Isoxazoline-substituted benzamide derivative and pesticide

FIELD: chemistry.

SUBSTANCE: invention relates to an isoxazoline-substituted benzamide derivative of formula or salt thereof, where A1 denotes a carbon or nitrogen atom, A2 and A3 independently denote a carbon atom, G denotes a benzene ring, W denotes an oxygen or sulphur atom, X denotes a halogen atom or C1-C6alkyl, arbitrarily substituted with a radical R4, Y denotes a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkyl arbitrarily substituted with radical R4, -OR5, -N(R7)R6, phenyl, D-41, when n equals 2, each Y can be identical or different from each other, R1 denotes -C(R1b)=NOR1a, M-5, -C(O)OR1c, -C(O)SR1c, -C(S)OR1c, -C(S)SR1c, -C(O)N(R1e)R1d, -C(S)N(R1e)R1d, -C(R1d)=NN(R1e)R1lf, phenyl, phehnyl substituted with (Z)p1, or D-3, D-8, D-13-D-15, D-21, D-35, D-52-D-55 or D-57-D-59, R2 denotes C1-C6alkyl, -CH2R14a, E-5, C3-C6alkynyl, -C(O)R15, -C(O)OR15, -C(O)C(O)OR15 or -SR15, where, when R1 denotes -C(R1b)=NOR1a, M-5, or -C(R1b)=NN(R1e)R1f, R2 can denote a hydrogen atom, when R1 denotes -C(O)OR1c, -C(O)SR1c, -C(S)OR1c or -C(S)SR1c, R2 can denote hydrogen, when R denotes -C(O)N(R1e)R1d or -C(S)N(R1c)R1d, R2 can denote a hydrogen atom, when R1 denotes phenyl, phenyl substituted with (Z)p1, or D-3, D-8, -D-13-D-15, D-21, D-35, D-52-D-55 or D-57-D-59 R2 can denote C1-C6halogenalkyl, C1-C6alkyl arbitrarily substituted with a radical R14a, C3-C6alkenyl, -C(O)NH2, -C(O)N(R16)R15, or R2 together with R1 can form =C(R2b)R2a, R3 denotes C1-C6alkyl arbitrarily substituted with radical R4, D-1, D-3, D-8, D-13-D-15, D-21, D-35, D-41, D-52-D-55, D-57-D-59 denote aromatic heterocyclic rings, m equals an integer from 2 to 3, n equals an integer from 0 to 2.

EFFECT: isoxazoline-substituted benzamide derivative and salt thereof are used in pest control, against harmful arthropods in agriculture and horticulture or in livestock farming and in the field of hygiene.

12 cl, 18 tbl, 73 ex

 

The text descriptions are given in facsimile form.

1. Derived isoxazolidinone benzamide of formula (1) or its salt:

where a1represents a carbon atom or a nitrogen atom,
And2and3independently from each other represent a carbon atom,
G represents a benzene ring,
W represents an oxygen atom or a sulfur atom,
X represents a halogen atom or C1-C6alkyl optionally substituted by the radical R4,
Y represents a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkyl optionally substituted by the radical R4, -OR5, -N(R7R6, phenyl, D-41, when n is an integer 2, each Y may be the same or different from each other,
R1represents-C(R1b)=NOR1aM-5, -C(O)or SIG1c, -C(O)SR1c, -C(S)OR1c,-C(S)SR 1cC(O)N(R1eR1d-C(S)N(R1eR1d, -C(R1d)=NN(R1eR1f, phenyl, phenyl substituted (Z)p1or D-3, D-8, D-13 to D-15, D-21, D-35, D-52 to D-55 D-57 D-59,
R1arepresents a hydrogen atom, a C1-C6alkyl, C1-C6halogenated,3-C6alkenyl,
R1brepresents a hydrogen atom, a C1-C6alkyl,
R1crepresents a C1-C6alkyl, C1-C6alkyl optionally substituted radical
R14With3-C6cycloalkyl, E-5, E-6, and C3-C6alkenyl,3-C6halogenoalkanes or3-C6quinil,
R1drepresents a hydrogen atom, -C(O)R15, -C(O)OR15,
R1erepresents a hydrogen atom, a C1-C6alkyl,
R1frepresents-C(O)R15or-C(O)OR15,
R2represents a C1-C6alkyl, -CH2R14aE-5, p3-C6quinil, -C(O)R15, -C(O)OR15, -C(O)C(O)OR15or-SR15,
moreover, when R1represents-C(R1b)=NOR1aM-5 or-C(R1b)=NN(R1eR1f, R2may be a hydrogen atom when R1represents-C(O)SR1c, -C(O)SR1c, -C(S)OR1cor-C(S)SR1c, R2may be a hydrogen atom when R1represents-C(O)N(R1e R1dor-C(S)N(R1eR1d, R2may be a hydrogen atom when R1represents phenyl, phenyl, substituted (Z)p1or D-3, D-8, D-13 to D-15, D-21, D-35, D-52 to D-55 D-57 D-59, R2can be a C1-C6halogenated, C1-C6alkyl optionally substituted by the radical R14aWith3-C6alkenyl, -C(O)NH2, -C(O)N(R16R15,
or R2together with R1may form a =C(R2bR2a,
R2arepresents-OR1cor di(C1-C6alkyl)amino,
R2bis an R1bC1-C6alkylthio, -SCH2R14aor-SC(O)R15,
R3represents a C1-C6alkyl optionally substituted by the radical R4D-1, D-3, D-8, D-13 to D-15, D-21, D-35, D-41, D-52 to D-55, D-57 D-59 are aromatic heterocyclic compounds of the following formulas, respectively

Z represents a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6halogenated or C1-C6alkoxy, when P1 is an integer of 2, each Z may be the same or different from each other,
E-5, E-6, E-12 represent a saturated heterocyclic compounds of the following formulas, respectively

R4represents a halogen atom, -OR5or-N(R7R 6,
R5represents a C1-C6alkyl or C1-C6alkyl optionally substituted by the radical R24,
R6represents a C1-C6alkyl, -C(O)R9,
R7represents a hydrogen atom or a C1-C6alkyl,
R9represents a C1-C6alkyl,
R12represents a C1-C6alkyl,
R12Aand R12bindependently of one another represent C1-C6alkyl,
R13represents a C1-C6alkyl,
R14represents a cyano, nitro, C3-C8cycloalkyl, E-5, E-12, -OR25, -N(R26R25, -S(O)rR27With5-C8cycloalkenyl, -C(O)R28, -C(O)OR28, -Si(R12a)(R12bR12, phenyl, phenyl substituted (Z)p1D-1 or D-52,
M-5 is a partially saturated, a heterocycle of the following formula, respectively

