Organic compounds

FIELD: chemistry.

SUBSTANCE: invention describes compounds of formula (I) in free or salt form, where Q is a bond, R1 and R2 independently represent H or C1-C8alkyl, or R3 is C1-C8alkyl, R4 and R5 independently represent halogen, C1-C8alkyl, C1-C8haloalkyl, C3-C15carbocyclic group, nitro group, cyano-group, C1-C8alkylsulphonyl group, R6 is H or C1-C8alkyl; W is a group of formula (Wa1) or (Wa2), where A independently represents C or N, or W represents a group of formula (Wb); where Y independently represents C or N; and Z represents N, O or S, or W represents a group of formula (Wc), where Y independently represents C or N; and Z represents O or S; X represents -SO2-, -CH2-, -CH(C1-C8alkyl)- or a bond; m and n each independently represents an integer from 0 to 3; and p is 1, to a pharmaceutical composition with CRTh2 antagonist activity, as well as to use thereof as a medicinal agent and production method thereof.

EFFECT: new compounds which can be used in medicine are obtained and described.

10 cl, 153 ex, 1 tbl

 

The text descriptions are given in facsimile form.

1. The compound of formula (I)

in free or salt form,
where Q denotes the relationship,
R1and R2independently represent N or C1-C8alkyl, or
R3stands With1-C8alkyl,
R4and R5independently represent halogen, C1-C8alkyl, C1-C8haloalkyl,3-C15carbocyclic group, a nitrogroup, cyano, C1-C8alkylsulfonyl, C1-C8alkoxycarbonyl,1-C8alkoxygroup or1-C8haloalkoxy,
R6denotes N or C1-C8alkyl;
W denotes a group of formula (Wa1) or (Wa2)
or,
where And independently represents C or N,
or W represents a group of formula (Wb);
,
where Y independently represents C or N; and
Z represents N, O or S, or
W denotes a group of formula (Wc)
,
where Y independently represents C or N; and
Z represents O or S;
X denotes-SO2-, -CH2-, -CH(C1-C8alkyl)- or a bond;
m and n each independently represents an integer from 0 to 3; p represents 1.

2. The compound of formula (I) according to claim 1 in free or salt form,
where Q denotes the relationship,
R1and R2n is dependent denote H or C 1-C4alkyl,
R3stands With1-C4alkyl,
R4and R5independently represent halogen, C1-C4alkyl, C1-C4haloalkyl,3-C10carbocyclic group, cyano, C1-C4alkoxycarbonyl, C1-C4alkylsulfonyl, C1-C4alkoxygroup or1-C4haloalkoxy,
R6denotes N or C1-C4alkyl;
W denotes a group of formula (Wa1) or (Wa2), as defined in claim 1, or W represents a group of formula (Wb), as defined in claim 1,
X denotes-SO2-, -CH2- or-CH(C1-C4alkyl)-,
m and n each independently represents an integer from 0 to 3; and
p denotes 1.

