Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-06-16
1997-10-07
Gupta, Yogendra N.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514272, 514273, 544292, 544320, 544321, A61K 31505, C07D23984, C07D23988
Patent
active
056748680
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
EP-0,389,037, published on Sep. 26, 1990 discloses N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin) carboxamide derivatives and EP-0,445,862, published on Sep. 11, 1991 discloses N-(4-piperidinyl)(dihydrobenzofuran or dihydrobenzo-2H-benzopyran)carboxamide derivatives. Both applications disclose gastrointestinal motility stimulating properties for said compounds. The dimethyl-dihydrobenzofuran and dimethyl-dihydro-2H-benzopyran derivatives of the present invention show 5-HT.sub.3 -antagonism.
DESCRIPTION OF THE INVENTION
The present invention is concerned with a method of treating warm-blooded animals suffering from 5-HT.sub.3 mediated disorders such as anxiety, psychosis, depression, schizophrenia, cognitive disorders, drug abuse, migraine, emesis, irritable bowel syndrome and related disorders, which comprises the systemic administration to said warm-blooded animals of an effective 5-HT.sub.3 antagonistic amount of a compound of formula ##STR2## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein
The present invention is also concerned with the use of the compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof for the manufacture of a medicament for treating 5-HT.sub.3 mediated disorders such as anxiety, psychosis, depression, schizophrenia, cognitive disorders, drug abuse, migraine, emesis, irritable bowel syndrome and related disorders.
In the foregoing definitions and hereinafter the term halo defines fluoro, chloro, bromo and iodo, preferably chloro; C.sub.1-4 alkyl defines straight and branch chained saturated hydrocarbon radicals having from 1 to 4 carbon atoms such as methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl and 1,1-dimethylethyl, preferably methyl. C.sub.1-6 alkyl defines C.sub.1-4 alkyl and the higher homologues thereof such as, for example, pentyl and hexyl. C.sub.1-3 alkylcarbonyl defines straight and branch chained acyl radicals such as methylcarbonyl, ethylcarbonyl, propylcarbonyl, preferably methylcarbonyl.
The term pharmaceutically acceptable acid addition salt as used hereinbefore defines the non-toxic, therapeutically active acid addition salt forms which the compounds of formula (I) may form. The compounds of formula (I), having basic properties, may be converted into the corresponding therapeutically active, non-toxic acid addition salt forms by treating the free base form with a suitable amount of an appropriate acid following conventional procedures. Examples of appropriate acids are inorganic acids, for example, hydrohalic acid, e.g. hydrochloric, hydrobromic and the like acids, sulfuric acid, nitric acid, phosphoric acid and the like; or organic acids, such as, for example, acetic, propanoic, hydroxyacetic, 2-hydroxypropanoic, 2-oxopropanoic, propanedioic, butanedioic, (Z)-2-butenedioic, (E)-2-butenedioic, 2-hydroxybutanedioic, 2,3-dihydroxybutanedioic, 2-hydroxy-1,2,3-propanetricarboxylic, cyclohexanesulfamic, 2-hydroxybenzoic, 4-amino-2-hydroxybenzoic and the like acids. The term pharmaceutically acceptable addition salts also comprises the solvates which the compounds of formula (I) may form such as alcoholates and in particular hydrates.
The compounds of formula (I) may also exist in their tautomeric form. Said form although not explicitly indicated hereinabove is intended to be included within the scope of the present invention.
The term stereochemically isomeric forms as used hereinbefore defines the different isomeric forms which the compounds of formula (I) may possess. Unless otherwise mentioned or indicated, the chemical designation of compounds denotes the mixture of all possible stereochemically isomeric forms, said mixtures containing all diastereomers, and/or enantiomers of the basic molecular structure. All stereochemically isomeric forms of the compounds of formula (I) both in pure form or in admixture with each other are intended to b
Bosmans Jean-Paul Rene Marie Andre
Van Daele Georges Henri Paul
Van Laerhoven Willy Joannes Carolus
Gupta Yogendra N.
Janssen Pharmaceutica N.V.
Metz Charles J.
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