Novel insecticides

FIELD: chemistry.

SUBSTANCE: compounds with formula I are described, where each of E and Z is oxygen; A is C1-C6alkylene or a 3-member monocyclic ring system, which can be monosubstituted; Y is C1-C6alkylene; p equals 0; q equals 0 or 1; B represents a 3- or 4-member ring system which is completely or partially saturated and can contain a heteroatom selected from oxygen, possibly substituted; each R1 independently represents halogen, nitro group, C1-C6alkyl; or each R1 independently represents an amino group; n equals 1, 2; each of R2 and R3 represents hydrogen; D represents a group and agronomically acceptable salts of said compounds. Also described is a method of producing formula I compounds, intermediate compounds, a pesticide composition containing a formula I compound, as well as an insect control method and a method of protecting plant propagation material.

EFFECT: novel anthranylamide derivatives have good insecticidal activity.

16 cl, 8 tbl, 19 ex

 

The text descriptions are given in facsimile form.

1. The compound of the formula I

in which each of E and Z represents oxygen;
And represents C1-C6alkylene or 3-membered monocyclic ring system which may be monogamist using1-C6of alkyl, C1-C6alkoxycarbonyl;
Y represents C1-C6alkylen;
q is 0 or 1;
In denotes a 3-4 membered ring system, which is fully or partially saturated and may contain a heteroatom selected from oxygen, while the 3-4 membered ring system may be mono-, di - or tizamidine with halogen, C1-C6of alkyl, C1-C6halogenoalkane,1-C4alkoxygroup,1-C4halogenlampe,1-C4allylthiourea,1-C4halogenation,1-C4alkylsulfonyl,1-C4alkylsulfonyl,2-C6alkoxycarbonyl;
each R1independently denotes a halogen, a nitro-group, With1-C6alkyl;
or each R1independently represents an amino group;
n is 1, 2;
each of R2and R3denotes hydrogen;
D refers to a group

where R4and R4' independently of one another denote hydrogen, C1-C6halogenated, halogen, C1-C4halogenlampe;
R5represents 2-pyridyl, monosubstituted with halogen;
and agronomically acceptable salts of these compounds,
with the exception of [2-methyl-6-(oxiranylmethyl)-phenyl]-amide 2-(3-chloropyridin-2-yl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid.

2. The compound according to claim 1, in which R4' denotes adored and each R 4independently represents halogen, nitrogroups1-C6alkyl.

3. The compound according to claim 1, which means 3-4 membered ring system, which is fully or partially saturated, and which may be mono-, di - or tizamidine with halogen, C1-C6of alkyl, C1-C6halogenoalkane,1-C4alkoxygroup,1-C4halogenlampe,1-C4allylthiourea,1-C4halogenation,1-C4alkylsulfonyl,1-C4alkylsulfonyl,2-C6alkoxycarbonyl.

4. The compound according to claim 1, in which And indicates With1-C6alkylen.

5. The compound according to claim 1, where In denotes cyclopropyl or cyclobutyl, which can be mono-, di - or triamese with halogen, C1-C4of alkyl, C1-C4alkoxygroup or1-C4ancilliary.

6. Pesticide composition for combating insects, which as the active ingredient includes at least one compound according to claim 1 of formula I, in each case in free base form or agrokhimichesky acceptable salt, and at least one auxiliary substance.

7. A method of combating insects which comprises applying the composition according to claim 6 for insects or their living environment.

8. The method for which the ITA material for the propagation of plants from pest infestation, such as insects, which includes the handling of material for reproduction or land on which the seeded material for propagation, the composition according to claim 6.

9. Material for propagation processed by the method according to item 8.

10. The method of obtaining the compounds of formula I according to claim 1, in each case in free base form or in salt form, which includes the interaction of the compounds of formula II
,
in which R1, n and D have the meanings given for formula I in claim 1, or, if appropriate, salts thereof, with the compound of the formula III
,
in which R3, A, X, Y, p, q, and have the values given for formula I, or, if appropriate, with its salt.