3. The compound according to claim 1, selected from the group
(1-Benzyl-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
[1-(3,4-Dichlorobenzyl)-2-methyl-1H-pyrrolo[2,3-6]pyridine-3-yl]acetic acid;
[2-Methyl-1-(2-methylbenzyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chlorobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Cyanobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chlorobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyanobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(3-methylbenzyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[Methyl-1-(3-trifloromethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Terbisil)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chlorobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(4-trifloromethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Terbisil)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3,4-Diferensial)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(4-methylbenzyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Fluoro-3-methylbenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Fluoro-4-methylbenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chloro-4-terbisil)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Fluoro-4-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Terbisil)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(2-trifloromethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Cyanobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(1-phenylethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid the acid,
[2-Methyl-1-(toluene-4-sulfonyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
2-Methyl-1-(4-nitrobenzenesulfonyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(naphthalene-2-sulfonyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Isopropylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Brabanthallen)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid,
[2-Methyl-1-(3-trifloromethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(Biphenyl-4-sulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Deformationsvetsaren)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chloro-2-methylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Zenobe solarpanel)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
1-(2,5-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3,4-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
(1-Benzazolyl-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
[1-(4-Chlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
(2-Methyl-1-pyridin-3-ylmethyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
(2-Methyl-1-pyridin-2-ylmethyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
(2-Methyl-1-pyridin-4-ylmethyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
1-(3-Chloro-4-methylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(4-trifloromethyl)-1H-pyrrolo[2,3-b)pyridin-3-yl]acetic acid;
1-(2-Chloro-4-permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
2-[1-(3,4-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]propionic acid;
[1-(3-Cyano-4-permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,4-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(3-trifloromethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,5-Differentiality)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Tzianabos sulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(2,3,4-tripersonality)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
Methyl ester 3-(3-carboxymethyl-2-methyl-pyrrolo[2,3-b]pyridine-1-sulfonyl)thiophene-2-carboxylic acid;
[1-(3,5-Differentiality)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,5-Dichlorothiophene-3-sulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3,5-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,3-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chloro-4-permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Fluoro-4-methylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,4-Differentiality)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(pyridine-3-sulfonyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
1-(4-Chlorophenyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3,4-Differentiality)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-methylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
(1-Furan-3-ylmethyl-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
(1-Furan-2-ylmethyl-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
[4-Chloro-1-(3,-Dichlorobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,5-Dimethyl-2-pyrazole-3-ylmethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3,5-Dimethylisoxazol-4-ylmethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(5-methyl-2-triptorelin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(5-methylisoxazol-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,4-Dimethylthiazol-5-ylmethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
(1-Benzofuran-2-ylmethyl-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl)acetic acid;
{1-[1-(4-Chlorophenyl)ethyl]-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid;
[2-Ethyl-1-(4-trifloromethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Econsultancy)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[4-Chloro-1-(4-methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chloro-4-methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Methanesulfonyl-3-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Econsultancy-2-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chloro-4-econsultancy)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Econsultancy-2-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
1-(4-Methanesulfonylaminoethyl)-2-methyl-1H-what irolo[2,3-b)pyridin-3-yl]acetic acid;
{1-[1-(4-Methanesulfonyl)ethyl]-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid enantiomers 1 and 2;
[1-(4-Methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[6-Chloro-1-(4-methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[6-Chloro-1-(4-methanesulfonyl-2-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Fluoro-3-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(4-triftormetilfullerenov)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
{2-Methyl-1-[4-(propane-2-sulfonyl)benzyl]-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid;
[1-(3-Fluoro-4-methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Fluoro-3-methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(6-triptorelin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Cyano-4-terbisil)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chloro-5-terbisil)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Methanesulfonyl-2-methylbenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Methoxybenzyl)-2-methyl-1H-pyrrol the[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Methoxybenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
{2-Methyl-1-[1-(4-triptoreline)ethyl]-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid;
{1-[1-(3-Chlorophenyl)ethyl]-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid;
{1-[1-(4-Methanesulfonyl)ethyl]-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid;
1-(4-fluoro-2-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2,4-Bis-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
{2-Methyl-1-[1-(2-triptoreline)ethyl]-1H-pyrrolo[2,3-b]pyridine-3-yl}acetic acid;
[1-(3-Methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(4-nitrobenzyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Bromobenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chloro-4-methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Fluoro-4-methanesulfonylaminoethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyano-3-ethoxybenzylidene)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-fluoro-2-methylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl] acetic acid;
[1-(4-Cyano-3-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyano-3-propoxybenzaldehyde)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[-(3-Butoxy-4-cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyano-3-pentyloxybenzaldehyde)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(6-Cyano-3-sulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chloro-5-cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyano-3-methylbenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-2-fluoro-5-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(5-Cyano-2-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(5-Chloro-2-cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo [2,3-b] pyridine-3-yl]acetic acid;
[1-(2-Chloro-4-cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(2-Chloro-5-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(5-Chloro-2-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[2-Methyl-1-(thiophene-2-sulfonyl)-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Cyano-3-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chloro-4-cyanobenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-permentantly)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3-Chloro-4-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid is;
[1-(3-Fluoro-4-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-methoxybenzenesulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(3,4-Dicyanomethylene)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
[1-(4-Chloro-3-trifloromethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;
and
[1-(4-Chloro-3-cyanobenzenesulfonyl)-2-ethyl-1H-pyrrolo[2,3-b]pyridine-3-yl]acetic acid;

4. The connection according to one of claims 1 to 3 for use as drugs having activity of CRTh2 receptor antagonist.

5. Pharmaceutical composition having activity of CRTh2 receptor antagonist comprising the compound according to one of claims 1 to 3.

6. The use of compounds according to one of claims 1 to 3 to obtain drugs for the treatment of diseases mediated by CRTh2 receptor.

7. The use of compounds according to one of claims 1 to 3 to obtain drugs for the treatment of inflammatory or allergic diseases, in particular inflammatory or obstructive diseases of the respiratory tract.

8. The method of obtaining compounds of formula (I)as defined in claim 1, in free or salt form, comprising the steps:
(i) to obtain compounds of formula (I), where R6denotes H, splitting difficult ester group-COOR6in connection of the attachment of the formula (I),
where R6stands With1-C8alkyl; and
Q, R1, R2, R3, R4, R5, W, X, m, n and p are defined above; and (ii) the allocation of the formed compounds of formula I in free or salt form.

