Aminoquinazoline compounds

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) which are protein tyrosine kinase 1B(PTP-1B) inhibitors and can be used in medicinal preparations for treating and preventing diseases related to high concentration of glucose in blood, for example diabetes and obesity. In formula (I) X is a X-1 group or X-2: , where R1 and R2 are each independently selected from a group consisting of hydrogen, lower alkyl, alkoxy-lower alkyl and hydroxyl-lower alkyl, under the condition that, R1 and R2 both represent hydrogen; R3, R4, R6 and R7 are each independently selected from a group consisting of hydrogen, lower alkyl; lower alkyl substituted with halogen or hydroxy; lower alkoxy; lower alkoxy substituted with halogen, hydroxy or lower alkoxy; hydroxyl, halogen, lower alkylthio, lower alkylsufanyl, lower alkylsufanyl, aminosufonyl, cyano, nitro, carbamoyl, lower mono- or dialkylcarbamoyl, lower alkanoyl, benzoyl, phenyl, phenyl substituted with halogen, phenyloxy, lower mono- or dialkylamino, hydroxy-substituted lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, heterocycloalkyl, hydroxy-substituted heterocycloalkyl, heterocyclyloxy, heterocyclylcarbonyl; where each heterocycloalkyl in the said values represents a 5-6-membr ring containing 1-2 heteroatoms selected from nitrogen and oxygen, and which can be substituted with lower alkyl or phenyl-lower alkyl; carboxyl, lower alkoxycarbonyl and a substitute of formula: ; R8 is selected from a group consisting of hydrogen, lower alkylthio, halogen, alkoxy-lower alkoxy, lower alkoxy, halogen-lower alkyl, hydroxy-lower alkyl; represents a 5-member heteroaromatic ring containing 1 or 2 heteroatoms selected from a group consisting of hydrogen, sulphur and nitrogen; R8 and R9 each independently represents hydrogen or lower alkyl.

EFFECT: novel compounds have useful biological properties.

31 cl, 7 dwg, 152 ex

 

The text descriptions are given in facsimile form.

1. The compounds of formula

where X represents a group X-1 formula

or X represents a group X-2 formula

where R1 and R2 each independently selected from the group consisting of hydrogen, lower alkyl, alkoxy-lower alkyl and hydroxy-lower alkyl, provided that R1 and R2 both represent hydrogen;
R3, R4, R6 and R7 each independently selected from the group consisting of hydrogen, lower alkyl; lower alkyl substituted by halogen or hydroxy; lower alkoxy; lower alkoxy substituted by halogen, g is droxy or lower alkoxy; hydroxy, halogen, lower alkylthio, lower alkylsulfonyl, lower alkylsulfonyl, aminosulfonyl, cyano, nitro, carbamoyl, lower mono - or dialkylamino, lower alkanoyl, benzoyl, phenyl, phenyl substituted by halogen, phenyloxy, lower mono - or dialkylamino, replacement lower alkylamino, lower alkanolamine, lower alkylsulfonyl, geterotsiklicheskie, replacement of geterotsiklicheskie, heterocyclics, geterotsiklicheskikh; and each heterophylly in these values represents a 5-6-membered ring containing 1-2 heteroatoms selected from nitrogen and oxygen, and which may be substituted by lower alkyl or phenyl-lower by alkyl; carboxyl, lower alkoxycarbonyl and Deputy formula

R5 is selected from the group consisting of hydrogen, lower alkylthio, halogen, alkoxy-lower alkoxy, lower alkoxy, halogeno-lower alkyl,
hydroxy-lower alkyl; ℗ represents a 5-membered heteroaromatic ring containing 1 or 2 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen;
R8 and R9 each independently represents hydrogen or lower alkyl;
or their pharmaceutically acceptable salts.

2. Compounds according to claim 1, where X represents a group X-1 formula

or X represents a group X-2 formula

where R1 and R2 each independently selected from the group consisting of hydrogen, lower alkyl, alkoxy-lower alkyl and hydroxy-lower alkyl, provided that both R1 and R2 do not represent hydrogen;
R3, R4, R6 and R7 each independently selected from the group consisting of hydrogen; lower alkyl; lower alkyl substituted by halogen or hydroxy; lower alkoxy; alkoxy-lower alkoxy; hydroxy-lower alkoxy; halogen-lower alkoxy; hydroxy, halogen, lower alkylthio, lower alkylsulfonyl, lower alkylsulfonyl, aminosulfonyl, cyano, nitro, carbamoyl, benzoyl, phenyl, phenyloxy, lower mono - or dialkylamino, lower alkanolamine, lower alkylsulfonyl, geterotsiklicheskie, heterocyclics, geterotsiklicheskikh and Deputy formula

R5 is selected from the group consisting of hydrogen, lower alkylthio, halogen, alkoxy-lower alkoxy, lower alkoxy, halogeno-lower alkyl, hydroxy-lower alkyl;
℗ represents a 5-membered heteroaromatic ring containing 1 or 2 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen;
R8 and R9 each independently represents hydrogen or lower alkyl.

3. Compounds according to claim 1 of the formula

where R1, R2, R3, R4, R5, R6, R7 are as defined in claim 1 or 2, or their pharmaceutically acceptable salts.

4. Compounds according to claim 3, where R4, R5 and R6 each independently represents hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl or performansi alkyl.

5. Compounds according to claim 3, where R6 represents hydrogen.

6. Compounds according to claim 3, where R6 and only one of R4 and R6 represents hydrogen.

7. Compounds according to claim 3, where R4, R5 and R6 represent hydrogen.

8. Compounds according to claim 6 wherein R4 or R6 that is not represents hydrogen, represents hydroxy, halogen, lower alkyl, lower alkoxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl or performansi alkyl.

9. Join one of PP 8, wherein R3 and R7 each independently represents hydrogen, halogen, lower alkyl, lower alkoxy, alkoxy-lower alkoxy, nitro, hydroxy, hydroxy-lower alkoxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl and perferibly alkyl.

10. Compounds according to claim 6, where R3 and R7 each independently represents halogen, lower alkyl, lower alkoxy, alkoxy-lower alkoxy, nitro, hydroxy, hydroxy-lower alkoxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl and perferibly alkyl.

11. Connection p is 3, where R1 or R2 represents hydrogen.

12. Compounds according to claim 11, where R1 or R2 is not hydrogen, represents C1-Salkil or hidroxi-Salkil.

13. Compounds according to claim 11 wherein R4, R5 and R6 each independently represents hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl or performansi alkyl.

14. Compounds according to claim 11, where R6 represents hydrogen.

15. Compounds according to claim 11, where R6 and only one of R4 or R6 is a hydrogen.

16. Connections § 15, where R4 or R6 that is not represents hydrogen, represents halogen, lower alkyl, lower alkoxy, hydroxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl or performansi alkyl.

17. Compounds according to claim 11 wherein R4, R5 and R6 represent hydrogen.

18. Connection 17, where R1 or R2 does not represent hydrogen, represent C1-Salkil or hidroxi-Salkil.

19. Compounds according to claim 11, where R3 and R7 each independently represents hydrogen, halogen, lower alkyl, lower alkoxy, alkoxy-lower alkoxy, nitro, hydroxy, hydroxy-lower alkoxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl and perferibly alkyl.

