Neurologically active compositions

FIELD: medicine.

SUBSTANCE: compounds can be used for treating neurological conditions, more specifically for treating neurodegenerative conditions, such as Alzheimer's disease. In a compound of formula I R2 represents H or CH2NR1R4 where R1 and R4 are independently selected from H, unsubstituted C1-6alkyl, substituted or unsubstituted C3-6 cycloalkyl, R3 represents H; substituted or unsubstituted C1-4alkyl; substituted or unsubstituted C2-4alkenyl; substituted or unsubstituted 6-members aryl condensed or uncondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl, containing 1-2 nitrogen atoms in a cycle; substituted or unsubstituted saturated or unsaturated 5 or 6-members N-containing heterocycle which can additionally contain nitrogen, oxygen or the sulphur atom condensed or ucondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl containing nitrogen in a cycle; (CH2)nR6 where n is an integer from 1 to 6, and the values of R6 and the values of other radicals are specified in the patent claim.

EFFECT: increased antiamyloidogenic action.

20 cl, 20 tbl, 6 dwg, 7 ex

 

The text descriptions are given in facsimile form.

1. The compound of the formula I

in which
R2represents N or CH2NR1R4where R1and R4independently selected from H, unsubstituted C1-6of alkyl, substituted or unsubstituted With3-6cycloalkyl;
R3represents H; substituted or unsubstituted With1-4alkyl; substituted or unsubstituted With2-4alkenyl; substituted or unsubstituted 6-membered aryl, condensed or not condensed with a substituted or unsubstituted 6-membered aryl or 5-6-membered heteroaryl containing 1-2 nitrogen atom in the cycle; substituted or unsubstituted saturated or unsaturated 5 - or 6-membered N-containing heterocycle, which may optionally contain a nitrogen atom, oxygen or sulfur, condensed or not condensed with a substituted or unsubstituted 6-membered aryl or 5-6-membered heteroaryl, soderjasimi in a loop; (CH2)nR6where n is an integer from 1 to 6, and R6represents a substituted or unsubstituted With1-4alkyl, substituted or unsubstituted With3-6cycloalkyl, substituted or unsubstituted saturated or unsaturated 5 - or 6-membered N-containing heterocycle, which may contain in the cycle additional heteroatom selected from nitrogen, oxygen, or sulfur; NR8R9where R8and R9independently selected from H, substituted or unsubstituted With1-4of alkyl, substituted or unsubstituted With3-6cycloalkyl, substituted or unsubstituted saturated or unsaturated 5-or 6-membered N-containing heterocycle may contain an additional heteroatom selected from nitrogen and sulfur, and substituted or unsubstituted 6-membered aryl; CH2CONR11R12where R11and R12independently selected from H, substituted or unsubstituted C1-6of alkyl, substituted or unsubstituted With2-6the quinil and substituted or unsubstituted 5 - or 6-membered N-containing heterocycle fused or unfused with substituted or unsubstituted 6-membered aryl; and (CH2)mOther13where R13selected from substituted or unsubstituted C1-6the alkyl and SO2R14where R14selected from substituted or unsubstituted C1-6the alkyl and C is displaced or unsubstituted 6-membered aryl, a m is from 1 to 6;
when the substituents are selected from the following groups:1-4alkyl, C2-4alkenyl, C2-4quinil, halogen, hydroxy, C1-4alkoxy, 6-membered heterocycle with 1 or 2 heteroatoms in the cycle selected from nitrogen, oxygen or sulfur, amino, C1-4alkylamino, dis1-4alkylamino,2-4alkenylamine;
R5and R7independently selected from H and halogen; and
X represents Oh, under the following conditions:
(i) at least one of R2and R3is not H;
(ii) at least one of R5and R7is a halogen;
(iii) if X represents Oh, R5and R7represent Cl, a R2represents H, R3is not cyclopropyl or paraterphenyl; and
(iv) if X represents Oh, R5represents H, R7is a I, a
R2represents H, R3isn't C2-4the alkyl, and their pharmaceutically acceptable salts.