9. The method of obtaining compounds of formula (I)as defined in claim 1, in
free or salt form, comprising the steps:
(i) to obtain compounds of formula (I), where R6represents C1-C8alkyl, the reaction of the compound of formula (II)
,
where R6stands With1-C8alkyl; and
Q, R1, R2, R3, R4, m, n and p are defined above, with a compound of formula (III)
,
where G denotes a leaving group; and
R5, W, X and n are defined above; and
(ii) isolation of the resulting compound of formula I in free or salt form.

10. The method of obtaining compounds of formula (I)as defined in claim 1, in free or salt form, comprising the steps:
(i) to obtain compounds of formula (I),
where R6represents C1-C8alkyl;
R1denotes N or C1-C8alkyl;
R2stands With1-C8alkyl; and
p denotes 1,
the reaction of the compound of formula (I),
where R1denotes N or C1-C8alkyl; and
R2denotes H,
with the compound of the formula
RAG,
where RAabout who appoints C 1-C8alkyl;
G defined above; and
(ii) isolation of the resulting compound of formula I in free or salt form.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention concerns compounds of general formula I or to their pharmaceutically acceptable salts, where X1 - CH; X2 - N or CH; Q1 represents ,

where X11 - CH or C-halogen; X12 - CH, C-halogen or C-CF3; X13 - CH; X14 - C-E11, and E11 represents C0-10alkyl or C0-10alkoxy; X15 - CH or N; X16 - N or N+ -0; G1 - phenyl or 5-6-members unsaturated ring containing one heteroatom N or S; R1 - C0-10alkyl, cycloC3-10alkyl or piperidinyl, any of which is optionally substituted with 1-2 independent substitutes G11, or R1 represents phenyl; G11 is chosen from: OR21 where R21 represents C0-10alkyl; -oxo; -cycloC3-8alkyl; -C0-10alkyl optionally substituted with group N(C0-10alkyl)(C0-10alkyl) wherein C0-10alkyl is optionally substituted with group N(C0-10alkyl)C(O)C0-10alkyl; group OR2221, where R2221 - C0-10alkyl; group N(C0-10alkyl)C(O)C0-10alkyl; group N(C0-10alkyl)SO2(C0-10alkyl); group -N(C0-10alkyl)C(O)N(C0-10alkyl)(C0-10alkyl); group -N(C0-10alkyl)C(=O)R3331, where R3331 - C1-10alkoxy C1-10alkyl or tetrahydrofuranyl; -N(R21)R31 where R21 and R31 independently represent C0-10alkyl optionally substituted with thiophenyl, morphlinyl, furanyl; cycloC3-8alkyl; C1-10alkoxyC1-10alkyl; tetrahydropyranyl; piperidylC0-10alkyl; or piperidyl optionally substituted with C0-10alkyl; or R21 and R31 optionally taken together with nitrogen atom whereto attached, form 3-10-members saturated ring optionally substituted with one or more independent substitutes G1111, and optionally including one or more heteroatoms different from nitrogen whereto R21 and R31 are attached; where G1111 - C0-10alkyl optionally substituted with group OR77 where R77 - C0-10alkyl, or G1111 represents C1-10alkoxyC1-10alkyl, pirimidinyl, pyrazinyl, imidazolylmethyl; C(O)N(R21)R31 where R21 and R31 independently represent C0-10alkyl; -C(O)O(C0-10alkyl); -C(O) C0-10alkyl optionally substituted with N(C0-10alkyl)(C0-10alkyl) or halogen; -heterocyclylC0-10alkyl where heterocyclyl represents 4-6-members saturated ring containing 1 or 2 heteroatoms, independently chosen from N, O or S optionally substituted with a substitute chosen from: 1) OR2221, where R2221 - pyrimidinyl or C0-10lkyl; 2) C(O)OR2221, where R2221 - C0-10alkyl or phenyl-C0-10alkyl; 3) C(O)C0-10alkyl optionally substituted with N(C0-10alkyl)(C0-10alkyl) or C1-10alkoxy C1-10alkyl; 4) C(O)N(C0-10alkyl)(C0-10alkyl); 5) S(O)2C0-10alkyl; 6) SO2N(C0-10alkyl)(C0-10alkyl); 7) -NR2221R3331, where R2221 and R3331 taken together with nitrogen atom whereto attached, form pyrrolidinyl; or G11 represents C, which taken together with carbon whereto attached, forms C=C double bond substituted with R5 and G111 where R5 and G111 are hydrogens. The invention also specifically concerns cys-3-[8-amino-1-(2-phenylquinoline-7-yl)-imidazo[1,5-α]pyrazine-3-yl]-1-methl-cyclobutanole or its pharmaceutically acceptable salt. The specified compounds and their pharmaceutically acceptable salts are applicable in treatment of conditions mediated by activity IGF-1R proteinkinase, particularly angiogenesis, vascular permeability, immune response, cell apoptosis, tumour growth or inflammation. The invention also concerns a pharmaceutical composition.

