Organic compounds

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I, in which R1 denotes alkyl or cycloalkyl; R2 denotes phenyl-C1-C7-alkyl, di-(phenyl)- C1-C7-alkyl, naphthyl- C1-C7-alkyl, phenyl, naphthyl, pyridyl-C1-C7-alkyl, indolyl- C1-C7-alkyl, 1H-indazolyl- C1-C7-alkyl, quinolyl C1-C7-alkyl, isoquinolyl- C1-C7-alkyl, 1,2,3,4-tetrahydro-1,4-benzoxazinyl- C1-C7-alkyl, 2H-1,4-benzoxazin-3(4H)-onyl-C1-C7-alkyl, 9-xanthenyl-C1-C7-alkyl, 1-benzothiophenyl-C1-C7-alkyl, pyridyl, indolyl, 1H-indazolyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydro-1,4-benzoxazonyl, 2H-1,4-benzoxazin-3(4H)-onyl, 9-xanthenyl, 1-benzothiophenyl, 4H-benzo[1,4]thiazin-3-only, 3,4-dihydro-1H-quinolin-2-onyl or 3H-benzoxazol-2-onyl, where each phenyl, naphthyl, pyridyl, indolyl, 1H-indazolyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydro-1,4-benzoxazonyl, 2H-1,4-benzoxazin-3(4H)-onyl, 1-benzothiophenyl, 4H-benzo[1,4]thiazin-3-only, 3,4-dihydro-1H-quinolin-2-onyl or 3H-benzoxazol-2-onyl are unsubstituted or contain one or up to 3 substitutes independently selected from a group comprising C1-C7-alkyl, hydroxy-C1-C7-alkyl, C1-C7-alkoxy- C1-C7-alkyl, C1-C7-alkoxy- C1-C7-alkoxy-C1-C7-alkoxy- C1-C7-alkyl, C1-C7-alkanoyloxy- C1-C7-alkyl, amino- C1-C7-alkyl, C1-C7-alkoxy- C1-C7-alkylamino- C1-C7-alkyl, C1-C7-alkanoylamino- C1-C7-alkyl, C1-C7-alkylsulphonylamino- C1-C7-alkyl, carboxy- C1-C7-alkyl, C1-C7-alkoxycarbonyl- C1-C7-alkyl, halogen, hydroxy group, C1-C7-alkoxy group, C1-C7-alkoxy- C1-C7-alkoxy group, amino- C1-C7-alkoxy group, N-C1-C7-alkanoylamino-C1-C7-alkoxy group, carbamoyl- C1-C7-alkoxy group, N-C1-C7-alkylcarbamoyl-C1-C7-alkoxy group, C1-C7-alkanoyl, C1-C7-alkoxy-C1-C7-alkanoyl, C1-C7-alkoxy- C1-C7-alkanoyl, carboxyl, carbamoyl and N-C1-C7-alkoxy-C1-C7-alkylcarbamoyl; W denotes a fragment selected from residues of formulae IA, IB and IC, where () indicates the position in which the fragment W is bonded to the carbon atom in position 4 of the piperidine ring in formula I, and where X1, X2, X3, X4 and X5 are independently selected from a group containing carbon and oxygen, where X4 in formula IB and X1 in formula IC can assume one of these values or can be additionally selected from a group comprising S and O, where carbon and nitrogen ring atoms can include a number of hydrogen atoms or substitutes R3 or R4 if contained, taking into account limitations given below, required to bring the number of bonds of the carbon ring atom to 4 and 3 for the nitrogen ring atom; provided that in formula IA at least 2, preferably at least 3 of the atoms X1-X5 denote carbon and in formulae IB and IC at least one of X1-X4 denotes carbon, preferably 2 of the atoms X1-X4 denote carbon; y equals 0 or 1; z equals 0 or 1; R3, which can be bonded with any of the atoms X1, X2, X3 and X4, denotes hydrogen or a C1-C7-alkyloxy-C1-C7-alkyloxy group, phenyloxy-C1-C7-alkyl, phenyl, pyridinyl, phenyl- C1-C7-alkoxy group, phenyloxy group, phenyloxy-C1-C7-alkoxy group, pyridyl-C1-C7-alkoxy group, tetrahydropyranyloxy group, 2H,3H-1,4-benzodioxynyl-C1-C7-alkoxy group, phenylaminocarbonyl or phenylcarbonylamino group, where each phenyl or pyridyl is unsubstituted or contains one or up to 3 substitutes, preferably 1 or 2 substitutes independently selected from a group comprising C1-C7-alkyl, hydroxy group, C1-C7-alkoxy group, phenyl-C1-C7-alkoxy group, where phenyl is unsubstituted or substituted with a C1-C7-alkoxy group and/or halogen; carboxy- C1-C7-alkyloxy group, N-mono- or N,N-di-(C1-C7-alkyl)aminocarbonyl-C1-C7-alkyloxy group, halogen, amino group, N-mono- or N,N-di-(C1-C7-alkyl)amino group, C1-C7-alkanoylamino group, morpholino-C1-C7-alkoxy group, thiomorpholino-C1-C7-alkoxy group, pyridyl-C1-C7-alkoxy group, pyrazolyl, 4- C1-C7-alkylpiperidin-1-yl, tetrazolyl, carboxyl, N-mono- or N,N-di-(C1-C7-alkylamino)carbonyl or cyano group; or denotes 2-oxo-3-phenyltetrahydropyrazolidin-1-yl, oxetidin-3-yl-C1-C7-alkyloxy group, 3-C1-C7-alkyloxetidin-3-yl- C1-C7-alkyloxy group or 2-oxotetrahydrofuran-4-yl- C1-C7-alkyloxy group; provided that if R3 denotes hydrogen, then y and z are equal to 0; R4, if contained, denotes a hydroxy group, halogen or C1-C7-alkoxy group; T denotes carbonyl; and R11 denotes hydrogen, or pharmaceutically acceptable salts thereof. The invention also relates to use of formula I compounds, a pharmaceutical composition, as well as a method of treating diseases.