R14arepresents cyano, -OR25N(R26R25, -S(O)rR27, -C(O)R28, -C(O)OR28or phenyl,
R15represents a C1-C6alkyl, C1-C6alkyl optionally substituted radical
R31With3-C8cycloalkyl,2-C6alkenyl, phenyl, phenyl substituted (Z)p1or D-52,
R16represents a C -C6alkyl,
R22represents a C1-C6alkyl, when q3 is an integer of 2 or more, each R22may be the same or different from each other, and when two R22are one and the same carbon atom, two R22together may form oxo,
R24represents a halogen atom,
R25represents a C1-C8alkyl, C1-C8alkyl optionally substituted radical
R31, -C(O)R32, -C(O)OR32or phenyl,
R26represents a hydrogen atom, a C1-C6alkyl,
R27represents a C1-C8alkyl, -C(O)R32, -C(S)OR32or D-52,
R28represents a C1-C6alkyl or phenyl,
R31represents a halogen atom, -OR32or-S(O)rR32,
R32represents a C1-C6alkyl,
m is an integer from 2 to 3,
n is an integer from 0 to 2,
P1 is an integer 1 or 2,
P2 is an integer from 0 to 1,
p3 is an integer from 0 to 1,
P4 is an integer from 0 to 1,
the P5 is an integer 0,
q2 is an integer 2,
q3 is an integer from 0 to 4,
q6 is an integer from 0 to 1,
r is an integer from 0 to 2 and
t is the number 0.

2. Derived isoxazolidinone benzamide or its salt according to claim 1, where
G depict is to place a benzene ring,
X represents a halogen atom or C1-C6alkyl optionally substituted by the radical R4when m is an integer 2 or 3, each X may be the same or different from each other,
Y represents a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkyl optionally substituted by the radical R4, -OR5or-N(R7R6when n is 2, each Y may be the same or different from each other,
R1represents-C(R1b)=NOR1a, M-5, -C(O)OR1c, -C(O)SR1c, -C(S)OR1c, -C(S)SR1c, -C(O)N(R1eR1d, -C(S)N(R1eR1dC(R1b)=NN(R1eR1f, phenyl, phenyl substituted (Z)p1, D-3, D-8, D-13 to D-15. D-21, D-35, D-52 to D-55 D-57 D-59,
R1arepresents a hydrogen atom, a C1-C6alkyl, C1-C6halogenated or3-C6alkenyl,
R1brepresents a hydrogen atom, a C1-C6alkyl,
R1crepresents a C1-C6alkyl, C1-C4alkyl optionally substituted radical
R14With3-C6cycloalkyl, E-5, E-6, and C3-C6alkenyl,3-C6halogenoalkanes or3-C6quinil,
R1drepresents a hydrogen atom, -C(O)R15or-C(O)OR15,
R1crepresents a hydrogen atom or a C1-C6al is Il,
R1frepresents a C1-C6alkylaryl or C1-C6alkoxycarbonyl,
R2represents a C1-C6alkyl, -CH2R14aE-5, p3-C6quinil, -C(O)R15, -C(O)OR15, -C(O)C(O)OR15or C1-C6allogenicity, and when R1represents-C(R1b)=NOR1a, M-5 or-C(R1b)=NN(R1eR1f, R2may be a hydrogen atom when R1represents C(O)OR1c, -C(O)SR1c, -C(S)OR1cor-C(S)SR1c, R2may be a hydrogen atom when R1represents-C(O)N(R1eR1dor-C(S)N(R1eR1d, R2may be a hydrogen atom when R1represents phenyl, phenyl, substituted (Z)p1or D-3, D-8, D13-D-15, D21, D-35, D-52 to D-55 D-57 D-59, R2can be a C1-C6halogenated,3-C6alkenyl, -C(O)NH2or di(C1-C6alkyl)aminocarbonyl, or R2together with R1can form a =C(R2bR2a,
R2arepresents-OR1cor di(C1-C6alkyl)amino,
R2bis an R1bC1-C6alkylthio, -SCH2R14aor-SC(O)R15,
R3represents a C1-C6halogenated,
Z represents an atom is alogena, cyano, nitro, C1-C6alkyl, C1-C6halogenated or C1-C6alkoxy, when P1 is an integer of 2, each Z may be the same or different from each other,
R4represents a halogen atom, a C1-C6alkoxy or C1-C6halogenoalkane,
R5represents a C1-C6alkyl or C1-C6halogenated,
R6represents a C1-C6alkyl or C(O)R9;
R7represents a hydrogen atom or a C1-C6alkyl,
R9represents a C1-C6alkyl,
R14represents a cyano, nitro, C3-C6cycloalkyl, E-5, E-12, -OR25, -N(R26R25, -S(O)rR27With5-C6cycloalkenyl, C1-C6alkylaryl, -C(O)OR28three(C1-C6alkyl)silyl, phenyl, substituted (Z)p1D-1 or D-52,
R14arepresents cyano, -OR25, -N(R26R25, -S(O)rR27C1-C6alkylsulphonyl, phenylcarbinol, C1-C6alkoxycarbonyl or phenyl,
R15represents a C1-C6alkyl, C1-C6halogenated,1-C4alkyl optionally substituted by the radical R31With3-C6cycloalkyl,2-C6alkenyl, phenyl, phenyl substituted (Z)p1or D-52,
22represents a C1-C6alkyl, when q2 is 2, each R22may be the same or different from each other,
R25represents a C1-C6alkyl, C1-C6halogenated,1-C4alkyl optionally substituted by the radical R31, -C(O)R32, -C(O)OR32or phenyl,
R26represents a hydrogen atom or a C1-C6alkyl,
R27represents a C1-C8alkyl, -C(O)R32, -C(S)OR32or D-52,
R28represents a C1-C6alkyl or phenyl,
R31represents-OR32With1-C4alkylthio,1-C4alkylsulfonyl,1-C4alkylsulfonyl,
R32represents a C1-C6alkyl,
m is an integer from 2 to 3,
n is an integer from 0 to 2,
q2 is an integer from 0 to 2,
q3 is 0,
q6 is an integer of 0 or 1.