2. The compound according to claim 1, which is a compound of formula IA

in which
R5, R7and X correspond to the definitions given in claim 1; and
R3represents a substituted or unsubstituted With2-4alkyl; substituted or unsubstituted With2-4alkenyl; substituted or unsubstituted saturated or unsaturated with the first 5 - or 6-membered N-containing heterocycle, condensed or not condensed with a substituted or unsubstituted 6-membered aryl or 5-6-membered heteroaryl; (CH2)nR6in which n is from 1 to 3, and R6represents a substituted or unsubstituted With3-6cycloalkyl or substituted or unsubstituted saturated or unsaturated 5 - or 6-membered N-containing heterocycle; NR8R9in which R8represents H, a R9-H, or substituted or unsubstituted With1-4alkyl, or substituted or unsubstituted 6-membered aryl.

3. The compound according to claim 2, in which R3represents a substituted or unsubstituted With1-4alkyl; substituted or unsubstituted With2-4alkenyl; substituted or unsubstituted saturated or unsaturated 5 - or 6-membered N-containing heterocycle, condensed or not condensed with a substituted or unsubstituted 6-membered aryl or heteroaryl, (CH2)nR6where n is from 1 to 3, and R6represents a substituted or unsubstituted With3-6cycloalkyl or substituted or unsubstituted saturated or unsaturated 5 - or 6-membered N-containing heterocycle; or NR8R9where R8represents H, a R9-H, or substituted or unsubstituted With1-4alkyl, or substituted or unsubstituted 6-membered aryl.

4. The compound according to any one of p is.1-3, having the following form:





















5. The compound according to claim 1, which is the is the group of formula IB:

in which R2, R5, R7and X correspond to the definition given in claim 1.

6. The compound according to claim 5, in which R2represents CH2NR1R4where R1and R4independently selected from H, substituted or unsubstituted C1-6of alkyl and substituted or unsubstituted With3-6cycloalkyl.

7. The compound according to any one of claims 1, 5 or 6, which has the following form:

8. The compound according to claim 1, which compound of formula 1C

in which
R5, R7and X correspond to the definition given in claim 1; and
R2Crepresents CH2NR1R4where R1and R4independently selected from H and substituted or unsubstituted C1-6of alkyl; and
R3Cis substituted or unsubstituted With1-4the alkyl.

9. The connection of claim 8, which has the following form:


10. The compound according to claim 1, in which R5and R7both are halogen-free.

11. The connection of claim 10, in which R5and R7both are chlorine.

12. The compound according to claim 1, having antiamyloidogenic action for skin is ment as an active ingredient of a medicinal product.

13. The connection section 12, in which the drug can be used in amyloidogenic neurological disorders.

14. Drug, possess antiamyloidogenic effect, containing a therapeutically effective amount of the compounds of formula I according to claim 1 and a pharmaceutically or veterinary acceptable excipient.

15. The use of the compounds of formula I according to claim 1 for the manufacture of a medicinal product for the treatment of amyloidogenic neurological disorders.

16. The application indicated in paragraph 15, in which the compound of formula I is administered orally, topically or parenterally.

17. The compound of formula I according to claim 1 for use as a drug for inhibiting the toxicity of beta-amyloid protein.

18. The compound of formula I according to claim 1 for use as antiamyloidogenic agent.

19. The method of obtaining the compounds of formula I according to claim 1, containing the following:
(a) conducting a reaction of a protected or unprotected compounds of formula V

in which R5and R7meet the definition given in claim 1, with H2NR3where R3corresponds to the definition given in claim 1, with the formation of protected or unprotected compounds of formula VII

(b) reconnection VII with the formation of protected or unprotected compounds of formula VIII

cyclization of the compounds of formula VIII with the formation of protected or unprotected compounds of formula I in which R2represents N, and R5and R7meet the definition given in claim 1, with the removal of the protective groups as necessary at any stage; or
(d) cyclization of the compounds of formula VIII in the presence of R2CHO, R2CO2H, or R2C(ORX)3where RXis substituted or unsubstituted With1-4the alkyl, and R2corresponds to the definition given in claim 1, with the exception of hydrogen, with the formation of protected or unprotected compounds of formula I in which R2meet the definition given in claim 1, with the exception of N, and R5and R7meet the definition given in claim 1, with the removal of the protective groups as necessary at any stage.

