Novel derivatives of benzimidazole, methods for their preparing, their using and pharmaceutical composition containing thereof

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to therapeutic agents showing effectiveness in treatment of pain, cancer, cerebrospinal sclerosis, Parkinson's disease, Huntington's chorea and/or Alzheimer's disease. Invention describes compound of the formula (I): or its pharmaceutically acceptable salts wherein RF1 and RF2 represent independently electron-acceptor groups; Z is chosen from O=; R1 is chosen from (C1-C10)-alkyl, heterocyclyl-(C1-C6)-alkyl, substituted heterocyclyl-(C1-C6)-alkyl; R2 is chosen from (C1-C6)-alkyl; X represents bivalent (C1-C10)-group that separates groups added to it by one or two atoms; Ar represents bivalent (C4-C12)-aromatic group, and Y is chosen from =CH=. Also, invention describes fields wherein compounds of the formula (I) are used, a pharmaceutical composition based on thereof, and methods for their synthesis. Invention provides synthesis of novel compounds possessing useful biological properties.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

17 cl, 2 tbl, 35 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula (I) or its pharmaceutically acceptable salt

where RF1and RF2independently represent an electron-withdrawing group;

Z is selected from O=;

R1selected from C1-10of alkyl; heterocyclyl-C1-6of alkyl; substituted heterocyclyl-C1-6of alkyl;

R2selected from C1-6of alkyl;

X represents a C1-10divalent group that divides groups attached to it by one or two atoms;

Ar represents a C4-12the divalent aromatic group; and Y is selected from-CH=.

2. The compound according to claim 1,

where RF1and RF2independently represent a1-6alkyl, substituted one or more than one group selected from-F, -Cl, -Br, -NO2, -CN, -OH, -Cho, -C(=O)-R' and-OR', where R' represents a C1-3alkyl.

3. The compound according to claim 1,

where RF1and RF2independently chosen from-CF3, -CH2CF3, -CH2CHF2, -CHFCF3, -CHFCHF2, -CHFCH2F, -CF2CF3, -CF2CH3, -CF2CH2F, -CF2CHF2, -CCl3, -CH2CCl3, -CH2CHCl2, -CH2CBr3, -CH2CHBr2, -CH2NO2, -CH2CH2NO2, -CH2CN, -CH2CH2CN and CH2CH2OCH3.

4. The compound according to claim 1, where RF1and RF2independently represents a C1-6groups that include at least 30% fluorine by weight, and Z represents O=.

5. The compound according to claim 1, where R1selected from the 1-10of alkyl; heterocyclyl-C1-6of alkyl; substituted heterocyclyl-C1-6of alkyl;

R2selected from C1-6of alkyl; and

X is selected from-NR6-, -C(=O)-, -CH2-CH2-, -CH=CH-, -O-, -C(R6)(R7)- and-S(O)n-, in which n represents 0, 1 or 2, in which R6and R7independently represent a1-6alkyl, C2-6alkenyl,2-6quinil, C1-6alkoxy, HE or N.

6. The compound according to claim 1,

where R1selected from C1-8of alkyl; heteroseksualci-C1-6of alkyl; heteroseksualci-C1-6of alkyl with heterocyclization, substituted by at least one group selected from C1-8of alkyl, acetoxymethyl, nitro and halogen; heteroaryl-C1-6of alkyl; heteroaryl-C1-6of alkyl with heteroaryl, substituted by at least one group selected from C1-6of alkyl, acetoxymethyl, nitro and halogen;

R2selected from-CH3, -CH2CH3, -CH(CH3)2;

Ar is selected from arylene; heteroaryl; arylene, substituted by at least one group selected from C1-6of alkyl, halogen, trifloromethyl, cyano, nitro, hydroxy and C1-6alkoxy; and heteroaryl, substituted by at least one group selected from C1-6of alkyl, halogen, trifloromethyl, cyano, nitro, hydroxy and C1-6alkoxy.

Caetanina according to claim 6,

where Allen is a pair-Allen; and heteroaryl selected from a pair of heteroarenes with six-membered ring and meta-heteroaryl with the five-membered ring.

