Derivatives oksiminoalkil acid, pharmaceutical composition and a means for regulation of retinoid receptors

 

The invention relates to new derivatives oksiminoalkil acid of the formula (I), where R1is oxazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl, teinila, furil; thiazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl; unsubstituted chinoline and so on; X represents a bond or the group-NR6- where R6represents hydrogen or C1-4alkyl; n represents an integer from 1 to 3; Y represents an oxygen atom or the group-NR7- where R7is hydrogen; ring a represents a benzene ring, optionally substituted by one or two1-4alkoxy; p is an integer from 1 to 3; R2represents phenyl, optionally substituted lower alkyl, halogen, and so on; unsubstituted furyl; unsubstituted pyridyl; pyridinyl-1-oxide; q is an integer from 0 to 6; m represents 0 or 1; R3represents a hydroxy-group, lower alkoxy or-NR9R10where R9and R10represent identical or different groups selected from hydrogen, lower alkyl and lower alkylsulfonyl; R4and R5represent identical or different groups selected from the waters of omicheskim action containing the compound of formula (I) and a pharmacologically acceptable carrier. Means for regulation of retinoid receptors containing the compound of formula (I). The technical result - obtaining new derivatives oksiminoalkil acid having hypoglycemic and hypolipidemic effect. 3 S. and 18 C.p. f-crystals, 2 Il.

Description text in facsimile form (see graphic part).

Claims

1. Derivatives oksiminoalkil acid represented by the formula (I)where R1is oxazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl, teinila, furil; thiazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl; unsubstituted chinoline; 1,2,4-oxadiazolyl, substituted phenyl; imidazo[1,2-a] pyridyl, optionally substituted with halogen or phenyl; pyridyl, optionally substituted lower alkyl; pyrimidyl; isoxazolyl, optionally substituted by phenyl; phenyl; X represents a bond or the group-NR6- where R6represents hydrogen or C1-4alkyl; n represents an integer number is dstanley benzene ring, optionally substituted by one or two1-4alkoxy; p is an integer from 1 to 3; R2represents phenyl, optionally substituted lower alkyl, halogen, phenoxy, lower alkoxy, teinila, phenyl, anilinium or phenylcarbinol; unsubstituted furyl; unsubstituted pyridyl; pyridinyl-1-oxide;
q represents an integer from 0 to 6;
m represents 0 or 1;
R3represents a hydroxy-group, lower alkoxy or-NR9R10where R9and R10represent identical or different groups selected from hydrogen, lower alkyl and lower alkylsulfonyl;
R4and R5represent identical or different groups selected from hydrogen or lower alkyl,
or their salt.

2. Connection on p. 1, in which X represents a bond or a group represented by-NR6- where R6is1-4alkyl.

3. Connection on p. 1, in which n represents 1 or 2.

4. Connection on p. 1, in which Y represents an oxygen atom.

5. Connection on p. 1, in which q represents an integer from 0 to 4.

6. Connection on p. 1, in which R2represents phenyl, optionally substituted lower alkyl, halogen, phenoxy, lower alkoxy, teinila, phenyl, is catholicmatch)benzylamino]-4-phenylalanyl acid or its salt.

8. Connection on p. 1, which is selected from the group consisting of E-4-[4-(5-methyl-2-phenyl-4-oxazolidinone)benzylamino] -4-phenyl-butyramide and E-8-[4-(5-methyl-2-phenyl-4-oxazolidinone)benzylamino]-8-phenyloctanoic acid.

9. Connection on p. 1, in which R1represents a

where Ph represents phenyl;
R" represents hydrogen or C1-6alkyl.

10. Connection on p. 1, represented by formula

where R' represents phenyl, furyl or thienyl;
R" represents hydrogen or C1-6alkyl;
R2'represents phenyl, optionally substituted by at least one group selected from C1-6of alkyl, C1-6alkoxy and halogen;
q represents an integer from 1 to 6;
R3'represents hydroxy, C1-6alkoxy or-NR9R10where R9and R10independently selected from the group consisting of hydrogen atom, lower alkyl and lower alkylsulfonyl,
or its salt.

11. Pharmaceutical composition having hypoglycemic and hypolipidemic action, containing the compound of formula (I)

where R1is oxazolyl, optional is substituted by 1-2 substituents, selected from lower alkyl, phenyl; unsubstituted chinoline; 1,2,4-oxadiazolyl, substituted phenyl; imidazo[1,2-a] pyridyl, optionally substituted with halogen or phenyl; pyridyl, optionally substituted lower alkyl; pyrimidyl; isoxazolyl, optionally substituted by phenyl; phenyl;
X represents a bond or the group-NR6- where R6represents hydrogen or C1-4alkyl;
n represents an integer from 1 to 3;
Y represents an oxygen atom or the group-NR7- where R7represents hydrogen;
ring a represents a benzene ring, optionally substituted by one or two1-4alkoxy;
p represents an integer from 1 to 3;
R2represents phenyl, optionally substituted lower alkyl, halogen, phenoxy, lower alkoxy, teinila, phenyl, anilinium or phenylcarbinol; unsubstituted furyl; unsubstituted pyridyl; pyridinyl-1-oxide;
q represents an integer from 0 to 6;
m represents 0 or 1;
R3represents a hydroxy-group, lower alkoxy or-NR9R10where R9and R10represent identical or different groups selected from hydrogen, lower alkyl and lower alkylsulfonyl;
R4and R5are Aiumlamai media.

12. The pharmaceutical composition according to p. 11, which is a composition for prevention or treatment of diabetes.

13. The pharmaceutical composition according to p. 11, which is a composition for prevention or treatment of hyperlipemia.

14. The pharmaceutical composition according to p. 11, which is a composition for the prevention or treatment of impaired glucose tolerance.

15. The pharmaceutical composition according to p. 11, which is a composition for the prevention or treatment of inflammatory diseases.

16. The pharmaceutical composition according to p. 11, which is a composition for prevention or treatment of arteriosclerosis.

17. Means for regulation of retinoid receptors containing the compound represented by the formula

where R1is oxazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl, teinila, furil; thiazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl; unsubstituted chinoline; 1,2,4-oxadiazolyl, substituted phenyl; imidazo[1,2-a] pyridyl, optionally substituted with halogen or phenyl; pyridyl, optionally substituted lower alkyl; pyrimidyl; isoxazolyl, which allows hydrogen or C1-4alkyl;
n represents an integer from 1 to 3;
Y represents an oxygen atom or the group-NR7- where R7represents hydrogen;
ring a represents a benzene ring, optionally substituted by one or two1-4alkoxy;
p represents an integer from 1 to 3;
R2represents phenyl, optionally substituted lower alkyl, halogen, phenoxy, lower alkoxy, teinila, phenyl, anilinium or phenylcarbinol; unsubstituted furyl; unsubstituted pyridyl; pyridinyl-1-oxide;
q represents an integer from 0 to 6;
m represents 0 or 1;
R3represents a hydroxy-group, lower alkoxy or-N9R10where R9and R10represent identical or different groups selected from hydrogen, lower alkyl and lower alkylsulfonyl;
R4and R5represent identical or different groups selected from hydrogen or lower alkyl,
or its salt.

18. Means under item 17, which represents a ligand receptors activated by proliferation peroxisomes.

19. Means under item 17, which represents a ligand retinoid X receptor.

20. Means on p. 17, which is a tool that improves the sensitivity to insuli

 

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