WO1999025350A1 - Traitement de la retinopathie diabetique - Google Patents

Traitement de la retinopathie diabetique Download PDF

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Publication number
WO1999025350A1
WO1999025350A1 PCT/US1998/021423 US9821423W WO9925350A1 WO 1999025350 A1 WO1999025350 A1 WO 1999025350A1 US 9821423 W US9821423 W US 9821423W WO 9925350 A1 WO9925350 A1 WO 9925350A1
Authority
WO
WIPO (PCT)
Prior art keywords
antagonist
glutamate
diabetic retinopathy
antagonists
nmda receptor
Prior art date
Application number
PCT/US1998/021423
Other languages
English (en)
Inventor
Louis Desantis, Jr.
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 AU97975/98A priority Critical patent/AU9797598A/en
Publication of WO1999025350A1 publication Critical patent/WO1999025350A1/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

  • This invention relates to the use of suitable antagonists of glutamate-induced excitotoxicity for the treatment of diabetic retinopathy, particularly that of the proliferative type.
  • Panretinal photocoagulation and the dietary and/or pharmacological control of hyperglycemia are the only methods currently in use to treat diabetic retinopathy. Nision loss is associated with the use of panretinal photocoagulation. Consequently, there is a need for new ways for treating diabetic retinopathy.
  • the present compositions and methods fill that need. Summary of the Invention
  • the present invention is directed to compositions and methods for treating diabetic retinopathy using an antagonist of the excitatory amino acid receptors involved in glutamate- induced excitotoxicity.
  • an antagonist of the excitatory amino acid receptors involved in glutamate- induced excitotoxicity hi particular, N-methyl-D-aspartate (NMD A) receptor antagonists and more particularly antagonists of the polyamine receptor are useful for treating diabetic retinopathy.
  • NMD A N-methyl-D-aspartate
  • Tliis invention provides a pharmacological method for preventing further damage to retinal ganglion cells resulting from diabetes and associated with glutamate-induced excitotoxicity. It is expected to be used instead of panretinal photocoagulation and thus avoid the near-term loss of vision that accompanies such photocoagulation.
  • the invention is a treatment for diabetic retinopathy, particularly of the proliferative type, comprising the local or systemic administration of a suitable antagonist of the excitatory amino acid receptors involved in glutamate-induced excitotoxicity.
  • the purpose is to prevent damage to retinal ganglion cells resulting from the excitotoxic effects produced by excessive glutamate found in the retinas of patients who have proliferative diabetic retinopathy.
  • a suitable glutamate antagonist is one which has the appropriate physicochemical properties to allow it to gain access to the site of action, i.e., the retina, following administration, either locally to the eye or systemically, of a pharmaceutically effective amount of such antagonist.
  • the glutamate antagonist can work directly or indirectly to prevent the sequence of cellular events that ensues from the action of glutamate upon excitatory amino acid receptors at which glutamate can act. Glutamate receptors are classified as NMDA and non-NMDA receptors.
  • Tliis invention includes antagonists that act on NMDA and non-NMDA receptors for glutamate.
  • Particularly preferred antagonists are those which act on the NMDA receptor- calcium channel complex.
  • Such antagonists may act by competing with glutamate at the receptor site, may act at one or all of several regulatory or modulatory sites associated with the NMDA receptor-calcium channel complex, or can inhibit one or more of the downstream effects that result from activation of the NMDA receptor-calcium channel complex. Examples include, but are not limited to, polyamine site antagonists, receptor antagonists (compete with NMDA), and channel blockers that operate uncompetitively to block the NMDA receptor channel. Polyamine site antagonists are particularly useful according to this invention. Examples of specific examples are set out in U.S. Patent No.
  • the antagonist be able to cross these barriers to reach the site of action.
  • the antagonist could be given intraocularly or periocularly by an acceptable method to deliver the antagonist to its site of action. All modes of delivery that result in placing the antagonist at its site of action are contemplated.
  • the antagonists useful in the present invention will be administered orally.
  • Daily dosage of these compounds will range between about 0.1 and about 500 milligrams (mg), preferably between about 5 and about 100 mg.
  • Local administration of these compounds will require a dosage range of between about 0.1 and about 50 mg, preferably between about 0.5 and about 5 mg.
  • An aqueous composition will generally contain between about 0.1 and about 10 percent by weight (wt%) of the active, preferably between about 1 and about 5 wt%.

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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention se rapporte à l'utilisation de compositions d'antagonistes de l'excitotoxicité induite par le glutamate, dans le traitement de la rétinopathie diabétique.
PCT/US1998/021423 1997-11-14 1998-10-09 Traitement de la retinopathie diabetique WO1999025350A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU97975/98A AU9797598A (en) 1997-11-14 1998-10-09 Treatment of diabetic retinopathy

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6569497P 1997-11-14 1997-11-14
US60/065,694 1997-11-14

Publications (1)

Publication Number Publication Date
WO1999025350A1 true WO1999025350A1 (fr) 1999-05-27

Family

ID=22064483

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/021423 WO1999025350A1 (fr) 1997-11-14 1998-10-09 Traitement de la retinopathie diabetique

Country Status (4)