20. Connections § 15, where R3 and R7 each independently represents a halogen, NISS the th alkyl, lower alkoxy, alkoxy-lower alkoxy, nitro, hydroxy, hidrogenesse alkoxy, hydroxy-lower alkyl, lower alkylthio, lower alkylsulfonyl and perferibly alkyl.

21. Connection 17, where R3 and R7 are chlorine, fluorine, trifluoromethyl, C1-Salkil, C1-Saltillo, C1-Sarkilarini, C1-Sarcoxie, C1-Celecoxi substituted by a group selected from hydroxy, methoxy, ethoxy.

22. Compounds according to item 21, where R1 or R2 is not hydrogen, represents C1-Salkil or hidroxi-Salkil.

23. Compounds according to claim 1 of the formula

where R1, R2, R8, R9 and ℗ are as defined in claim 1, or its pharmaceutically acceptable salt.

24. Compounds according to item 23, where R1 or R2 represents hydrogen.

25. Compounds according to item 23, where R8 and R9 each independently represents a lower alkyl.

26. Connection point 24, where R1 or R2 is not hydrogen, represents C1-Salkil or hidroxi-Salkil.

27. Compounds according to claim 1, selected from the group consisting of the following compounds:
7-(2,5-dimetilfenil)-N4-methylpyrazole-2,4-diamine,
N4-methyl-7-(2-triptoreline)hinzelin-2,4-diamine,
N4,N4-dimethyl-7-(2-triptoreline)hinzelin-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-thiophene-2-imaginaton-2,4-diamine, salt with triperoxonane acid,
N4,N4-dimethyl-7-thiophene-2-Ilgin the Zolin-2,4-diamine, salt triperoxonane acid,
N4-methyl-7-o-trilinolein-2,4-diamine,
N4,N4-dimethyl-7-o-trilinolein-2,4-diamine, salt with triperoxonane acid,
7-(2,6-dimetilfenil)-N4-methylpyrazole-2,4-diamine,
7(2,6-dimetilfenil)-N4,N4-dimethylthiazole-2,4-diamine,
N4-ethyl-7-o-trilinolein-2,4-diamine, salt with triperoxonane acid,
N4,N4-diethyl-7-o-trilinolein-2,4-diamine, salt with triperoxonane acid,
N4-propyl-7-o-trilinolein-2,4-diamine, salt with triperoxonane acid,
N4,N4-dipropyl-7-o-trilinolein-2,4-diamine, salt with triperoxonane acid,
7-(2,6-dimetilfenil)-N4-utilisation-2,4-diamine, salt with triperoxonane acid,
7-(2,6-dimetilfenil)-N4,N4-determination-2,4-diamine, salt with triperoxonane acid,
7-(2,6-dimetilfenil)-N4-propylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2,6-dimetilfenil)-N4,N4-dipropionate-2,4-diamine, salt with triperoxonane acid,
N4,N4-dimethyl-7-(2-phenoxyphenyl)hinzelin-2,4-diamine,
7-(2,6-differenl)-N4,N4-dimethylthiazole-2,4-diamine,
7-(2-ethylphenyl)-N4-methylpyrazole-2,4-diamine,
7-(2,6-acid)-N4-methylpyrazole-2,4-diamine,
N4-methyl-7-(1,3,5-trimethyl-1H-pyrazole-4-yl)hinzelin-2,4-diamine,
7-(2,6-differenl)-N4-methylpyrazole-2,4-diamine,
7-(2,6-dichlorophenyl)-N4-methylpyrazole-2,4-diamine,
7-(2-isopropylphenyl)-N4-methylpyrazole-2,4-diamine,
7-(2-isopropylphenyl)-N4,N4-dimethylene the Olin-2,4-diamine,
7-(2-ethylphenyl)-N4,N4-dimethylthiazole-2,4-diamine,
7-(2-bromophenyl)-N4-methylpyrazole-2,4-diamine,
N4-methyl-7-phenylindolin-2,4-diamine, salt with triperoxonane acid,
7-(2'-bromobiphenyl-2-yl)-4-methylpyrazole-2,4-diamine,
N4-methyl-7-o-trilinolein-2,4-diamine,
7-(2-methoxyphenyl)-N4-methylpyrazole-2,4-diamine,
2-[amino-7-(2-ethylsulfanyl)hinzelin-4-ylamino]ethanol,
N4,N4-dimethyl-7-(2,3,5,6-tetramethylene)hinzelin-2,4-diamine,
N4-methyl-7-(2-phenoxyphenyl)hinzelin-2,4-diamine,
2-[2-amino-7-(2,6-dimetilfenil)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2-phenoxyphenyl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,6-dichlorophenyl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,6-differenl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,5-differenl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2-forfinal)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,3-dichlorophenyl)hinzelin-4-ylamino]ethanol,
2-(2-amino-7-o-trilinolein-4-ylamino)ethanol,
7-(2-fluoro-6-methoxyphenyl)-N4-methylpyrazole, 4-diamine,
1-(2-amino-7-o-trilinolein-4-ylamino)propan-2-ol,
3-(2-amino-7-o-trilinolein-4-ylamino)propan-1-ol,
2-(2-amino-7-o-trilinolein-4-ylamino)propan-1-ol,
N4-(2-amino-ethyl)-7-o-trilinolein-2,4-diamine,
[3-(2-amino-4-methylaminophenol-7-yl)phenyl]methanol, salt with triperoxonane acid,
7-(5-isopropyl-2-methoxyphenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane to what slotow,
7-(3-isopropylphenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(3,5-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2-chlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2,5-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-biphenyl-3-yl-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2,3-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-[2-amino-7-(2-triptoreline)hinzelin-4-ylamino]ethanol,
N4-methyl-7-(2-methylsulfinylphenyl)hinzelin-2,4-diamine,
7-biphenyl-2-yl-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(3-methylsulfinylphenyl)hinzelin-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(4-methylsulfinylphenyl)hinzelin-2,4-diamine, salt with triperoxonane acid,
7-(3-ethoxyphenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
3-(2-amino-4-methylaminophenol-7-yl)benzonitrile, salt with triperoxonane acid,
N-[3-(2-amino-4-methylaminophenol-7-yl)phenyl]ndimethylacetamide, salt with triperoxonane acid,
2-(2-amino-4-methylaminophenol-7-yl)benzaldehyde,
7-(3,5-dimethylisoxazol-4-yl)-N4-methylpyrazole-2,4-diamine,
N-[3-(2-amino-4-methylaminophenol-7-yl)phenyl]methanesulfonamide, salt with triperoxonane acid,
7-(4-utils llanerfyl)-N4-methylpyrazole-2,4-diamine, salt triperoxonane acid,
7-(4-fluoro-2-were)-N4-methylpyrazole-2,4-diamine,