EFFECT: improved efficiency of the composition and method of treatment.

14 cl, 3 tbl, 171 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel cyclic amine compounds of formula (1) or pharmaceutically acceptable salts thereof: . In formula (1), X is O, S, NR2 (where R2 is H, C1-C12 alkyl); when X is O, S, then R1 is H, CN, COOH, C2-C13 alkoxycarbonyl, carbamoyl group; and when X is NR2 (where R2 assumes values given above), R1 is CN; Ar1 and Ar2 are identical or different and each represents an aryl which can be substituted with 1-3 halogens; or Ar1 and Ar2 together with neighbouring carbon atoms to which they are bonded form a group with formula (b): (where ring S and ring T are identical and each is a benzene ring; Y is O); ring B is a benzene ring which can be substituted with 1-3 substitutes independently selected from a group comprising halogen, C1-C12 alkyl, C1-C8 halogenalkyl, C1-C12 alkoxy, C1-C8 halogenalkoxy group; n is an integer from 1 to 10; p, q are identical or different and each is an integer equal to 1 or 2. Formula (1) compounds are bonding inhibitors of the α2C-adrenoreceptor.

EFFECT: possibility of using compounds in pharmaceutical compositions.

7 cl, 1 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to novel pyrrolo[3,2-c]pyridine derivatives of formula (I) or their pharmaceutically acceptable salts in which R1 is hydrogen; straight or branched C1-C6alkyl group optionally substituted with one or more substitutes selected from a group consisting of C1-C5alkoxy, hydroxyl, C3-C7 cycloalkyl, C1-C3 alkylthiazolyl and 1,3-dioxolanyl; straight or branched C2-C6 alkenyl group; straight or branched C2-C6 alkynyl group; C3-C7cycloalkyl group; or benzyl group optionally substituted with one or more substitutes selected from a group consisting of halogen, C1-C3alkyl and C1-C3alkoxy, R2 is a straight or branched C1-C6 alkyl group, R3 is hydrogen; straight or branched C1-C6 alkyl group; straight or branched C2-C6alkenyl group; or a benzyl group optionally substituted with one or more halogens, and R4 is 1,2,3,4-tetrahydroisoquinolinyl group; a benzyloxy group optionally substituted with one or more halogens; or an amine group substituted with one or two substitutes selected from a group consisting of hydrogen, straight or branched C1-C5alkylcarbonyl, phenoxycarbonyl, benzyl, optionally substituted with one or more halogens, and benzoyl, optionally substituted with one or more halogens, as well as to method of producing said compounds and a pharmaceutical composition with inhibitory effect on a proton pump containing these compounds.

EFFECT: new compounds are obtained and described, which exhibit excellent inhibitory effect on a proton pump and can provide reversible inhibitory effect on a proton pump.

7 cl, 82 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-H-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazole[3,4-b]pyridine-5-carboxamide, which is a compound of formula or its pharmaceutically acceptable salt, as well as to a method of producing said compounds. The invention also relates to use of the said compound or its pharmaceutically acceptable salt as phosphodiesterase IV (PDE4) inhibitor, for example in treatment and/or prevention of inflammatory and/or allergic disease, cognitive impairment or depression in mammals. The invention particularly pertains to use of the compound or its pharmaceutically acceptable salt in treating and/or preventing atopic dermatitis in mammals, for example via external local administration to a mammal, for example a human being.

EFFECT: pharmaceutical compositions are also provided, which contain the said compound or its pharmaceutically acceptable salt, particularly suitable for external local administration.

35 cl, 1 tbl, 19 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a quinazoline compound of formula or its pharmaceutically acceptable salts, used as inhibitors of potential-dependant sodium and calcium channels, where R1, R2, R3, R5a, R5, y and x are defined in the formula of invention. The invention also relates to a pharmaceutical composition containing the disclosed compound and to methods of inhibiting one or more of NaV1.2, NaV1.3, NaV1.8, or CaV2.2.

EFFECT: 4-aminoquinazoline antagonists of selective sodium and calcium ion channels.

17 cl, 3 tbl, 1 ex

FIELD: pharmacology.

