Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-01-08
1994-07-05
Prescott, Arthur C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A01N 4338
Patent
active
053267818
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use of imidazole derivatives in the manufacture of medicaments having anxiolytic and nootropic activities and a method of treating anxiety or cognitive disorders by administering them.
EP-A-125033 and EP-A-125783 disclose imidazole derivatives as dopamine-.beta.-hydroxylase (DBH) inhibitors having utility as diuretic, natriuretic, cardiotonic, antihypertensive, vasodilator, anti-ulcerogenic or anti-parkinson disease agents. 1-Benzyl-2-(hydroxymethyl)imidazole has previously been disclosed for example in U.S. Pat. No. 4,746,669 as an intermediate in the synthesis of immunoregulants. There has been no suggestion of any pharmacological activity for this compound.
It has now been discovered that 1-benzyl-2-(hydroxymethyl)imidazole and certain of the imidazole compounds disclosed in the above-noted European patent applications surprisingly have anxiolytic and nootropic activities.
Accordingly the present invention provides the use of a compound of the formula (1): ##STR1## wherein Ar is 3,5-difluorophenyl, 2,6-dichlorophenyl, 3,4-dihydroxyphenyl, or 3-fluoro-4-methoxyphenyl and medicament having anxiolytic and/or nootropic activity.
In another aspect this invention provides a method of treating anxiety and/or cognitive disorders in a host in need thereof which comprises administering an effective amount of a compound of the formula (I) as hereinbefore defined or a pharmaceutically acceptable salt thereof.
Particular compounds of the formula (1) are: 1-benzyl-2-(hydroxymethyl)imidazole, 1-benzyl-2-(aminomethyl)imidazole, and pharmaceutically acceptable salts thereof.
In another aspect this invention provides 1-benzyl-2-(hydroxymethyl)imidazole or a pharmaceutically acceptable salt thereof for use as a medicament.
Suitable pharmaceutically acceptable salts can be formed with hydrochloric, hydrobromic, sulphuric, phosphoric, nitric, acetic, citric, tartaric, maleic, lactic, ascorbic, fumaric, oxalic, methanesulphonic and ethanesulphonic acids.
In order to use a compound of this invention or a pharmaceutically acceptable salt thereof for the treatment of humans and other mammals it is normally formulated in accordance with standard pharmaceutical practice as a pharmaceutical composition.
Compounds of this invention and their pharmaceutically acceptable salts can be administered in standard manner for example orally, sublingually, parenterally, transdermally, rectally, via inhalation or via buccal administration.
Compounds of this invention and their pharmaceutically acceptable salts which are active when given orally or via buccal administration can be formulated appropriately in dosage forms such as liquids, syrups, tablets, capsules and lozenges. An oral liquid formulation will generally consist of a suspension or solution of the compound or salt in a liquid carrier for example, ethanol, glycerine or water with a flavouring or colouring agent. Where the composition is in the form of a tablet, any pharmaceutical carrier routinely used for preparing solid formulations can be used. Examples of such carriers include magnesium stearate, starch, celluloses, lactose and sucrose. Where the composition is in the form of a capsule, any routine encapsulation is suitable, for example using the aforementioned carriers in a hard gelatin capsule shell. Where the composition is in the form of a soft gelatin shell capsule any pharmaceutical carrier routinely used for preparing dispersions or suspensions can be considered, for example aqueous gums, celluloses, silicates or oils and are incorporated in a soft gelatin capsule shell.
Typical parenteral compositions consist of a solution or suspension of the compound or salt in a sterile aqueous or non-aqueous carrier optionally containing a parenterally acceptable oil or solubilising agent, for example polyethylene glycol, polyvinylpyrrolidone, 2-pyrrolidone, cyclodextrin, lecithin, arachis oil, or sesame oil.
A typical suppository formulation comprises a compound of this invention or a pharmaceutically acceptable salt thereof which is active when
REFERENCES:
patent: 4234594 (1980-11-01), Winn et al.
patent: 4767775 (1988-08-01), Jelich et al.
patent: 5049563 (1991-09-01), Haeck et al.
Kruse et al, "Some Benzyl-substituted Imidazoles . . . Copper Binding Site", J. Med. Chem., vol. 33, pp. 781-789, Feb., 1990.
Hunter Ann J.
Wood Lars M.
Young Rodney C.
Lentz Edward T.
McCarthy Mary E.
Prescott Arthur C.
Smith Kline & French Laboratories Limited
Venetianer Stephen
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