EFFECT: obtaining novel biologically active compounds having activity towards rennin.

11 cl, 338 ex, 1 tbl

 

The text description is given in facsimile form.

1. The compound of the formula I

in which R1 denotes alkyl or cycloalkyl;
R2 denotes a phenyl-C1-C7-alkyl, di-(phenyl)-C1-C7-alkyl, naphthyl-C1-C7-alkyl, phenyl, naphthyl, pyridyl-C1-C7-alkyl, indolyl-C1-C7-alkyl, 1H-indazole-C1-C7-alkyl, chinolin-C1-C7-alkyl, ethanolic-C1-C7and the keel, 1,2,3,4-tetrahydro-1,4-benzoxazine-C1-C7-alkyl, 2H-1,4-benzoxazin-3(4H)-IMT-C1-C7-alkyl, 9-xantener-C1-C7-alkyl, 1-benzothiophene-C1-C7-alkyl, pyridyl, indolyl, 1H-indazole, hinely, ethanolic, 1,2,3,4-tetrahydro-1,4-benzoxazine, 2H-1,4-benzoxazin-3(4H)-IMT, 9-xantener, 1-benzothiophenes, 4H-benzo[1,4]thiazin-3-IMT, 3,4-dihydro-1H-quinoline-2-IMT or 3H-benzoxazol-2-IMT, where each phenyl, naphthyl, pyridyl, indolyl, 1H-indazole, hinely, ethanolic, 1,2,3,4-tetrahydro-1,4-benzoxazines, 2H-1,4-benzoxazin-3(4H)-IMT, 1-benzothiophenes, 4H-benzo[1,4]thiazin-3-IMT, 3,4-dihydro-1H-quinoline-2-IMT or 3H-benzoxazol-2-IMT is unsubstituted or contains one or more, up to 3 substituents independently selected from the group comprising From1-C7-alkyl, hydroxy-C1-C7-alkyl, C1-C7-alkoxy-C1-C7-alkyl, C1-C7-alkoxy-C1-C7-alkoxy-C1-C7-alkyl, C1-C7-alkanoyloxy-C1-C7-alkyl, amino-C1-C7-alkyl, C1-C7-alkoxy-C1-C7-alkylamino-C1-C7-alkyl, C1-C7-alkanolamine-C1-C7-alkyl, C1-C7-alkylsulfonamides-C1-C7-alkyl, carboxy-C1-C7-alkyl, C1-C7-alkoxycarbonyl-C -C7-alkyl, halogen, hydroxy-group, With1-C7-alkoxygroup,1-C7-alkoxy-C1-C7-alkoxygroup, amino-C1-C7-alkoxygroup, N-C1-C7-alkanolamine-C1-C7-alkoxygroup, carbarnoyl-C1-C7-alkoxygroup, N-C1-C7-allylcarbamate-C1-C7-alkoxygroup,1-C7-alkanoyl,1-C7-alkyloxy-C1-C7-alkanoyl,1-C7-alkoxy-C1-C7-alkanoyl, carboxyl, carbarnoyl and N1-C7-alkoxy-C1-C7-allylcarbamate;
W denotes the fragment, selected from among residues of the formulae IA, IB and IC,

where the asterisk (*) indicates the position in which the fragment W is attached to the carbon atom in position 4 piperidino ring in the formula I, and where X1, X2, X3, X4and X5independently selected from the group comprising carbon and nitrogen, where X4in formula IB and X1in formula IC may have one of these values or optionally selected from the group comprising S and O, where the ring atoms of carbon and nitrogen may contain the number of hydrogen atoms or substituents R3 or - if contains with regard to the following restrictions - R4, are necessary to bring the number of links of the ring carbon atoms to , ring nitrogen atom and up to 3; provided that in formula IA at least 2, preferably at least 3 atoms of X1-X5mean carbon and in formulae IB and IC at least 1 of X1-X4denotes carbon, preferably 2 atoms of X1-X4represent carbon;
y is 0 or 1;
z is 0 or 1;
R3, which may be associated with any atom of X1, X2, X3and X4denotes hydrogen or C1-C7-alkyloxy-C1-C7-alkyloxy, phenyloxy-C1-C7-alkyl, phenyl, pyridyl, phenyl-C1-C7-alkoxygroup, fenoxaprop, phenyloxy-C1-C7-alkoxygroup, pyridyl-C1-C7-alkoxygroup, tetrahydropyranyloxy, 2H,3H-1,4-benzodioxin-C1-C7-alkoxygroup, phenylenecarbonyl or phenylcarbonylamino, where each phenyl or pyridyl is unsubstituted or contains one or more, up to 3 substituents, preferably 1 or 2 substituent, independently selected from the group comprising From1-C7-alkyl, hydroxy-group, With1-C7-alkoxygroup, phenyl-C1-C7-alkoxygroup, where phenyl is unsubstituted or substituted With1-C7-alkoxygroup and/or halogen; carboxy-C1-C7-alkyloxy, N-mono - or N,N-di(C1 -C7-alkyl)aminocarbonyl-C1-C7-alkyloxy, halogen, amino, N-mono - or N,N-di-(C1-C7-alkyl)amino, C1-C7-alkanolamines, morpholino-C1-C7-alkoxygroup, thiomorpholine-C1-C7-alkoxygroup, pyridyl-C1-C7-alkoxygroup, pyrazolyl, 4-C1-C7-alkylpiperazine-1-yl, tetrazolyl, carboxyl, N-mono - or N,N-di-(C1-C7-alkylamino)carbonyl and cyano;
or denotes a 2-oxo-3-vinyltetrahydrofuran-1-yl, oxacilin-3-yl-C1-C7-alkyloxy, 3-C1-C7-alkyloxyalkyl-3-yl-C1-C7-alkyloxy or 2-oxitetraciclina-4-yl-C1-C7-the alkyl oxygraph;
provided that if R3 denotes hydrogen, y and z are 0;
R4 - if it contains, refers to a hydroxy-group, halogen or1-C7-alkoxygroup;
T denotes a carbonyl; and
R11 denotes hydrogen,
or its pharmaceutically acceptable salt.

