Derivatives of 1,3-diaryl-2-pyridin-2-yl-3-(pyridine-2-ylamino) propanol and pharmaceutical composition based on them

 

The invention relates to new derivatives of 1,3-diaryl-2-pyridin-2-yl-3-(pyridine-2-ylamino)propanol of the formula (I)

where Z denotes-NH-(C1-C16-alkyl)-(C=O)-; -(C=O)-(C1-C16-alkyl)-(C=O)-;

-(C=O)-phenyl-(C=O)-; And1And2And3And4denote independently of each amino-acid residue, E represents-SO2-R4and-CO-R4; R1- phenyl, thiazolyl, oxazolyl, thienyl, thiophenyl and others, R2- N., HE, CH2HE, OMe; R3Is h, F, methyl, OMe; R4denotes -(C5-C16-alkyl), -(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylene)-NH-R5and others, R5denotes-COO-R6, -(C=O)-R6-(C1-C6-alkylen)-R7, phenyl, naphthyl and others, R6denotes H, -(C1-C6) alkyl; R7denotes H, -(C1-C7-cycloalkyl, phenyl, naphthyl and others, l, q, m, n, o, p denote 0 or 1, and l+q+m+n+o+p is greater than or equal to 1, and their pharmaceutically acceptable salts. The compounds of formula (I) possess hypolipidemic activity and can be used in medicine. 2 S. and 2 C.p. f-crystals, 7 PL.

1. Derivatives of 1,3-diaryl-2-pyridin-2-yl-3-(pyridine-2-ylamino)-propanol of the formula I

where Z denotes-NH-(C1-C16-alkyl)-(C=O)-;

-(C=O)-(C1-C16-alkyl)-(C=O)-;

-(C=O)-phenyl-(C=O)-;

And1And2And3And4denote independently of each amino acid residue, amino acid residue, which one - or multi-substituted aminoadenine groups;

E represents-SO2-R4, -CO-R4;

R1denotes phenyl, thiazolyl, oxazolyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, and rings can be up to three times substituted by F, Cl, Br, OH, CF3, NO2CN, OCF3-(C1-C6)-alkyl, O-(C1-C6)-alkyl, S-(C1-C6)-alkyl, SO-(C1-C6)-alkyl, SO2-(C1-C6)-alkyl, (C1-C6)alkyl, (C3-C6)cycloalkyl, COOH, COO(C1-C6)alkyl, COO(C3-C6)cycloalkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, CONH(C3-C6)cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl;

R2denotes H, HE, CH2HE, OMe;

R3denotes H, F, methyl, OMe;16-alkylen)-R5, -(C=O)-(C0-C16-alkylene)-NH-R5-(C1-C8-albaniles)-R5-(C1-C8-quinil)- (C1-C4-alkylen)-S(O)o-2-R5-(C1-C4-alkylene)-O-R5-(C1-C4-alkylene)-NH-R5;

R5denotes-COO-R6, -(C=O)-R6-(C1-C6-alkylen)-R7,

-(C1-C6-albaniles)-R7-(C1-C7-cycloalkyl, phenyl, naphthyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, dihydropyrimidine-2,4-Dion-6-yl, bromanil, phthalimido, thiazolyl, and rings can be up to three times substituted by F, Cl, Br, OH, CF3, NO2CN, OCF3-(C1-C6)-alkyl, O-(C1-C6)-alkyl, S-(C1-C6)-alkyl, SO-(C1-C6)-alkyl, SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C6-cycloalkyl, COOH, COO(C1-C6)alkyl, COO(C3-C6)cycloalkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, CONH(C3-C6-cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl, pyridium;

R6denotes H, -(C1-C6) alkyl;

R7denotes H, -(C1- 3, NO2CN, OCF3-(C1-C6)-alkyl, O-(C1-C6)-alkyl, S-(C1-C6)-alkyl, SO-(C1-C6)-alkyl, SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C6-cycloalkyl, COOH, COO(C1-C6)alkyl, COO(C3-C6)cycloalkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, CONH(C3-C6-cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl;

l, q, m, n, o, p independently of one another denote 0 or 1,

moreover, l+q+m+n+o+p is greater than or equal to 1;

and their pharmaceutically acceptable salts.