11. The compound of formula V
,
in which R1, R2, R3, n, A, X, Y, Z and a have the meanings given for formula I in claim 1.

12. Connection by claim 11, in which
R1stands With1-C4alkyl, halogen, the nitro-group;
R2and R3represent hydrogen;
And indicates With1-C6alkylen;
p is 0;
q is 0 or 1;
Y represents C1-C4alkylen;
In denotes cyclopropyl or cyclobutyl, which can be mono-, di - or tizamidine with halogen, C1-C4of alkyl, C1-C4alkoxygroup is s or 1-C4ancilliary; or denotes CH(CH2O), CH(Sneo), CH-(CME2O), CH(CH2Och2), SN(Sposn2), SN(CME2Och2), CH(CH2S(O)2CH2), CH(CHMeS(O)2CH2), CH(CMe2S(O)2CH2), C(Me)-(CH2O) (IU)(Sneo), (IU)-(CME2O), S(IU)-(CH2Och2) (IU)(Simeon2), (IU)-(CME2Och2), C(Me)-(CH2S(O)2CH2), C(Me)-(CHMeS(O)2CH2) or(IU)-(CMe2S(O)2CH2).

13. The connection 11, which indicates cyclopropyl or cyclobutyl, which can be mono-, di - or triamese with halogen, C1-C4of alkyl, C1-C4alkoxygroup or1-C4ancilliary.

14. The compound of formula III
,
in which R3, A, X, Y, p, q, and have the values given for formula I in claim 1.

15. The connection 14, in which R3denotes hydrogen;
And indicates With1-C6alkylen;
p is 0;
q is 0 or 1;
Y represents C1-C4alkylen;
In denotes cyclopropyl or cyclobutyl, which can be mono-, di - or tizamidine with halogen, C1-C4of alkyl, C1-C4alkoxygroup or1-C4ancilliary; or denotes CH(CH2O), CH(Sneo), SN(CME2O), CH(CH2Och22), SN(CME2Och2), CH(CH2S(O)2CH2), CH(CHMeS(O)2CH2), CH(CMe2S(O)2CH2), C(Me)-(CH2O) (IU)(Sneo), (IU)-(CME2O), S(IU)-(CH2Och2) (IU)(Sposn2), (IU)-(Sleep2Och2), C(Me)-(CH2S(O)2CH2), C(Me)-(CHMeS(O)2CH2) or(IU)-(CMe2S(O)2CH2).

16. The connection 15, which indicates cyclopropyl or cyclobutyl, which can be mono-, di - or triamese with halogen, C1-C4of alkyl, C1-C4alkoxygroup or1-C4ancilliary.



 

Same patents:

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: invention relates to novel quinoline derivatives of formula I or pharmaceutically acceptable salts thereof or esters with tyrosine kinase inhibitor properties. In formula I , R1 is selected from hydroxy, C1-C4-alkoxy, hydroxy(C2-C4-alkoxy), C1-C3-alkoxy-(C2-C4-alkoxy) or from a group of formula Q2-X3 - in which X3 is O, and Q2 is azetidin-1-yl-C2-C4-alkyl, pyrrolidin-1-yl- C2-C4-alkyl, piperidino-C2-C4-alkyl, piperazino-C2-C4-alkyl or morpholino-C2-C4-alkyl; b is 1, 2, or 3; each R2, which can be identical or different, is selected from fluorine, chlorine, bromine, C1-C4-alkyl, C2-C4-alkenyl and C2-C4-alkenyl; Q1 is piperidinyl; a is 0; X1 is CO; X2 is a group of formula: -(CR12R13)P-(Q5)m-, where m is 0 or 1, p is 0, 1, 2, 3 or 4; each of R12 and R13, which can be identical or different, is selected from hydrogen, C1-C6-alkyl, amino, C1-C6-alkylamino and di-[C1-C6-alkyl]amino, and Q5 is C3-C7cycloalkylene; Z is selected from hydroxy, amino, C1-C6-alkylamino, di-[C1-C6-alkyl]amino, C1-C6-alkoxy and a group of formula: Q6-X9-, in which X9 is a single bond and Q6 is heterocyclyl or heterocyclyl-C1-C4 alkyl; under the condition that, if m and p are equal to 0, Z is heterocyclyl.

