Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-10-06
1999-11-30
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31445
Patent
active
059943696
DESCRIPTION:
BRIEF SUMMARY
FIELD OF APPLICATION OF THE INVENTION
The invention relates to the novel use of known active compounds in the treatment of illnesses which are favorably affected by substances having affinity for sigma receptors.
KNOWN TECHNICAL BACKGROUND
British Patent 1313781 describes substituted piperidines which are distinguished by a long-lasting, centrally stimulating action. One of the active compounds coming under the British patent, for which the INN budipine was later recommended, is being tested in the therapy of Parkinsonism. Furthermore, the prior art (e.g. German Patent Specification 10 05 067, German Patent Specification 871 899, German Patent Specification 875 660, East German Patent Specification 50 603 and U.S. Pat. No. 2,411,664) discloses a number of 1-pyrrolidino- and 1-piperidinopropanols and -butanols, such as, for example, biperidin, cycrimine, pridinol, procyclidine, trihexyphenidyl, triperidin or difenidol, which in some cases can likewise be employed in the therapy of Parkinsonism.
DESCRIPTION OF THE INVENTION
Surprisingly, it has now been found that the compounds described below in greater detail have a high affinity for sigma receptors and are therefore advantageously suitable for the treatment of illnesses which can be favorably affected by alterations in the function of sigma receptors.
The invention relates to the use of compounds of the formula I ##STR2## in which either
R1 is phenyl,
R2 is phenyl,
R3 is hydrogen or 1-4C-alkyl,
R4 is hydrogen or 1-4C-alkyl,
R5 is hydrogen or 1-4C-alkyl,
m is the number 2
n is the number 0,
R1 is hydrogen,
R2 is hydrogen,
R3 is phenyl,
R4 is cyclopentyl, cyclohexyl, phenyl, 2-norbornen-5-yl or tricyclo[2.2.1.0.sup.2,6 ]hept-2-yl,
R5 is hydroxyl
m is the number 1 or 2
n is the number 2 or 3, sigma receptor-modulated illnesses.
1-4C-Alkyl represents straight-chain or branched alkyl radicals having 1 to 4 carbon atoms. Examples which may be mentioned are the butyl, isobutyl, sec-butyl, tert-butyl, propyl, isopropyl, ethyl and, in particular, the methyl radical.
Suitable salts of compounds of the formula I are preferably all pharmacologically tolerable acid addition salts with the inorganic and organic acids customarily used in pharmacy. Those which are suitable are water-soluble and water-insoluble acid addition salts with acids such as, for example, hydrochloric acid, hydrobromic acid, phosphoric acid, nitric acid, sulfuric acid, acetic acid, citric acid, D-gluconic acid, benzoic acid, 2-(4-hydroxybenzoyl)benzoic acid, butyric acid, sulfosalicylic acid, maleic acid, lauric acid, malic acid, fumaric acid, succinic acid, oxalic acid, tartaric acid, embonic acid, stearic acid, toluenesulfonic acid, methanesulfonic acid or 3-hydroxy-2-naphthoic acid, it being possible to employ the acids in salt preparation - depending on whether it is a mono- or polybasic acid and depending on which salt is desired--in an equimolar quantitative ratio or one differing therefrom.
Depending on the nature of the substituents, the compounds of the formula I can be optically active compounds. The invention therefore includes both the enantiomers and their mixtures and racemates.
Illnesses which may be mentioned which are favorably affected by substances having affinity for sigma receptors are psychoses (schizophrenia), hallucinations in combination with psychotic disorders and chronic psychological depressions, psychoneuroses, brain function disorders (cerebral ischemia, cognitive dysfunction), disorders of intestinal function (absorption, secretion, motility) and of other smooth muscular organs, such as vas deferens and bladder (urinary incontinence), and other disorders such as are connected with affinities for sigma receptors and such as are described, for example, in the literature surveys of B. L. Largent et al. (Eur. J. Pharmacol., 155, 345-7, 1988), S. I. Deutsch et al. (Clinical Neuropharmacology, 11(2), 105-119, 1988), T. P. Su (Eur. J. Biochem., 200, 633-642, 1991) and J. M. Walker et al. (Pharmacol. Rev. 42, 355-402, 1990).
In the use according to the invention of t
REFERENCES:
Hudkins et al., Life Sci., 49(1), 1229-35, 1991.
Walker et al., Pharmacological Reviews, 42(4), 355-402, 1990.
Kolassa Norbert
Kornhuber Johannes
ByK Gulden Lomberg Chemische Fabrik GmbH
Spivack Phyllis G.
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