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WO1993023035A2 - Emploi de derives d'indolone dans le traitement de troubles de la memoire, du dysfonctionnement sexuel et de la maladie de parkinson - Google Patents

Emploi de derives d'indolone dans le traitement de troubles de la memoire, du dysfonctionnement sexuel et de la maladie de parkinson Download PDF

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Publication number
WO1993023035A2
WO1993023035A2 PCT/EP1993/001099 EP9301099W WO9323035A2 WO 1993023035 A2 WO1993023035 A2 WO 1993023035A2 EP 9301099 W EP9301099 W EP 9301099W WO 9323035 A2 WO9323035 A2 WO 9323035A2
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
memory disorders
parkinson
disease
sexual dysfunction
Prior art date
Application number
PCT/EP1993/001099
Other languages
English (en)
Other versions
WO1993023035A3 (fr
Inventor
Robin Bradshaw Fears
Original Assignee
Smithkline Beecham Plc
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
Priority claimed from GB929210576A external-priority patent/GB9210576D0/en
Priority claimed from GB929210594A external-priority patent/GB9210594D0/en
Priority claimed from GB929210595A external-priority patent/GB9210595D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Priority to JP5519830A priority Critical patent/JPH07506823A/ja
Priority to EP93912699A priority patent/EP0641202A1/fr
Publication of WO1993023035A2 publication Critical patent/WO1993023035A2/fr
Publication of WO1993023035A3 publication Critical patent/WO1993023035A3/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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Definitions

  • the present invention relates to the use of selective dopamine D3 receptor agonists in therapy, for example in the treatment of memory disorders.
  • the present invention resides in the identification of such a utility and, in a first aspect, provides selective dopamine D3 receptor agonists for use in therapy.
  • the present invention relates to selective dopamine D3 receptor agonists for use in the treatment or prophylaxis of diseases in which agonism of the D3 receptors will prove advantageous, for example, in the treatment of memory disorders, sexual dysfunction and Parkinson's disease.
  • Particular selective dopamine D3 receptor agonists include, for example, compounds of the structure (I) :
  • each group R is the same or different and is hydrogen or
  • R 1 and R ⁇ are the same or different and are each hydrogen or C ⁇ _4alkyl; and n is 1 to 3, or a pharmaceutically acceptable salt thereof.
  • the compound ropinirole and other compounds of structure (I) are known in the art, for example as having utility in the treatment of Parkinson's disease (EP 0299602-A) .
  • the compounds of structure (I) and, in particular, ropinirole can be prepared according to the procedures described in EP 113964-B.
  • Selective dopamine D3 receptor agonists are of use in therapy, in particular in the treatment of memory disorders, for example, in the treatment of impaired cerebral functionality, as well as dementia, amnesia and decreased cognitive capacity; in the treatment of sexual dysfunction in both males and females, in particular in the treatment of male and female impotence; and in the treatment of Parkinson's disease.
  • the compounds of structure (I) are formulated into a standard pharmaceutical composition, for example as described in EP 113964-B and EP 0299602-A.
  • each dosage unit for oral administration contains preferably from 1 to 50 mg (and for parenteral administration contains preferably from 0.1 to 15 mg) of a compound of the formula (I) or a pharmaceutically acceptable salt thereof calculated as the free base.
  • the daily dosage regimen for an adult patient may be, for example, an oral dose of between 1 mg and 100 mg, preferably between 1 mg and 50 mg, or an intravenous, subcutaneous, or
  • -y intramuscular dose of between 0.1 mg and 50 mg, preferably 5 between 0.1 mg and 15 mg, of the compound of the formula (I) or a pharmaceutically acceptable salt thereof calculated as the free base, the compound being administered 1 to 4 times per day.
  • the compounds will be administered for a period of continuous therapy.
  • the membrane pellet was resuspended in ice-cold 50 mM Tris salts (pH 7.4 @ 37°C) , using an Ultra-Turrax, and recentrifuged at 18,000 - A - r.p.m for 15 in at 4°C in a Sorvall RC5C.
  • the membranes were washed two more times with ice-cold 50 mM Tris salts (pH 7.4 ⁇ a 37°C) .
  • the final pellet was resuspended in 50 mM Tris salts (pH 7.4 @ 37°C) , and the protein content determined using bovine serum albumin as a standard (Bradford, M. M. (1976) Anal. Biochem. 72, 248-254) .
  • the binding data revealed the existence of two binding sites in both human D 2 and D3 receptors.