2. The compounds of formula I on p. 1, characterized in that Z represents-NH-(C1-C16-alkyl)-(C=O)-; -(C=O)-(C1-C16-alkyl)-(C=O)-; -(C=O)-phenyl-(C=O)-;

And1And2And3And4denote independently of each amino acid residue, amino acid residue, which one - or multi-substituted aminoadenine groups;

E represents-SO2-R4, -CO-R4;

R1denotes phenyl, thiazolyl, oxazolyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl,kilometres, O-(C1-C6)-alkyl, S-(C1-C6)-alkyl, SO-(C1-C6)-alkyl, SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C6-cycloalkyl, COOH, COO(C1-C6)alkyl, COO(C3-C6)cycloalkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, CONH(C3-C6)cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl;

R2denotes H, HE, CH2HE, OMe;

R3denotes H, F, methyl, OMe;

R4denotes -(C5-C16-alkyl), -(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylene)-NH-R5-(C1-C8-albaniles)-R5-(C1-C8-quinil)- (C1-C4-alkylen)-S(O)o-2-R5-(C1-C4-alkylene)-O-R5-(C1-C4-alkylene)-NH-R5;

R5denotes-COO-R6, -(C=O)-R6-(C1-C6-alkylen)-R7-(C1-C6-albaniles)-R7-(C1-C7-cycloalkyl, phenyl, naphthyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, dihydropyrimidine-2,4-Dion-6-yl, bromanil, phthalimido, thiazolyl, and rings can be d)-alkyl, S-(C1-C6)-alkyl, SO-(C1-C6)-alkyl, SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C6-cycloalkyl, COOH, COO(C1-C6)alkyl, COO(C3-C6)cycloalkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, CONH(C3-C6-cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl, pyridium;

R6denotes H, -(C1-C6)alkyl;

R7denotes H, -(C1-C7-cycloalkyl, phenyl, naphthyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, dihydropyrimidine-2,4-Dion-6-yl, bromanil, phthalimido, thiazolyl, and rings can be up to three times substituted by F, Cl, Br, OH, CF3, NO2CN, OCF3-(C1-C6)-alkyl, O-(C1-C6)-alkyl, S-(C1-C6)-alkyl, SO-(C1-C6)-alkyl, SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C6-cycloalkyl, COOH, COO(C1-C6)alkyl, COO(C3-C6)cycloalkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)alkyl]2, CONH(C3-C6-cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl;

l 0 Il is inane formula I under item 1 or 2, wherein Z represents-NH-(C1-C12-alkyl)-(C=O)-; -(C=O)-(C1-C12-alkyl)-(C=O)-; -(C=O)-phenyl-(C=O)-;

And1And2And3And4denote independently of each amino acid residue, amino acid residue, which one - or multi-substituted aminoadenine groups;

E represents-SO2-R4, -CO-R4;

R1denotes phenyl, thiazolyl, oxazolyl, and the ring may be substituted up to three times -(C1-C6)-alkyl;

R2denotes H, HE, CH2HE, OMe;

R3denotes H, F, methyl, OMe;

R4denotes -(C5-C16-alkyl), -(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylen)-R5, -(C=O)-(C0-C16-alkylene)-NH-R5-(C1-C8-albaniles)-R5-(C1-C8-quinil)- (C1-C4-alkylen)-S(O)o-2-R5-(C1-C4-alkylene)-O-R5-(C1-C4-alkylene)-NH-R5;

R5denotes-COO-R6, -(C=O)-R6-(C1-C7-cycloalkyl, phenyl, naphthyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, dihydropyrimidine-2,4-Dion-6-yl, bromanil, phthalimido, thiazolyl, and rings can be up to two times Zam is, The PA(C1-C6)alkyl, CONH2, CONH(C1-C6)alkyl, CON[(C1-C6)-alkyl]2, CONH(C3-C6)cycloalkyl, NH2, NH-CO-(C1-C6)-alkyl, NH-CO-phenyl, pyridium;

R6denotes H, -(C1-C6)alkyl;

l, m, n is 0; o is 1; p is 0 or 1; q is 0 or 1;

and their pharmaceutically acceptable salts.

4. The pharmaceutical composition exhibiting hypolipidemic activity and containing one or more compounds according to paragraphs.1-3.

 

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