3. Derived isoxazolidinone benzamide or its salt according to claim 2, where
And1represents a carbon atom or a nitrogen atom,
And2and3represent carbon atoms,
G represents a benzene ring,
X represents a halogen atom, a C1-C6halogenated when m is 2 or 3, each X may be the same or different from each other,
Y represents a halogen atom, is iano, nitro, C1-C6alkyl, C1-C6halogenated, C1-C4alkyl optionally substituted by the radical R4, -OR5or-N(R7R6when n is 2, each Y may be the same or different from each other,
R1represents-C(R1b)=NOR1a, -C(O)OR1c, -C(O)SR1c, -C(S)OR1c, -C(O)N(R1eR1d, -C(S)N(R1eR1d, phenyl, phenyl substituted (Z)p1, D-3, D-8, D-13 to D-15, D-35, D-52 to D-55 D-57 D-59,
R1arepresents a hydrogen atom, a C1-C6alkyl, C1-C6halogenated or3-C6alkenyl,
R1brepresents a hydrogen atom or a C1-C6alkyl,
R1crepresents a C1-C6alkyl, C1-C4alkyl optionally substituted by the radical R14or3-C6cycloalkyl,
R1drepresents a hydrogen atom, -C(O)R15or-C(O)OR15,
R2represents a C1-C6alkyl, -CH2R14aE-5, p3-C6quinil, -C(O)R15, -C(O)OR15, -C(O)C(O)OR15or C1-C6allogenicity, and when R1represents-C(R1b)=NOR1a, -C(O)OR1c, -C(O)SR1c, -C(S)OR1c, -C(O)N(R1eR1dor-C(S)N(R1eR1d, R2may be a hydrogen atom when R1 represents phenyl, phenyl, who ewenny (Z) p1, D-3, D-8, D-13 to D-15, D-35, D-52 to D-55 D-57 D-59, R2can be a C1-C6halogenated or3-C6alkenyl, or R2together with R1can form a =C(R2bR2a,
R2arepresents a C1-C6alkoxy or di(C1-C6alkyl)amino,
R2bis an R1bC1-C6alkylthio, -SCH2R14aor C1-C6alkylcarboxylic,
R3represents a C1-C6halogenated,
R4represents a C1-C6alkoxy or C1-C6halogenoalkane,
R5represents a C1-C6alkyl or C1-C6halogenated
R6represents a C1-C6alkyl or C1-C6alkylsulphonyl,
R7represents a hydrogen atom or a C1-C6alkyl,
R14represents cyano, C3-C6cycloalkyl, C1-C6alkoxy, C1-C4alkoxyl1-C4alkoxy, C1-C6alkylthio, -S(D-52), C1-C6alkylsulfonyl, -NHC(O)R32, -NHC(O)OR32C1-C6alkylaryl or C1-C6alkoxycarbonyl,
R14arepresents cyano, -OR25, -NHC(O)OR32, -S(O)rR27C1-C6alkylsulphonyl, C1-C6alkoxycarbonyl or phenyl,br/> R15represents a C1-C6alkyl, C1-C6halogenated,1-C4alkyl optionally substituted by the radical R31With3-C6cycloalkyl,2-C6alkenyl, phenyl, phenyl substituted (Z)p1or D-52,
R25represents a C1-C6alkyl, C1-C6halogenated,1-C4alkoxyl1-C4alkyl, -C(O)R32or-C(O)OR32,
R27represents a C1-C6alkyl, -C(O)R32or-C(S)OR32,
R31represents a C1-C4alkoxy, C1-C4alkylthio,1-C4alkylsulfonyl,
R32represents a C1-C6alkyl,
P1 is an integer from 1 to 2,
P2 and p3 is an integer of 0 or 1, and
P4 is an integer of 0 or 1.

4. Derived isoxazolidinone benzamide or its salt according to claim 3, where
And1represents a carbon atom,
W represents an oxygen atom,
X represents a halogen atom, a C1-C6halogenated when m is 2 or 3, each X may be the same or different from each other,
Y represents a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6halogenated, -OR5or-N(R7R6,
R1represents-CH=NOR1a, -C(O)OR1c, -C(O)N(R1eR1d,phenyl, substituted (Z)p1, D-52, D-55, D-57 D-58,
R1arepresents a C1-C6alkyl,
R1crepresents a C1-C6alkyl or C3-C6cycloalkyl,
R1drepresents a hydrogen atom, -C(O)R15or-C(O)OR15,
R2represents a C1-C6alkyl, -CH2R14aE-5, p3-C6quinil, -C(O)R15, -C(O)OR15, -C(O)C(O)OR15or C1-C6allogenicity, and when R1represents-CH=NOR1a, -C(O)OR1cor-C(O)N(R1eR1d, R2can represent a hydrogen atom,
R3represents a C1-C6halogenated,
Z represents a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6halogenated or C1-C6alkoxy, when P1 is an integer of 2, each Z may be the same or different from each other,
R5represents a C1-C6alkyl or C1-C6halogenated,
R6represents a C1-C6alkylsulphonyl,
R14arepresents cyano, -OR25or-NHC(O)OR32,
R15represents a C1-C6alkyl, C1-C6halogenated,1-C4alkoxyl1-C4alkyl, C1-C4alkylthio1-C4alkyl, C1-C4alkyls thinls 1-C4alkyl, C3-C6cycloalkyl,2-C6alkenyl, phenyl, phenyl substituted (Z)p1or D-52,
R25represents a C1-C4alkyl, C1-C4halogenated, -C(O)R32or-C(O)OR32,
R32represents a C1-C6alkyl,
n is an integer of 0 or 1,
q3 is 0, and
t is 0.

5. Derived isoxazolidinone benzamide or its salt according to claim 4, where
R1represents-CH=NOR1a,
R1arepresents a C1-C6alkyl,
R2represents a hydrogen atom, -CH2R14aWith3-C6quinil or1-C6alkoxycarbonyl,
R14arepresents cyano or-OR25,
R25represents a C1-C4alkyl, and
R32represents a C1-C6alkyl.

6. Derived isoxazolidinone benzamide or its salt according to claim 4, where
R1represents-C(O)or SIG1c,
R1crepresents a C1-C6alkyl or C3-C6cycloalkyl,
R2represents a hydrogen atom, a C1-C6alkyl, -CH2R14aE-5, -C(O)R15C1-C6alkoxycarbonyl, C1-C6gelegenheitsarbeit or C1-C6allogenicity,
R14arepresents cyano, -OR25or-NHC(O)OR 32,
R15represents a C1-C6alkyl, C1-C6halogenated,1-C4alkoxyl1-C4alkyl, C1-C4alkylthio1-C4alkyl or C3-C6cycloalkyl,
R25represents a C1-C4alkyl, C1-C4halogenated or C(O)R32and
R32represents a C1-C6alkyl.

7. Derived isoxazolidinone benzamide or its salt according to claim 4, where
R1represents-C(O)N(R1eR1d,
R1drepresents a hydrogen atom, -C(O)R15or-C(O)OR15,
R2represents a hydrogen atom or a C1-C6alkyl and
R15represents a C1-C6alkyl or C1-C6halogenated.

8. Derived isoxazolidinone benzamide or its salt according to claim 4, where
R1represents phenyl, substituted (Z)p1, D-52, D-55, D-57 D-58,
R2represents a C1-C6alkyl, -CH2R14aWith3-C6quinil, -C(O)R15, -C(O)OR15or-C(O)C(O)OR15,
Z represents a halogen atom, cyano, nitro, C1-C6alkyl, C1-C6halogenated or C1-C6alkoxy,
R14arepresents cyano or-OR25,
R15represents a C1-C6alkyl, C1-C 6halogenated,1-C4alkoxyl1-C4alkyl, C1-C4alkylthio1-C4alkyl, C1-C4alkylsulfonyl1-C4alkyl, C3-C6cycloalkyl,1-C6alkenyl,3-C6quinil, phenyl, phenyl substituted (Z)p1or D-52,
R25represents a C1-C4alkyl, C1-C4halogenated, -C(O)R32or-C(O)OR32and
R32represents a C1-C6alkyl.