EFFECT: proposed derivatives can be used in treating proliferative diseases, particularly for treating malignant growths.

32 cl, 4 dwg, 2 tbl, 37 ex

FIELD: medicine.

SUBSTANCE: invention is related to compound represented by formula (1) , in formula A represents nitrogen-containing saturated ring; m represents integer number, equal to 0, 1 or 2; n represents integer number, equal to 1, 2, 3 or 4; G1 represents atom of hydrogen, hydroxyl group or alkoxygroup; G2 represents atom of halogen, hydroxyl group, cyanogroup, alkyl group, alkenyl group, alkinyl group, which may be substituted with hydroxyalkyl group, alkoxygroup, alkyl thiogroup, aminogroup or aryl group; G3 represents atom of hydrogen; G4 represents hydroxyl group or -N(R1)(R2) (R1 and R2 may be identical or different, and independently represent atom of hydrogen, alkyl group, aralkyl group, alkenyl group or saturated heterocyclic group); and G5 represents substituent at carbonic atom, which constitutes nitrogen-containing saturated ring, represented with A, and represents atom of hydrogen, to medicinal agent on the basis of this compound for treatment and prophylaxis of glaucoma, to inhibitor of phosphorylation of regulatory light chain of myosin and inhibitor of kinase Rho/Rho path, and also to method of therapeutical and/or prophylactic treatment of glaucoma.

EFFECT: new compounds have been produced and described, which efficiently inhibit phosphorylation of regulatory light chain of myosin.

32 cl, 42 ex, 4 tbl

FIELD: medicine.

SUBSTANCE: invention is related to compounds with common formulae I , III , IV and V , value of radicals such as given in formula of invention. Also suggested invention is related to pharmaceutical composition in the basis of above-mentioned compounds, to their use, and also to method of frequent urination treatment, enuresis and increased activity of urinary bladder.

EFFECT: increased efficiency of diseases treatment, in particular for treatment of frequent urination and enuresis, increased activity of urinary bladder and pain.

16 cl, 406 ex, 73 tbl

V:

Amide derivatives // 2375352

FIELD: medicine.

SUBSTANCE: invention refers to new compounds of formula I, to its pharmaceutically acceptable salts exhibiting properties of inhibitors of cytokine production, such as TNF (tumour necrosis factor) and various members of interleukins (IL) family, and properties of kinase inhibitors, particularly p38α kinase. The invention also concerns methods for producing; pharmaceutical compositions and application thereof for making the medicines for treating diseases affected by the compound of the invention with specified activity. In formula I , m represents 0, 1 or 2; R1 represents halogeno, hydroxy, (1-6C) alkyl, (1-6C)alkoxy, (2-6C)alkenyl, (2-6C) alkinyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, amino-(2-6C) alkoxy, (1-6C)alkylamino-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, N-(1-6C)alkylcarbamoyl - (1-6C)alkoxy, di[(1-6C) alkyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkylamino, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy and wherein any heteroaryl or heterocyclyl group in substitute representing R1, can probably have 1 or 2 substitutes chosen from hydroxy, halogeno, (1-6C) alkyl, (2-6C)alkinyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl-(1-6C)alkyl, (1-6C)alkoxycarbonyl, (2-6C) alkanoyl, halogen-(1-6C)alkyl, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, cyano-(1-6C)alkyl, carboxy- (1-6C)alkyl and methylsulphonyl and wherein any said substitute representing R1 which contains group CH2 attached to 2 carbon atoms, or group CH3 attached to carbon or nitrogen atom, can probably have with each specified group CH2 or CH3, one or two substitutes chosen from halogeno, hydroxy, amino, triflouromethyl, oxo, carboxy, acetamido, (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)alkoxy, (1-6C)alkyamino, di-[(1-6C)alkyl]amino, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, halogen-(1-6C)alkyl, (1-6C)alkoxycarbonyl, carbamoyl, N, N-di-[(1-6)alkyl]carbamoyl, (1-6C)alkylsulphonyl, heteroaryl, heteroaryl-(1-6)alkyl and heterocyclyloxy and wherein any heterocyclyl group in substitute representing R1, can probably have 1 oxo-subsitute; R2 represents trifluoromethyl or (1-6C)alkyl; R3 represents hydrogen or (1-6C)alkyl; and R4 represents (3-6C)cycloalkyl, and R4 can be optionally substituted with one or more substitutes chosen from (1-6C)alkyl; and wherein heteroaryl represents aromatic 5- or 6-merous monocyclic ring containing one or two heteroatoms chosen from oxygen, nitrogen and sulphur; heterocyclyl represents saturated 3-10-merous monocyclic or bicyclic ring, each containing one or two heteroatoms chosen from oxygen, nitrogen and sulphur.