2-(2-amino-4-methylaminophenol-7-yl)benzonitrile,
7-(2-methanesulfonyl)-N4-methylpyrazole-2,4-diamine,
7-(2-methanesulfonyl)-N4-methylpyrazole-2,4-diamine,
7-(2,6-dimetilfenil)hinzelin-4-ylamino]propan-2-ol, salt with triperoxonane acid,
1-[2-amino-7-(2,6-dichlorophenyl)hinzelin-4-ylamino]propan-2-ol, salt with triperoxonane acid,
2-[2-amino-7-(2-methylsulfinylphenyl)hinzelin-4-ylamino]ethanol,
2-[2-amino-4-(2-hydroxyethylamino)hinzelin-7-yl]benzonitrile,
2-[2-amino-7-(2-methanesulfonyl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2-methanesulfonyl)hinzelin-4-ylamino]ethanol,
2-(2-amino-4-methylaminophenol-7-yl)-N-hydroxybenzamide,
N-[2-(2-amino-4-methylaminophenol-7-yl)phenyl]methanesulfonamide,
7-(2-ethylsulfanyl)-N4-methylpyrazole-2,4-diamine,
7-(2-ethanolgasoline)-N4-methylpyrazole-2,4-diamine,
7-[2-(4-benzylpiperazine-1-yl)-6-forfinal]-N4-methylpyrazole-2,4-diamine,
7-(2-fluoro-6-pyrrolidin-1-ylphenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(2-pyrrolidin-1-yl-6-triptoreline)hinzelin-2,4-diamine,
N4-methyl-7-(2-methylsulfanyl-6-triptoreline)hinzelin-2,4-diamine,
[2-(2-amino-4-methylaminophenol-7-yl)-3-were]methanol,
7-(2-ethylsulfanyl-6-triptoreline)-N4-matilha azolin-2,4-diamine,
7-(2-chloro-6-were)-N4-methylpyrazole-2,4-diamine,
7-(2,6-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt
triperoxonane acid,
7-(3,5-debtor-2-pyrrolidin-1-ylphenyl)-N4-methylpyrazole-2,4-diamine,
7-[2-(2-methoxyethoxy)phenyl]-N4-methylpyrazole-2,4-diamine,
N4-methyl-7-[2-(2,2,6,6-tetramethylpiperidine-4-yloxy)phenyl]hinzelin-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(2,4,6-tryptophanyl)hinzelin-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-[2,4,6-Tris(2-methoxyethoxy)phenyl]hinzelin-2,4-diamine, salt with triperoxonane acid,
7-[4-chloro-2,3,5,6-tetrakis(2-methoxyethoxy)phenyl]-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-[4-chloro-2-(2-methoxyethoxy)phenyl]-N4-methylpyrazole-2,4-diamine,
1-[2-(2-amino-4-methylaminophenol-7-yl)-5-chlorophenyl]piperidine-4-ol,
2-(2-amino-4-methylaminophenol-7-yl)-3-methylbenzamide,
2-(2-amino-4-methylaminophenol-7-yl)-3,N,N-trimethylbenzene,
2-(2-amino-4-methylaminophenol-7-yl)-3,N-dimethylbenzamide,
2-(2-amino-4-methylaminophenol-7-yl)-N-ethyl-3-methylbenzamide,
7-(4-chloro-2-ethoxyphenyl)-N4-methylpyrazole-2,4-diamine,
7-(2-ethoxy-6-fluoro-4-methoxyphenyl)-N4-methylpyrazole-2,4-diamine,
7-(2-ethoxy-4-triptoreline)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2-ethoxy-6-triptoreline)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-(2-what Mino-4-methylaminophenol-7-yl)-N,N-diethyl-3-methylbenzamide,
1-[2-(2-amino-4-stramenopiles-7-yl)phenyl]alanon,
2-[2-(2-amino-4-methylaminophenol-7-yl)phenyl]ethanol,
7-(2-fluoro-4,6-acid)-N4-methylpyrazole-2,4-diamine,
7-[2-(2-methoxyethoxy)-4-triptoreline]-N4-methylpyrazole-2,4-diamine,
7-[6-fluoro-4-methoxy-2-(2-methoxyethoxy)phenyl]-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-(2-amino-4-methylaminophenol-7-yl)-3,N-dimethyl-N-propylbenzamide,
2-[2-(2-amino-4-methylaminophenol-7-yl)-3-triptoreline]ethanol,
[2-(2-amino-4-methylaminophenol-7-yl)phenyl]phenylmethanone,
N-[2-(2-amino-4-methylaminophenol-7-yl)phenyl]acetamide", she
7-(2-deformational)-N4-methylpyrazole-2,4-diamine,
[2-(2-amino-4-methylaminophenol-7-yl)-3-were]piperidine-1-ylmethanone,
2-[2-(2-amino-4-methylaminophenol-7-yl)-3-triptoreline]ethanol,
2-(2-amino-4-methylaminophenol-7-yl)-N,N[-dimethylbenzenesulfonamide,
2-(2-amino-4-methylaminophenol-7-yl)benzosulfimide,
3-[2-(2-amino-4-methylaminophenol-7-yl)-3-triptoreline]propane-1,2-diol,
7-[2-(2-methoxyethoxy)-6-triptoreline]-N4-methylpyrazole-2,4-diamine,
7-[5-fluoro-4-methoxy-3-(2-methoxyethoxy)phenyl]-N4-methylpyrazole-2,4-diamine,
2-(2-amino-4-methylaminophenol-7-yl)benzosulfimide,
N-methyl-2-(2-amino-4-methylaminophenol-7-yl)benzosulfimide,
7-[6-fluoro-2-(2-hydroxyethoxy)fennel]-N4-methylpyrazole-2,4-diam is h,
7-[2-(2,2-dimethyl-[1,3]dioxolane-4-ylethoxy)-6-forfinal]-N4-methylpyrazole-2,4-diamine, cleaners containing hydrochloride salt,
3-[2-(2-amino-4-methylaminophenol-7-yl)-3-fervency]propane-1,2-diol,
2-[2-(2-amino-4-methylaminophenol-7-yl)-5-fervency]ethanol,
2-[2-amino-4-(2-hydroxyethylamino)hinzelin-7-yl]-3,N,N-trimethylbenzene, salt with triperoxonane acid,
N-{2-[2-amino-4-(2-hydroxyethylamino)hinzelin-7-yl]phenyl}methanesulfonamide, salt with triperoxonane acid,
2-(2-amino-4-methylaminophenol-7-yl)benzoic acid, salt with triperoxonane acid,
2-(N4-methyl-2,4-diaminoquinazoline-7-yl)benzamid,
methyl ester 2-(2-amino-4-methylaminophenol-7-yl)benzoic acid
7-(2-fluoro-6-triptoreline)-N4-methylpyrazole-2,4-diamine,
7-(2,6-bistrifluormethylbenzene)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(2-methyl-6-nitrophenyl)hinzelin-2,4-diamine, salt with triperoxonane acid,
methyl ester 2-(2-amino-4-methylaminophenol-7-yl)-3-methylbenzoic acid,
2-(2-amino-4-methylaminophenol-7-yl)-3-methylbenzoic acid,
[4-(2-amino-4-methylaminophenol-7-yl)-2-pyrrolidin-1-ylphenyl]methanol, salt with triperoxonane acid,
7-(3,5-debtor-2-ethoxyphenyl)-N4-methylpyrazole-2,4-diamine,
2-[2-amino-7-(2-methylsulfanyl-6-triptoreline)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,6-bis-methylsulfinylphenyl)hinzelin--ylamino]ethanol,
7-(2,6-balticuniversity)-N4-methylpyrazole-2,4-diamine and
7-(2-methanesulfonyl-6-triptoreline)-N4-methylpyrazole-2,4-diamine,
and their pharmaceutically acceptable salts, if they (salt) not stated above.