20. The method of obtaining the compounds of formula I according to claim 1, where R2represents N, containing the following:
a) amination of the formamide protected or unprotected compounds of formula VI

in which R5and R7meet the definition given in claim 1, with the formation of protected or unprotected compounds of formula IX
;
b) conducting the reaction of compounds of formula IX br/> R3-L or R3OSO2RXwhere L is a leaving group, R3corresponds to the definition given in claim 1 and Rxcorresponds to the definition given in claim 19, with the removal of the protective groups as necessary at any stage.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention describes a compound of structural formula IIIm: or pharmaceutically acceptable salt thereof, where: R81 is selected from a group comprising hydrogen, halogen, possibly substituted C1-6alkyl, possibly substituted C2-6alkenyl, possibly substituted C2-6alkynyl, possibly substituted cycloalkyl, possibly substituted heterocycloalkyl, possibly substituted aryl, possibly substituted heteroaryl, -OH, -NH2, -CN, -NO2, -C(O)OH, -S(O)2NH2, -C(O)NH2, -C(S)NH2, -NHC(O)NH2, -NHC(S)NH2, -NHS(O)2NH2, -OR68, -SR68, -NR69R68, -C(O)R68, -C(S)R68, -C(O)OR68, -C(O)NR69R68, -C(S)NR69R68, -S(O)2NR69R68; -NR69C(O)R68, -NR69C(S)R68, -NR69S(O)2R68, -NR69C(O)NH2, -NR69C(O)NR69R68, -NR69C(S)NH2, -NR69C(S)NR69R68, -NR69S(O)2NH2, -NR69S(O)2NR69R68, -S(O)R68 and -S(O)2R68, R83 is selected from a group comprising hydrogen, fluro and chloro; R112 is selected from a group comprising possibly substituted C2-6alkyl, possibly substituted aryl, possibly substituted heteroaryl and -NR79 R80; R68 is selected from a group comprising possibly substituted C1-6alkyl, possibly substituted C2-6alkenyl, but provided that when R68 is possibly substituted C2-6alkenyl, then one of its alkene carbons is not bonded with N, S, O, S(O), S(O)2, C(O) or C(S) from -OR68, -SR68, -NR69R68, -C(O)R68, -C(S)R68, -C(O)OR68, -C(O)NR69R68, -C(S)NR69R68, -S(O)2NR69R68, -NR69C(O)R68, -NR69C(S)R68, -NR69S(O)2R68, -NR69C(O)NH2, -NR69C(O)NR69R68, -NR69C(S)NH2, -NR69C(S)NR69R68, -NR69S(O)2NH2, -NR69S(O)2NR69R68, -S(O)R68 or -S(O)2R68, possibly substituted C2-6alkynyl, but provided that when R68 is possibly substituted C2-6alkynyl, then one of its alkyne carbons is not bonded with N, S, O, S(O), S(O)2, C(O) or C(S) from -OR68, -SR68, -NR69R68, -C(O)R68, -C(S)R68, -C(O)OR68, -C(O)NR69R68, -C(S)NR69R68, -S(O)2NR69R68, -NR69C(O)R68, -NR69C(S)R68, -NR69S(O)2R68, -NR69C(O)NH2, -NR69C(O)NR69R68, -NR69C(S)NH2, -NR69C(S)NR69R68, -NR69S(O)2NH2, -NR69S(O)2NR69R68, -S(O)R68 or -S(O)2R68, possibly substituted cycloalkyl, possibly substituted heterocycloalkyl, possibly substituted aryl and possibly substituted heteroaryl; R69 is selected from a group comprising hydrogen and possibly substituted C1-6alkyl; and R79 and R80 independently denote hydrogen or possibly substituted C1-6alkyl or R79 and R80 together with the nitrogen atom to which they are bonded form a possibly substituted 5-7-member heterocycloalkyl. Described also is a composition and a set for modulating protein kinase based on said compounds and use of said compounds in preparing a medicinal agent.

EFFECT: novel compounds which are active towards protein kinase are obtained and described.

71 cl, 59 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to heterocyclic derivatives of general formula (I) where R1 denotes hydrogen, halogen, cyano, lower alkoxy or lower alkyl; R2 denotes aryl or a 5- or 6-member heteroaryl; R3 denotes hydrogen, aryl, a 5- or 6-member heteroaryl, where aryl, cycloalkyl, heterocycloalkyl or 5- or 6-member heteroaryl groups for R2 and R3 may be unsubstituted or substituted with halogen, cyano, lower alkyl, possibly substituted with one or more halogens, lower alkoxy, S(O)2-alkyl, -C(O)R', where R' is a lower alkyl, lower alkoxy; as well as pharmaceutically acceptable salts thereof. The invention also relates to a medicine based on said compounds for treating and preventing diseases mediated by the mGIuR5 receptor and use of compounds of formula (I) in preparing medicines.