9. Derived 4-gidroksiiminobetulonovoi benzamide of formula (2) or its salt:

where a1represents a carbon atom,
J represents a hydrogen atom,
W represents an oxygen atom,
Y represents a C1-C6alkyl,
R1represents-C(R1b)=NOR1a, -C(O)OR1cor D-55,
R1arepresents a C1-C6alkyl,
R1brepresents a hydrogen atom,
R1crepresents a C1-C6alkyl,
R2represents a hydrogen atom or-C(O)R15,
D-55 is an aromatic heterocycle of the following formula, respectively,

Z represents a halogen atom,
R15represents a C1-C6alkyl, and
p3 is 1.

10. A means to address issues such as the s pests applied against harmful arthropods in agriculture and horticulture, in animal husbandry and health, containing as an active ingredient one or more compounds selected from the derived isoxazolidinone benzamide and its salt according to any one of claims 1 to 8.

11. Endo - or ectoparasitic for mammals or birds containing as an active ingredient one or more compounds selected from the derived isoxazolidinone benzamide and its salt according to any one of claims 1 to 8.

12. Insecticide or acaricide containing as an active ingredient one or more compounds selected from the derived isoxazolidinone benzamide and its salt according to any one of claims 1 to 8.



 

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11 cl, 1 dwg, 1 tbl, 1 ex

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30 cl, 3 tbl, 7 ex

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,

A is O or S; G is N; B is a 6-member aryl or 5-6-member heteroaryl ring containing a sulphur atom as a heteroatom; E is

, , , , , X is N or CH; D1, D2 and D3 independently denote N or CR19; D4 and D5 independently denote N or CR19 and D6 is O, S or NR20, where at least one of D4 and D5 is CR19; D7, D8, D9 and D10 independently denote N or CR19, where at least one of D7, D8, D9 and D10 is N; R1 is H or C1-C6 alkyl; each R2 independently denotes halogen, cyano, nitro etc, trifluoromethyl, difluoromethyl, fluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, azido, -SR18, -OR15, -C(O)R15, -C(O)OR15, -NR14C(O)OR18, -OC(O)R15, -NR14SO2R18, -SO2NR15R14, -NR14C(O)R15, -C(O)NR15R14, -NR15C(O)NR15R14, -NR13C(NCN)NR15R14, -NR15R14, C1-C12alkyl, C2-C12 alkenyl, alkynyl, saturated or partially unsaturated C3-C10cycloalkyl, C3-C10cycloalkyl-C1-C12alkyl, -S(O)p(C1-C6alkyl), -S(O)p(CR13R14)q-phenyl, phenyl, phenyl-C1-3-alkyl, 5-6-member heteroaryl, 5-6-member heteroaryl-C1-C3-alkyl, saturated or partially unsaturated 3-8-member heterocyclyl, 5-6-member heterocyclyl-C1-C3-alkyl, -O(CR13R14)q-phenyl, NR15(CR13R14)q-phenyl, O(CR13R14)q-(5-6-member heteroaryl), NR13(CR13R14)q-(5-6-member heteroaryl, -O(CR13R14)q-(3-8-member heterocyclyl) or -NR15(CR13R14)q-3-8-member heterocyclyl), each R3 denotes Z, where Z is selected from and , W is O or S; W2 is O or S;V is CR8R9, R8b is H or C1-C6alkyl; each of R6, R8, R8a and R9 independently denotes hydrogen, trifluoromethyl, C1-C12alkyl etc.

EFFECT: improved properties and high efficiency of using the compounds.

25 cl, 13 dwg, 1 tbl, 36 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula (11) given below and pharmaceutically acceptable salts thereof: chemical formula 1

in which: each of G1, G2, G3 and G8 independently denotes -N=, -CR1= or -C(-G9-X)=; one of G1, G2, G3 and G8 is-C(-G9-X)=; X is C1-6 alkyl (where C1-6 can be optionally substituted with a group selected from a halogen atom, hydroxy, cyano and -NR56R57), aryl, heterocycle (where the heterocycle denotes a 5-9-member saturated or unsaturated cyclic group containing one or more heteroatoms selected from nitrogen, oxygen and sulphur atoms, and can be a monocycle or condensed ring, and can be optionally substituted with a halogen atom, C1-6 alkyl; C1-6 alkoxy, R33R34NCS-, R3R4NCO-); G9 denotes a single bond, an oxygen atom, a sulphur atom, ring G6 denotes a divalent aryl group or divalent pyridyl group (where the divalent pyridyl group can be optionally substituted with a halogen atom); A is a group of formula (2) given below, or a group of formula (3) given below. Chemical formula 2

, chemical formula 3 , G4 is an oxygen atom or sulphur atom; G5 is an oxygen atom or sulphur atom; G7 is an oxygen atom, -CR42R43-, -CONR44-, -NR44CO, -NR45-, CR42R43NR45-, -S-, -NR44S(=O)2-; R1 is a hydrogen atom, a halogen atom, cyano, C1-6 alkyl (where C1-6 alkyl can be optionally substituted with a halogen atom), carbamoyl or C2-7 alkynyl (where C2-7 alkynyl can be optionally substituted with C1-4 acyl); when G2 or G3 denotes -CR1=, then G8 is -C(-G9-X)=, and X is R3R4NCO-, R33R34NCS-; when G8 is -CR1=, then G3 denotes -C(-G9-X)=, and X is R3R4NCO, or R33R34NCS-; when G1 or G8 denotes -CR4 then G2 is -C(-G9-X)=, and X denotes R3R4NCO-, or R33R34NCS-; or when G2 is -CR1=, then G1 denotes -C(-G9-X)=, and X denotes R3R4NCO-, or R33R34NCS-; R1 can form a single bond or -CH2- with R4 or R34; R2 denotes hydroxy or C1-6 alkyl (where C1-6 alkyl can be optionally substituted with a group selected from a halogen atom, hydroxy, C1-6 alkoxy, formyl and -CO2R50); R3, R4, R9 and R10 each independently denotes a hydrogen atom, C3-8 cycloalkyl or C1-6 alkyl (where C1-6 alkyl can be optionally substituted with a group selected from cyano, a halogen atom, hydroxy, C1-6 alkoxy, -NR13R14, and CONR28R29); R6 and R7 each independently denotes a hydrogen atom, C1-6 alkoxy, C3-8 cycloalkyl or C1-6 alkyl (where C1-6 alkyl can be optionally substituted with a group selected from cyano, halogen atom, hydroxy, C1-6 alkoxy, -NR13R14, and CONR28R29); R33 and R34 each independently denotes a hydrogen atom, C1-6 alkyl, the combination of R3 and R4 together with a nitrogen atom to which they are bonded can form a 5-6-member heterocyclic group containing at least one nitrogen atom (where the 5-6-member heterocyclic group which contains at least one nitrogen atom is a saturated or unsaturated heterocyclic group containing 5-6 atoms in the ring and which, in addition to one or more nitrogen atoms, can contain one or more heteroatoms selected from oxygen and sulphur atoms (where the 5-6-member heterocyclic group can be optionally condensed with a benzene ring); and which can be optionally substituted with a halogen atom or C1-6 alkyl; the combination of R6 and R7 together with the nitrogen atom to which they are bonded can form a 5-6-member heterocyclic group containing at least one nitrogen atom (where the 5-6-member heterocyclic group which contains at least one nitrogen atom is a saturated or unsaturated heterocyclic group containing 5-6 atoms in the ring and which, in addition to one or more nitrogen atoms, can contain one or more heteroatoms selected from oxygen and sulphur atoms (where the 5-6-member heterocyclic group can be optionally condensed with a benzene ring); and which can be optionally substituted with a halogen atom, C1-6 alkyl or an oxo group; R45 is a hydrogen atom, R13 and R14 each independently denotes a hydrogen atom, C1-6 alkyl or COR32; R56 and R57 each independently denotes a hydrogen atom or C1-6 alkyl, and R5, R8, R28, R29, R32, R42, R43, R44, and R50 each independently denotes a hydrogen atom or C1-6 alkyl. The invention also relates to a pharmaceutical composition, as well as to a medicinal agent for treating cell proliferative disorder.