28. Compounds according to claim 1, selected from the group consisting of the following compounds:
7-(2,5-dimetilfenil)-N4-methylpyrazole-2,4-diamine,
N4-methyl-7-(2-triptoreline)hinzelin-2,4-diamine,
N4-methyl-7-o-trilinolein-2,4-diamine,
7-(2,6-dimetilfenil)-N4-methylpyrazole-2,4-diamine,
7-(2,6-dimetilfenil)-N4,N4-dimethylthiazole-2,4-diamine,
7-(2,6-dimetilfenil)-N4-utilisation-2,4-diamine, salt with triperoxonane acid,
7-(2,6-dimetilfenil)-N4-propylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2-ethylphenyl)-N4-methylpyrazole-2,4-diamine,
7-(2,6-acid)-N4-methylpyrazole-2,4-diamine,
7-(2,6-differenl)-N4-methylpyrazole-2,4-diamine,
7-(2,6-dichlorophenyl)-N4-methylpyrazole-2,4-diamine,
7-(2-isopropylphenyl)-N4-methylpyrazole-2,4-diamine,
7-(2-bromophenyl)-N4-methylpyrazole-2,4-diamine,
7-(2'-bromobiphenyl-2-yl)-4-methylpyrazole-2,4-diamine,
2-[amino-7-(2-ethylsulfanyl)hinzelin-4-ylamino]ethanol,
N4-methyl-7-(2-phenoxyphenyl)hinzelin-2,4-diamine,
2-[2-amino-7-(2,6-dimetilfenil)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,6-dichlorophenyl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2-forfinal)hinzelin-4-ylamino]ethanol,
2-(2-amino-7-o-tomilinson is n-4-ylamino)ethanol,
7-(2-fluoro-6-methoxyphenyl)-N4-methylpyrazole-2,4-diamine,
2-(2-amino-7-o-trilinolein-4-ylamino)propan-1-ol,
[3-(2-amino-4-methylaminophenol-7-yl)phenyl]methanol, salt with triperoxonane acid,
7-(2-chlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2,5-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
7-(2,3-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-[2-amino-7-(2-triptoreline)hinzelin-4-ylamino]ethanol,
N4-methyl-7-(2-methylsulfinylphenyl)hinzelin-2,4-diamine,
7-biphenyl-2-yl-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-(2-amino-4-methylaminophenol-7-yl)benzaldehyde,
7-(3,5-dimethylisoxazol-4-yl)-N4-methylpyrazole-2,4-diamine,
7-(4-fluoro-2-were)-N4-methylpyrazole-2,4-diamine,
2-(2-amino-4-methylaminophenol-7-yl)benzonitrile,
7-(2-methanesulfonyl)-N4-methylpyrazole-2,4-diamine,
7-(2-methanesulfonyl)-N4-methylpyrazole-2,4-diamine,
2-[2-amino-7-(2-methylsulfinylphenyl)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2-methanesulfonyl)hinzelin-4-ylamino]ethanol,
2-(2-amino-4-methylaminophenol-7-yl)-N-hydroxybenzamide,
N-[2-(2-amino-4-methylaminophenol-7-yl)phenyl]methanesulfonamide,
7-(2-ethylsulfanyl)-N4-methylpyrazole-2,4-diamine,
7-(2-ethanolgasoline)-N4-methylpyrazole-2,4-diamine,
7-[2-(4-bentilee Azin-1-yl)-6-forfinal]-N4-methylpyrazole-2,4-diamine,
7-(2-fluoro-6-pyrrolidin-1-ylphenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(2-pyrrolidin-1-yl-6-triptoreline)hinzelin-2,4-diamine,
N4-methyl-7-(2-methylsulfanyl-6-triptoreline)hinzelin-2,4-diamine,
[2-(2-amino-4-methylaminophenol-7-yl)-3-were]methanol,
7-(2-ethylsulfanyl-6-triptoreline)-N4-methylpyrazole-2,4-diamine,
7-(2-chloro-6-were)-N4-methylpyrazole-2,4-diamine,
7-(2,6-dichlorophenyl)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-(2-amino-4-methylaminophenol-7-yl)-3-methylbenzamide,
2-(2-amino-4-methylaminophenol-7-yl)-3,N,N-trimethylbenzene,
2-(2-amino-4-methylaminophenol-7-yl)-3,N-dimethylbenzamide,
2-(2-amino-4-methylaminophenol-7-yl)-1N-ethyl-3-methylbenzamide,
7-(2-ethoxy-6-triptoreline)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
2-(2-amino-4-methylaminophenol-7-yl)-N,N-diethyl-3-methylbenzamide,
1-[2-(2-amino-4-methylaminophenol-7-yl)phenyl]alanon,
2-[2-(2-amino-4-methylaminophenol-7-yl)phenyl]ethanol,
2-(2-amino-4-methylaminophenol-7-yl)-3,N-dimethyl-N-propylbenzamide,
2-[2-(2-amino-4-methylaminophenol-7-yl)-3-triptoreline]ethanol,
[2-(2-amino-4-methylaminophenol-7-yl)phenyl]phenylmethanone,
7-(2-deformational)-N4-methylpyrazole-2,4-diamine,
[2-(2-amino-4-methylaminophenol-7-yl)-3-were]piperidine-1-ylmethanone br/> 2-[2-(2-amino-4-methylaminophenol-7-yl)-3-triptoreline]ethanol,
2-(2-amino-4-methylaminophenol-7-yl)-N,N-dimethylbenzenesulfonamide,
2-(2-amino-4-methylaminophenol-7-yl)benzosulfimide,
3-[2-(2-amino-4-methylaminophenol-7-yl)-3-triptoreline]propane-1,2-diol,
7-[2-(2-methoxyethoxy)-6-triptoreline]-N4-methylpyrazole-2,4-diamine,
2-(2-amino-4-methylaminophenol-7-yl)benzosulfimide,
N-methyl-2-(2-amino-4-methylaminophenol-7-yl)benzosulfimide,
7-[6-fluoro-2-(2-hydroxyethoxy)phenyl]-N4-methylpyrazole-2,4-diamine,
7-[2-(2,2-dimethyl-[1,3]dioxolane-4-ylethoxy)-6-forfinal]-N4-methylpyrazole-2,4-diamine, cleaners containing hydrochloride salt,
3-[2-(2-amino-4-methylaminophenol-7-yl)-3-fervency]propane-1,2-diol,
2-(N4-methyl-2,4-diaminoquinazoline-7-yl)benzamid,
methyl ester 2-(2-amino-4-methylaminophenol-7-yl)benzoic acid
7-(2-fluoro-6-triptoreline)-N4-methylpyrazole-2,4-diamine,
7-(2,6-bistrifluormethylbenzene)-N4-methylpyrazole-2,4-diamine, salt with triperoxonane acid,
N4-methyl-7-(2-methyl-6-nitrophenyl)hinzelin-2,4-diamine, salt with triperoxonane acid,
methyl ester 2-(2-amino-4-methylaminophenol-7-yl)-3-methylbenzoic acid,
2-[2-amino-7-(2-methylsulfanyl-6-triptoreline)hinzelin-4-ylamino]ethanol,
2-[2-amino-7-(2,6-balticuniversity)hinzelin-4-ylamino]ethanol,
7-(2,6-balticuniversity)-N4-metil is Natolin-2,4-diamine
7-(2-methanesulfonyl-6-triptoreline)-N4-methylpyrazole-2,4-diamine,
and their pharmaceutically acceptable salts, if they (salt) not stated above.