EFFECT: improved efficiency.

24 cl, 16 tbl, 66 ex

FIELD: medicine.

SUBSTANCE: invention relates to derivatives of 5- or 6-substituted benzimidazoles, being inhibitory active as regards replication of respiratory syncytial viruses and having formula (I), wherein Q is R6a, piperidinyl, substituted with R6; G is methylene; R1 is piridyl, substituted with 2 substitutes, chosen from hydroxy, C1-6alkyl; one of R2a and R2b is cyano-C2-6alkenyl, Ar3C1-6alkyl, Het-C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Ar3-amino-C1-6alkyl, Het-amino-C1-6alkyl, Het-C1-6alkyl-amino-C1-6alkyl, Ar3tioC1-6alkyl, Ar3amino-carbonyl, Het-amino-carbonyl, Ar3(CH2)ncarbonyl-amino, Het-(CH2)ncarbonyl-amino; and the other of R2a and R2b represents hydrogen; R3 represents hydrogen or C1-6alkyl; in the case when R2a represents hydrogen, R3 represents hydrogen; in the case when R2b represents hydrogen, R3 represents hydrogen or C1-6alkyl; R5 represents hydrogen; R6 represents C1-6alkyl, optionally substituted with one or two substitutes, each of which is independently chosen from group consisting of NR7aR7b, Ar2, hydroxy, amino-carbonyl, amino-sulphonyl; R6a is C1-6alkyl, substituted with one or two substitutes, each of which is independently chosen from group consisting of Ar2, hydroxy or heterocyclic, chosen from a group consisting of piperidinyl, piperazinyl; R7a represents hydrogen; R7b represents hydrogen; R8a represents Ar3, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy C1-6alkyl, cyanoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, Ar3C1-6alkyl, HetC1-6alkyl, amino-carbonyl C1-6alkyl, carboxylC1-6alkyl; R8b represents Ar3, C1-6alkyl, hydroxyC1-6alkyl, Ar3C1-6alkyl, HetC1-6alkyl; each independently represents 1; Ar1 represents phenyl; Ar2 represents phenyl or phenyl substituted with one C1-6alkyl-oxy; Ar3 represents phenyl, naphtalenyl, 1,2,3,4-tetra-hydro- naphtalenyl or indanyl, wherein said phenyl, naphtyl, 1,2,3,4- tetra-hydro- naphtalenyl or indanyl can be optionally and each individually substituted with one or more, for example, 2 or 3 substitutes chosen from group consisting of halogen, hydroxy-, mercapto- cyano-, C1-6alkyl, C2-6alkinyl, Ar3 , hydroxy-C1-6alkyl, CF3, cyano-C1-6alkyl, amino-carbonyl, C1-6alkyl-oxy, C1-6alkyltio, Ar1-oxy, Ar1-amino, amino-sulphonyl, amino-carbonylC1-6alkyl, C1-4alkyl-carbonyl, C1-4alkyl-carbonyl-amino and C1-4alko-oxy-carbonyl; Het represents heterocycle chosen from phuranyl, imidazolyl, morpholinyl, piridyl, quinolene, iso-quinolene, each of said heterocycles can be optionally substituted with hydroxyl-Sibalkyl, as well as to acid additional salt thereof and stereo-chemical isomeric forms. In addition, the invention relates to pharmaceutical composition on the basis of compound of formula I and to application of compound of formula I and for production of medicinal preparation.