EFFECT: obtaining novel biologically active compounds having inhibitory effect on cell proliferation.

15 cl, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In formula (I) Y is C-R4 and Z is CH; or Y is C-R4 and Z is N; or Y is N and Z is CH; R1 is a 5- or 6-member ring of formula (II) or (III): R2 is H, C1-C7-alkyl; R3 is phenyl, pyrazolyl, isoxazolyl, pyridinyl, pyrimidinyl or pyrazinyl, which can possibly be substituted with one, two or three substitutes selected from a group consisting of: CN, CI, F, Br, CF3, CHF2, C1-C7-alkyl, -O-C1-C7-alkyl, -(CH2)m-Rc, -O-CH2F, -O-CHF2, -O-CF3, -S(O)2-Rd; R4 is H, C1-C7-alkyl; R5 is H, CI, F, Br, CN, CF3, CHF2, C1-C7-alkyl, -C3-C6-cycloalkyl, -(CH2)m-Re or -(CO)-NRiRj; R6 is C1-C7-alkyl; R7 is H, CI, F, CN or C1-C7-alkyl; Rc is -OH; Rd is C1-C7-alkyl; Re is -CH2F, -CHF2, -CF3, CN, C1-C7-alkoxy; Ri, Rj independently denote H or C1-C7-alkyl; m equals 1-4. The invention also relates to a medicinal agent having mGluR5a receptor antagonist properties, containing one or more of the disclosed compounds as an active component.

EFFECT: high efficiency of the medicinal agent.

24 cl, 208 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel imidazole derivatives of general formula I and pharmaceutically acceptable salts thereof, where R1 is selected from a group comprising aryl and alkyl, optionally substituted hydroxy; R2 is selected from a group comprising hydrogen and alkyl; R3 is selected from a group comprising hydrogen and -X-A, where X is selected from a group comprising -C(O)- and -S(O)2-; and A is selected from a group comprising hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycle and optionally substituted cycloalkyl, where the optionally substituted groups are substituted with 1-2 substitutes selected from a group comprising alkyl, substituted alkyl, alkoxy, substituted amine which is a -NRR group, substituted aryloxy, heteroaryl, heterocycle, halogen, hydroxy and -S(O)2-R9, where R9 is an alkyl; or R1 and R3 together with a carbon atom bonded to R1 and a nitrogen atom bonded to R3 form a heterocyclic or substituted heterocyclic group; R4 is selected from a group comprising hydrogen, linear alkyl, -alkylene-aminoacyl-, -alkylene-hydroxy-, -[alkylene]p-nitrogen-containing heterocycle, -[alkylene]p-nitrogen-containing substituted heterocycle, -[alkylene]p-nitrogen-containing heteroaryl, -[alkylene]p-nitrogen-containing substituted heteroaryl and -[alkylene]p-NR10R11, where p equals 0 or 1, the alkylene contains 1-5 carbon atoms and can have 1 or 2 substitutes selected from a group comprising amine, hydroxy and halogen, aminoacyl relates to a group -C(O)NRR, where each R is independently selected from a group comprising hydrogen and alkyl, R10 and R11 are independently selected from a group comprising hydrogen, alkyl, substituted alkyl, -S(O)2-alkyl, substituted aryl, substituted heteroaryl, cycloalkyl, or when R10 is hydrogen, R11 is hydroxy, alkoxy or substituted alkoxy; or when R1 and R3 together with carbon and nitrogen atoms respectively bonded to them do not form a heterocyclic or a substituted heterocyclic group, R3 and R4 together with a nitrogen atom to which they are bonded form a spiro-condensed heterocyclic group; R5 is selected from a group comprising L-A1, where L is selected from a group comprising C1-C5alkylene, where the alkylene is defined above; and A1 is selected from a group comprising aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle; and one of R6 or R7 is selected from a group comprising aryl and heteroaryl, each of which can optionally be substituted with -(R8)m, where m equals a whole number from 1 to 2, and the other of R6 or R7 is selected from a group comprising hydrogen, halogen and alkyl; or R6 as well as R7 denotes hydrogen; R8 is selected from a group comprising cyano, alkyl, -CF3, alkoxy, halogen, where alkyl, aryl, aryloxy, cycloalkyl, heterocycle, heteraryl and substituted alkyl, aryl, aryloxy, cycloalkyl, heterocycle and heteroaryl are described in claim 1. The invention also relates to specific compounds, a pharmaceutical composition based on the compound of formula I, a method of inhibiting KSP and use of the composition to prepare a medicinal agent.

EFFECT: novel imidazole derivatives are useful as kinesin spindle protein inhibitors for treating cancer.

25 cl, 27 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula as well as separate enantiomers, diastereomers, racemic mixures and pharmaceutically acceptable salts thereof, having mitotic kinesin KSP inhibiting activity, as well as inhibitory action on tumour cells, use thereof in preparing a medicinal agent and a pharmaceutical composition based on said compounds. In said formula, R denotes Z-NR2R3, Z-OH, Ar1 and Ar2 independently denote a phenyl which, if needed, is substituted with one or more groups independently selected from: F, CI, Br, I, OH, Z denotes an alkylene having 1-6 carbon atoms which, if needed, is substituted with C1-6alkyl, and R1 assumes values given in the claim.

EFFECT: improved method.

