C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 513/04 (2006.01) A61K 31/407 (2006.01)
Patent
CA 2562864
Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH- CH2C=CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH=NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti- psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic- depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.
L'invention concerne des dérivés de pyrrolo[2,1-b]benzothiazépines représentés par la formule (I) dans laquelle A représente CH-CH¿2?C=CH; R représente hydrogène, halogène, alcoxy C¿1?-C¿4?, alkylthio C¿1?-C¿4?, alkyle C¿1?-C¿4?, cycloalkyle C¿5?-C¿6?; R¿1? représente 1-pipérazinyle, 1-homopipérazinyle et 1-pipéridinyle; R¿2? représente hydrogène, alcoxy C¿1?-C¿4?, alkylthio C¿1?-C¿4?, alkyle C¿1?-C¿4?, CHO, CH=NOH,CH¿2?OH. Les composés de la formule (I) présentent une activité antipsychotique atypique caractéristique et sont, de ce fait, utilisés comme médicaments, en particulier, pour traiter et prévenir la schizophrénie, les états paranoïdes, les états maniaco-dépressifs, les troubles de la sphère affective, la régression sociale, la régression de la personnalité et les hallucinations. Lesdits composés possèdent également des propriétés pharmacocinétique.
Carminati Paolo
Di Cesare Maria Assunta
Ghirardi Orlando
Minetti Patrizia
Tinti Maria Ornella
Fetherstonhaugh & Co.
Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.
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