EFFECT: new derivatives of benzimidazole having useful biological properties.

22 cl, 6 tbl, 18 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new a compound of formula I or formula II, or to its pharmaceutically acceptable salts, I II, where X is S; R1 is H or C1-C6alkyl; R2 is NR5R6; R3 is aryl, substituted with a halogen; R4 is H; R5 is H; R6 is H; R7 is CH2NR8R9 where R8 is H, C1-C10alkyl, C3-C8cycloalkyl, aryl, aryl(C1-C6alkyl), aryl(C2-C6alkenyl), heterocycle(C1-C6alkyl), heterocycle(C2-C6alkenyl), hydroxyl(C1-C6alkyl), hydroxyl(C2-C6alkyl), C1-C6alkoxycarbonyl, aryl(C1-C6alkoxy)carbonyl, carbamoyl(C1-C6alkyl); where the above mentioned aryl is an aromatic ring and is not substituted or substituted with one to three substituting groups, each of which, independently from the others, is chosen from: methylenedioxy, hydroxy, C1-C6-alkoxy, halogen, C1-C6alkyl, trifluoromethyl, trifluoromethoxy, NO2, NH2, NH(C1-C6alkyl), N(C1-C6alkyl)2, NH-acyl, N(C1-C6alkyl)-acyl, hydroxy(C1-C6alkyl), dihydroxy(C1-C6alkyl), CN, C(=O)O(C1-C6alkyl), phenyl, phenyl(C1-C6alkyl), phenyl(C1-C6alkenyl), phenoxy and phenyl(C1-C6alkoxy), R9 is H, C1-C10alkyl, heterocycle(C1-C6alkyl) or heterocycle(C2-C6alkenyl); where the above mentioned heterocycle represents a 5-member saturated monocyclic ring system, consisting of carbon atoms, as well as heteroatoms, chosen from a group comprising N, O, and S, which can be unsubstituted or have one to three substituting groups, independently chosen from a list which includes NO2, aryl(C1-C6alkyl), arylsulphonyl; or R8 and R9 together with nitrogen, to which they are bonded, form a heterocycle, which represents a 5 - 7-member saturated monocyclic ring system, consisting of carbon atoms, as well as one to three heteroatoms, chosen from a group comprising N, O and S, which can be unsubstituted or have one to three substituting groups, independently chosen from a list which includes C1-C6alkoxy, hydroxy, C1-C6alkyl, C2-C6-alkenyl, C(=O)O(C1-C6alkyl), C(=O)NH2, C(=O)NH(C1-C6alkyl), C(=O)N(C1-C6-alkyl)2, hydroxy(C1-C6alkyl), dihydroxy(C2-C6alkyl), aryl, aryl(C1-C6alkyl), aryl(C2-C6alkenyl), aryl(C1-C6alkoxy) and pyrimidin-2-yl; and m equals 0. The invention also relates to a pharmaceutical composition, as well as to use of formula I or formula II compounds.

EFFECT: obtaining new biologically active compounds, with inhibitory properties towards casein kinase 1ε.