2. The compound of formula I according to claim 1, in which
R1 denotes a3-C8-cycloalkyl;
R2 denotes a phenyl-C1-C7-alkyl, di-(phenyl)-C1-C7-alkyl, phenyl, indolyl-C1-C7-alkyl, 1H-indazole-C1-C7-alkyl, 9-xantener-C1-C7-alkyl, 1,2,3,4-tetrahydro-1,4-benzoxazine or 2H-1,4-benzoxazin-3(4H)-he is l, where each phenyl, indolyl, 1H-indazole, 1,2,3,4-tetrahydro-1,4-benzoxazine or 2H-1,4-benzoxazin-3(4H)-IMT is unsubstituted or contains up to 3 substituents independently selected from the group comprising From1-C7-alkyl, C1-C7-alkoxy-C1-C7-alkyl, C1-C7-alkoxy-C1-C7-alkoxy-C1-C7-alkyl, C1-C7-alkanolamine-C1-C7-alkyl, C1-C7-alkylsulfonamides-C1-C7-alkyl, carboxy-C1-C7-alkyl, C1-C7-alkoxycarbonyl-C1-C7-alkyl, halogen, C1-C7-alkoxygroup, C1-C7-alkoxy-C1-C7-alkoxygroup, amino-C1-C7-alkoxygroup and C1-C7-alkoxy-C1-C7-alkanoyl;
W represents a fragment of formula IA

where the asterisk (*) indicates the position in which the fragment W is attached to the carbon atom in position 4 piperidino ring in the formula I, and where one of X1and X2represents nitrogen or CH, while the other and X3, X4and X5represent CH; provided that R3 is attached to the X1or X2or, it is preferable to X3or X4;
or a fragment of formula IC

where the asterisk (*) indicates the position in which the fragment W p is isodine to the carbon atom in position 4 piperidino ring in the formula I, and where X1=O, X2represents nitrogen or CH, X3represents CH and X4represents nitrogen or CH; provided that not more than one of X2and X4denotes nitrogen, and provided that R3 is attached to the X2or preferably to X3or X4; where in each case, when R3 denotes a joining fragment of formula IA or IC, instead of a hydrogen atom in a ring member NH or CH, mentioned, when attached R3, the residue R3 is present;
y is 0 or 1;
z is 0 or 1;
R3 denotes hydrogen or C1-C7-alkyloxy-C1-C7-alkyloxy, phenyl, pyridyl, phenyl-C1-C7-alkoxygroup, fenoxaprop, phenyloxy-C1-C7-alkoxygroup, pyridyl-C1-C7-alkoxygroup, tetrahydropyranyloxy, 2H,3H-1,4-benzodioxin-C1-C7-alkoxygroup, phenylenecarbonyl or phenylcarbonylamino, where each phenyl or pyridyl is unsubstituted or contains up to 3 substituents, for example 1 or 2 substituent, independently selected from the group comprising a hydroxy-group, With1-C7-alkoxygroup, halogen, amino, N-mono - or N,N-di-(C1-C7-alkyl)amino group, provided that if R3 denotes hydrogen, y and z are 0;
R4 - if it contains (z=1), denotes a hydroxy-group, halogen or1-C7 -alkoxygroup;
T denotes a carbonyl; and
R11 denotes hydrogen,
or its pharmaceutically acceptable salt.

3. The compound of formula I according to claim 1 or 2, with the following configuration

in which R1, R2, R11, T, and W are as defined for compounds of formula I in claim 1 or 2, or its pharmaceutically acceptable salt.

4. The compound of formula I according to claim 1, selected from the group of compounds having the following formula:
;
;
;
;

or in each case its pharmaceutically acceptable salt.

5. The compound of formula I according to claim 1, selected from among compounds of the formula
,
presented in the table below:






























































6. The compound of formula I or its pharmaceutically acceptable salt according to any one of claims 1 to 5, intended for the manufacture of pharmaceutical compositions used in the diagnosis or therapeutic treatment of a warm-blooded animal.

7. The compound of formula I or its pharmaceutically acceptable salt according to any one of claims 1 to 5, intended for use according to claim 6 for the treatment of a disease that depends on activity of renin.

8. The use of the compounds of formula I or its pharmaceutically acceptable salt according to any one of claims 1 to 5 for the manufacture of pharmaceutical compositions used in the treatment of hypertension.

9. The use of the compounds of formula I or its pharmaceutically acceptable salt according to any one of claims 1 to 5 for the treatment of hypertension.

10. Pharmaceutical composition, which has activity against renin, comprising a compound of formula I or its pharmaceutically acceptable salt according to any one of claims 1 to 5 and at least one pharmaceutically acceptable carrier.

11. The method of treatment of a disease that depends on activity of renin, including the introduction of a warm-blooded animal, especially a human in need of such treatment, a pharmaceutical is effective amounts of compounds of formula I or its pharmaceutically acceptable salt according to any one of claims 1 to 7.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of pyrrolo[3,2-c]pyridine-4-one 2-indolinone of formula (I). Compound of formula (I): , where: represents single or binary bond; X and Y independently on each other are selected from C or N; X and Y represent N, then R5 and R7 are absent; R1 and R2 represent H; R3 is selected from alkyl, trifluormethyl, aryl and aralkyl, where said alkyl, aryl or aralkyl iis substituted by one or more halogens or hydroxyls; R4 is selected from alkyl, cycloalkyl, heterocycloalkyl, -[CH2CH(OH)]rCH2NR9R10 and -(CH2)nNR9R10, where said alkyl or heterocycloalkyl is probably substituted by one or more groups, selected from group, consisting of hydroxyl, amino, aminoalkyl, hydroxyalkyl and -NR9R10; X and Y represent C, then R5, R6, R7, R8 are independently on each other selected from hydrogen, halo, alkyl, heterocycloalkyl, aryl, heteroaryl, hydroxyl, -OR9, -NR9R10, -NSO2R9, -NR9COR10, -NHCO2R10, where said aryl, heteroaryl, heterocycloalkyl are substituted by one or more groups, consisting of alkyl, alkoxyl and halogen; R9 and R10 independently on each other are selected from hydrogen, alkyl, cycloalkyl, where said alkyl, aryl, independently on each other are substituted by one or more groups, consisting of alkyl, aryl, hydroxyl, alkoxyl; R9 and R10 together with atom, to which they are bound, form 4-6-member rings, where 4-6-member rings can, in addition, contain one-two heteroatoms, selected from group, consisting of N and O, and each 4-6-member ring, formed in said way, is probably substituted by one or more groups, consisting of alkyl; n represents 2-6 and their pharmaceutically acceptable salts, where R1, R2, R3, R4, R5, R6, R7, R8, X, Y and -have values given in description. Also described is pharmaceutical composition, containing said compounds and possessing activity of proteinkinase inhibitor, methods of obtaining and pharmaceutical applications.