8. The compound according to claim 1, where R1selected from ethyl, propyl, isopentyl, 4-pyridylmethyl, 2-pyridylmethyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, N-methyl-2-pyrrolidinyl, N-methyl-3-pyrrolidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, N-methyl-2-piperidinyl, N-methyl-3-piperidinyl, N-methyl-4-piperidinylmethyl, 3-thienylmethyl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, (2-nitrothiophen-5-yl)methyl, (1-methyl-1H-imidazol-2-yl)methyl, (5-(acetoxymethyl)-2-furanyl)methyl, (2,3-dihydro-1H-isoindole-1-yl)methyl 5-(2-methylthiazolyl);

R2selected from-CH3, -CH2CH3, -CH(CH3)2;

RF1and RF2represent-CH2CF3and Z represents O=;

Ar is selected from the vapor-arylene; a pair of arylene, substituted C1-6by alkyl, halogen, trifluoromethyl, cyano, nitro, hydroxy and C1-6alkoxy; a pair of heteroarenes with six-membered ring; and a pair of heteroarenes with six-membered ring, substituted by a group selected from C1-6of alkyl, halogen, trifloromethyl, cyano, NITR is, hydroxy and C1-6alkoxy.

9. The compound according to claim 1,

where RF1and RF2represent-CH2CF3and Z represents O=;

R2represents-CH2CH3;

Ar is selected from para-phenylene and para-peradilan; and

X is selected from-CH2- , and-CH(CH3)-.

10. Compound, selected from

2-[(4-Ethoxyphenyl)methyl]-1-(3-methylbutyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclopropylmethyl)-2-[(4-ethoxyphenyl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclohexylmethyl)-2-[(4-ethoxyphenyl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-(2-furylmethyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[(2S)-2-pyrrolidinyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[(2R)-2-pyrrolidinyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-(4-pyridinylmethyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[1-(4-Ethoxyphenyl)ethyl]-1-(4-pyridinylmethyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[(tetrahydro-2H-Piran-4-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[[(2S)-tetrahydro-2-furanyl]methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[(tetrahydro-2H-Piran-2-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[(2R)-2-piperidinylmethyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxy-2-pyridyl)methyl]-1-[(tetrahydro-2H-Piran-4-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxy-2-pyridinyl)methyl]-1-(3-methylbutyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[[(2R)-1-methyl-2-pyrrolidinyl]methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(4-Ethoxyphenyl)methyl]-1-[[(2R)-1-methyl-2-piperidinyl]methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxy-2-pyridinyl)methyl]-1-[(2R)-2-pyrrolidinyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[1-(4-Ethoxyphenyl)ethyl]-1-[(2R)-2-pyrrolidinyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxy-2-pyridinyl)methyl]-1-[[(2R)-1-methyl-2-piperidinyl]methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxy-2-pyridinyl)methyl]-1-[[(2R)-1-m is Teal-2-pyrrolidinyl]methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclobutylmethyl)-2-(4-ethoxybenzyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclobutylmethyl)-2-[(5-ethoxypyridine-2-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclopentylmethyl)-2-[(5-ethoxypyridine-2-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-(4-Ethoxybenzyl)-1-[(2S)-piperidine-2-ylmethyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxypyridine-2-yl)methyl]-1-(3-furylmethyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxypyridine-2-yl)methyl]-1-(3-thienylmethyl)-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclohexylmethyl)-2-[(5-ethoxypyridine-2-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

1-(Cyclohexylmethyl)-2-[(5-isopropoxypyridine-2-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-(4-Ethoxybenzyl)-1-[(4-methylmorpholin-3-yl)methyl]-N,N-bis(2,2,2-triptorelin-1H-benzimidazole-5-carboxamide;

2-[(5-Ethoxypyridine-2-yl)methyl]-1-[(4-methylmorpholin-3-yl)methyl]-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-(4-Ethoxybenzyl)-1-{[(2S)-1-methylpiperidin-2-yl]methyl}-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-carboxamide;

2-(4-Isopropoxyphenyl)-1-{[(2R)-1-methylpiperidin-2-yl]methyl}-N,N-bis(2,2,2-triptorelin)-1H-benzimidazole-5-to rockslide;

and their pharmaceutically acceptable salts.

11. The compound according to any one of claims 1 to 10 for use as a medicinal product with the activity of a selective agonist of the receptor SV2.

12. The use of compounds according to any one of claims 1 to 10 in the manufacture of medicaments for the treatment of pain.