SUBSTANCE: present invention refers to compounds of formula (I) , to its N-oxides, salts, stereoisomer forms where n is equal 1, 2 or 3; R1 means cyano group; X means bivalent radical NR2 or O; R2 means hydrogen or C1-10alkyl, each Q1 independently stands for direct coupling, -CH2- or -CH2-CH2-; each R4 independently means hydrogen or C1-4alkyl; each R5a, R5b, R5c independently means hydrogen, C1-4alkyl or arylC1-4alkyl; each R5e, R5f independently means hydrogen, C1-4alkyl or arylC1-4alkyl, or R5e and R5f together can form bivalent alkandiyl radical of formula -CH2-CH2- or -CH2-CH2-CH2-; R11 means aryl, arylC1-4alkyl, C1-4alkylcarbonyl, arylcarbonyl, arylC1-4alkylcarbonyl, C1-4alkyloxycarbonyl, arylC1-4alkyloxycarbonyl, R5aR5bN-carbonyl, hydroxyC1-4alkyl, C1-4alkyloxyC1-4alkyl, arylC1-4alkyloxyC1-4alkyl, aryloxyC1-4alkyl, pyridyl; -a1=a2-a3=a4- means a bivalent radical of formula -CH=CH-CH=CH- (c-1); where one or two hydrogen atoms in (c-1) are substituted by radical C1-6alkyl, C1-4alkoxy, halogen, hydroxy group, (R5g)(R5h)N-(C1-4alkandiyl)-O-trifluoromethyl, cyano group, radical -COOR4, (R5a)(R5b)N-sulphonyl, pyrrolidinyl-sulphonyl, piperidinyl sulphonyl, radical N(R5a)(R5b), radical (a-1), (a-7), morpholinyl, (R5g)(R5h)N-(C1-4alkandiyl)-N(R5c)-, C1-6alkylcarbonylamino, C1-6alkyloxycarbonylamino, C1-6alkylsulphonylamino, (R5a)(R5b)N-C1-4alkyl; R20 means hydrogen, spiro (C2-4alkylenedioxy), spiro (diC1-4alkyoxy) or -NR5gR5h; each R5g or R5h independently means either hydrogen, or C1-4alkyl, or R5g and R5h together with nitrogen atom whereto attached form pyrrolidinyl, piperidinyl or morpholinyl; R3 means nitro group, cyano group, amino group, halogen, hydroxy group or C1-4alkoxy; aryl means phenyl optionally substituted with one or more substitutes chosen from the group consisting of C1-6alkyl, C1-4alkoxy, halogen, hydroxy, amino and trifluoromethyl. Besides it relates to the pharmaceutical composition with antiviral activity, and method for making said compounds.

EFFECT: there are prepared and described new compounds with antiviral activity.

9 cl, 15 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: present invention is related to new crystalline forms of salt of mesylate2,3-dimethyl-8-(2,6-dimethylbenzylamino)-N-hydroxyethyl-imidaso[1,2-a]pyridine-6-carboxamide and to their mixture. Besides the present invention is also related to methods of their preparation, application and pharmaceutical composition for inhibition of gastric acid secretion, which contains them. Production of new salt of 2,3-dimethyl-8-(2,6-dimethylbenzylamino)-N-hydroxyethyl-imidaso[1,2-a]pyridine-6-carboxamide and its crystalline forms for production of medicinal agent for use in treatment or prophylaxis of gastrointestinal disorders such as gastritis, gastric ulcer, duodenal ulcer, peptic ulcerous diseases, reflux-esophagitis, Zollinger-Ellison syndrome, ulcerogenic adenomas of pancreas, acute bleeding from upper compartments of gastrointestinal tract.

EFFECT: wider area of compounds application.

33 cl, 1 tbl, 12 dwg, 8 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 monohydrate of sodium salt S-tenatoprazol, which complies with the following formula: . Invention is also related to method for production of monohydrate of sodium salt of S-tenatoprazol, to application and pharmaceutical composition on its basis for treatment of gastrointestinal pathologies.

EFFECT: production of new compound and pharmaceutical composition on its basis, which may be used in medicine for production of medicinal agents for treatment of gastrointestinal pathologies, gastroesophageal reflux and gastrointestinal haemorrhages in patients, which are prescribed polymedicamental therapy.

19 cl, 9 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of hydantoin with common formula I , where R1 represents cyclobutyl or cyclopropyl; where mentioned group cyclopropyl may be additionally substituted with CH3; R2 represents C1-3alkyl or cyclopropyl; and A, A1 and B independently represent CH or N. Invention is also related to method for production of compounds of formula I, pharmaceutical composition on its basis, its use for making of medicinal agent and to method for inhibition of metal proteinases, based on use of compound of formula I.