32 cl, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to N-substituted aniline and diphenylamine analogues, chosen from 3,4-bisdifluoromethoxy-(3-carboxyphenyl)-N-(5-(2-chloropyridinylmethyl))-aniline, 3,4-bisdifluoromethoxy - N-(3-carboxyphenyl) - N-(3-(2-chloropyridylmethyl))-aniline, 3,4 - bisdifluoromethoxy - N-(3-carboxyphenyl) - N-(4-(3,5-dimethylisoxazolylmethyl)) aniline, 3 - cyclopentyloxy - 4-methoxy - N-(3-aminocarbonylphenyl) - N-(3-pyridylmethyl) aniline and other compounds given in paragraph 1 of the formula of invention and to their pharmaceutically acceptable salts as inhibitors of PDE4 enzyme.

EFFECT: compounds can be used for treating and preventing diseases caused by activity of the PDE4 enzyme.

15 cl, 8 dwg, 58 ex

FIELD: chemistry.

SUBSTANCE: invention refers to the new compounds of general formula (II) , whereat values R1, R2, X, R11, R12, R18, R19, m, n are displayed in claim 1 of the formula.

EFFECT: compounds display agonistic and antagonistic activity which allows to propose their usage in pharmaceutical compositions for treatment of diseases and distresses connected with histamine H3 receptor.

38 cl, 80 ex

Cynnamide compound // 2361872

FIELD: chemistry.

SUBSTANCE: invention relates to a compound with formula (I) , where Ar1 is an imidazolyl group, which can be substituted with 1-3 substitutes; Ar2 is a pyridinyl group, pyrimidinyl group or phenyl group, which can be substituted with 1-2 substitutes; X1 is (1) -C≡C- or (2) double bond etc., which can be substituted, R1 and R2 are, for example, C1-6-alkyl group or C3-8-cycloalkyl group, which can be substituted; or to a pharmacologically acceptable salt of the said compound and pharmaceutical drugs for lowering production of Aβ42, containing formula (I) compound as an active ingredient.

EFFECT: wider field of use of the compounds.

26 cl, 1119 ex, 31 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds with general formula (I), where W is oxygen or sulphur; X1 and X3 are independently hydrogen or C1-C6-alkoxy; X2 is hydrogen, halogen, C1-C6-alkyl or C1-C6-alkoxy and X4 is hydrogen, Y is in position (N2) or (N3); when Y is in position (N2), Y is C1-C6-alkyl, C1-C6-fluoroalkyl, phenyl, pyridinyl or pyrazinyl; when Y is in position (N3), Y is phenyl, pyridinyl or pyrimidinyl, where phenyl is optionally substituted with one or more atoms or groups selected from halogen, C1-C5 alkyl, C1-C6-alkoxy; the bond in position C4-C5 is a single or double bond; R1 and R2 each independently represent phenyl and C1-C6-alkyl, where at least one of R1 and R2 represents C1-C6-alkyl; or R1 and R2 together with the nitrogen atom to which they are bonded form a cyclic group containing from 4 to 7 links and a nitrogen atom and possibly another heteroatom, such as nitrogen or oxygen, possibly substituted with one or more C1-C6-alkyl groups; or to their pharmaceutically acceptable salts. The invention also relates to methods of producing the proposed compounds with formula (I), and specifically to compounds with formulae (Ia) and (Ib), in which X1, X3, X3, X4 and Y are as described in general formula (I). The invention also relates to intermediate compounds of synthesis of formula (I) compounds - compounds with formulae (Va) and (Vb). In formula (Va) X1, X3 and X4 represent hydrogen; X2 is hydrogen, halogen or C1-C6-alkoxy and Y is C1-C6-alkyl, C1-C6-fluoroalkyl, phenyl, pyridinyl or pyrazinyl; where phenyl is possibly substituted with one or more atoms or groups selected from halogen, C1-C6-alkyl, C1-C6-alkoxy. In formula (Vb) X1 and X3 represent hydrogen or C1-C6-alkoxy; X2 is hydrogen, halogen, C1-C6-alkyl or C1-C6-alkoxy, X4 is hydrogen; Y is phenyl, pyridinyl or pyrmidinyl; phenyl is possibly substituted with one or more atoms or groups selected from halogen, C1-C6-alkyl, C1-C6-alkoxy. The invention also relates to a medicinal agent based on a formula (I) compound or its pharmaceutically acceptable salt for preventing and treating pathologies where peripheral type benzodiazepine receptors take part. The invention also relates to use of formula (I) compounds in preparing the said medicinal agent and to a pharmaceutical composition for preventing and treating pathologies in which peripheral type benzodiazepine receptors take part.

