxy-l-indanon- 2yl)methyl]piperidine
  • Compound stereo and optical isomers
  • the Compound can be administered systemically or topically to the eye, preferably topically in pharmaceutically acceptable formulations at concentrations from about 0.01 to 1.0 weight percent (wt.%), preferably .05 to 0.5 wt.%.
  • Ophthalmic solution formulations may be prepared by dissolving the Compound in a physiologically acceptable isotonic aqueous buffer. Further, the ophthalmic solution may include an ophthalmologically acceptable surfactant to assist in dissolving the Compound.
  • the ophthalmic solution may contain a thickener such as hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethyl-cellulose, methylcellulose, polyvinylpyrrolidone, or the like, to improve the retention of the formulation in the conjunctival sac.
  • a thickener such as hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethyl-cellulose, methylcellulose, polyvinylpyrrolidone, or the like.
  • the active ingredient is combined with a preservative in an appropriate vehicle, such as, mineral oil, liquid lanolin, or white petrolatum.
  • Sterile ophthalmic gel formulations may be prepared by suspending the active ingredient in a hydrophilic base prepared from the combination of, for example, carbopol-940, or the like, according to the published formulations for analogous ophthalmic preparations; preservatives and tonicity agents can be incorporated.
  • a formulation containing the Compound is administered to the eye of a person suffering from glaucoma or ocular hypertension 1-4 times per day according to the discretion of a skilled clinician.

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

L'invention concerne des compositions et des procédés permettant d'abaisser et de réguler l'hypertension oculaire.
PCT/US1998/010779 1997-06-11 1998-06-09 Compositions et procedes de traitement des glaucomes WO1998056379A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU77998/98A AU7799898A (en) 1997-06-11 1998-06-09 Compositions and methods for treating glaucoma

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4928997P 1997-06-11 1997-06-11
US60/049,289 1997-06-11

Publications (1)

Publication Number Publication Date
WO1998056379A1 true WO1998056379A1 (fr) 1998-12-17

Family

ID=21959054

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/010779 WO1998056379A1 (fr) 1997-06-11 1998-06-09 Compositions et procedes de traitement des glaucomes

Country Status (2)

Country Link
AU (1) AU7799898A (fr)
WO (1) WO1998056379A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002002526A1 (fr) * 2000-07-03 2002-01-10 Eisai Co., Ltd. Compositions pharmaceutiques servant a stabiliser la tension intraoculaire
JP2008013580A (ja) * 1999-07-06 2008-01-24 Naryx Pharma Inc 副鼻腔炎を処置するためのエアロゾル化された抗感染剤、抗炎症剤および鬱血除去剤

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, 1 January 1900, Columbus, Ohio, US; abstract no. 121-169, XP002913930 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008013580A (ja) * 1999-07-06 2008-01-24 Naryx Pharma Inc 副鼻腔炎を処置するためのエアロゾル化された抗感染剤、抗炎症剤および鬱血除去剤
WO2002002526A1 (fr) * 2000-07-03 2002-01-10 Eisai Co., Ltd. Compositions pharmaceutiques servant a stabiliser la tension intraoculaire

Also Published As

Publication number Publication date
AU7799898A (en) 1998-12-30

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