29. Pharmaceutical composition having the properties of inhibitors of PTP-1B containing the compound according to any one of claims 1 to 28 and a pharmaceutically acceptable carrier and/or adjuvant.

30. Compounds according to claim 1, having the properties of inhibitors of PTP-1B to obtain the drug.

31. Compounds according to claim 1 for use as therapeutic active substances for the treatment and/or prevention of diseases which are modulated by inhibitors of PTP-1B.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a combined product containing compounds of formula (I): where: R1 and R2 represent CF3; R3 and R4 represent fluoro; R5 and R6 represent hydrogen; R7 presents Cl, X represents CR8, where R8 represents Cl; and R9 represents NH2; or its veterinary acceptable salt, and b) doramectin. The invention also relates to an antiparasitic veterinary composition based on the said combined product.

EFFECT: obtaining a combined product which can be used in veterinary for treating parasitic infections in mammals.

4 cl, 1 dwg, 1 tbl, 37 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (I) or to salts thereof: , where R1 is a hydrogen atom, amino group, R11-NH-, where R11 is a C1-6alkyl group, hydroxy-C1-6alkyl group, C1-6alkoxycarbonyl-C1-6alkyl group, R12-(CO)-NH-, where R12 is a C1-6alkyl group or C1-6alkoxy-C1-6alkyl group, C1-6alkyl group, hydroxy-C1-6-alkyl group, C1-6alkoxy group or C1-6alkoxy-C1-6alkyl group; R2 is a hydrogen atom, C1-6alkyl group, amino group or di-C1-6alkylamino group; one of X and Y represents a nitrogen atom, while the other represents a nitrogen or oxygen atom; ring A is a 5- or 6-member heteroaryl ring or benzene ring which can have 1 or 2 halogen atoms; Z is a single bond, methylene group, ethylene group, oxygen atom, sulphur atom, -CH2O-, -OCH2-, -NH-, -CH2NH-, -NHCH2-, -CH2S- or -SCH2-; R3 is hydrogen or a halogen atom, or C1-6alkyl group, C3-8cycloalkyl group, C6-10aryl group, 5- or 6-member heteroaryl group, where these groups can have 1 or 2 substitutes selected from a group of α substitutes: and [group of α substitutes] group of α substitutes is a group consisting of a halogen atom, cyano group, C1-6alkyl group, C1-6alkoxy group, C1-6alkoxycarbonyl group, C3-8cycloalkyl group, C1-6alkenyl group and C1-6alkynyl group; R4 is a hydrogen atom or halogen atom; except compounds in which all of R1, R2 and R4 represent a hydrogen atom while Z represents a single bond or R3 is a hydrogen atom; as well as a pharmaceutical composition and a medicinal agent with antifungal activity, based on these compounds, to an antifungal agent and use of formula I compounds for preparing an antifungal agent.

EFFECT: novel compounds with excellent antifungal effect are obtained and described.

36 cl, 228 ex, 8 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzyloxy-derivatives of general formula (I) , where R1 is a halogen; R2 is a 5-member heteroaryl group containing 2 or 3 heteroatoms selected from a group consisting of N, O or S, which can be substituted with R3, where R3 is a lower alkyl or -C(O)R; R is -NR'R" or lower alkoxy; R'/R" independently represent H; as well as to their pharmaceutically acceptable salts. Formula I compounds inhibit monoamine oxidase B.

EFFECT: compounds can be used for preparing a medicinal agent.

5 cl, 15 ex

FIELD: pharmacology.

SUBSTANCE: described are enantiomer-free compounds with a general formula of (1) wherein the R1, R2, R3, R4 and X- residue may have as specified in the invention formula, intermediary compounds, a pharmaceutical composition as well as their application in the capacity of medications intended for respiratory tract diseases treatment.

EFFECT: new enantiomer-free b-agonists, their preparation method and application in the capacity of medications.

11 cl, 5 dwg, 3 tbl, 37 ex

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of aryl and heteroarylpiperidinecarboxylates, of formula (I): , where: type means integer numbers from 1 to 3, such that m+n is integer number from 2 to 5; p means integer number from 1 to 7; A means simple connection or is selected from one or several groups X, Y; X means -CH2-; Y means C2-alkynilene group; R1 means group R5, substituted with one or several groups R6 and/or R7; R2 means H, F, OH; R3 means H; R4 means H, C1-6-alkyl; R5 means group selected from phenyl, pyridinyl, pyrimidinyl, pyrrolyl, imidazolyl, thiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, naphthyl, chinolynyl, tetrahydrochinolinyl, isochinolinyl, tetrahydroisochinolinyl, indolyl, indolinyl, isoindolyl, benzimidazolyl, benzoxazolyl, benzizoxazolyl, benzothiazolyl, benzithiazolyl, benzotriazolyl, benzoxadiazolyl, pyrrolopyridinyl; R6 means halogen, CN, C1-6-alkyl, C3-7-cycloalkyl, C1-6-alkoxy, OH, C1-6-fluoroalkyl, C1-6-fluoroalkoxy, or cycle selected from pyrrolidine and piperidine cycle, besides this cycle is unnecessarily substituted with C1-6-alkyl group; R7 means phenyl group, besides group or groups R7 may be substituted with one or several groups R6, identical or differing from each other, selected from halogen, C1-6-alkyl and C1-6-fluoroalkyl, C1-6-alkoxy, in the form of pharmaceutically acceptable base or acid-additive salt.

EFFECT: compounds are applicable as inhibitors of FAAH ferment.