EFFECT: new compounds have useful biological activity.

11 cl, 3 tbl, 6 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: 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: invention covers new compounds of formula I: or its pharmaceutically acceptable salt with antagonist activity to corticotrophin release factor (CRF). In formula (I) X means heteroaryl chosen of pyrazolyl and imidazolyl optionally substituted with (C1-C6)alkyl, haloid or phenyl; Y means -NRaRb where Ra means hydrogen, and Rb means phenyl optionally substituted with (C1-C6)alkyl or haloid; Z means (C1-C6)alkyl; and R1 means hydrogen, (C1-C6)alkyl or haloid.

EFFECT: compounds can find application in treatment, eg of neurodegenerative diseases, neuropsychiatric disorders and stresses.

19 cl, 1 dwg, 2 tbl, 4 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: medicine.

SUBSTANCE: there are described new isoindole derivatives of general formula (1), wherein A1, A2 and A4 stands for CH, and A3 means N or C-OH; n is equal to 2; R1 represents O; R2-stands for H; and a pharmaceutical composition containing thereof.

EFFECT: new compounds are inhibitors of chaperone protein Hsp90 activity and can be used in chemotherapy of cancerous diseases.

6 cl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new indolylmaleimide derivatives of formula I: , where: Ra is H, C1-4alkyl; one of Ra, Rc, Rd and Re is C1-4alkyl; and the other three substitutes are H; or Rb, Rd, Re are all H; and R is a radical of formula (a): , where R1 is -(CH2)n-NR3R4, where each of R3 and R4 are independently H, C1-4alkyl; n is 0, 1, 2; R2 is H; halogen; or its pharmaceutically acceptable salt.

EFFECT: wider field of use of the compounds.

8 cl, 1 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: in compounds of formula (I) , Q is: (IIa) or (IIb) , R1 is chosen from a group which consists of carboxylic aryl and carboxylic aryl which is substituted with substitute(s) independently chosen from a group which consists of halogen, cyano, nitro, C1-10alkyl, C1-10alkyl which is substituted with substitute(s) independently chosen from a group which consists of halogen, C1-9alkoxy, C1-9alkoxy which is substituted with substitute(s) independently chosen from a group which consists of halogen, mono-C1-5alkylamino, and heterocyclyl or heterocyclyl which is substituted with substitute(s) independently chosen from a group which consists of halogen, C1-5alkyl; R2 is C1-5alkyl, C1-5alkyl which is substituted with halogen, C1-5alkyl which is substituted with carboxylic aryl, C1-5alkoxy, -N(R2a)(R2b); where R2a and R2b are each independently hydrogen, C1-5alkyl or C1-5alkyl, substituted with substitute(s) independently chosen from a group which consists of hydroxyl, carboxylic aryl; L represents formula (IIIa); , where R3 and R4 are each hydrogen; A is a single bond, and B is a single bond or -CH2-; Z1, Z3, and Z4 are each independently hydrogen, halogen, C1-5alkyl, C1-5alkyl, substituted with carboxylic aryl, C1-5alkoxy, mono-C1-5alkylamino, di-C1-5alkylamino, carboxylic aryl, heterocyclyl or substituted heterocyclyl; Z2 is hydrogen, C1-5alkyl, C1-5alkyl which is substituted with carboxylic aryl, C1-5alkoxy, mono-C1-5alkylamino, di-C1-5alkylamino, carboxylic aryl, heterocyclyl or substituted heterocyclyl; Y is -C(O)NH-, -C(O)-, -C(S)NH-, -C(O)O- or -CH2-; where carboxylic aryl is phenyl; heterocyclyl is 1H-indolyl, 9H- xanthenyl, benzo[1,3]dioxolyl, furyl, imidazolyl, isoxazolyl, morpholinyl, piperazinyl, pyridyl, pyrrolidyl; halogen is fluorine, chlorine, bromine or iodine. The invention also relates to a pharmaceutical composition.