EFFECT: novel compounds which are metabotropic glutamate receptor antagonists are obtained and described.

17 cl, 81 ex

FIELD: chemistry.

SUBSTANCE: invention relates to use of compounds, characterised by formulae (I) and (IB), or pharmaceutically acceptable salts thereof, isomers or hydrates to prepare a medicinal agent for treating or preventing diseases or conditions mediated by the sigma-receptor, selected from psychosis, neuropathic pain or inflammatory pain and movement disorder, such as dystonia or tardive dyskinesia, motor defects, including allodynia/or hyperalgesia. Radicals and symbols in compounds of formulae (I) and (IB) are described in claims 1 and 2. The invention also relates to novel compounds of formulae (I') and (IB'), in which radicals and symbols are described in claims 4 and 5, having pharmacological activity on the sigma-receptor, methods of producing such compounds, a pharmaceutical composition containing said compounds and use of said compounds in preparing a medicinal agent for treating and/or preventing diseases or conditions whose development involves the sigma-receptor. (I), (IB) (I') and (IB').

EFFECT: high effectiveness of the inhibitors.

22 cl, 1 tbl, 3 dwg, 64 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) where R1 is chosen from a group consisting of phenyl, unsubstituted or substituted by one or two groups independently chosen from (lower) alkyl, (lower) phenylalkyl wherein a phenyl ring can be unsubstituted or substituted by one or two groups independently chosen from halogen; R2 represents hydrogen; or R1 and R2 together with nitrogen atom whereto attached, form a saturated 5- or 6-members heterocyclic ring optionally containing an additional oxygen heteroatom, said saturated heterocyclic ring is unsubstituted or substituted by one, two or three groups independently chosen from (lower) alkyl, halogen; R3 is chosen from a group consisting of hydrogen, (lower) alkyl, (lower) hydroxyalkyl, (lower) alkoxyalkyl, (lower) haloalkyl, (lower) cycloalkylalkyl, (lower) cyanoalkyl, (lower) alkylsulfonyl, phenyl unsubstituted or substituted by one or two groups independently chosen from halogen; R4 represents hydrogen or halogen; R5 represents a group chosen from where m represents 0 or 1; n represents 0,1 or 2; X represents CR13R13'; R6, R6', R7, R7', R8,R8', R13, R13' are independently chosen from a group consisting of hydrogen, (lower) alkyl, halogen; p represents 0 or 1; R9 is chosen from (lower) alkyl, cycloalkyl, (lower) cycloalkylalkyl; q represents 0 or 1; R10 represents (lower) alkyl; and to their pharmaceutically acceptable salts, as well as to a pharmaceutical composition exhibiting histamine 3 receptor antagonistic and/or antagonistic activity and based on the compounds of formula I.

EFFECT: there are prepared and described new compounds which can be effective in treatment and/or prevention of the diseases associated with H3 receptor modulation.

24 cl, 34 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oxazolidinone derivatives covered by general graphic formula (I) and to their pharmaceutically acceptable salts. In formula (I) R1, R2, R3 and R4 are independently chosen from a group including -H and halogen; A is chosen from a group including R5 and R6 are independently chosen from a group including -H, -F, -CI, -Br, -OH, alkyl(C1-C6), haloalkyl(C1-C6), alkoxygroup(C1-C6); R7 is chosen from a group including -H, alkyl(C1-C6); either R7 and R5 or R6 taken together form a cycle of 2 carbon atoms and include 1 group chosen from O which in turn can be substituted by one substitute chosen from alkyl(C1-C6); R12 is chosen from a group including -H, -COR14, -CSR14, -COOR14; R14 is chosen from a group including alkyl (C1-C6), cycloalkyl(C3-C6), alkenyl(C2-C6), R16, R17 and R18 represent -H; R21 is chosen from a group including -H, alkyl(C1-C6); X is chosen from a group including O, S, and Y is chosen from a group including O, S, SO, SO2, and NR12; and optional substitutes of alkyl(C1-C6) groups can represent one or two groups chosen from the following: -OR21, -CN.

EFFECT: invention refers to methods for preparing the compounds of the invention, to application of oxazolidinone derivatives for preparing a drug for treating bacterial infections and to a pharmaceutical composition for treating bacterial infections, including a therapeutically effective amount of the compound of the invention.