EFFECT: new derivatives of hydantoin have activity of metal proteinase inhibitor.

11 cl, 1 tbl, 9 ex

FIELD: medicine.

SUBSTANCE: there is described thiomorpholine compound presented by formula (I) wherein the ring A represents benzene ring; the ring B represents benzene ring; R1 represents hydrogen atom, R2 represents C1-6-alkyl group; R3a and R3b are identical or different, each representing hydrogen atom or C1-6-alkyl group, and n represents an integer equal to 2, or its pharmaceutically acceptable salt. There is also described method for making the compound of formula (1), a pharmaceutical composition and application of the compound of formula (1) for making a medical product used for treatment and prevention of the disease chosen from inflammation, allergic diseases, pain, migraine, neuralgia, itch, cough, central nervous system diseases, alimentary organ diseases, nausea, vomiting and urological disorders.

EFFECT: compounds exhibits affinity to neurokinine-1 receptor.

6 cl, 4 tbl, 16 ex

FIELD: medicine.

SUBSTANCE: invention refers to compounds of formula I or formula II, to their pharmaceutically acceptable salts, enantiomers and diastereoisomers as metalloprotease inhibitors, and also to a pharmaceutical composition based thereon and to versions of application thereof. Said compounds can find application in treatment of the diseases mediated by activity of metalloproteases, Her-2 SHEDDASE, ADAM-10 and ADAM-17, such as arthritis, cancer, cardiovascular disorders, skin diseases, inflammatory and allergic conditions, etc. In general formula I or II: A represents CWNHOH; B represents CH2; G represents CH2; D represents oxygen; X represents CH2NRb; Y represents CH2; M represents C; U is absent or represents NRb; V is absent or represents phenyl, or 4-10-members heterocyclyl containing 1-2 heteroatoms chosen from N and S, substituted with 0-5 groups Re; U' is absent or represents C1-10alkylene, O or combinations thereof; V' represents H, C1-8alkyl, NRbRc, C6-10carbocyclyl substituted with 0-3 groups Re, or 5-14-members heterocyclyl containing 1-3 heteroatoms chosen from N, O and C substituted with 0-4 groups Re; Ra and Re, independently represents H, T, C1-8alkylene-T, C(O)NRa'(CRb'Rc')r-T, (CRb'Rc')r-O-(CRb'Rc')r-T, OH, Cl, F, CN, NO2, NRIRII, COORIV, ORIV, CONRIRII, C1-8halogenalkyl, C3-13carbocyclyl; Rb and Rc independently represents H, T, C1-6alkylene-T, C(O)O(CRb'Rc')r-T, C(O)(CRb'Rc')r-T, S(O)p(CRb'Rc')r-T; T represents H, C1-10alkyl substituted with 0-1 groups Rb'; C3-6carbocyclyl, 5-6-members heterocyclyl containing one oxygen atom; Ra' Rb' and Rc' independently represents H, ORIV or phenyl; R1 represents hydrogen; R2 represents hydrogen; R3 represents: (i) C1-10alkyl; (ii) 4-14-members heterocyclyl containing 1-3 nitrogen atoms optionally substituted with one or two substitutes chosen from C1-6alkyl, OR13, 5-10-members heterocyclyl containing 1-3 heteroatoms chosen from N O and C, or phenyl; (iii) NR16R17; R4 represents H; R4' represents H; R5' represents H; W represents oxygen; R13 represents C1-C6alkyl; R16 and R17 independently represents C1-C10alkyl or phenyl where each is optionally substituted with one C1-4alkyl; RI and RIIindependently represents H or C1-6alkyl; RIV represents C1-6alkyl; i is equal to 0; p is equal to 1 or 2 and r is equal to 0, 1 or 2; provided that a) a spiro ring represents a stable chemical base unit and b) NR8 and NRb do not contain neither N-N, nor N-O bonds.

EFFECT: higher efficiency of the composition and method of treatment.

54 cl, 1 tbl, 9 dwg, 284 ex

FIELD: medicine.

SUBSTANCE: invention concerns derivatives of thiazolidine-4-one of general formula (I) and general formula (II), to their isomers and pharmaceutically acceptable salts which can be used as a medical product with immunosuppressive activity. In formulae (I) and (II), R1 and R14 independently represent lower alkyl, lower alkenyl; cycloalkyl; 5,6,7,8-tetrahydronaphth-1-yl; phenyl group or phenyl group independently mono- or disubstituted with lower alkyl, halogen, lower alkoxy or group -CF3; R2 and R15 independently represent lower alkyl; allyl; cyclopropyl; or di- lower alkylamino; R3 represents -NR5R6 or -O-CR7R8-CR9R10-(CR11R12)n-O-R13; R23 represents hydrogen; hydroxycarbonyl-lower alkyl or 1-glyceryl. Values of the other radicals are specified in the patent claim. The invention also concerns application of one or more compounds of general formula (I) or (II) for preparation of a medical product with immunosuppressive activity.