16 cl, 3 dwg, 124 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) and to their pharmaceutically acceptable salts exhibiting P2X3 receptor antagonist activity. In formula (I), X represents -O-; Y represents -NRdRe where one of radicals Rd and Re means hydrogen, and the other means hydrogen; C1-C12alkyl; C5-C7cycloalkyl; C5-C7cycloalky-C1-C12alkyl; hydroxy-C1-C12alkyl; acetyl; aminocarbonyloxy- C1-C12alkyl or heterocyclyl representing a 6-members saturated ring containing heteroatom S substituted by two oxo groups; D represents optional oxygen; R1 represents isopropyl; R2 represents hydrogen; R5 represents hydrogen or C1-C12alkyl; R4 means hydrogen; C1-C12alkyl; halogen; halogen- C1-C12alkyl; C1-C12alkoxy; hydroxy; halogen- C1-C12alkoxy; nitro; amino; hydroxy- C1-C12alkyl; C1-C12alkoxyalkyl; hydroxy- C1-C12alkoxy; C1-C12alkylsulphonyl; cyano; heteroaryl representing a 5-members aromatic ring containing one, two or three heteroatoms selected from O, S and N which can be optionally substituted by a thio group, C1-C12alkyl or C1-C12alkylsulphonyl; heterocyclyl representing a 6-members saturated ring containing two heteroatoms N, one of which is substituted C1-C12alkylsulphonyl; -(CH2)m-(Z)n-(CO)-Rf or -(CH2)m-(Z)n-SO2-(NRg)n-Rf where each m and n independently represents 0 or 1, Z means NR8, Rf means C1-C12alkyl, hydroxy, amino or hydroxy- C1-C12alkyl, and Rg means hydrogen; R3 represents methoxy; R6 represents hydrogen; and one of radicals R7 and R8 represents hydrogen, and the other represents hydrogen, acetyl or phenyl.

EFFECT: also, the invention refers to a pharmaceutical composition and to an application of the compound of formula (I) for preparing a drug.

8 cl, 3 tbl, 70 ex

FIELD: medicine.

SUBSTANCE: in formula (I) , the ring A represents 6-members aryl or 5-6-members heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulphur; Q means C3-8 cycloalkyl, 5-6-members heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulphur, C1-6 alkyl or C2-6 alkenyl; the ring T represents 5, 6, 9 or 10-members heteroaryl or 9-members heterocycle optionally additionally substituted by 1-3 heteroatoms independently selected from nitrogen or sulphur. The values of other substitutes are specified in the patent claim. Also, the invention refers to methods for preparing oxime derivatives of general formula (I), to pharmaceutical compositions containing the compound of the invention as an active ingredient and to applications of the compounds of the invention in preparing a drug.

EFFECT: compounds of the invention exhibit properties of a glucokinase activator.

33 cl, 1499 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I, where R1 denotes H; R6, R7, R8, R9, R10 independently denote H, F, Cl, Br, CF3, OCH3, OCF3, OCHF2, SCH3, SCF3, phenyl, (C1-C6)-alkyl, O-(C1-C6)-alkyl or NR3R4, where the alkyl and phenyl can be substituted with R2 once or many times, and where any two residues from R6, R7, R8, R9, R10 in neighbouring positions of the phenyl ring can form a -CH=CH-CH-CH- residue together; m equal 0, 1, 2 or 3; X denotes -(CH2)2-; R2 denotes F, Cl, Br, CN, OCH3, OCF3, CH3, CF3, (C1-C6)-alkyl or O-(C1-C6)-alkyl, where the alkyl can be substituted once or many times with OH, F, Cl, Br or CN; R3, R4 independently denote H or (C1-C6)-alkyl; or physiologically acceptable salts thereof, provided that the compound 3-(2-o- tolylamino-benzoxazol-6-yl)-propionic acid is excluded. The invention also relates to use of compounds of formula (I) to prepare a medicinal agent which activates GPR40 receptors and use of said compounds to prepare a medicinal agent for lowering blood sugar level, for treating diabetes and for increasing insulin secretion.

EFFECT: compounds of formula I which activate GPR40 receptors are obtained.

6 cl, 2 tbl, 146 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (1), where A1, A2, A3, A4, A5 ad A6 are independently selected from a group comprising CR3 and N; provided that the biggest one of A1, A2, A , A4, A5 and A6 denotes N; B1, B2 and B3 are independently selected from a group comprising CR2 and N; each R3 independently denotes H or C1-C6 alkyl; and R1, R2, R4, R5, W and n are as given in the description, or salts thereof which are suitable for use in agriculture. The invention also relates to compositions containing compounds of formula (1), and insect-pest control methods which involve contact between the pest or habitat thereof with a biologically effective amount of the compound or composition according to the present invention, as well as to methods of protecting seeds and animals from insects-pests.

EFFECT: high effectiveness of the obtained compounds in insect-pest control.

29 cl, 12 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound of formula I: or salt thereof, where: y equals 0; R1 and R2 are taken together to form a 3-tetrahydrofuran ring; R9 is hydrogen; R10 is 5-oxazolyl; R11 is a methoxy-, ethoxy- or isopropoxy group; each V1 is independently selected from halogen, NO2, CN, OR12, OC(O)R13, OC(O)R12, OC(O)OR13, OC(O)OR12, OC(O)N(R13)2, OP(O)(OR13)2, SR13, SR12, S(O)R13, S(O)R12, SO2R13, SO2R12, SO2N(R13)2, SO2NR12R13, SO3R13, C(O)R12, C(O)OR12, C(O)R13, C(O)OR13, NC(O)C(O)R13, NC(O)C(O)R12, NC(O)C(O)OR13, NC(O)C(O)N(R13)2, C(O)N(R13)2, C(O)N(OR13)R13, C(O)N(OR13)R12, C(NOR13)R13, C(NOR13)R12, N(R13)2, NR13C(O)R12, NR13C(O)R13, NR13C(O)OR13, NR13C(O)OR12, NR13C(O)N(R13)2, NR13C(O)NR12R13, NR13SO2R13, NR13SO2R12, NR13SO2N(R13)2, NR13SO2NR12R13, N(OR13)R13, N(OR13)R12, P(O)(OR13)N(R13)2 and P(O)(OR13)2; where each R12 is a monocyclic or bicyclic ring system consisting of 5-6 members in each ring, where said ring system optionally contains up to 4 heteroatoms selected from N, O or S, and where CH2 lying next to said N, O or S can be substituted with C(O); and each R12 optionally contains up to 3 substitutes selected from R11; where each R13 is independently selected from H, (C1-C4)-straight or branched alkyl or (C2-C4)-straight or branched alkenyl; and where each R13 optionally contains a substitute which is R14; where R14 is a monocyclic or bicyclic ring system consisting of 5-6 members in each ring, where said ring system optionally contains up to 4 heteroatoms selected from N, O or S, and where CH2 lying next to said N, O or S can be substituted with C(O); and each R14 optionally contains up to 2 substitutes independently selected from H, (C1-C4)-straight or branched alkyl or (C2-C4)-straight or branched alkenyl, 1,2-methylenedioxy-, 1,2-ethylenedioxy group or (CH2)n-Z; where Z is selected from halogen, CN, NO2, CF3, OCF3, OH, S(C1-C4)alkyl, SO(C1-C4)alkyl, SO2(C1-C4)alkyl, NH2, NH(C1-C4)-alkyl, M((C1-C4)alkyl)2, COOH, C(O)O(C1-C4)alkyl or O(C1-C4)-alkyl; and where any carbon atom in any R13 is optionally substituted with O, S, SO, SO2, NH or N(C1-C4)alkyl; where said method includes a step for reacting a compound of formula II with a compound of formula III in a polar or nonpolar aprotic, virtually anhydrous solvent or mixture thereof, and optionally in an acceptable base selected from an organic base, inorganic base or a combination of an organic base and an inorganic base; and while heating the reaction mixture to temperature ranging from approximately 30°C to approximately 180°C for approximately 1 to 48 hours in a virtually inert atmosphere: where: LG is -OR16; where R16 is -(C1-C6)-straight or branched alkyl; -(C2-C6)-straight or branched alkenyl or alkynyl; or a monocyclic ring system consisting of 5-6 members in each ring, where said ring system optionally contains up to 3 heteroatoms selected from N, O or S, and each R16 optionally contains up to 5 substitutes independently selected from (C1-C4)-straight or branched alkyl, (C2-C4)-straight or branched alkenyl or (CH2)n-Z; n equals 0, 1, 2, 3 or 4; V1, y, Z, R1, R2, R9, R10 and R11 are as indicated above; and provided that R16 is not a halogen-substituted (C2-C3)-straight alkyl.