36 cl, 10 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel imidazoquinoline derivatives or pharmaceutically acceptable salts thereof, tautomers thereof and pharmaceutically acceptable salts of tautomers, having general formula where R1 is -NR6R7, -(CH2)mCH=CH(CH2)nR9, -(CH2)mC=C(CH2)nR9 or -S(O)qR10; R2 is C1-6alkyl or C1-6alkyl which is substituted with one group selected from -OH and -OMe; each R4 and R5 is independently H, C6aryl-C1alkyl or a protective group; each of R6 and R7 is independently H, C1-6alkyl, C1-6alkyl which is substituted with one group selected from -OH and -OMe, C1-6alkoxy-C1-2alkyl or -(CH2)mCH=CH(CH2)nR9; each R9 is independently H, C1-6alkyl, or C6-10aryl; each R10 is independently C1-3alkyl or C6-10aryl-C1-6alkyl; each of m and n is independently equal to 0 or 1; and each q is independently equal to 0; provided that if R1 is -S-Me, R2 is isobutyl. The invention also relates to specific compounds, methods for synthesis of compounds of formulae and which are versions of formula I, a pharmaceutical composition based on formula I compounds and compositions based on formula I compounds and an additional immunogenic composition or antigen.

EFFECT: novel imidazoquinoline derivatives, which are suitable for modulating immune response in a subject, are obtained.

37 cl, 4 dwg, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to the following compounds: 4-[1-(2-chlorophenyl)-3-methyl-4-oxo-5-piperidin-1-yl-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]phenyl ether 3,3,3-trifluoropropane-1-sulphonic acid; 4-[1-(2,4-dichlorophenyl)-3-methyl-4-oxo-5-piperidin-1-yl-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]phenyl ether 3,3,3-trifluoropropane-1-sulphonic acid; 4-[1-(2-chloro-4-fluorophenyl)-3-methyl-4-oxo-5-piperidin-1 -yl-4,5,6,7-tetrahydro-1 H-pyrrolo[3,2-c]pyridin-2-yl] phenyl ether 3,3,3-trifluoropropane-1-sulphonic acid; 1-(2-chlorophenyl)-3-methyl-5-piperidin-1-yl-2-[4-(4,4,4-trifluorobutoxy)phenyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one; a pharmaceutical composition based on said compounds, having CB1(cannabinoid)-modulator activity, as well as use of said compounds in preparing a medicinal agent for treating diabetes or obesity.

EFFECT: possibility of using compounds in treating psychiatric and neurological disorders.

7 cl, 15 ex

FIELD: chemistry.

SUBSTANCE: compounds are suitable for use as kinase 1β-adrenergic receptor (βARK-1) inhibitors. The invention also relates to compositions containing such compounds and to use of compounds of formula to treat and prevent chronic heart failure, hypertension myocardial ischemia and hepatitis C viral infections (HCV) and for preventing opiate addiction. The invention also pertains to methods of producing formula (I) compounds.

EFFECT: more effective use of the compounds.

11 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described 3,4-substituted piperidines applicable in diagnostics and drug therapy of a warm-blooded animal, preferentially for therapy of a disease which depends on renin activity; application of a compound of such kind for preparing a pharmaceutical composition for therapy of the disease which depends on renin activity; application of the compound of such kind for therapy of the disease which depends on renin activity; the pharmaceutical compositions containing 3,4-substituted piperidine, and/or a therapeutic mode involving administration of 3,4-substituted piperidine, a method for producing 3,4-substituted piperidine. The preferential compound (which also can be presented in the form of salts) are described by formula I' wherein R1, R2, T, R3 and R4 are such as described by the patent claim.

EFFECT: production of the compounds for therapy of the disease which depends on renin activity.

28 cl, 1 tbl, 375 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to novel pyrazole derivatives of formula (I) or pharmaceutically acceptable salts thereof, having tyrosine kinase Trk inhibiting properties and used for treating or preventing malignant growths accompanied by high level of Trk, to a method of producing said derivatives, use thereof to prepare a medicinal agent, pharmaceutical compositions based on said derivatives, a method of inhibiting Trk activity and a method of obtaining antiproliferative action. where A denotes a single bond or C1-2alkylene; where the said C1-2alkylene can be optionally substituted with one R22; ring C is a phenyl or a 5-6-member heterocyclic ring with 1-2 heteroatoms selected from N or S. Values of R1-R7, R22 and n are given in the formula of invention.