EFFECT: obtained and described are novel compounds, which can be useful as proteinkinase inhibitors.

20 cl, 131 ex, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula pharmaceutically acceptable salts thereof, where ---- independently denotes a single or double bond; ring Q is imidazole, triazole (for example 1,2,3-triazole or 1,3,4-triazole), tetrazole or oxadiazole; B denotes C(R7)(R8) or C(R7), where if the bond between B and Y is a single bond, B denotes C(R7)(R8), and when the bond between B and Y is a double bond, B denotes C(R7); Y denotes C(R7), C(R7)(R8) or O, where if the bond between B and Y is a single bond, Y denotes C(R7)(R8) or O, and when the bond between B and Y is a double bond, B denotes C(R7); Z1 denotes -CH2-, -(CH2)2-, -CH2CH-CH3-, where Z1 is bonded on the left side to a nitrogen atom or -(CH2)3-; X denotes C(R1) or N; A denotes quinolyl, quinazolinyl or benzofuranyl, any of which is optionally substituted with 1-4 substitutes, which can be identical or different and are selected from a group comprising halogen, cyano, C1-6-alkyl, halogen-C1-6-alkyl, C(O)N(R3)(R4), 5-member heterocyclic ring containing 1-3 heteroatoms selected from N or O. The heterocyclic ring is optionally substituted with C1-6-alkyl; when R is present, each independently denotes halogen, C1-6-alkyl; each R1 denotes hydrogen or methyl; each R2 denotes cyano, C1-6-alkyl, C1-6-alkoxy, halogen-C1-6-alkyl, =O, -C(O)N(R3)(R4), -C(O)N(R3)-C1-6-alkoxy, -C(NOR5)R6, -C(O)R6, -C(O)OR7, -C(O)NHNHC(O)R6, 5-member heterocyclic ring containing 1-3 heteroatoms selected from N or O. The heterocyclic ring is optionally substituted with C1-6-alkyl; R3 and R4 independently denote hydrogen; C1-6-alkyl; C3-7-cycloalkyl; C3-7-cycloalkyl-C1-6-alkyl; or when R3 and R4 are bonded to the same nitrogen atom, they, together with the nitrogen atom, they form a 4-, 5- or 6-member ring which optionally contains one extra O atom in the ring; R5 denotes C1-4-alkyl; R6 denotes C3-7-cycloalkyl or C1-6-alkyl; R7 and R8 independently denote hydrogen or C1-6-alkyl; p equals 0, 1 or 2; r equals 0, 1, 2 or 3; s equals 0, 1, 2 or 3. The invention also relates to 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazin-3-carboxamide, 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperidinyl]ethyl}imidazo-[1,5-a]quinoline-3-carboxamide, dihydrochloride 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperidinyl]ethyl}[1,2,3]triazolo[1,5-a]quinoline-3-carboxamide, 7-methyl-6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4,5-dihydroimidazo[1,5-a]quinoline-3-carboxamide, to use of the compound in any of claims 1-16, as well as a pharmaceutical composition.

EFFECT: obtaining novel biologically active compounds, having 5-HT1 receptor mediated activity.

23 cl, 195 ex

FIELD: chemistry.

SUBSTANCE: invention describes dibenzo[b,f]pyrido[1,2-d][1,4]diazepinyl derivatives of general formula I: or pharmaceutically acceptable salts thereof (values of radicals are listed in the claim), which are glucocorticoid receptor modulators.

EFFECT: derivatives can be used in treating immunological and inflammatory diseases.

11 cl, 49 ex

FIELD: chemistry.

SUBSTANCE: invention relates to systems containing an imidazole ring, which correspond to a substance of formula (I-1): , in which: X denotes alkylene which is facultatively interrupted with one or more -O- groups; Z denotes -C(O)-; R1-1 is selected from a group comprising: hydrogen, alkyl, phenyl, -N(CH3)(OCH3), and phenyl which is substituted with one or more halogens; R2 denotes hydrogen; alkyl; hydroxyalkyl; or alkoxyalkyl; RA and RB taken together form an open phenyl ring, or to pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions for inducing biosynthesis of cytokine, which contains such substances.

EFFECT: substances can be used in medicine as immunomodulators for inducing or inhibiting biosynthesis of cytokines in animals and when treating diseases, including viral and malignant diseases.

18 cl, 37 ex

FIELD: chemistry.

SUBSTANCE: invention relates to imidazo[1,2-a]pyridine derivatives of formula in which radicals R1, R2, R3 and R4 independently denote a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a (C1-C12)alkyl radical which can be substituted with one or more halogen atoms or OH, and a O-(C1-C12)alkyl radicalwhich is substituted with phenyl, or two of radicals R1, R2, R3 and R4 can denote part of a phenyl ring; R5 denotes a (C1-C12)alkyl radical which can be substituted with one or more OH, methanesulphanyl, COOH or a halogen atom, (C2-C12)alkenyl radical, (C2-C12)alkynyl radical, (C6-C10)aryl radical, heteroaryl radical, which is an aromatic groupcontaining 5-10 ring members and 1-2 nitrogen or oxygen ring atoms, (C3-C10)cycloalkyl radical, (C1-C12)alkyl(C3-C10)cycloalkyl radical, (C6-C10)aryl(C1-C12)alkyl radical; radicals R6 and R7 independently denote a hydrogen atom or a (C1-C12)alkyl radical, which can be substituted with COOH, (C6-C10)aryl radical; and X denotes a group of formula - CO-NHOH or formula where U denotes a bond, CH2, V denotes O, S, W denotes NH, and Y denotes OH, or pharmaceutically acceptable salts thereof, solvates, hydrates. The invention also relates to the pharmaceutical composition based on the formula I compound and use of the formula I compound.