EFFECT: improved method.

19 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula

,

where: X is a nitrogen or carbon atom; Ar is phenyl or a heteroaromatic ring selected from pyrazolyl, furanyl, thiophenyl and isoxazolyl; R1 is hydrogen, halogen, CN or (C1-C4)alkyl; R2 is halogen or (C1-C3)alkoxy optionally fluorinated with 1-3 fluorine atoms; R3 and R5 independently denote hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkenyl or hydroxymethyl; R4 is hydrogen, halogen, optionally fluorinated (C1-C4)alkoxy or aryl(C1-C4)alkoxy; R6 is hydrogen, optionally fluorinated (C1-C4)alkyl; each R7 independenlty denotes hydrogen, halogen, optionally fluorinated (C1-C4)alkyl or (C1-C4)alkoxy optionally fluorinated with 1-3 fluorine atoms; or pharmaceutically acceptable acid addition salts thereof. The invention also relates to use of compounds of formula (I) in a pharmaceutical composition and when preparing a medicinal agent meant for treatment, the aim of which is to change the secondary signal activity level after activation of glucocorticoid receptors.

EFFECT: compounds of formula I for changing the secondary signal activity level after activation of glucocorticoid receptors.

7 cl, 5 dwg, 49 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I or pharmaceutically acceptable salts thereof, which have receptor tyrosine kinase type I inhibiting properties and can be used in treating hyperproliferative disorders in mammals. In general formula

,

A is O or S; G is N; B is a 6-member aryl or 5-6-member heteroaryl ring containing a sulphur atom as a heteroatom; E is

, , , , , X is N or CH; D1, D2 and D3 independently denote N or CR19; D4 and D5 independently denote N or CR19 and D6 is O, S or NR20, where at least one of D4 and D5 is CR19; D7, D8, D9 and D10 independently denote N or CR19, where at least one of D7, D8, D9 and D10 is N; R1 is H or C1-C6 alkyl; each R2 independently denotes halogen, cyano, nitro etc, trifluoromethyl, difluoromethyl, fluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, azido, -SR18, -OR15, -C(O)R15, -C(O)OR15, -NR14C(O)OR18, -OC(O)R15, -NR14SO2R18, -SO2NR15R14, -NR14C(O)R15, -C(O)NR15R14, -NR15C(O)NR15R14, -NR13C(NCN)NR15R14, -NR15R14, C1-C12alkyl, C2-C12 alkenyl, alkynyl, saturated or partially unsaturated C3-C10cycloalkyl, C3-C10cycloalkyl-C1-C12alkyl, -S(O)p(C1-C6alkyl), -S(O)p(CR13R14)q-phenyl, phenyl, phenyl-C1-3-alkyl, 5-6-member heteroaryl, 5-6-member heteroaryl-C1-C3-alkyl, saturated or partially unsaturated 3-8-member heterocyclyl, 5-6-member heterocyclyl-C1-C3-alkyl, -O(CR13R14)q-phenyl, NR15(CR13R14)q-phenyl, O(CR13R14)q-(5-6-member heteroaryl), NR13(CR13R14)q-(5-6-member heteroaryl, -O(CR13R14)q-(3-8-member heterocyclyl) or -NR15(CR13R14)q-3-8-member heterocyclyl), each R3 denotes Z, where Z is selected from and , W is O or S; W2 is O or S;V is CR8R9, R8b is H or C1-C6alkyl; each of R6, R8, R8a and R9 independently denotes hydrogen, trifluoromethyl, C1-C12alkyl etc.

EFFECT: improved properties and high efficiency of using the compounds.

25 cl, 13 dwg, 1 tbl, 36 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel imidazole derivatives of general formula I and pharmaceutically acceptable salts thereof, where R1 is selected from a group comprising aryl and alkyl, optionally substituted hydroxy; R2 is selected from a group comprising hydrogen and alkyl; R3 is selected from a group comprising hydrogen and -X-A, where X is selected from a group comprising -C(O)- and -S(O)2-; and A is selected from a group comprising hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycle and optionally substituted cycloalkyl, where the optionally substituted groups are substituted with 1-2 substitutes selected from a group comprising alkyl, substituted alkyl, alkoxy, substituted amine which is a -NRR group, substituted aryloxy, heteroaryl, heterocycle, halogen, hydroxy and -S(O)2-R9, where R9 is an alkyl; or R1 and R3 together with a carbon atom bonded to R1 and a nitrogen atom bonded to R3 form a heterocyclic or substituted heterocyclic group; R4 is selected from a group comprising hydrogen, linear alkyl, -alkylene-aminoacyl-, -alkylene-hydroxy-, -[alkylene]p-nitrogen-containing heterocycle, -[alkylene]p-nitrogen-containing substituted heterocycle, -[alkylene]p-nitrogen-containing heteroaryl, -[alkylene]p-nitrogen-containing substituted heteroaryl and -[alkylene]p-NR10R11, where p equals 0 or 1, the alkylene contains 1-5 carbon atoms and can have 1 or 2 substitutes selected from a group comprising amine, hydroxy and halogen, aminoacyl relates to a group -C(O)NRR, where each R is independently selected from a group comprising hydrogen and alkyl, R10 and R11 are independently selected from a group comprising hydrogen, alkyl, substituted alkyl, -S(O)2-alkyl, substituted aryl, substituted heteroaryl, cycloalkyl, or when R10 is hydrogen, R11 is hydroxy, alkoxy or substituted alkoxy; or when R1 and R3 together with carbon and nitrogen atoms respectively bonded to them do not form a heterocyclic or a substituted heterocyclic group, R3 and R4 together with a nitrogen atom to which they are bonded form a spiro-condensed heterocyclic group; R5 is selected from a group comprising L-A1, where L is selected from a group comprising C1-C5alkylene, where the alkylene is defined above; and A1 is selected from a group comprising aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle; and one of R6 or R7 is selected from a group comprising aryl and heteroaryl, each of which can optionally be substituted with -(R8)m, where m equals a whole number from 1 to 2, and the other of R6 or R7 is selected from a group comprising hydrogen, halogen and alkyl; or R6 as well as R7 denotes hydrogen; R8 is selected from a group comprising cyano, alkyl, -CF3, alkoxy, halogen, where alkyl, aryl, aryloxy, cycloalkyl, heterocycle, heteraryl and substituted alkyl, aryl, aryloxy, cycloalkyl, heterocycle and heteroaryl are described in claim 1. The invention also relates to specific compounds, a pharmaceutical composition based on the compound of formula I, a method of inhibiting KSP and use of the composition to prepare a medicinal agent.

