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).


1. 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, R3indicates

R4denotes 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


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5 cl, 5 ex