EFFECT: novel derivatives have peptide deformylase inhibiting activity.

16 cl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof, having CRP receptor antagonist activity. In formula (I) R1 denotes C3-C8 alkyl, optionally substituted with hydroxyl; phenyl optionally substituted with 1-3 substitutes selected from halogen, nitro, amino, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, optionally substituted with hydroxyl or C1-C4 alkylamino; naphthyl; C-bonded 5-6-member heteroaryl with 1-2 heteroatoms selected from S, N or O, optionally substituted with C1-C4 alkyl, C1-C4 alkoxy or acetyl; N-bonded 5-member heteroaryl with 1-2 heteroatoms selected from N, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl or phenyl; R2 denotes phenyl, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl, halogenC1-C4alkyl, C1-C4 alkoxy, halogenC1-C4alkoxy, halogen, hydroxy, di(C1-C4 alkyl)amino or di(C1-C4 alkyl)aminocarbonyl; or a heterocyclic group which is pyridyl, optionally substituted with 1-3 substitutes selected from C1-C4 alkyl, C1-C4 alkoxy or di(C1-C4 alkyl)amino; X denotes -NR3-, where R3 denotes C1-C4 alkyl, optionally substituted with hydroxyl, carboxyl or C1-C4 alkoxycarbonyl; Y1 denotes CR3a, where R3a denotes hydrogen, halogen, cyano, hydroxy, C1-C4 alkyl, optionally substituted with hydroxyl or halogen, C1-C4 alkoxy optionally substituted with halogen; Y2 denotes CR3b, where R3b denotes hydrogen or halogen; Y3 denotes N or CR3c, where R3c denotes hydrogen; and Z denotes O or -NR4-, where R4 denotes hydrogen.

EFFECT: invention also pertains to a method of producing compounds of formula (I), a pharmaceutical composition, an inhibiting method, CRF receptor antagonists and use thereof to prepare a medicinal agent.

25 cl, 9 tbl, 163 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I: or its pharmaceutically acceptable salt or stereoisomer, where a is independently equal to 0 or 1; b is independently equal to 0 or 1; R1 is selected from aryl, heterocyclyl and NR10R11; said aryl or heterocyclyl group is optionally substituted with between one and five substitutes, each independently selected from R8; R5 is selected from C1-6alkyl, C2-6alkenyl, -C(=O)NR10R11, NHS(O)2NR10R11 and NR10R11, each alkyl, alkenyl or aryl is optionally substituted with between one and five substitutes, each independently selected from R8; R8 independently denotes (C=O)aObC1-C10alkyl, (C=O)aObaryl, (C=O)aObheterocyclyl, OH, Oa(C=O)bNR10R11 or (C=O)aCbC3-C8cycloalkyl, said alkyl, aryl, heterocyclyl are optionally substituted with one, two or three substitutes selected from R9; R9 is independently selected from (C=O)aCb(C1-C10)alkyl and N(Rb)2; R10 and R11 is independently selected from H, (C=O)Cb(C1-C10)alkyl, C1-C10alkyl, SO2Ra, said alkyl is optionally substituted with one, two or three substitutes selected from R8 or R10 and R11 can be taken together with nitrogen to which they are bonded with formation of a monocyclic heterocycle with 5 members in each ring and optionally contains one or two heteroatoms, in addition to the nitrogen, selected from N and S, said monocyclic heterocycle is optionally substituted with one, two or three substitutes selected from R9; Ra is independently selected from (C1-C6)alkyl, (C2-C6)alkenyl; and Rb is independently selected from H, (C1-C6)alkyd, as well as to a pharmaceutical composition for inhibiting receptor tyrosine kinase MET based on this compound, as well as a method of using said compound to produce a drug.

EFFECT: novel compounds which can be used to treat cell proliferative diseases, disorders associated with MET activity and for inhibiting receptor tyrosine kinase MET are obtained and described.

8 cl, 32 ex, 4 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel ligands, including novel compounds of general formula 1, a wide range of biological activity which simultaneously includes alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, including serotonin 5-HT7 receptors, in form of free bases, geometric isomers, racemic mixtures or separate optical isomers, as well as in form of pharmaceutically acceptable salts and/or hydrates. In formula 1

R1 denotes hydrogen; C1-C4alkyl optionally substituted with C1-C4alkoxycarbonyl, aromatic or saturated optionally annelated or optionally substituted with a five- or six-member heterocycle containing 1-2 N heteroatoms; C1-C3acyl; saturated optionally substituted six-member N-heterocycle; C1-C4alkoxycarbonyl; optionally substituted arylsulphonyl, R2 denotes a substitute of a cyclic system, including hydrogen; halogen; optionally substituted C1-C4alkyl;CF3, CN, C1-C4alkoxy; C1-C4alkoxycarbonyl; carboxyl; unsaturated six-member N-containing heterocyclyl or optionally substituted arylsulphonyl, Ar denotes phenyl, optionally substituted with C1-C4alkyl, dimethylamino group, one or more C1-C4alkoxy groups, one or more halides, CF3 group, nitro group, carboxyl, C1-C4alkoxycarbonyl, C1-C4acylamino group, CN, optionally annelated with a saturated heterocycle; optionally annelated and optionally substituted unsaturated five- or six-member heterocycle containing one or two heteroatoms selected from nitrogen, oxygen or sulphur; W denotes an optionally substituted (CH2)m group, optionally substituted CH=CH group, optionally substituted CH2-CH=CH group, C≡C group, SO2 group; n = 1 or 2; m=1, 2 or 3, the solid line accompanied by a dotted line (---) denotes a single or double bond.