13. The use of compounds according to any one of claims 1 to 10 in the manufacture of drugs for cancer treatment.

14. The use of compounds according to any one of claims 1 to 10 in the manufacture of drugs for the treatment of multiple sclerosis, Parkinson's disease, Horai Huntington, transplant rejection or Alzheimer's disease.

15. Pharmaceutical composition having activity selective agonist of the receptor SV2containing the compound according to any one of claims 1 to 10 and a pharmaceutically acceptable carrier.

16. The method of obtaining the compounds of formula (I) according to claim 1, comprising a stage of interaction of the compounds represented by formula (II)

with R2OArXCOA.

where RF1and RF2independently represent an electron-withdrawing group;

Z is selected from O=;

R1selected from C1-10of alkyl; heterocyclyl-C1-6of alkyl; substituted heterocyclyl-C1-6of alkyl;

R2selected from C1-6of alkyl;

X represents a C1-10divalent group, to the which parts of the group, attached to it by one or two atoms;

Ar represents a C4-12the divalent aromatic group;

Y is selected from-CH=; and

And selected from-OH, -Cl, -Br, and-J.

17. A method of obtaining a compound according to claim 1 of formula (I),

where R1represents a substituted heterocyclyl-C1-6the alkyl of the formula

including the stage of interaction of the compounds represented by formula (III)

where r and s is selected from 0, 1 and 2;

R10selected from C1-6alkylene;

RF1and RF2independently represent an electron-withdrawing group;

X represents a C1-10divalent group that divides groups attached to it by one or two atoms;

Ar represents a C4-12the divalent aromatic group;

R2selected from C1-6of alkyl; and

Y is selected from-CH=;

with formaldehyde.



 

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22 cl, 3 tbl, 8 dwg, 6 ex

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12 cl, 12 tbl, 17 dwg, 5 ex

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7 cl, 3 tbl, 11 ex

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EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical agent.

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27 cl, 3 tbl, 352 ex

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EFFECT: valuable medicinal properties of compounds.

18 cl, 1 tbl, 49 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method for treatment.

26 cl, 17 tbl, 221 ex

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EFFECT: valuable medicinal properties of compound and pharmaceutical composition.

39 cl, 3 tbl, 31 ex

FIELD: organic chemistry, biochemistry.

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EFFECT: valuable biochemical properties of compounds and pharmaceutical composition.

25 cl, 134 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds, namely, to N-substituted derivatives of piperidine of the formula (I): or their pharmaceutically acceptable salts, amides, esters wherein values R1, R, R3, m, X, n, W, Ar1 and Ar2 are disclosed in the invention claim. Also, invention relates to methods for inhibition of activity and methods for inhibition of activation of monoamine receptors. Methods involve contacting monoamine receptors or system comprising monoamine receptors with the effective amount of one or some compounds of the formula (I). Except for, invention relates to using compounds of the formula (I) in treatment of psychotic diseases.

EFFECT: valuable medicinal properties of compounds.

35 cl, 1 tbl

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to phthalimido-derivatives of the general formula (I): wherein X means -N= or -CH=; R1 means -CO-NR5R6, -CHR7-(CH2)n-CO-NR5R6, -(CH2)n-NR5R6, -(CH2)n-COOR8, -(CH2)n-CN, -CHR7-(CH2)n-CF3, -(CH2)n-NH-COR9, -(CH2)n-NH-COOR8, -(CH2)n-piperidinyl, -(CH2)n-morpholinyl, -(CH2)n-tetrahydrofuranyl, -(CH2)n-thiophenyl or -(CH2)n-isoxazolyl wherein a heterocyclic ring can be substituted with (C1-C6)-alkyl; -(CH2)n-phenyl wherein phenyl ring can be substituted with halogen atom or halogen-(C1-C6)-alkyl; -(CH2)p-OR8, -(CH2)p-SR8, -(CH2)p-SO-R9 or -(CH2)n-CS-NR5R6; R2 means hydrogen atom (H), (C1-C6)-alkyl, -(CH2)p-OR10, -(CH2)p-SR or benzyl; R3 means H, (C1-C6)-alkyl; R4 means halogen atom, halogen-(C1-C6)-alkyl, cyano-, (C1-C6)-alkoxy- or halogen-(C1-C6)-alkoxy-group; Each R5 and R6 means independently of one another H, (C1-C6)-alkyl; R7 means H, -OH, (C1-C6)-alkoxy-group; R8 means H, (C1-C6)-alkyl; R9 means (C1-C6)-alkyl; R10 means H, (C1-C6)-alkyl; m = 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2, and their pharmaceutically acceptable salts. Compounds of the formula (I) inhibit activity of monoamine oxidase B (MAO B) that allows their using as a drug.