EFFECT: novel imidazole derivatives are useful as kinesin spindle protein inhibitors for treating cancer.

25 cl, 27 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to drugs and concerns a combination for tumour cell growth inhibition containing a cytotoxic compound selected from camptothecin compounds; metabolic antagonists; periwinkle alkaloids; taxanes; platinum compounds; topoisomerase 2 inhibitors; and a combination of two or more said types, or a signal transfer inhibitor selected from antibodies a target of which is EGFR receptor; tyrosine kinase EGFR inhibitors; from antibodies a target of which is a VEGF/VEGF receptor system; PDGFR inhibitors; Raf inhibitors and PKB transfer inhibitors in an effective amount and a compound of formula (IV).

, where R1, R2, R11, T, U and g have the values specified in formula.

EFFECT: what is offered is a pharmaceutical composition, a method for tumour cell growth inhibition, a method of treating a malignant growth in a patient and application of the combination for preparing a drug; the new effective combinations for tumour cell growth inhibition are presented.

77 cl, 20 dwg, 7 tbl, 257 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula

,

where R1 is selected from formulae

, and ,

n equals 0; R6 and R7 are independently selected from hydrogen, C1-C6alkyl, cyanoC1-C6alkyl, C3-C6cycloalkylC0-C4alkyl and C6arylC0-C4alkyl; or R6 and R7 together with a carbon atom to which they are bonded form a 6-member heterocycloalkyl with one nitrogen atom; wherein any alkyl in R6 and R7 can optionally contain a methylene group substituted with an O atom; wherein any aryl in R6 and R7 or formed by a combination of R6 and R7 can be optionally substituted with one radical independently selected from: halide, C1-C6alkyl, -XC(O)OR10; where X denotes a bond; R10 is independently selected from C1-C6alkyl; R8 is selected from C5-C9heteroarylC0-C4alkyl containing 2-3 heteroatoms independently selected from N, O and S; wherein any heteroaryl in R8 can be optionally substituted with one radical independently selected from: halide, C1-C6alkyl, C3-C6cycloalkyl; R2 denotes hydrogen; R3 and R4 are independently selected from hydrogen, C1-C6alkyl, C3-C6cycloalkylC0-C4alkyl and C6arylC0-C4alkyl; wherein any alkyl in R3 and R4 can optionally contain a methylene group substituted with a S(O)2 group; R5 is selected from C5-C6heterocycloalkyl with 1-2 heteroatoms selected from N and O, and NR12R13; where R12 and R13 are independently selected from C1-C6alkyl; as well as pharmaceutically acceptable salts and isomers thereof. The invention also relates to use of compounds of formula (I) in preparing a medicinal agent, and to a pharmaceutical composition having cathepsin S inhibiting properties, which contains a therapeutically effective amount of the compound of formula (I) in combination with a pharmaceutically acceptable filler.

EFFECT: obtaining compounds which can be used as cathepsin S inhibitors.

10 cl, 12 dwg, 2 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) and to their pharmaceutically acceptable salts exhibiting P2X3 receptor antagonist activity. In formula (I), X represents -O-; Y represents -NRdRe where one of radicals Rd and Re means hydrogen, and the other means hydrogen; C1-C12alkyl; C5-C7cycloalkyl; C5-C7cycloalky-C1-C12alkyl; hydroxy-C1-C12alkyl; acetyl; aminocarbonyloxy- C1-C12alkyl or heterocyclyl representing a 6-members saturated ring containing heteroatom S substituted by two oxo groups; D represents optional oxygen; R1 represents isopropyl; R2 represents hydrogen; R5 represents hydrogen or C1-C12alkyl; R4 means hydrogen; C1-C12alkyl; halogen; halogen- C1-C12alkyl; C1-C12alkoxy; hydroxy; halogen- C1-C12alkoxy; nitro; amino; hydroxy- C1-C12alkyl; C1-C12alkoxyalkyl; hydroxy- C1-C12alkoxy; C1-C12alkylsulphonyl; cyano; heteroaryl representing a 5-members aromatic ring containing one, two or three heteroatoms selected from O, S and N which can be optionally substituted by a thio group, C1-C12alkyl or C1-C12alkylsulphonyl; heterocyclyl representing a 6-members saturated ring containing two heteroatoms N, one of which is substituted C1-C12alkylsulphonyl; -(CH2)m-(Z)n-(CO)-Rf or -(CH2)m-(Z)n-SO2-(NRg)n-Rf where each m and n independently represents 0 or 1, Z means NR8, Rf means C1-C12alkyl, hydroxy, amino or hydroxy- C1-C12alkyl, and Rg means hydrogen; R3 represents methoxy; R6 represents hydrogen; and one of radicals R7 and R8 represents hydrogen, and the other represents hydrogen, acetyl or phenyl.

EFFECT: also, the invention refers to a pharmaceutical composition and to an application of the compound of formula (I) for preparing a drug.

8 cl, 3 tbl, 70 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel oxadiazole compounds of formula (1) and pharmaceutically acceptable salts thereof, where R1 and R2 assume values given in the description, Y is a single bond. The invention also relates to use of said compounds as DGAT1 inhibitors, for example for treating obesity and diabetes, and a method of inhibiting.

EFFECT: high treatment efficiency.

13 cl, 65 tbl, 712 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 1H-quinazoline-2,4-diones of formula and to their pharmaceutically acceptable salts where R1 and R2 have the values specified in cl. 1 of the patent claim. The specified compounds exhibit antagonistic activity with respect to the AMPA receptor.

EFFECT: reception of a pharmaceutical composition for preparing a preparation used for treating a condition mediated by the AMPA receptor and first of all for treating epilepsy or schizophrenia.

8 cl, 81 ex

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