1-Aryl-2,2,2-tri:fluoro-ethoxy-alkanoic acid derivs. - useful as hypolipaemic agents
Cpds. of formula Ar-A-Nr2-Ar'-CH(CF3)-Z-CHR1-COX (I) and their salts are new (where Ar is phenyl opt. substd. by 1-3 gps. selected from halogen, lower alkyl, lower alkoxy, CF3 and alkylenedioxy; A is a direct bond or 1-4C alkylene; Ar' is phenylene; Z is O or S; R1 is 1-5C alkyl; R2 is H o...
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Zusammenfassung: | Cpds. of formula Ar-A-Nr2-Ar'-CH(CF3)-Z-CHR1-COX (I) and their salts are new (where Ar is phenyl opt. substd. by 1-3 gps. selected from halogen, lower alkyl, lower alkoxy, CF3 and alkylenedioxy; A is a direct bond or 1-4C alkylene; Ar' is phenylene; Z is O or S; R1 is 1-5C alkyl; R2 is H or lower alkyl; X is OH, OM (where M is a cation), lower alkoxy, hydroxyalkoxy, polyhydroxyalkoxy, mono- or dialkylaminoalkoxy, NH2, mono- or dialkylamino, alkyleneamino, aralkylamino, alkyl(aralkyl)amino, NHOH, alkoxyamino, acyloxyamino or R3-1-piperazinyl, where R3 is lower alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl). (I) may be prepd. by reacting Ar-A-N(R2)Ar'-C(ZH)H-CF3 with (R1)CHYCOX. (where Y is Cl, Br or I and X' is OH or alkoxy). The products can be converted to other cpds. (I) by standard methods. (I) are hypolipaemic agents giving reduced blood cholesterol and triglyceride levels, e.g. at doses of 0.5- 25 mg/kg (p.o.).
LA PRESENTE ADDITION SE RAPPORTE A DE NOUVEAUX ACIDES (PHENYLAMINO) ARYLALCANOIQUES DE FORMULE GENERALE:(CF DESSIN DANS BOPI)DANS LAQUELLE A REPRESENTE UNE LIAISON DIRECTE OU UNE CHAINE ALCOYLENE:Z EST DE L'OXYGENE OU DU SOUFRE;R EST UN RADICAL ALCOYLE INFERIEUR;R EST DE L'HYDROGENE OU UN RADICAL ALCOYLE INFERIEUR;R EST UN SUBSTITUANT;X EST UN HYDROXYLE, UN ALCOXY OU UN GROUPE AMINE.L'INVENTION SE RAPPORTE AUX SELS DES COMPOSES DE FORMULE GENERALEI, AUX FORMES DIASTEREOISOMERIQUES ET AUX ISOMERES OPTIQUES DES COMPOSES DE FORMULE GENERALEI.L'INVENTION S'ETEND AUSSI AUX PROCEDES D'OBTENTION DES COMPOSES DE FORMULE GENERALEI.LES COMPOSES SELON L'INVENTION SONT DOUES DE PROPRIETES PHARMACOLOGIQUES INTERESSANTES ET TROUVENT LEUR EMPLOI SOUS FORME DE COMPOSITIONS PHARMACEUTIQUES EN TANT QUE PRINCIPES ACTIFS DE MEDICAMENT. |
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