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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Agonistes de récepteurs de dopamine D3 sélectifs et leur utilisation en thérapie, inter alia, dans le traitement de troubles de la mémoire.
PCT/EP1993/001099 1992-05-18 1993-05-04 Emploi de derives d'indolone dans le traitement de troubles de la memoire, du dysfonctionnement sexuel et de la maladie de parkinson WO1993023035A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP5519830A JPH07506823A (ja) 1992-05-18 1993-05-04 記憶障害，性的機能不全およびパーキンソン氏病の治療のためのインドロン誘導体の使用
EP93912699A EP0641202A1 (fr) 1992-05-18 1993-05-04 Emploi de derives d'indolone dans le traitement de troubles de la memoire, du dysfonctionnement sexuel et de la maladie de parkinson

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB9210576.6 1992-05-18
GB929210576A GB9210576D0 (en) 1992-05-18 1992-05-18 Medical use
GB9210595.6 1992-05-18
GB929210594A GB9210594D0 (en) 1992-05-18 1992-05-18 Medical use
GB9210594.9 1992-05-18
GB929210595A GB9210595D0 (en) 1992-05-18 1992-05-18 Medical use

Publications (2)

Publication Number Publication Date
WO1993023035A2 true WO1993023035A2 (fr) 1993-11-25
WO1993023035A3 WO1993023035A3 (fr) 1994-03-03

Family

ID=27266192

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1993/001099 WO1993023035A2 (fr) 1992-05-18 1993-05-04 Emploi de derives d'indolone dans le traitement de troubles de la memoire, du dysfonctionnement sexuel et de la maladie de parkinson

Country Status (4)

Country Link
EP (1) EP0641202A1 (fr)
JP (1) JPH07506823A (fr)
AU (1) AU4312593A (fr)
WO (1) WO1993023035A2 (fr)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997011696A1 (fr) * 1995-09-29 1997-04-03 Cygnus, Inc. Administration transdermique de ropinirole et de ses analogues
WO1998008819A1 (fr) * 1996-08-27 1998-03-05 American Home Products Corporation Derives de 4-aminoethoxy indolone
WO1999052870A1 (fr) * 1998-04-13 1999-10-21 American Home Products Corporation 4-amino-(ethylamino)-oxindoles utilises comme agonistes des autorecepteurs de la dopamine
WO1999066909A3 (fr) * 1998-06-22 2000-06-29 Queen's University At Kingston Procede et compositions pour le traitement ou l'amelioration des dysfonctionnements sexuels de la femme
WO2000023056A3 (fr) * 1998-10-20 2000-08-24 Univ Mcgill Utilisation d'agents dopaminergiques dans la gestion des dysfonctionnements sexuels
US6395744B1 (en) 1994-04-22 2002-05-28 Queen's University At Kingston Method and compositions for the treatment or amelioration of female sexual dysfunction
EP0779284B1 (fr) * 1995-12-11 2002-07-10 Institut National De La Sante Et De La Recherche Medicale (Inserm) Nouveaux dérivés de 2-naphthamides et leurs applications thérapeutiques comme agonistes des récepteurs D3
WO2005116027A3 (fr) * 2004-05-26 2006-04-13 Pfizer Limted Nouveaux derives indazole et indolone et leur utilisation pharmaceutique
EP1056419A4 (fr) * 1998-01-30 2007-05-02 Pentech Pharmaceuticals Inc Traitement de la dysfonction sexuelle chez la femme
US7927624B2 (en) 2000-04-14 2011-04-19 Jagotec Ag Hydrophilic/lipophilic polymeric matrix dosage formulation
WO2012021629A2 (fr) 2010-08-11 2012-02-16 Philadelphia Health & Education Corporation Nouveaux agonistes du récepteur dopaminergique d3 pour traiter la dyskinésie dans la maladie de parkinson
US8604076B2 (en) 2000-08-24 2013-12-10 Ucb Pharma Gmbh Method for producing a pharmaceutical composition comprising rotigotine
US8609641B2 (en) 2003-12-18 2013-12-17 Ucb Pharma Gmbh (S)-2-N-propylamino-5-hydroxytetralin as a D3-agonist
US9861594B2 (en) 2013-10-28 2018-01-09 Drexel University Treatments for attention and cognitive disorders, and for dementia associated with a neurodegenerative disorder

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10041478A1 (de) 2000-08-24 2002-03-14 Sanol Arznei Schwarz Gmbh Neue pharmazeutische Zusammensetzung

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4452808A (en) * 1982-12-07 1984-06-05 Smithkline Beckman Corporation 4-Aminoalkyl-2(3H)-indolones
GB8712073D0 (en) * 1987-05-21 1987-06-24 Smith Kline French Lab Medicament
FR2663638B2 (fr) * 1990-04-06 1995-02-10 Institut Nal Sante Recherc Medic Polypeptides ayant une activite de recepteur dopaminergique, acides nucleiques codant pour ces polypeptides et utilisation de ces polypeptides pour le criblage de substances actives sur ces polypeptides.
GB9015095D0 (en) * 1990-07-09 1990-08-29 Smith Kline French Lab Therapeutic method