Country Link
AR (1) AR013749A1 (fr)
AU (1) AU9797598A (fr)
WO (1) WO1999025350A1 (fr)
ZA (1) ZA989514B (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005058293A1 (fr) * 2003-12-12 2005-06-30 Allergan, Inc. Utilisation de memantine destinee au traitement de maladies retiniennes proliferatives
WO2006015075A1 (fr) * 2004-07-26 2006-02-09 Allergan, Inc. Techniques de traitement d'etats pathologiques ophtalmiques
WO2007084473A2 (fr) * 2006-01-17 2007-07-26 Allergan, Inc. Utilisation de mémantine et de brimonidine pour réduire les taux vitréo-rétiniens de protéines facteurs de croissance de l'endothélium vasculaire (vegf) chez des animaux
US20120329879A1 (en) * 2010-03-08 2012-12-27 The University Of Tennessee Research Foundation Beta-adrenergic receptor agonists and uses thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990006118A1 (fr) * 1988-12-05 1990-06-14 Houston Biotechnology Incorporated Utilisation therapeutique de dihydropyrimidones et de derives de benzazepine et de benzothiazepine dans le disfonctionnement du nerf optique ou retinien
US5521215A (en) * 1989-11-07 1996-05-28 Ramot University Authority For Applied Research And Industrial Development Ltd. NMDA-blocking pharmaceuticals
WO1997001339A1 (fr) * 1995-06-28 1997-01-16 Allergan Procede d'utilisation de (2-imidazolin-2-ylamino) quinoxalines pour traiter des lesions nerveuses oculaires
FR2738568A1 (fr) * 1995-09-08 1997-03-14 Synthelabo Derives de 4-(cycloalkyl)piperidines et 4-(cycloalkylalkyl) piperidines, leur preparation et leur application en therapeutique
WO1997038691A1 (fr) * 1996-04-17 1997-10-23 Sumitomo Pharmaceuticals Co., Ltd. Medicament pour neuropathie retinienne

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990006118A1 (fr) * 1988-12-05 1990-06-14 Houston Biotechnology Incorporated Utilisation therapeutique de dihydropyrimidones et de derives de benzazepine et de benzothiazepine dans le disfonctionnement du nerf optique ou retinien
US5521215A (en) * 1989-11-07 1996-05-28 Ramot University Authority For Applied Research And Industrial Development Ltd. NMDA-blocking pharmaceuticals
WO1997001339A1 (fr) * 1995-06-28 1997-01-16 Allergan Procede d'utilisation de (2-imidazolin-2-ylamino) quinoxalines pour traiter des lesions nerveuses oculaires
FR2738568A1 (fr) * 1995-09-08 1997-03-14 Synthelabo Derives de 4-(cycloalkyl)piperidines et 4-(cycloalkylalkyl) piperidines, leur preparation et leur application en therapeutique
WO1997038691A1 (fr) * 1996-04-17 1997-10-23 Sumitomo Pharmaceuticals Co., Ltd. Medicament pour neuropathie retinienne

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Section Ch Week 9802, Derwent World Patents Index; Class B02, AN 98-018014, XP002088198 *
KAPIN M A ET AL: "PROTECTIVE EFFECTS OF THE POLYAMINE ANTAGONIST, ELIPRODIL HYDROCHLORIDE IN RETINA SUBJECTED TO AN EXITOTOXIC-OR ISCHEMIC- INSULT", SOCIETY FOR NEUROSCIENCE ABSTRACTS, vol. 22, no. 1 - 03, 16 November 1996 (1996-11-16), pages 1279, XP000677227 *
LANGEVIN J. ET AL.: "Etude du tartrate d' ifenprodil dans le traitement des accidents vasculaires cérébraux aigus", OUEST MÉDICAL, vol. 29, 1976, pages 853 - 854, XP002088157 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005058293A1 (fr) * 2003-12-12 2005-06-30 Allergan, Inc. Utilisation de memantine destinee au traitement de maladies retiniennes proliferatives
WO2006015075A1 (fr) * 2004-07-26 2006-02-09 Allergan, Inc. Techniques de traitement d'etats pathologiques ophtalmiques
WO2007084473A2 (fr) * 2006-01-17 2007-07-26 Allergan, Inc. Utilisation de mémantine et de brimonidine pour réduire les taux vitréo-rétiniens de protéines facteurs de croissance de l'endothélium vasculaire (vegf) chez des animaux
WO2007084473A3 (fr) * 2006-01-17 2007-11-29 Allergan Inc Utilisation de mémantine et de brimonidine pour réduire les taux vitréo-rétiniens de protéines facteurs de croissance de l'endothélium vasculaire (vegf) chez des animaux
EP2380632A1 (fr) * 2006-01-17 2011-10-26 Allergan, Inc. Utilisation de antagonistes de NMDA pour réduire les taux vitréo-rétiniens de protéines facteurs de croissance de l'endothélium vasculaire (vegf) chez des animaux
US20120329879A1 (en) * 2010-03-08 2012-12-27 The University Of Tennessee Research Foundation Beta-adrenergic receptor agonists and uses thereof

Also Published As

Publication number Publication date
AU9797598A (en) 1999-06-07
AR013749A1 (es) 2001-01-10
ZA989514B (en) 1999-06-15

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