EFFECT: valuable medicinal and biochemical properties of compounds.

14 cl, 4 sch, 1 tbl, 53 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with describing the efficient quantity of, at least, one heterocyclic compound of formula (I) or its salts, moreover, the compound of formula (I) should be chosen out of (i) the compounds of formula (III) or their salts, in which Z, Z' indicate O, X indicates S (thiazolidine dionic group), G indicates O or S; at least, one out of R2 and R3 indicates CF3, OR0 or COOR0, where R0 indicates H or saturated linear or branched C1-C20-alkyl and, preferably, C10-C10-alkyl, (ii) compounds (VI) or their salts: in which Z, Z' and G independently indicate O or S, at least, one out of R2 and R3 indicates hydrogen, CN, CF3, NO2, OR0, COOR0 or saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl, possibly substituted OR0, where R0 indicates H or saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl, (iii) compounds (VII) or their salts in which Z, Z' and G independently indicate O or S; R indicates saturated linear or branched C1-C10-alkyl; at least, one out of R2 and R3 indicates saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl, NO2, OR0, where R0 indicates H or saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl. The compounds in question reveal improved action upon stimulation of keratin fibers growth, particularly, human keratin fibers, that prevents their falling down and increases their density.

EFFECT: higher efficiency.

31 cl, 13 ex, 6 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel indolyl-derivatives of the formula (I): and their pharmaceutically acceptable salts and esters wherein R1 means phenyl optionally substituted with from one to three substitutes chosen independently from halogen atom, (C1-C8)-alkyl, (C1-C8)-alkoxy-group and (C1-C8)-alkyl substituted with from one to three halogen atoms; R2 means hydrogen atom, (C1-C8)-alkyl; R3 means (C1-C8)-alkoxy-group; R4 means hydrogen atom; A means oxygen atom or sulfur atom; n = 1,2 or 3. Synthesized compounds possess agonistic activity with respect to PPARα- and/or PPARγ-receptors. Also, invention relates to methods for their synthesis, a pharmaceutical composition based on thereof and their using for preparing medicinal agents, and to a method for treatment and/or prophylaxis of diseases.

EFFECT: improved method of synthesis and treatment, valuable medicinal properties of compounds and pharmaceutical composition.

29 cl, 1 tbl, 7 sch, 17 ex

FIELD: organic chemistry, medicine, oncology, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I): wherein R1 means hydrogen atom or lower alkyl; R2 means substituted or unsubstituted thiazolinyl or oxazolinyl residue; each R5 and R6 means independently hydrogen atom or protective group; X means oxygen (O), sulfur atom (S) or -NR7 wherein in each case R7 means hydrogen atom or lower alkyl; RB means in each case independently hydrogen atom, (C1-C6)-alkyl, -CY3, -CHY2 or -CH2Y wherein Y means F, Br, Cl or J. Also, invention relates to a pharmaceutical composition containing compounds of the formula (I) and possessing cytotoxic activity, and using this compound in treatment of malignant tumor with multiple drug resistance.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

44 cl, 77 dwg, 13 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes derivatives of aminotetraline of the formula (I) wherein R1 means (C1-C6)-alkyl; R2 means halogen atom or -OR'; R3 means hydrogen atom (H) or -OR' wherein R' means (C1-C6)-alkyl or -SO2R'' wherein R'' means phenyl, thienyl, isoxazolyl; R4 means (C1-C6)-alkyl, phenyl, piperidinyl, pyrrolidinyl, morpholinyl, piperazinyl, diazepinyl, furanyl, isoxazolyl, imidazolyl and pyrazolyl that can be substituted optionally, and pharmaceutical compositions containing derivatives of aminotetraline. Proposed compounds are selective antagonists of M2/M3 muscarinic receptors and designated for treatment and prophylaxis of diseases associated with smooth muscle disorder.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

23 cl, 1 tbl, 16 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to alkylated (1H-benzimidazol-5-yl)-(-4-substituted phenyl)-amine derivatives, in particular compound of formula and pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, and R9, are independently hydrogen, halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluorimethoxy, azido, etc.; R7 is optionally substituted C1-C10-alkyl, C3-C10-cycloalkyl, etc.; A is-OR3 or NR4R3; R8 is hydrogen, -Cl, -Br, -F, cyano, nitro, etc.; and meanings of the rest substituents are as defined in specification. Also disclosed is composition for MEK inhibition and uses of benzinidazole compounds.