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6395744B1 (en) 1994-04-22 2002-05-28 Queen's University At Kingston Method and compositions for the treatment or amelioration of female sexual dysfunction
US6756407B2 (en) 1994-04-22 2004-06-29 Queen's University At Kingston Method and compositions for the treatment or amelioration of female sexual dysfunction
WO1997011696A1 (fr) * 1995-09-29 1997-04-03 Cygnus, Inc. Administration transdermique de ropinirole et de ses analogues
EP0779284B1 (fr) * 1995-12-11 2002-07-10 Institut National De La Sante Et De La Recherche Medicale (Inserm) Nouveaux dérivés de 2-naphthamides et leurs applications thérapeutiques comme agonistes des récepteurs D3
WO1998008819A1 (fr) * 1996-08-27 1998-03-05 American Home Products Corporation Derives de 4-aminoethoxy indolone
EP1056419A4 (fr) * 1998-01-30 2007-05-02 Pentech Pharmaceuticals Inc Traitement de la dysfonction sexuelle chez la femme
WO1999052870A1 (fr) * 1998-04-13 1999-10-21 American Home Products Corporation 4-amino-(ethylamino)-oxindoles utilises comme agonistes des autorecepteurs de la dopamine
WO1999066909A3 (fr) * 1998-06-22 2000-06-29 Queen's University At Kingston Procede et compositions pour le traitement ou l'amelioration des dysfonctionnements sexuels de la femme
WO2000023056A3 (fr) * 1998-10-20 2000-08-24 Univ Mcgill Utilisation d'agents dopaminergiques dans la gestion des dysfonctionnements sexuels
EP3175848A1 (fr) 2000-04-14 2017-06-07 Jagotec AG Comprimé à libération contrôlée multicouche comprenant une couche active et une ou plusieurs couches barrières
US7927624B2 (en) 2000-04-14 2011-04-19 Jagotec Ag Hydrophilic/lipophilic polymeric matrix dosage formulation
EP2343060A1 (fr) 2000-04-14 2011-07-13 Jagotec AG Comprimés à plusieurs couches et à une liberation controlée, qui contiennent une couche active et une ou plusieurs couches de barrière
US8303986B2 (en) 2000-04-14 2012-11-06 Jagotec Ag Hydrophilic/lipophilic polymeric matrix dosage formulation
US8460706B2 (en) 2000-04-14 2013-06-11 Jagotec Ag Hydrophilic/lipophilic polymeric matrix dosage formulation
US8604076B2 (en) 2000-08-24 2013-12-10 Ucb Pharma Gmbh Method for producing a pharmaceutical composition comprising rotigotine
US9108900B2 (en) 2003-12-18 2015-08-18 Ucb Pharma Gmbh Method of treating diseases that respond to therapy by dopamine or dopamine agonists
US8609641B2 (en) 2003-12-18 2013-12-17 Ucb Pharma Gmbh (S)-2-N-propylamino-5-hydroxytetralin as a D3-agonist
WO2005116027A3 (fr) * 2004-05-26 2006-04-13 Pfizer Limted Nouveaux derives indazole et indolone et leur utilisation pharmaceutique
EP2603215A4 (fr) * 2010-08-11 2015-08-05 Philadelphia Health & Educatio Nouveaux agonistes du recepteur dopaminergique d3 pour traiter la dyskinesie dans la maladie de parkinson
WO2012021629A2 (fr) 2010-08-11 2012-02-16 Philadelphia Health & Education Corporation Nouveaux agonistes du récepteur dopaminergique d3 pour traiter la dyskinésie dans la maladie de parkinson
US9289400B2 (en) 2010-08-11 2016-03-22 Drexel University D3 dopamine receptor agonists to treat dyskinesia in parkinson's disease
US9675565B2 (en) 2010-08-11 2017-06-13 Drexel University D3 dopamine receptor agonists to treat dyskinesia in parkinson's disease
US10543180B2 (en) 2010-08-11 2020-01-28 Drexel University D3 dopamine receptor agonists to treat dyskinesia in Parkinson's disease
US11266612B2 (en) 2010-08-11 2022-03-08 Drexel University D3 dopamine receptor agonists to treat dyskinesia in Parkinson's disease
US9861594B2 (en) 2013-10-28 2018-01-09 Drexel University Treatments for attention and cognitive disorders, and for dementia associated with a neurodegenerative disorder
US10695302B2 (en) 2013-10-28 2020-06-30 Drexel University Treatments for attention and cognitive disorders, and for dementia associated with a neurodegenerative disorder
US11744810B2 (en) 2013-10-28 2023-09-05 Drexel University Methods of treating or preventing an attention disorder, cognitive disorder, and/or dementia associated with a neurodegenerative disorder

Also Published As

Publication number Publication date
JPH07506823A (ja) 1995-07-27
EP0641202A1 (fr) 1995-03-08
WO1993023035A3 (fr) 1994-03-03
AU4312593A (en) 1993-12-13

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