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)
• Endocrinology (AREA)
• Reproductive Health (AREA)
• Epidemiology (AREA)
• Urology & Nephrology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Indole Compounds (AREA)

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• 1993
  • 1993-05-04 AU AU43125/93A patent/AU4312593A/en not_active Abandoned
  • 1993-05-04 JP JP5519830A patent/JPH07506823A/ja active Pending
  • 1993-05-04 WO PCT/EP1993/001099 patent/WO1993023035A2/en not_active Application Discontinuation
  • 1993-05-04 EP EP93912699A patent/EP0641202A1/de not_active Withdrawn

Non-Patent Citations (1)

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