EFFECT: compounds can be used for treating central nervous system diseases, and for improving memory functioning, sleep, awakening, diabetes.

16 cl, 8 dwg, 4 tbl, 525 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new indolylmaleimide derivatives with formula I , where: Ra is H; C1-C4alkyl; one of Rb, Rc, Rd and Re is C1-C4alkyl, and the others are H; or Rb, Re, Rd and Re are all H; and R is a radical with formula (a), (b) and (c), presented in the claim.

EFFECT: compounds inhibit protein kinase C (PKC), which allows for their use in making a medicinal agent for treating or preventing diseases or disorders mediated by T lymphocytes and/or PKC, particularly during transplantation.

8 cl, 11 tbl, 47 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds with general formula (I), where W is oxygen or sulphur; X1 and X3 are independently hydrogen or C1-C6-alkoxy; X2 is hydrogen, halogen, C1-C6-alkyl or C1-C6-alkoxy and X4 is hydrogen, Y is in position (N2) or (N3); when Y is in position (N2), Y is C1-C6-alkyl, C1-C6-fluoroalkyl, phenyl, pyridinyl or pyrazinyl; when Y is in position (N3), Y is phenyl, pyridinyl or pyrimidinyl, where phenyl is optionally substituted with one or more atoms or groups selected from halogen, C1-C5 alkyl, C1-C6-alkoxy; the bond in position C4-C5 is a single or double bond; R1 and R2 each independently represent phenyl and C1-C6-alkyl, where at least one of R1 and R2 represents C1-C6-alkyl; or R1 and R2 together with the nitrogen atom to which they are bonded form a cyclic group containing from 4 to 7 links and a nitrogen atom and possibly another heteroatom, such as nitrogen or oxygen, possibly substituted with one or more C1-C6-alkyl groups; or to their pharmaceutically acceptable salts. The invention also relates to methods of producing the proposed compounds with formula (I), and specifically to compounds with formulae (Ia) and (Ib), in which X1, X3, X3, X4 and Y are as described in general formula (I). The invention also relates to intermediate compounds of synthesis of formula (I) compounds - compounds with formulae (Va) and (Vb). In formula (Va) X1, X3 and X4 represent hydrogen; X2 is hydrogen, halogen or C1-C6-alkoxy and Y is C1-C6-alkyl, C1-C6-fluoroalkyl, phenyl, pyridinyl or pyrazinyl; where phenyl is possibly substituted with one or more atoms or groups selected from halogen, C1-C6-alkyl, C1-C6-alkoxy. In formula (Vb) X1 and X3 represent hydrogen or C1-C6-alkoxy; X2 is hydrogen, halogen, C1-C6-alkyl or C1-C6-alkoxy, X4 is hydrogen; Y is phenyl, pyridinyl or pyrmidinyl; phenyl is possibly substituted with one or more atoms or groups selected from halogen, C1-C6-alkyl, C1-C6-alkoxy. The invention also relates to a medicinal agent based on a formula (I) compound or its pharmaceutically acceptable salt for preventing and treating pathologies where peripheral type benzodiazepine receptors take part. The invention also relates to use of formula (I) compounds in preparing the said medicinal agent and to a pharmaceutical composition for preventing and treating pathologies in which peripheral type benzodiazepine receptors take part.

EFFECT: new compounds have useful biological activity.

11 cl, 3 tbl, 6 ex

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