EFFECT: obtaining pharmaceutically acceptable salts having tyrosine kinase Trk inhibiting properties and used for treating or preventing malignant growths.

20 cl, 5 dwg, 193 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I): where: A is a monocyclic or polycyclic aryl or heteroaryl group, where the heteroaryl radical denotes a 5-10-member cyclic system containing at least one heteroaromatic ring and containing at least one heteroatom selected from O, S and N; optionally substituted with one or more substitutes independently selected from a group comprising halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, C1-4alkoxy and a hydroxyl group; B is a monocyclic nitrogen-containing heteroaryl group, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from S and N; optionally substituted with one or more substitutes selected from a group consisting of halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, aryl and C1-8alkylthio; either a) R1 is a group of formula: -L-(CR'R")n-G, where L is a binding group selected from a group consisting of a direct bond, -(CO)-, -(CO)NR'- and -SO2-; R' and R" is independently selected from hydrogen atoms; n assumes values from 0 to 1; and G is selected from a group consisting of a hydrogen atom and C1-4alkyl, aryl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O, S and N; C3-8cycloalkyl and saturated heterocyclic groups, where heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one or two carbon atoms are substituted with a N heteroatom; where alkyl, C3-8cycloalkyl, aryl or heteroaryl groups are unsubstituted or substituted with one or more substitutes selected from halogen atoms; and R2 is a group selected from hydrogen atoms, halogen atoms and C1-4alkyl, C2-5alkynyl, C1-4alkoxy, -NH2 and cyano groups, where alkyl and alkynyl groups may be unsubstituted or substituted with one aryl group; or b) R2, R1 and -NH- group to which R1 is bonded form a group selected from groups of formulae and , where: Ra is selected from a hydrogen atom or groups selected from C1-4alkyl, C3-8cycloalkyl, aryl, aryl-C1-4alkyl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O and N; saturated heterocyclic rings, where the heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one carbon atom is substituted with a heteroatom selected from O and N; and C1-4alkylthio; where the aryl or heteroaryl groups are unsubstituted or substituted with one or more groups selected from halogen atoms, cyano group, trifluoromethoxy and carbamoyl; Rb denotes hydrogen; and pharmaceutically acceptable salts thereof and N-oxides; provided that the compound is not selected from N-[6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, and N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]formamide. The invention also relates to a pharmaceutical composition, use of compounds in any of claims 1-20, a method of treating a subject, as well as a composite product.

EFFECT: obtaining novel biologically active compounds having adenosine A2B receptor antagonist activity.

27 cl, 160 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted 2-quinolyloxazoles of formula (I) or pharmaceutically acceptable salts thereof, having PDE4 inhibiting properties, a pharmaceutical composition based on said compounds and use thereof to prepare a medicinal agent which inhibits inflammatory cell recruitment in respiratory tracts. , where is , X is O, R1 is alkyl, R3 and R4 are independently selected from H, R5 and R6 are independently selected from a group comprising H, alkyl, hydroxyalkyl, t equals 1 or 2. Values of substitutes R7-R11, R13 are given in the formula of invention.

EFFECT: high efficiency of using the composition.

24 cl, 1 dwg, 64 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oxazolidinone derivatives covered by general graphic formula (I) and to their pharmaceutically acceptable salts. In formula (I) R1, R2, R3 and R4 are independently chosen from a group including -H and halogen; A is chosen from a group including R5 and R6 are independently chosen from a group including -H, -F, -CI, -Br, -OH, alkyl(C1-C6), haloalkyl(C1-C6), alkoxygroup(C1-C6); R7 is chosen from a group including -H, alkyl(C1-C6); either R7 and R5 or R6 taken together form a cycle of 2 carbon atoms and include 1 group chosen from O which in turn can be substituted by one substitute chosen from alkyl(C1-C6); R12 is chosen from a group including -H, -COR14, -CSR14, -COOR14; R14 is chosen from a group including alkyl (C1-C6), cycloalkyl(C3-C6), alkenyl(C2-C6), R16, R17 and R18 represent -H; R21 is chosen from a group including -H, alkyl(C1-C6); X is chosen from a group including O, S, and Y is chosen from a group including O, S, SO, SO2, and NR12; and optional substitutes of alkyl(C1-C6) groups can represent one or two groups chosen from the following: -OR21, -CN.

EFFECT: invention refers to methods for preparing the compounds of the invention, to application of oxazolidinone derivatives for preparing a drug for treating bacterial infections and to a pharmaceutical composition for treating bacterial infections, including a therapeutically effective amount of the compound of the invention.