10 cl, 1 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention is related to new heterocyclic compounds of common formula (I), and also their pharmaceutically acceptable salts, hydrates and/or solvates, possessing properties of human neutrophil elastase. In common formula (I) , A means phenyl or pyridyl cycle, R1 and R3 each means atom of hydrogen, R2 means atom of fluorine, chlorine, bromine, nitro group or cyano group, R4 means cyano group, alkyl carbonyl group with number of carbon atoms in alkyl residue from one to four, or alkoxycarbonyl group with number of carbon atoms in alkoxyl residue from one to four, besides alkoxycarbonyk group with number of carbon items in alkoxyl residue from one to four, may be substituted with substituent, which is selected from the group that includes hydroxyl group, alkoxygroup with number of carbon atoms from one to four, alkoxycarbonyl group with number of carbon atoms in alkoxyl residue from one to four, mono- or dialkylaminogroup, with number of carbon atoms in each of alkyl residues from one to four, 5-6-member heteroaryl group, which contains from 1 to 4 heteroatoms in heteroaryl ring, selected from nitrogen, oxygen or sulfur, possibly susbstituted with alkyl group, which contains from 1 to 4 atoms of carbon and possibly condensed with benzene ring, and 5-8 member heterocyclyl group, which contains from 1 to 3 heteroatoms from group of nitrogen, oxygen or sulfur, or SO, SO2 possibly substituted with ketogroup, R5 means methyl group, R6 means atom of hydrogen, alkyl group with number of carbon atoms from one to four, mono- or dialkylaminocarbonyl group with number of carbon atoms in each of alkyl residues from one to four, etc., Y1, Y2, Y3, Y4 and Y5 each means CH-group. Invention is also related to pharmaceutical composition.

EFFECT: possibility of application for treatment of chronic obstructive lung diseases, acute coronary syndrome, acute myocardial infarction and progressing cardiac decompensation.

8 cl, 1 dwg, 111 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 2-heteroaryl derivatives of benzothiazole and benzoxazole of formula by boiling amine with general formula with acid chloride of general formula , where R=2-furyl or 2-thienyl, X = S or O, in 1-methyl-2-pyrrolidone.

EFFECT: method increases output of product to 78 to 90% and environmental friendliness of the process.

1 cl, 2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I-a), where R1 and R2, each independently, represent -COORA (where RA is hydrogen or C1-8 alkyl), -CONRBSO2RC (where RB is hydrogen or C1-8 alkyl, RC is C1-8 hydrocarbon), -D-R1 is -CO-(CH2)2-R1, -CO-(CH2)3-R1, -CO-(CH2)4-R1 or C1-4alkylene-R1; E is a bond or C1-4alkylene; ring formula represents a 3,4-dihydro-2H-1,4-benzoxazine or 1H-indole ring; V is , where R110 is hydrogen or C1-8 alkyl, and the arrow shows that it is bonded to ring A; the group with formula is a phenyl group, which can contain a group with formula , where ring 2 is a C5-10 mono- or bicyclic aromatic carbocyclic ring, which can be partially or completely saturated, spirobicyclic carbocyclic ring, or a carbocyclic ring bonded by a bridge bond; where W is -O-CH2-, -O-(CH2)2, -O-(CH2)3, -O-(CH2)4, -O-(CH2)5, -CH2-O, -(CH2)2-O-, -(CH2)3-O-, -(CH2)4-O-, -(CH2)5-O-, -O-(CH2)3-O-, -O-(CH2)4-O-, -O-(CH2)5-O-, C1-6 alkylene, its N-oxide, its salt or its solvate. The invention also relates to a pharmaceutical composition based on formula I-a compound and its use.

EFFECT: obtaining new derivatives of benzoxazine and indole, with antagonistic effect on cysLT2 and which are useful for preventing and/or curing respiratory diseases, such as bronchial asthma, chronic obstructive lung diseases.

8 cl, 57 tbl, 261 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new benzimidazole derivatives with general formula (I), where A represents -CH2-, -C(O), -C(O)-C(Ra)(Rb)-, X represents a -CH- radical; Ra and Rb independently represent a hydrogen atom or (C1-C6)alkyl radical; R1 represents a hydrogen atom or (C1-C8)alkyl radical; R2 represents a (C1-C8)alkyl radical; R3 represents -(CH2)P-Z3, -C(O)-Z'3 or -C(O)-NH-Z"3; Z3 represents (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)alkoxy, (C1-C6)alkylcarbonyl, (C1-C6)alkoxycarbonyl, (C1-C6)alkyl-N(RN)carbonyl, (C3-C7)cycloalkyl, aryl, arylthio or heteroaryl radical, Z3 is bonded to the -(CH2)P- through a carbon atom, heteroaryl radical, which is a 5-10- member heteroaryl, which contains 1-2 identical or different heteroatoms, chosen from sulphur, nitrogen or oxygen, and optionally substituted with one or more identical or different substitutes, chosen from halogen, nitro group or -(CH2)P'-V30-Y3; aryl radical, chosen from phenyl or naphthyl, optionally substituted with one or more identical or different substitutes, chosen from halogen, nitro group, cyano group, (C2-C6)alkenyl, pyrrolidinyl, phenyl, phenyloxy, phenylalkyloxy, 5-7- member heteroaryl, containing 1-3 nitrogen atoms and -(CH2)p'-V31-Y3; V30 represents -O-, -C(O)-, -C(O)-O- or a covalent bond; V31 represents -O-, -S-, -SO2-, -C(O)-, -C(O)-O-, -N(RN)-, -NH-C(O)- or a covalent bond; Y3 represents a hydrogen atom or (C1-C6)alkyl radical, optionally substituted with one or more identical or different halogen radicals; RN represents a hydrogen atom or (C1-C6)alkyl radical; Z3 represents a radical with a given formula (see below); Z'3 represents a phenyl radical, optionally substituted with one ore more identical or different substitutes, chosen from -(CH2)P"-V'3-Y'3; V'3 represents -O-; Y'3 represents a hydrogen atom or (C1-C6)alkyl radical; Z"3 represents a hydrogen atom or -(CH2)q-A"3 radical; A"3 represents (C1-C6)alkyl, phenyl or thienyl radical; alkyl or phenyl radical can be optionally substituted with one or more identical or different substitutes, chosen from halogen and -V"3-Y"3; V"3 represents -O-, -C(O)-, -C(O)-O- or a covalent bond; Y"3 represents a hydrogen atom or (C1-C6)alkyl radical; p is an integer from 0 to 6; p' and p" independently represent an integer from 0 to 1; q is an integer from 0 to 2; R4 represents a radical with formula -(CH2)S-R'4; R'4 represents a 5-7- member heterocycloalkyl, containing at least one nitrogen atom and optionally substituted with (C1-C6)alkyl; or a radical with formula -NW4W'4; W4 represents a hydrogen atom; W'4 represents a hydrogen atom; s is an integer from 0 to 6; in racemic or enantiomeric form or any combination of the said forms, or its pharmaceutically acceptable salt. The invention also relates to a method of obtaining a compound in paragraph 1, a pharmaceutical composition based on the said compound and its use in making a medicinal agent.

EFFECT: new benzimidazole derivatives have good affinity to certain subtypes of melanocortin receptors.