EFFECT: new compounds with value biological properties.

32 cl, 56 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): wherein R means -C(O)R1 wherein R1 is chosen from the series: (C1-C6)-alkyl, -C=CH-COOH, -NHCH2-CH2R2, -N(CH2-CH2OH)CH2-CH2OH, -N(CH3)CH2-CH2-NHCH3, -N(CH3)CH2-CH2N(CH3)CH3, saturated 4-, 5- and 6-membered cycles and saturated and unsaturated 5- and 5-membered cycles comprising at least one heteroatom from a series sulfur (S), nitrogen (N) and oxygen (O), and optionally substituted with a group chosen from the series: (C1-C6)-alkyl, -C=O-R5, -OH, (C1-C6)-alkyl substituted with hydroxy-group optionally, (C1-C6)-alkyl substituted optionally with a group of the series: -NH2, -N-(C1-C6)-alkyl, -SO2CH3, =O, and 5- and 6-membered saturated cycles comprising at least one heteroatom chosen from N and O, and wherein R5 is chosen from the series: hydrogen atom (H), (C1-C6)-alkyl, (C1-C6)-alkyl substituted with hydroxy-group optionally, and (C1-C6)-alkyl substituted with NH2-group optionally; R2 is chosen from the series: -N(CH3)CH3, -NH2, morpholinyl and piperazinyl; X1, X2 and X3 are chosen independently from the series: -OH, (C1-C2)-alkyl, (C1-C6)-alkoxy-group, -Cl, -Br, -F, -CH2OCH3 and -CH2OCH2CH3, or one among X1, X2 or X3 means hydrogen atom, and two others are chosen independently from the series: hydroxy-group, (C1-C6)-alkyl, (C1-C6)-alkoxy-group, -Cl, -Br, -F, -CF3, -CH2OCH3, -CH2OCH2CH3, -OCH2-CH2R3, -OCH2-CF3 and -OR4, morpholylmethyl, -N(CH3)CH3, -CH2OH, -COOH, or one among X1, X2 or X3 means hydrogen atom, and two others in common with two carbon atoms including bonds between them in benzene cycle to which they are bound optionally form 5- or 6-membered saturated cycle comprising at least one heteroatom chosen from S, N and O, and wherein R3 is chosen from the series: -F, -OCH3, -N(CH3)CH3, saturated 5-membered cycle comprising at least one heteroatom N; R4 means 3-5-membered saturated cycle, and each Y1 and Y2 is chosen independently from the series: -Cl, -Br, -NO2,-C≡N and C≡N, and compound of the formula (II) also given in the invention description. Also, invention relates to a pharmaceutical composition possessing anti-proliferative activity and based on these compounds. Invention provides preparing novel compounds possessing the useful biological properties.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

28 cl, 39 ex

Novel benzodioxols // 2304580

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of benzodioxol of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and X are given in the description and the invention claim, and to their pharmaceutically acceptable salts. Also, invention relates to pharmaceutical compositions based on compounds of the formula (I) and their using for preparing medicinal agents used in treatment and/or prophylaxis of diseases associated with modulation of CB1 receptors.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

19 cl, 279 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of pyrrolidinium of the general formula (I): possessing antagonistic effect with respect to muscarinic receptors M3 wherein B means phenyl or thienyl group; each radical among R1, R2 and R means independently hydrogen, fluorine, chlorine atom or hydroxyl; n means a whole number from 0 to 1; A means group chosen from groups -CH2 and -O-; m means a whole number from 0 to 6; R means (C1-C8)-alkyl; X- represents a pharmaceutically acceptable anion of mono- or multibasic acid, and involving all separate stereoisomers and their mixtures. Also, invention relates to methods for synthesis of such compounds, pharmaceutical compositions containing such compounds and to their using in therapy as antagonists of muscarinic receptors M3.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

17 cl, 51 ex

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