Peripherally-selective inhibitors of dopamine-β-hydroxylase and method of their preparation
AssigneePortela & C.A., S.A.
InventorsDavid Alexander Learmonth, Patricio Manuel Viera Araújo Soares da Silva, Alexander Beliaev
Life of this patent
Estimating the term…
Abstract
Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X is CH2, O or S, and n is 1, 2 or 3, with the proviso that if X is CH2, n is not 1, and a method for their preparation. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.
Claims19
A compound of Formula I:
- where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl groups, alkyloxy groups, hydroxy groups, nitro groups, amino groups, alkylcarbonylamino groups, alkylamino groups or dialkylamino groups;
- R4 signifies hydrogen, an alkyl group or an alkylaryl group;
- X signifies CH2, an oxygen atom or a sulphur atom;
- n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2;
- and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof;
- wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl groups, alkoxy groups, halogen groups, alkoxycarbonyl groups or hydroxycarbonyl groups;
- the term aryl means a phenyl or naphthyl group, optionally substituted by an alkyloxy group, halogen or nitro group;
- and the term halogen means fluorine, chlorine, bromine or iodine.
A pharmaceutical composition comprising (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising (S)-5-(2-aminoethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1,3-dihydroimidazole-2-thione or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising (R)-5-aminomethyl-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.