36 cl, 10 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates or tautomers thereof, where substitute M is selected from groups D1 and D2, having structural formulae given below, and R1, E, A and X are as described in the formula of invention. Disclosed also are pharmaceutical compositions which contain these compounds, methods for synthesis of these compounds, intermediate compounds and synthesis methods thereof, as well as use of compounds of formula (I) in preventing or treating diseases mediated by CDK kinases, GSK-3 kinases or Aurora kinases.

EFFECT: high effectiveness of the compounds.

40 cl, 8 dwg, 18 tbl, 84 ex

Aromatic compound // 2416608

FIELD: chemistry.

SUBSTANCE: invention describes a novel compound of general formula (1), where radicals R1, R2, X1, Y and A are as described in claim 1 of the invention. The invention also describes a method of obtaining compounds of formula (1), as well as a pharmaceutical composition based on said compounds, for treating fibrosis.

EFFECT: novel compounds with excellent collagen formation suppression, cause fewer side-effects and which are safer are obtained.

62 cl, 2717 ex, 432 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: compound of formula pharmaceutically acceptable salt or solvate of a compound or salt (I), ring Q represents optionally substituted monocyclic or condensed (C6-C12)aryl or optionally substituted monocyclic or condensed heteroaryl where said substitutes are chosen from: halogen; (C1-C6)alkyl optionally substituted by 1-3 halogen atoms; (C1-C6)alkylsulphonyl; phenyl optionally substituted by 1 or 2 substitutes chosen from halogen, (C1-C6)alkyl which can be substituted by 1-3 halogen atoms, groups (C1-C6)alkylamino, di(C1-C6)alkylamino, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and (C1-C6)alkylthio; monocyclic or condensed heteroaryl optionally substituted by halogen; or oxo; Y1 represents a bond or -NR6-CO-, where R6 represents hydrogen, ring A represents optionally substituted a nonaromatic heterocyclyldiyl where said substitutes are chosen from (C1-C6)alkyl optionally substituted by groups hydroxy, (C1-C6)alkylamino, di(C1-C6)alkylamino, morpholino, (C1-C6)alkylaminocarbonyl, di(C1-C6)alkylaminocarbonyl; cyano; (C3-C6)cycloalkyl; (C1-C6)alkoxy; (C1-C6)alkoxy(C1-C6)alkyl; phenyl; benzyl; benzyloxymethyl; thienyl; 4-8-members monocyclic nonaromatic heterocycle having 1 or 2 heteroatoms chosen from N or O, and optionally substituted by 1 or 2 substitutes chosen from (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and oxo; (C1-C6)alkylamino; di(C1-C6)alkylamino; a group of formula: -Y2Z'- represents a group of formula: [Formula 2] each R7 independently represents hydrogen, (C1-C6)alkyl or (C3-C6)cycloalkyl, each of R8 and R9 independently represents hydrogen or (C1-C6)alkyl, n is equal to an integer 0 to 3, Z1 represents a bond, -O-, -S- or-NR9 - where R9 represents hydrogen, (C1-C6)alkyl, acyl or (C1-C6)alkylsulphonyl, ring B represents optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl where said substitutes are chosen from (C1-C6)alkyl, halogen, (C1-C6)alkoxy and oxo; Y3 represents a bond optionally substituted (C1-C6)alkylene or (C3-C6)cycloalylene, optionally interrupted -O- or optionally substituted (C2-C6)alkenylene where said substitutes are chosen from (C1-C6)alkyl, (C3-C6)cycloalkyl, halogen and (C1-C6)alkoxycarbonyl; Z2 represents COOR3; R3 represents hydrogen or (C1-C6)alkyl.

EFFECT: preparation of new compounds.

30 cl, 9 tbl, 944 ex

FIELD: medicine.

SUBSTANCE: invention refers to the compound 3-{[5-(azetidine-1-ylcarbonyl)pyrazine-2-yl] oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazine-5-yl)benzamide or to its pharmaceutically acceptable salt. Also, it refers to a pharmaceutical composition for treating insulin-independent diabetes or obesity containing said compound.

EFFECT: there is produced and described a new compound which can be effective in treating insulin-independent diabetes and obesity.

5 cl, 64 ex

FIELD: chemistry.

