Derivatives of 3,3a,4,5-tetrahydro-1H-oxazolo/3,4-a/quionolin-1-one, process of their preparation, those derivatives used as a medicament as well as pharmaceutical preparations in which the derivatives are comprised

• Main Authors: PUECH FR•D•RIC, KOENIG JEAN JACQUES, BURNIER PHILIPPE, JEGHAM SAMIR, ZARD LYDIA
• Format: Patent
• Language: Czech; English
• Published: 12.01.2000
• Edition: 7
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; VINEGAR; WINE

In the present invention there are disclosed derivatives 3, 3a, 4, 5-tetrahydro-1H-oxazolo/3,4-a/quinolin-1-one of the general formula I in which n is 0 or 1, Ri1 represents a hydrogen atom, an ethylene group, a methyl group, an ethyl group, a phenyl group, a hydroxymethyl group or a methoxymethyl group and either Ri2 represents a methyl group, a trifluoromethyl group or a cyano group, Ri3 represents a hydrogen atom a hydroxyl group or a benzyl group and Ri4 and Ri5 represent each a hydrogen atom or Ri2 and Ri4 together form the group {-(CHi2)i4-}, Ri3 represents a hydroxyl group and Ri5 represents a hydrogen atom or Ri2 and Ri5 together form the group {-O-(CHi2)i3} and Ri3 and Ri4 represents hydrogen atoms or Ri2 and Ri4 together form the group {-(CHi2)i4-}, Ri3 represents a hydroxyl group and Ri4 represents a hydrogen atom . The above indicated derivatives can be used in therapy. In the present invention there are also described processes for preparing such derivatives as well as a pharmaceutical composition in which those derivatives are comprised. Deriváty 3,3a,4,5-tetrahydro-1H-oxazolo/3,4-a/chinolin-1-on obecného vzorce I, ve kterém n znamená 0 nebo 1, R.sub.1.n. znamená atom vodíku, ethenylovou skupinu, methylovou skupinu, ethylovou skupinu, fenylovou skupinu, hydroxymethylovou skupinu nebo methoxymethylovou skupinu a buď R.sub.2.n. znamená methylovou skupinu, trifluormethylovou skupinu, nebo kyano-skupinu, R.sub.3.n. znamená atom vodíku, hydroxylovou skupinu nebo benzyloxyskupinu a R.sub.4.n. a R.sub.5.n. znamenají atomy vodíku nebo R.sub.2.n. a R.sub.4.n. dohromady tvoří skupinu -(CH.sub.2.n.).sub.4.n.-, R.sub.3.n. znamená hydroxylovou skupinu a R.sub.5.n. znamená atom vodíku nebo R.sub.2.n. a R.sub.5.n. tvoří dohromady skupinu -O-(CH.sub.2.n.).sub.3.n.- a R.sub.3.n. a R.sub.4.n. znamenají atomy vodíku nebo R.sub.2.n. a R.sub.5.n. tvoří dohromady skupinu - (CH.sub.2.n.).sub.4.n.-, R.sub.3.n. znamená hydroxylovou skupinu a R.sub.4.n. znamená atom vodíku. Uvedené deriváty mají terapeutické použití. Jsou popsány i způsoby příŕ