Derivatives of 2-pyridylmethylamine and pharmaceutical composition based on them
This invention relates to substituted derivatives of propanolamine formula (I)and their pharmaceutically acceptable salts, where R1, R2, R3, R4, Z, m and n are specified in paragraph 1 of the claims. The compounds of formula (I) possess hypolipidemic activity and can be used in medicine. 2 S. and 2 C.p. f-crystals, 2 tab. Description text in facsimile form (see graphic part).
Claims1. Derivatives of 2-pyridylmethylamine formula I,where R1denotes phenyl, oxazolyl, isoxazolyl, thiazolyl, while heteroaryl residue may be substituted by phenyl or pyridium, which can also be substituted with halogen or (C1-C8)-alkyl;R2denotes hydrogen;R3denotes the residue of a monosaccharide, disaccharide, trisaccharide or tetrasaccharide;R4denotes hydrogen or fluorine;Z represents-NH-Co-C16-alkyl-(C=O), -O-Co16-alkyl-(C=O)-, -(C=O)m-C1-C16-alkyl-(C=O)n, amino acid or diaminotoluenes residue or a covalent bond;m and n equal 0 Il is 1 denotes phenyl, oxazolyl, isoxazolyl, thiazolyl, and the phenyl or heteroaryl residue may be substituted with halogen or (C1-C8) -alkyl, R2denotes hydrogen, R3denotes the residue of a monosaccharide or disaccharide, R4denotes hydrogen or fluorine, Z represents-NH-Co-C16-alkyl-(C=O), -O-Co16-alkyl-(C=O)-, -(C=O)m-C1-C16-alkyl-(C=O)mcovalent bond, n is 0 or 1, m is 0 or 1, and their pharmaceutically acceptable salts.3. The compounds of formula I under item 1 or 2, characterized in that the1denotes phenyl, thiazolyl, oxazolyl, isoxazolyl, with aromatic or heteroaromatic residue can be substituted by fluorine, chlorine, bromine, or (C1-C8)-alkyl, R2denotes H, R3indicatesR4denotes hydrogen or fluorine, Z represents-NH-C6-C12-alkyl-C=O-, -O-C6-C12-alkyl-C=O-, -(C=O)m-C6-C12-alkyl-(C=O)nn is 0 or 1,m is 0 or 1, and their pharmaceutically acceptable salts.4. Pharmaceutical composition, show
SUBSTANCE: the suggested preparation is being cytidine diphosphate choline (CDP-choline) known previously as the preparation to restore cerebral phospholipid structure and for treating mammalians, people among them, subjected to the action of stimulants. Moreover, it is necessary to note that CDP-choline decreases the duration of abstinence symptoms (tremor, convulsions, weakness, emotional instability, nervousness, social reserve) and causes either the decrease or stoppage of alcohol intake.
EFFECT: higher efficiency of therapy.
5 cl, 5 ex