EFFECT: compounds can be used to treat and/or prevent diseases or pathological conditions of the central nervous system, whose pathogenesis is associated with hyper- or hypo-activation of said receptors, for example anxiety or cognitive disorders, neurodegenerative and psychotic diseases.

42 cl, 26 dwg, 12 tbl, 20 ex

FIELD: chemistry.

SUBSTANCE: invention relates to use of 3,11b-cis-dihydrotetrabenazine or its pharmaceutically acceptable salts to prepare a medicinal agent for preventing or treating schizophrenia. The invention also relates to compounds for use in preventing or treating psychosis, methods of preventing or treating psychosis, as well as methods of preventing or alleviating a psychotic episode.

EFFECT: use of 3,11b-cis-dihydrotetrabenazine to prepare a medicinal agent for preventing or treating schizophrenia.

34 cl, 7 ex, 6 tbl, 4 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

and pharmaceutically acceptable salts thereof, where substitutes R1-R4 are as defined in claim 1. Said compounds have 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) enzyme inhibiting activity.

EFFECT: compounds can be used in form of a pharmaceutical composition.

15 cl, 1 tbl, 94 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method for selective production of N-[3-(1,3,5-dithiazinan-5-yl)propyl]-N-[4-(1,3,5-dithiazinan-5-yl)butyl]amine and N1,N4-bis-[3-(1,3,5-dithiazinan-5-yl)propyl]-1,4-butane diamine which involves reaction of an amine with a hydrogen sulphide saturated aqueous solution of formaldehyde, where the amine used is polymethylenepolyamine (spermidine or spermine) in molar ratio polyamine: formaldehyde: hydrogen sulphide equal to 1:6:4 and the reaction is carried out at 20°C for 3 hours.

EFFECT: compounds can be used as selective sorbents and extraction agents of precious metals, special reagents for inhibiting bacterial activity in various media.

1 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: described are novel derivatives of genera formula (1) (where A denotes an oxygen or sulphur atom, -CH2- or -NH- group; R1 denotes C1-6alkyl group, possibly substituted ; R1A denotes a hydrogen atom or a C1-6 alkyl group; or these two radicals together with a carbon atom to which they are bonded form a cyclic C3-6 alkyl group; R2 denotes a C1-6 alkyl group or a C3-6 cycloalkyl group; R3 denotes an aryl group or a heteroaryl group, which can be substituted; R4 denotes a hydrogen atom; R5 denotes C1-6 alkyl group, aryl or heteroaryl group, which can be substituted), a pharmaceutical composition containing said derivatives and intermediate compounds. Said compounds (1) can inhibit bonding between SIP and its receptor Edg-1 (SIP1).

EFFECT: possibility of use in medicine.

18 cl, 2 tbl, 28 ex

FIELD: chemistry.

SUBSTANCE: described are heterobicyclic derivatives of formula (I)

, in which V denotes -C(R7)-; W denotes a single bond or -C(R8R9)-; X denotes O, S, SO, SO2 or N(R10); Y denotes -C(R11R12)-, -C(R11R12)C(R13R14)C(R11R12)C(R13R14)C(R15R16)-, -C(R11R12)C(R13R14)C(R15R16)C(R17R18)- or- C(R11)=C(R12)-; R1, R2, R3, R4 and R5 independently denote hydrogen, halogen, (lower)alkyl, fluoro(lower)alkyl, (lower)alkoxy group, fluoro(lower)alkoxy group, NH2-C(O); R6 denotes a phenyl, pyridyl, pyrazolyl or thiazolyl group, where the group is optionally substituted with 1-4 substitutes selected from a group consisting of halogen, cyano group, (lower)alkyl, (lower)alkoxy group, COOH, 1H-tetrazol-5-yl, 5-oxo-4H-[1,2,4]oxadiazol-3-yl, where (lower)alkyl is optionally substituted with COOH. A pharmaceutical composition is also described.

EFFECT: said compounds inhibit L-CPT1 and can be used as medicinal agents.

27 cl, 120 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrazine-2-carboxamide derivatives of general

formula , where R1 denote a 5- or 6-member ring, having a formula given in claim 1, R2 denotes H or C1-C7-alkyl; R3 denotes phenyl, pyridinyl or pyrimidinyl, possibly substituted with the following substitutes: Cl, F or Br; R4 denotes H, CI, F, Br, CF3 or C1-C7-alkyl; R5 denotes C1-C7-alkyl; as well as pharmaceutically acceptable salts thereof. Disclosed compounds are metabotropic glutamate receptor (mGLUR 5) antagonists. The invention also pertains to a medicinal agent based on disclosed compounds.

EFFECT: improved method.

17 cl, 23 ex

FIELD: medicine.

SUBSTANCE: invention refers to derivatives of 2-pyridylmethylenecarboxamide of formula (I), where: -A represents a substituted or unsubstituted 5-member heterocyclyl group bound with carbonyl through carbon atom; -Z1 and Z2 which can be equal or different, represent hydrogen atom; C1-C5-alkyl; C5-alkoxycarbonyl; -Z3 represents substituted or unsubstituted C3-C7cycloalkyl; -Y represents C1-C5-halogenalkyl, containing to 5 halogen atoms which can be equal or different; X which can be equal or different, represents halogen atom, - n=0, 1, 2 or 3; and to their salts. Besides the invention describes a method of plant pathogenic fungi control with the use of such compounds.

EFFECT: there are prepared and described new derivatives of 2-pyridylmethylenecarboxamide which can be effective as fungicidal active agents.

8 cl, 96 ex, 4 tbl

FIELD: chemistry.