EFFECT: agent exhibits improved efficiency.

24 cl, 1 tbl, 157 ex

FIELD: chemistry.

SUBSTANCE: proposed phosphodiesterase 4 inhibitors are characterised by formulae II, III, V, VI, where X is CH or N; L is a single bond, -(CH2)nCONH-, -(CH2)nCON(CH2CH3)-, (CH2)nSO2, (CH2)nCO2 or alkylene, optionally substituted oxo or hydroxy; n assumes values from 0 to 3; R1 is optionally substituted alkyl; R3 - H, alkyl, cycloalkyl, alkoxyalkyl, optionally substituted phenyl, phenylalkyl, heterocyclyl, heterocyclylalkyl or cycloalkylalkyl; R4 and R5 represent alkyl; R6 - cycloalkyl, R7 is H; R8 is H, carboxy, alkoxycarbonyl, -CO-alkyl, optionally substituted alkyl.

EFFECT: new phosphodiesterase 4 inhibitors have improved properties.

55 cl, 30 ex

FIELD: chemistry.

SUBSTANCE: described is a compound of formula I , where R1 is C1-C6alkyl; R2 is a radical of formula a, where R6 is C1-C12alkyl, R7 is H, X is O, R3 is -A-B-COOH, where A and B each independently represents a chemical bond, or CDE, where D and E each independently represents H, and each R4 and R5 independently represents H, under the condition that, if R4 is H, R5 is H, R3 is COOH, R2 is a radical of formula a, and R7 is H, R1 is CH3, and XR6 is an unsubstituted OC1-C12alkyl radical, then XR6 is not in the meta-position to (CH2)2-CR1R3(NR4R5), in free form or in form of a pharmaceutically acceptable salt, as well a production method and use thereof primarily during transplantation, as well as pharmaceutical composition containing said compounds.

EFFECT: new compounds have useful biological properties.

7 cl, 3 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, namely medical products for HIV/AIDS infection therapy. There is offered application of Glimurid as a drug for HIV-infection treatment.

EFFECT: application of said drug ensures to increase the clinical effectiveness due to viral load reduction and immunocorrection.

1 ex, 2 dwg

FIELD: medicine.

SUBSTANCE: invention refers to pharmaceutical industry, particularly a preparation that is able to suppress an immune response underlying immunoglobulin-E-dependent allergic diseases. Application of water-soluble polysaccharides made of clover (Trifolium pretense L.), as a preparation able to suppress the immune response underlying immunoglobulin-E- dependent allergic diseases.

EFFECT: polysaccharides made of clover (Trifolium pretense L) exhibit effective antiallergic activity and affect the earliest stages of formation of Th2-dependent allergic reactions associated with development of immunoglobulins E and G1.

3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly gastroenterology and surgery, and covers prevention of dialysis peritonitis (DP). Therefor, prior to the peritoneal dialysis (PD), a bio-sample from the patient's intestines is analysed for dysbacteriosis by one of the standard methods. If dysbacteriosis is diagnosed, prior to the PD, dysbacteriosis is treated by elimination at the first stage of detected excess conditionally-pathogenic and pathogenic intestinal microflora with antibacterial preparations, taking into account sensitivity thereto of said microflora. The second stage involves compensation of deficiency and restoration of normal intestinal microflora. The restoration of intestinal microflora is followed with the PD.

EFFECT: method provides effective prevention of DP development, eliminating risk of DP development in multiple prolonged courses of the PD.

1 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry and concerns pharmaceutical composition for prevention and treatment of diseases and disease states connected with metabolic pathways of cycloxygenase-2 (CG-2) and 5-lipooxygenase (5-LO), which contains mixture of extract obtained from Scutellariae and enriched with flavonoids with free B-ring, which include baicalein, and extract obtained from Acacia and enriched with flavans, which include catechine and epicatechine. Claimed invention also relates to method of body weight loss and control over glucose level in blood. Methods by claimed invention include introduction to person, who needs it, of efficient amount of composition by claimed invention together with pharmaceutically acceptable carrier. Claimed invention mainly relates to prevention and treatment of diseases and states connected with metabolic pathways of cycloxygenase-2 (CG-2) and 5-lipooxygenase (5-LO), including, but not confining to it, stopping discomfort and pain in joints, induced by such states as osteoarthritis, rheumatoid arthritis and other injuries caused by overload.

EFFECT: composition possesses high efficiency.

