EP0641202A1 - 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

Info

Publication number
EP0641202A1
EP0641202A1 EP93912699A EP93912699A EP0641202A1 EP 0641202 A1 EP0641202 A1 EP 0641202A1 EP 93912699 A EP93912699 A EP 93912699A EP 93912699 A EP93912699 A EP 93912699A EP 0641202 A1 EP0641202 A1 EP 0641202A1
Authority
EP
European Patent Office
Prior art keywords
treatment
memory disorders
parkinson
disease
sexual dysfunction
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.)
Withdrawn
Application number
EP93912699A
Other languages
German (de)
English (en)
Inventor
Robin Bradshaw Smithkline Beecham Pharm. Fears
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.)
SmithKline Beecham Ltd
Original Assignee
SmithKline Beecham Ltd
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 GB929210594A external-priority patent/GB9210594D0/en
Priority claimed from GB929210576A external-priority patent/GB9210576D0/en
Priority claimed from GB929210595A external-priority patent/GB9210595D0/en
Application filed by SmithKline Beecham Ltd filed Critical SmithKline Beecham Ltd
Publication of EP0641202A1 publication Critical patent/EP0641202A1/fr
Withdrawn legal-status Critical Current

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
    • A61K31/40—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.

Landscapes

  • 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.
EP93912699A 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 Withdrawn EP0641202A1 (fr)

Applications Claiming Priority (7)

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

Publications (1)

Publication Number Publication Date
EP0641202A1 true EP0641202A1 (fr) 1995-03-08

Family

ID=27266192

Family Applications (1)

Application Number Title Priority Date Filing Date
EP93912699A Withdrawn 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

Country Status (4)

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

Families Citing this family (15)

* 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
US5807570A (en) * 1995-09-29 1998-09-15 Cygnus, Inc. Transdermal administration of ropinirole and analogs thereof
FR2742149B1 (fr) * 1995-12-11 1998-02-13 Inst Nat Sante Rech Med Nouveaux derives de 2-naphtamides et leurs applications therapeutiques
ATE218548T1 (de) * 1996-08-27 2002-06-15 American Home Prod 4-aminoethoxy-indolon-derivate
US5945117A (en) * 1998-01-30 1999-08-31 Pentech Pharmaceuticals, Inc. Treatment of female sexual dysfunction
EP1073636A1 (fr) * 1998-04-13 2001-02-07 American Home Products Corporation 4-amino-(ethylamino)-oxindoles utilises comme agonistes des autorecepteurs de la dopamine
EP1089736A2 (fr) * 1998-06-22 2001-04-11 Queen's University At Kingston Procede et compositions pour le traitement ou l'amelioration des dysfonctionnements sexuels de la femme
CA2251255A1 (fr) * 1998-10-20 2000-04-20 Mcgill University L'utilisation d'agents dopaminergique dans le gestion de dysfonctionnement sexuel
AR030557A1 (es) 2000-04-14 2003-08-27 Jagotec Ag Una tableta en multicapa de liberacion controlada y metodo de tratamiento
DE10041479A1 (de) 2000-08-24 2002-03-14 Sanol Arznei Schwarz Gmbh Neue pharmazeutische Zusammensetzung zur Verabreichung von N-0923
DE10041478A1 (de) 2000-08-24 2002-03-14 Sanol Arznei Schwarz Gmbh Neue pharmazeutische Zusammensetzung
DE10359528A1 (de) 2003-12-18 2005-07-28 Schwarz Pharma Ag (S)-2-N-Propylamino-5-hydroxytetralin als D3-agonistisches Therapeutikum
AU2005247696A1 (en) * 2004-05-26 2005-12-08 Pfizer, Inc. Indazole and indolone derivatives and their use as pharmaceuticals
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
US9861594B2 (en) 2013-10-28 2018-01-09 Drexel University Treatments for attention and cognitive disorders, and for dementia associated with a neurodegenerative disorder

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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9323035A2 *

Also Published As

Publication number Publication date
JPH07506823A (ja) 1995-07-27
WO1993023035A3 (fr) 1994-03-03
WO1993023035A2 (fr) 1993-11-25
AU4312593A (en) 1993-12-13

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