SUBSTANCE: disclosed compounds can be used as a medicinal agent having CXCR2 inhibiting properties. In formula I , X denotes -CR3=CR4-, -CR5=N-, -N=CR6-, -NR7- or -S-; R3, R4, R5 and R6 independently denote hydrogen, F, CI, Br, I; R7 denotes hydrogen; Y1, Y2, Y3 and Y4 independently denote -CR8- or nitrogen, provided that at least two of Y1, Y2, Y3 and Y4 denote -CR8-; where R8 denotes hydrogen, F, CI, Br, I; A denotes a cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms; a bicyclic partially saturated 9-member cycloalkyl; a bicyclic partially saturated 9-10-member heterocycle in which two atoms in the ring are oxygen atoms; phenyl; naphthyl; a 5-6-member heteroaryl in which 1-3 atoms in the ring are oxygen, sulphur and nitrogen atoms; a 9-10-member bicyclic heteroaryl in which 1-3 atoms in the ring are nitrogen, oxygen and sulphur atoms; a 6-member heterocycle in which one atom in the ring is a nitrogen atom and which can be unsubstituted or substituted with alkyl having 1, 2, 3 or 4 carbon atoms, -C(O)CH3, -C(O)CH2CH3, -C(O)cyclopropyl, -C(O)CF3 and -C(O)OC(CH3)3; where phenyl, heterocyclic or heteroaryl radical is substituted with 1, 2 or 3 radicals selected from a group consisting of F, O, Br, I, OH, CN, NO2, SCF3, SF3, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; cycloalkyl having 3, 4, 5 or 6 carbon atoms; alkoxy having 1, 2, 3, 4, 5 or 6 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; -S-alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; -NR9R10, C(O)R44, S(O)SR47, -(CH2)k-phenyl, 5-6-member heteroaryl, in which 1-3 atoms in the ring are nitrogen and sulphur atoms; where the phenyl radical may be substituted with F, CI, Br, I; R9 is an alkyl having 1, 2, 3 or 4 carbon atoms; R10 is an alkyl having 1, 2, 3 or 4 carbon atoms; R44 is an alkyl having 1, 2, 3 or 4 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; alkoxy having 1, 2, 3 or 4 carbon atoms, cycloalkyl having 3, 4, 5 or 6 carbon atoms; R47 is an alkyl having 1, 2, 3 or 4 carbon atoms; k equals 0, 1, 2 or 3; s equals 1 or 2; B is -O-C(R11R12), -C≡C-, -CR52=CR53-, -C(R13R14)C(R15R16), -NR17-C(R18R19); R11, R12, R13, R14, R15, R16, R17, R18, R19, R52, R53 independently denote hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; D is C(O)OH, C(O)NHR21 or C(=NR58)NHR22; R21 and R22 independently denote hydrogen, -SO2-alkyl having 1, 2, 3 or 4 carbon atoms, -SO2-phenyl; R58 is OH; R1 and R2 independently denote an alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, where the alkyl radicals are unsubstituted or substituted with 1 radical selected from a group consisting of F, Cl, Br, I, phenyl substituted with OH; or R1 and R2, taken together with a carbon atom with which they are bonded form a 3-, 4-, 5- or 6-member carbocycle. The invention also relates to use of formula I compounds in preparing a medicinal agent which has CXCR2 inhibiting properties, to a medicinal agent which containing an effective amount of the disclosed compound and having CXCR2 inhibiting properties, as well as to use of formula II compounds (formula and values of radicals are given in the formula of invention) in preparing a medicinal agent having CXCR2 inhibiting properties.

EFFECT: high effectiveness of application.

10 cl, 384 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described novel compounds of formula (I), where R1 represents hydroxymethyl; R2 is selected from -C(O)NR4R5; HET-1 represents 5- or 6-member heteroaryl ring, bound by atom C; R3 represents halogeno; R4 and R5 together with nitrogen atom, to which they are bound, can form heterocyclyl ring system, as it is defined for HET-3; HET-3 represents possibly substituted azetidinyl; m equals 1; n equals 0, 1 or 2; or their pharmaceutically acceptable salt, which can be applied as glucokinase (GLK) activators or active ingredient of pharmaceutical compositions, also described are methods of obtaining them.

EFFECT: creation of novel compounds applied as glucokinase (GLK) activators in treatment of diabetes.

13 cl, 40 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds, which possess properties inhibiting HIV replication, of general formula (I) , in form of E-isomer, in which -a1=a2-a3=a4- represents bivalent radical of formula -CH=CH-CH=CH- (a-1); -b1=b2-b3=b4. Represents bivalent radical of formula -CH=CH-CH=CH- (b-1); n equals 0; m equals 2; each of R1 radicals independently on each other stands for hydrogen atom; C1-6alkyl; R2a stands for cyanogroup; X1 stands for -NR1-; R3 represents C2-6alkenyl, substituted with cyanogroup; R4 stands for C1-6alkyl; R5 represents radical of formula -Y-Alk-L, -Alk'-Y-L or -Alk'-Y-Alk-L; each of radicals Alk or Alk' independently represents bivalent C1-6alkyl or C2-6 alkenyl group; L stands for aryl or Het; Y stands for NR1; -CH=N-O-; Het stands for 5- or 6-member fully saturated ring system, in which one, two or three ring elements represent heteroatoms, each of which is independently selected from group, including nitrogen, oxygen and sulphur, and in which other ring elements represent carbon atoms; and, if possible, any nitrogen ring element can be optionally substituted with C1-6alkyl; and ring system can be optionally bound with benzene ring; and in which any carbon atom of ring, including any carbon atom of optionally bound benzene ring, each independently can be substituted with substituent selected from such groups as halogen atom, C1-6alkyl, hydroxyC1-4alkyl, carboxyC1-4alkyl, C1-4 alkylcarbonyloxyC1-4alkyl, di(C1-4alkyl)aminoC1-4alkyl, aryloxy, morpholinyl, aryl, Het1; Het1 stands for thienyl, isoxazolyl, thiadiazolyl, each of which can be optionally substituted with one or two C1-4alkyl radicals; Q stands for hydrogen atom; each aryl represents phenyl or phenyl, substituted with one, two substituents, each of which is independently selected from such groups as halogen atom, C1-6alkyl, C2-6alkinyl, cyano, polyhalogen C1-6alkyl or Het1, as well as to its pharmaceutically acceptable additive salts Invention also relates to pharmaceutical composition.