SUBSTANCE: invention relates to oxazolidinone derivatives of formula (I) or pharmaceutically acceptable salts thereof, synthesis method thereof and pharmaceutical compositions containing said derivatives which are used as an antibiotic. Oxazolidinone derivatives, where R1 and R1' independently denote hydrogen or fluorine; R2 denotes -OR7, fluorine, monophosphate or metal phosphate; and R7 denotes hydrogen, C1-3alkyl or an acylated amino acid group, where the amino acid is alanine, glycine, proline, proline, isoleucine, leucine, phenylalanine, β-alanine or valine; R3 denotes hydrogen, a C1-4alkyl group which is unsubstituted or substituted cyano, , -(CH2)m-OR7 (m equals 0, 1, 2, 3, 4) or a ketone group. Oxazolidinone derivatives of formula (I) have antibacterial activity against different human and animal pathogens.

EFFECT: oxazolidinone derivatives, having inhibiting activity towards a wide range of bacteria and having low toxicity.

27 cl, 4 tbl, 73 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new pyrrolidine derivatives of general formula (1) or its pharmaceutically acceptable salts where R101 and R102 values are described by the patent claim. The compounds inhibit serotonin and/or norepinephrine and/or dopamine reabsorption thereby allowing to be used for treating depression and anxiety disorder. A method for preparing thereof is described.

EFFECT: preparation of new pyrrolidine derivatives.

10 cl, 162 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of formula I and to their pharmaceutically acceptable salts. In formula I p is integer, equal to 0-1; L2 is selected from group including -XOX-, -XSX- and -XSXO-; where X is independently selected from group, including bond and C1-C4alkylene; R13 is selected from group, including halogen, C1-C6alkyl, C1-C6alkoxygroup, -C(O) C1-C6alkyl; R14 is selected from group, including -XOXC(O)OR17 and -C1-C4alkylene-C(O)OR17; where X represents bond or C1-C4alkylene; and R17 is selected from group, including hydrogen and C1-C6alkyl; R15 and R16 are independently selected from group, including -R18 and -YR18; where Y represents C2-C6alkenylene, and R18 is selected from group, including C6-C10aryl, benzo[1,3]dioxolyl, pyridinyl, pyrimidinyl, quinolyl, phenoxatiinyl, benzofuranyl, dibenzofuranyl, benzoxasolyl, 2,3-dihydrobenzofuranyl, 2-oxo-2,3-dihydrobenzooxasolyl, indolyl, 3-oxo-3,4-dihydro-2H-benzo[1,4]oxazinyl, 2,3-dihydrobenzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, where any C6-C10aryl, pyridinyl, benzoxasolyl, indolyl in R18 is optionally substituted by 1-2 radicals, independently selected from group, including halogen, nitrogroup, cyanogroup, C1-C6alkyl, C1-C6alkoxygroup, C1-C6alkylthiogroup, hydroxy-C1-C6alkyl, halogen-substituted C1-C6alkyl, halogen-substituted C1-C6alkoxygroup, piperidinyl, morpholinyl, pyrrolidinyl, phenyl, XS(O)0-2R17, -XNR17R17, -XNR17S(O)2R17, -XNR17C(O)R17, -XC(O)NR17R17, -XC(O)NR17R19, -XC(O)R17, -XC(O)R19 and -XOXR19, where X represents bond; R17 is selected from group, including hydrogen, C1-C6alkyl, halogen-substituted C1-C6alkyl, and R19 is selected from group, including C3-C12cycloalkyl, phenyl, piperidinyl, morpholinyl.

EFFECT: ensuring application of invention compounds for production of medication, modulating activity of activated receptors of peroxisome proliferators δ (ARPPδ), to pharmaceutical composition, possessing properties of ARPPδ activity modulator, including therapeutically efficient quantity of invention compound and to application of pharmaceutical composition for medication manufacturing.

8 cl, 1 tbl, 301 ex

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, and concerns a EP2 agonist which exhibits the EP3 agonist action, and induce a neurotising and/or protective effect and thereby is effective as a therapeutic agent for a peripheral nerve disease, such as lower and upper motor neuron disorder, nerve root disease, plexopathy, brachial plexus compression syndrome, peripheral neuropathy, neurofibromatosis and nervomuscular conduction disease.

EFFECT: EP2 agonist which exhibits the EP3 agonist action; it is a safe and effective neurotisation and/or protection agent which has an insignificant impact on the cardiovascular system.

13 cl, 36 ex, 1 tbl

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