35 cl, 22 ex, 15 tbl

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine and concerns composition, which stimulates immune answer, containing nanoparticles, based on copolymer of methylvinyl ether of maleic anhydride. Mentioned nanoparticles can additionally contain allergen or antigen and/or immunostimulating agent, which can be inside of said nanoparticles and/or at least partially cover surface of mentioned nanoparticles and optionally crossing-linking agent. Composition, which stimulates immune response, can be applied as adjuvant in immunotherapy and vaccines.

EFFECT: increase of activity.

32 cl, 7 ex, 2 tbl, 13 dwg

FIELD: medicine.

SUBSTANCE: invention concerns compounds of general formula I or to their pharmaceutically acceptable salts, where X1 - CH; X2 - N or CH; Q1 represents ,

where X11 - CH or C-halogen; X12 - CH, C-halogen or C-CF3; X13 - CH; X14 - C-E11, and E11 represents C0-10alkyl or C0-10alkoxy; X15 - CH or N; X16 - N or N+ -0; G1 - phenyl or 5-6-members unsaturated ring containing one heteroatom N or S; R1 - C0-10alkyl, cycloC3-10alkyl or piperidinyl, any of which is optionally substituted with 1-2 independent substitutes G11, or R1 represents phenyl; G11 is chosen from: OR21 where R21 represents C0-10alkyl; -oxo; -cycloC3-8alkyl; -C0-10alkyl optionally substituted with group N(C0-10alkyl)(C0-10alkyl) wherein C0-10alkyl is optionally substituted with group N(C0-10alkyl)C(O)C0-10alkyl; group OR2221, where R2221 - C0-10alkyl; group N(C0-10alkyl)C(O)C0-10alkyl; group N(C0-10alkyl)SO2(C0-10alkyl); group -N(C0-10alkyl)C(O)N(C0-10alkyl)(C0-10alkyl); group -N(C0-10alkyl)C(=O)R3331, where R3331 - C1-10alkoxy C1-10alkyl or tetrahydrofuranyl; -N(R21)R31 where R21 and R31 independently represent C0-10alkyl optionally substituted with thiophenyl, morphlinyl, furanyl; cycloC3-8alkyl; C1-10alkoxyC1-10alkyl; tetrahydropyranyl; piperidylC0-10alkyl; or piperidyl optionally substituted with C0-10alkyl; or R21 and R31 optionally taken together with nitrogen atom whereto attached, form 3-10-members saturated ring optionally substituted with one or more independent substitutes G1111, and optionally including one or more heteroatoms different from nitrogen whereto R21 and R31 are attached; where G1111 - C0-10alkyl optionally substituted with group OR77 where R77 - C0-10alkyl, or G1111 represents C1-10alkoxyC1-10alkyl, pirimidinyl, pyrazinyl, imidazolylmethyl; C(O)N(R21)R31 where R21 and R31 independently represent C0-10alkyl; -C(O)O(C0-10alkyl); -C(O) C0-10alkyl optionally substituted with N(C0-10alkyl)(C0-10alkyl) or halogen; -heterocyclylC0-10alkyl where heterocyclyl represents 4-6-members saturated ring containing 1 or 2 heteroatoms, independently chosen from N, O or S optionally substituted with a substitute chosen from: 1) OR2221, where R2221 - pyrimidinyl or C0-10lkyl; 2) C(O)OR2221, where R2221 - C0-10alkyl or phenyl-C0-10alkyl; 3) C(O)C0-10alkyl optionally substituted with N(C0-10alkyl)(C0-10alkyl) or C1-10alkoxy C1-10alkyl; 4) C(O)N(C0-10alkyl)(C0-10alkyl); 5) S(O)2C0-10alkyl; 6) SO2N(C0-10alkyl)(C0-10alkyl); 7) -NR2221R3331, where R2221 and R3331 taken together with nitrogen atom whereto attached, form pyrrolidinyl; or G11 represents C, which taken together with carbon whereto attached, forms C=C double bond substituted with R5 and G111 where R5 and G111 are hydrogens. The invention also specifically concerns cys-3-[8-amino-1-(2-phenylquinoline-7-yl)-imidazo[1,5-α]pyrazine-3-yl]-1-methl-cyclobutanole or its pharmaceutically acceptable salt. The specified compounds and their pharmaceutically acceptable salts are applicable in treatment of conditions mediated by activity IGF-1R proteinkinase, particularly angiogenesis, vascular permeability, immune response, cell apoptosis, tumour growth or inflammation. The invention also concerns a pharmaceutical composition.

EFFECT: improved efficiency of the composition and method of treatment.

14 cl, 3 tbl, 171 ex

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