26 cl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new pyrimidine derivatives with general formula (I), their tautomeric or stereoisomeric form, in free form, in form of pharmaceutically acceptable salt or C1-6alkyl ester which are effective antagonists of CRTH2 (G-protein-associated chemoattractant receptor, ex prone on Th2 cells) and can be used for preventing and treating diseases related to CRTH2 activity, particularly in treatment of allergic diseases such as asthma, allergic rhinitis, atopic dermatitis, diseases related to eosinophil. In formula (I) R1 is hydrogen, or in which n is an integer from 0 to 6; -Q1- is -NH-, -N(C1-6alkyl)- or -O; Y is hydrogen, C1-6alkyl, C3-6cycloalkyl, optionally substituted with C1-6alkyl, C3-6cycloalkyl, condensed with a benzene ring, phenyl, naphthyl or 5-6-member heteroaryl, possibly condensed with a benzene ring, and containing at least one heteroatom, chosen from a group consisting of oxygen and nitrogen, where the said phenyl, naphthyl or heteroaryl are optionally substituted on the displaceable position with one or several substitutes, chosen from a group consisting of cyano, halogen, nitro, guanidine, pyrroyl, sulfamoyl, phenyloxy, phenyl, di(C1-6)alkylamino, C1-6alkanoylamino, C1-6alkyl, optionally mono-, di- or tri-substituted with halogen, C1-6alkoxy, optionally mono-, di- or tri-substituted with halogen and C1-6alkylthio, optionally mono-, di- or tri-substituted with halogen; or phenyl, condensed with 1,3-dioxolane; R2 is hydrogen or C1-6alkyl; R3 is a halogen, C1-6alkoxy, optionally mono-, di- or tri-substituted with halogen, or , R3a and R3b are independently C3-8cycloalkyl or C1-6alkyl, this C1-6alkyl is optionally substituted with hydroxyl, carboxy, C3-6cycloalkylcarbamoyl, C5-6heterocyclocarbonyl containing a heteroatom in form of nitrogen, or C1-6alkoxy, q is an integer from 1 to 3; R3c is hydrogen, hydroxyl or carboxy; Xa is -O-; R4 is hydrogen, halogen, di(C1-6alkyl) amino or C1-6alkyl, optionally substituted C1-6alkoxy or mono- , di- or tri-substituted with halogen; R5 is hydrogen or C1-6alkyl; and R6 is carboxy, carboxamide, nitrile or tetrazolyl.

EFFECT: wider field of use of compounds.

32 cl, 9 tbl, 13 ex

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of benzoindazole of formula I , where radicals A1, A2, A3, R1, R2, R3, R4 and n have values mentioned in formula of invention, and their pharmaceutically acceptable salts, and also to application of these compounds for production of medicinal agent intended for modulation of α2-subsort of GABA receptor, and pharmaceutical composition that contains it.

EFFECT: application of compounds for preparation of medicinal agent intended for treatment of depression, disorder in the form of anxiety, psychic disorder, disturbed ability to learning and cognition, sleep disturbance, disorder in the form of cramps or fits or pain.

16 cl, 5 tbl, 40 ex

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of common formula (I) , in which: A, if available, means (C1-C6)-alkyl; R1 means group NR6R7, (C4-C7)-azacycloalkyl, (C5-C9)-azabicycloalkyl, besides, these groups, unnecessarily, are substituted with one or more substituents, selected from (C1-C5)-alkyl or halogen; A-R1 is such that nitrogen of radical R1 and nitrogen in position 1 of pyrazole are necessarily separated at least by two atoms of carbon; R3 means radical H, OH, NH2, ORc, NHC(O)Ra or NHSO2Ra; R4 means phenyl or heteroaryl, unnecessarily, substituted with one or more substituents, selected from halogen, CN, NH2, OH, ORc, C(O)NH2, phenyl, polyfluoroalkyl, linear or ramified (C1-C6)-alkyl, besides these substituents, unnecessarily, are substituted with halogen, and moreover, heteroaryl radicals are 3-10-member, containing one or more heteroatoms, selected from sulphur or nitrogen; R5 means radical H, linear or ramified (C1-C6)-alkyl; Ra means linear or ramified (C1-C6)-alkyl; Rc means linear or ramified (C1-C6)-alkyl, (poly)fluoroalkyl or phenyl; R6 and R7, independently from each other, means hydrogen, (C1-C6)-alkyl; R6 and R7 may create 5-, 6- or 7-member saturated or non-saturated cycle, which includes one heteroatom, such as N, and which, unnecessarily, substituted with one or more atoms of halogen; to its racemates, enantiomers, diastereoisomers and their mixtures, to their tautomers and their pharmaceutically acceptable salts, excluding 3-(3-pyridinyl)-1H-pyrazole-1- butanamine, 4-(3-pyridinyl)-1H-pyrazole-1-butanamine and N-(diethyl)-4-phenyl-1H-pyrazole-1-ethylamine. Invention is also related to methods for production of compounds of formula (I) and to pharmaceutical composition intended for treatment of diseases that appear as a result of disfunction of nicotine receptors α7 or favorably responding to their modulation, on the basis of these compounds.

EFFECT: production of new compounds and pharmaceutically acceptable composition on their basis, which may find application in medicine for treatment, prophylaxis, diagnostics and observance over development of psychiatric or neurological disorders or diseases of central nervous system, when cognitive functions deteriorate or quality of sensor information processing drops.

16 cl, 106 ex

FIELD: medicine.

SUBSTANCE: invention is related to compound of formula (I), (values of radicals are described in formula of invention) or its pharmaceutically acceptable salts, to methods of its production, pharmaceutical composition, which contains it. Application of invention is described for manufacturing of medicinal agent intended for provision of inhibiting action in respect to HDAC in warm-blooded animal, in production of agent used for treatment of malignant tumor. Method is also described for provision of inhibiting action in warm-blooded animal.

EFFECT: compounds have inhibiting activity in respect to HDAC.

15 cl, 17 tbl, 24 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to use of compounds of formula (I) where R1 is lower alkyl or halogen; R2 is hydrogen or halogen; R3 is (CHR')nOH, phenyl, possibly substituted with a -(CHR')nOH group, or is a saturated, partially saturated or aromatic 5- or 6-member heterocyclic ring with one heteroatom, selected from a group which consists of -N(R4)-, -N=, -S- or -S(O)2, where the rings are possibly substituted with a -(CHR')nOH group; R' is hydrogen or a -(CH2)nOH, independent of the value of n; R4 is hydrogen, -S(O2)-lower alkyl group or -C(O)-lower alkyl; X is -O-, -CH2O-, -S- or a bond; n equals 1 or 2; or their pharmaceutically active acid addition salts for making medicine for treating schizophrenia, as well as to compounds of formula (I).

EFFECT: description is given of compounds which can be used in medicine.

8 cl, 16 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: new 5-sulphanyl-4H-1,2,4-triazole derivatives of general formula I (meaning of radicals R1-R3 are indicated in the description of the invention), methods of their preparation by liquid-phase parallel synthesis and pharmaceutical composition are claimed.

EFFECT: claimed compounds display high affinity to some subtypes of somostatin receptors of the SST2 and SST5 subtypes and possibility of their usage for treatment of pathological states or diseases involving one or more of the given somostatin receptors

9 cl, 708 ex

FIELD: chemistry; medicine.

SUBSTANCE: in novel triazole derivatives of general formula I or their pharmaceutically acceptable salts R4 is hydrogen; X is selected from group, consisting of single bond, NH- and groups: , values of R1-R3 radicals are given in description, pharmaceutical composition containing them, and application of novel compounds for obtaining medication for treating hyperglycemia, insulin-resistance, type 2 diabetes, fat exchange derangements, obesity, atheroslerosis and metabolic syndrome.