EFFECT: creation of novel compounds, which possess properties inhibiting HIV replication

5 cl, 7 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel derivatives of 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydrochinoline, represented by formula , where R1 represents (1-6C)alkyl; R2 represents halogen, (1-4C)alcoxy; R3 represents OH, NO2, CN, fluoridated with (1-4C)alkoxy, (1-4C)alkoxy(2-4C)alkoxy. hydroxy(2-4C)alkoxy, (1-4C)alkoxycarbonyl, R7, R8-amino, R9, R10-amino, R9, R10-aminocarbonyl, R9, R10-aminosulfonyl or phenyl(1-4C)alkoxy, where phenyl ring in composition phenyl(1-4C)alkoxy is optionally substituted with one or several substituents, selected from (1-4C)alkoxy; R4 represents R11-phenyl or R11-(4-5C)heteroaryl, which represents heteroaromatic group, containing 4-5 carbon atoms and at least one heteroatom, selected from N and S, where phenyl or heteroaryl group is optionally additionally substituted with one or several substituents, selected from nitro, (1-4C)alkyl, (1-4C)alkoxy; R7 represents H, (1-4C)alkyl; R8 represents (1-4C)alkylsulfonyl, (1-4C)alkylcarbonyl, (1-4C)alkoxycarbonyl, (1-4C)alkoxy(1-4C)alkylcarbonyl, furylcarbonyl; phenyl(1-4C)alkylcarbonyl, where phenyl ring is optionally substituted with one or several substituents, selected from (1-4C)alkoxy; R9 and R10 are not necessarily selected from H, (1-6C)alkyl and (1-4C)alkoxy(2-4C)alkyl; or R9 and R10 can be bound together with formation of morpholinyl ring; R11 represents H, R12, R13-amino, R14, R15-aminocarbonyl or R14, R15-aminosulfonyl; R12 represents H; R13 represents (1-4C)alkylsulfonyl, (1-4C)alkylcarbonyl, (1-4C)alkoxycarbonyl or pyperazinyl(1-4C)alkylcarbonyl; R14 and R15 are independently selected from H, (1-6C)alkyl, (1-4C)alkoxy(2-4C)alkyl and imidazolyl(1-4C)alkyl; X represents O or R16-N; Y represents CH2 or C(O);Z represents CN; R16 represents H, (1-4C)alkyl, (1-4C)alkylcarbonyl; or their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition, as well as to application of 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydrochinoline derivatives by any of i.i. 1-10.

EFFECT: obtaining novel biologically active compounds, which possess agonistic activity with respect to FSH receptor.

13 cl, 43 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to novel quinoline or quinazoline derivatives of general formula

Ib, where R1 is C1-6-alkyl or C1-6-alkoxy; X is N or CH; R3 and R4 independently denote hydrogen, C1-6-alkyl, C1-6-alkylsulphonyl or a group of formula (IIa), where A is oxygen or sulphur; D is -(CH2)t, -(CH2)tO- or -O(CH2)t, where t equals 0, 1, 2, 3 or 4; and E is C1-6-alkyl, C3-7-cycloalkyl, or a 3-7-member monocyclic aromatic ring or a 6-10-member bicyclic aromatic ring in which 1-3 carbon atoms in the ring(s) are optionally substituted with a heteroatom which is independently selected from nitrogen, oxygen and sulphur, (optionally substituted with 1 or 2 substitutes independently selected from halogen, C1-6-alkyl, CF3, cyano, hydroxy and C1-6-alkoxy); or a group of formula (IIb), where A is oxygen or sulphur; D is -(CH2)t-, -(CH2)tO- or -O(CH2)t, where t equals 0, 1, 2, 3 or 4; and E is C1-6-alkyl, C3-7-cycloalkyl, or a 3-7-member monocyclic aromatic ring or a 6-10-member bicyclic aromatic ring in which 1-3 carbon atoms in the ring(s) are optionally substituted with a heteroatom which is independently selected from nitrogen, oxygen and sulphur (optionally substituted with 1 or 2 substitutes independently selected from halogen, C1-6-alkyl, CF3, cyano, hydroxy and C1-6-alkoxy); or R3 and R4 together with the nitrogen atom with which they are bonded form a 3-7-member ring or a 6-10-member bicyclic ring which can be saturated, partially saturated or unsaturated and contain 1, 2 or 3 heteroatoms selected from nitrogen, sulphur and oxygen, where each group is optionally substituted with 1 or 2 substitutes selected from oxo, C1-6-alkyl, C1-6-alkoxy, aryl and aryl-C1-6-alkyl (where aryl and aryl-C1-6-alkyl are also optionally substituted with 1 or 2 with C1-6-alkyls or C1-6-alkoxy). The invention also relates to use of formula Ib compounds in preparing a medicinal agent, to a pharmaceutical composition based on formula Ib compound and preparation method thereof.

EFFECT: obtaining novel quinoline and quinazoline derivatives having high affinity to 5-HT1-receptors.

12 cl, 171 ex

FIELD: chemistry.

SUBSTANCE: described are novel derivatives of genera formula (1) (where A denotes an oxygen or sulphur atom, -CH2- or -NH- group; R1 denotes C1-6alkyl group, possibly substituted ; R1A denotes a hydrogen atom or a C1-6 alkyl group; or these two radicals together with a carbon atom to which they are bonded form a cyclic C3-6 alkyl group; R2 denotes a C1-6 alkyl group or a C3-6 cycloalkyl group; R3 denotes an aryl group or a heteroaryl group, which can be substituted; R4 denotes a hydrogen atom; R5 denotes C1-6 alkyl group, aryl or heteroaryl group, which can be substituted), a pharmaceutical composition containing said derivatives and intermediate compounds. Said compounds (1) can inhibit bonding between SIP and its receptor Edg-1 (SIP1).

EFFECT: possibility of use in medicine.

18 cl, 2 tbl, 28 ex

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