Amide derivatives and their therapeutic use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

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514432, 514456, 514429, 514408, 514183, 564180, 549 23, 549398, 549407, 548570, 548950, A61K 3165, A61K 3138, A61K 3140, A61K 3133

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057191867

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BRIEF SUMMARY
This application is filed pursuant to 35 U.S.C. .sctn.371 as a United States National Phase Application of International Application No. PCT/US95/01039 filed 09 May 1955 which claims priority from EP 94303351.4 filed 10 May 1994.
The present invention relates to substituted carbocyclic amides, to pharmaceutical compositions containing them, to methods for their preparation and their use in therapy, in particular as muscle relaxants.
The major limiting side effects of many clinically effective muscle relaxants and anticonvulsants are the induction of sedation and incoordination in the recipient, which severely limits the usefulness of these compounds. Similar side effects have been found with drugs used in the treatment of anxiety, such as, benzodiazepines. Although these effects may be transient, patients on such therapy are often unable to drive or participate in certain occupations.
We have now found novel carbocyclic amides which have muscle relaxant activity but with less of the sedation and incoordination side-effects observed with known muscle relaxants.
Accordingly, the present invention provides the following novel compounds: de mide mide ne)acetamide ne)acetamide de amide
Other uses of the compounds of the present invention are for the treatment or prophylaxis of conditions associated with:
As used herein the term: acceptable derivative of a compound of the present invention, for example an ester, which, upon administration to the recipient, such as a human, is capable of providing(directly or indirectly) the said compound or an active metabolite or residue thereof. the present invention with its solvent.
It will be appreciated that the compounds of the present inventions can exist in various geoisomeric forms and as mixtures thereof in any proportions. The present invention includes within its scope such geoisomeric forms or mixtures of geoisomers, including the individual E and Z isomers of the compounds as well as mixtures of such isomers, in any proportions. Preferred compounds of the present invention are those wherein the group adjacent to the exo double bond and the carbonyl group are on opposite sides of the exo double bond. The compounds of the present inventions may exist in forms wherein one or more carbon centers is/are chiral. The present invention includes within its scope each possible optical isomer substantially free, i.e., associated with less than 5%, of any other optical isomer(s), as well as mixtures of one or more optical isomers in any proportion, including racemic mixtures thereof. It will be evident to a skilled person that certain compounds of the present inventions can exist in enantiomeric forms according to the direction of rotation of plane polarized light when passed through a sample of the compound. Individual optical isomers as well as mixtures of such isomers in any proportion are considered to be within the scope of the invention. Pharmaceutically acceptable salts are within the scope of the invention and are particularly suitable for medical applications because of their greater aqueous solubility relative to the parent (i.e., basic) compounds. Such salts must clearly have a pharmaceutically acceptable anion or cation. Suitable pharmaceutically acceptable acid addition salts of the compounds of the present invention include those derived from inorganic acids, such as hydrochloric, hydrobromic, phosphoric, metaphosphoric, nitric, sulphonic and sulphuric acids, and organic acids, such as acetic, benzenesulphonic, benzoic, citric, ethanesulphonic, fumaric, gluconic, glycollic, isothionic, lactic, lactobionic, maleic, malic, methanesulphonic, succinic, p-toluenesulphonic, tartaric and trifluoroacetic acids. The chloride salt is particularly preferred for medical purposes. Suitable pharmaceutically acceptable base salts include ammonium salts, alkali metal salts, such as sodium and potassium salts, and alkaline earth salts, such as magnesium and calcium salts.
Salts having a non-pharmaceutically acceptable anion are also within the scope of the invention as useful in

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Derwent Publications, Ltd., Database, 24 Mar. 1992.
Angelova I. et al., "Conversion of 5-aryl-3-phenyl-2,4-pentadienoic acid and their amides into indan derivatives", Chemical Abstracts, 8 Jul. 1974, pp. 116-117.

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