EFFECT: medications possess higher efficiency.

26 cl, 8 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: claimed invention relates to compounds of formula (I), their obtaining and application as elastase inhibitors, and can be applied in medicine, where Y = CH; R№ represents H or alkyl; RІ represents phenyl or 5-6-memner heteroaryl, G1 represents phenyl; R5 represents H, halogen, alkyl, CN or fluorinated alkyl; n=1-3; R4 = H; L represents bond, O, NR29 or alkyl; or R4 and L are bound together in such way that group -NR4L- represents 5-7-member asacyclic ring; G2 represents phenyl, 5-6-member heteroaryl, cycloalkyl, C4-7-heterocycle, bicycle from two condensed, bound with direct bond or separated with O atom rings, selected from phenyl, 5-6-member heteroaryl, cycloalkyl or C4-7-heterocycle; or when L does not represent bond, G2 represents H; s = 0-2; R25 represents H, alkyl or cycloalkyl; R29 represents H or alkyl.

EFFECT: obtaining novel biologically active compounds.

10 cl, 95 ex, 1 tbl

FIELD: chemistry; pharmacology.

SUBSTANCE: invention refers to new benzofuran and benzothiophen derivatives of general formula I, , wherein X is chosen from O and S; R1 is chosen from H, (C1-C6)alkyl, C(O)(C1-C6) alkyl and benzoyl; R2 is chosen from phenyl optionally substituted with 1 or 2 substitutes, each independently chosen from CN, NO2, (C1-C6)alkyl, (C1-C6)alkoxy, halogen, halogen(C1-C6)alkyl, pyridyl or benzo[1,3]dioxolyl optionally substituted with (C1-C6)alkyl. There are disclosed pharmaceutical composition based on compounds I and method of treatment.

EFFECT: compounds can be used to treat or prevent diseases associated with malignant cell proliferation.

26 cl, 7 tbl, 365 ex

FIELD: chemistry.

SUBSTANCE: invention concerns method of treatment, alleviation and/or prevention of neurological state, particularly neurodegenerative disorders, involving administration of effective quantity of compound with formula I: . Also invention concerns application of compound of the formula I as neurotherapeutical, neuroprotective or antimyloid agent, pharmaceutical or veterinary composition for treatment, alleviation and/or prevention of neurological states, and compounds of the formula I on the following additional terms: (b) if R3, R and R' are H, and R2 is (CH2)2NR9R10, then both R9 and R10 are not ethyl or methyl; (c) if R3, R and R' are H, and R2 is (CH2)2NR9R10, then both R9 and R10 are not hydrogen or ethyl; (d) if R3, R and R' are H, and R2 is NR11R12, then both R11 and R12 are not hydrogen; (e) if R3, R and R' are H, and R2 is COR6, then R6 is not H, OH or CH2Cl; (f) if R3, R and R' are H, and R2 is not CH3 or CH2Cl; (g) if R3, R and R' are H, and R2 is HCNN R9R10, then both R9 and R10 are not H.

EFFECT: efficient treatment, alleviation and prevention of neurological state.

24 cl, 14 tbl, 21 ex, 14 dwg

FIELD: chemistry.

SUBSTANCE: present invention pertains to a new derivative of cyclic amine or its salts with the following formula (I): (where symbols stand for the following: A: 5-8-member cyclic amine, which may contain a double bond, a bridged structure and may contain substitutes R7-R11 in the ring, or -NH2, -NH(inferior alkyl), -N(inferior alkyl)2 or ) morpholin-1-yl; ring B: benzole, thiophene, furane, pyrrole, 5-7-member cycloalkane or 5-7-member cycloalkene; X1: a bond or inferior alkylene; X2: -(CR12R13)n-, -N(R14)-, -N(R14)CO-, -CON(R14)-, -CO-, -CH(OH)-, -N(R14)- (CR12R13)n-, (CR12R13)n-N(R14)-, -CON(R14)-(CR12R13)n-, -n(R14)CO-(CR12R13)n-, -(CR12R13)n-N(R14)CO-, -(CR12R13)n-CON(R14)-, -CO-(CR12R13)n- or -(CR12R13)n-CO-; Y1: -OH, -O-inferior alkyl, NH2 or -N3; R1 and R2: are identical or different and stand for a halogen atom, inferior alkyl or inferior alkylene-OH; R3-R6: are identical or different and stand for a hydrogen atom, a halogen atom, inferior alkyl, inferior alkenyl, inferior alkynyl, -O-inferior alkyl, -OH, -NH2, -NH(inferior alkyl), -N(inferior alkyl)2, -NH-CO- inferior alkyl, -N(inferior alkyl)-CO- inferior alkyl, -CN-, -NO2, -CF3, -O-inferior alkylene-OH, -inferior alkylene-OH, -inferior alkylene-halogen, -inferior alkylene-O-inferior alkyl, -CO-5-8-member cyclic amine, -COOH-inferior alkyl, -COO-inferior alkylene-aryl, pyridine, thiophene, -inferior alkylene-morpholine, aryl, which may contain a substitute: -O-inferior alkyl or -CF3; R7: hydrogen atom, inferior alkyl, -inferior alkylene-aryl or -inferior alkylene-pyridine: R7 is substitute on the nitrogen atom of the cyclic amine; R8-R14: are identical or different and stand for a hydrogen atom or inferior alkyl; n: is an integer, equal to 1, 2 or 3; where R5 and R6, R4 and R5 or R3 and R4 can form an inferior alkylene together, -O-inferior alkylene-O-, -O-inferior alkylene-, -inferior alkylene-O-, -C(R15)=C(R16)-O-, -O-C(R15)=C(R16)-, -C(R15)=C(R16)-C(R17)=C(R18)-; R3 and Y1 together can form -O-inferior alkylene-O- or -inferior alkylene-O-; R1 and Y1 together can form -inferior alkylene-O-; and Y1 and a branch on - X1-A together can form -O- or -O-inferior alkylene; R15-R18 stand for a hydrogen atom, under the condition that, 6-chloro-2,2-dimethyl-1-(1-methyl-4-piperidinyl)indan-1-ol is not included in the group of compounds). The invention also pertains to a derivative of cyclic amine or its salts with formula (II), to a derivative of cyclic amine or its salts with formula (III), to pharmaceutical composition, as well as their use.

EFFECT: obtaining new biologically active compounds and pharmaceutical compositions based on these compounds, with antagonist effect on NMDA receptors NMDA.

7 cl, 160 ex, 45 tbl

FIELD: chemistry.

SUBSTANCE: invention proposes 5-member heterocyclic inhibitors of kinase p38, including kinase p38α and kinase p38β, based on pyrazoles and imidazoles, with the general formula given below , in which ring B is phenyl, and C is a pyrazole or imidazole ring, and the rest of the symbols assume values given in paragraph 1 of the formula of invention.

EFFECT: there are described pharmaceutical compositions containing said compounds, as well as methods of using the compounds and compositions, including a method of treating, preventing or suppressing one or more symptoms of diseases and conditions mediated by kinase p38 which include, but not limited to, inflammatory diseases and conditions.

31 cl, 6 tbl, 175 ex

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