Condensed bicyclic compound

FIELD: medicine.

SUBSTANCE: invention relates to condensed bicyclic compounds, having affinity with mineralocorticoid receptor (VR) of formula [I] and formula [ii], as well as to pharmaceutical compositions on their basis. In general formula [I[ and [ii] ring A represents benzene ring, which has substituent R1, condensed with adjacent 6-membered heterocyclic ring, and said benzene ring additionally optionally is substituted with one or two substituent(s), selected from halogen atom and C1-8-alkyl group, R1 represents C1-8-alkylsulfonyl amino group or C1-8-alkyl aminosulfonyl group, R2 and R3 (a) are similar or different and represent group, selected from hydrogen atom, C1-8-alkyl group, and from 6- to 10-membered monocyclic or bicyclic aryl group (said aryl group is optionally substituted with halogen atom), (b) are combined with each other with formation of oxogroup or (c) are combined with each other on their ends together with adjacent carbon atom with formation of C3-10-cycloalkyl group, X represents the following group =N-, =C(R4)- or -CH(R4)-, R4 represents hydrogen atom, cyanogroup, halogen atom, C1-6-alkyl group, C2-6-alkenyl group, C3-10-dicloalkyl group, C1-7-alkanoyl group, carbamoyl group or C3-8cycloalkenyl group, Ar represents from 6- to 10-membered monocyclic or bicyclic aryl group, optionally containing one or several heteroatom(s), selected from sulphur atom, oxygen atom and nitrogen atom (said aryl group is optionally substituted with similar or different, one or two substituent(s), selected from halogen atom, cyanogroup, C1-8-alkyl group, trihalogen- C1-8-alkyl group and C1-8alkoxygroup), and dotted line represents presence or absence of double bond, Xa represents the following group =N- or =C(CN)-, RZ represents hydrogen atom or halogen atom, R25 and R35 represent alkyl group, and Ar3 represents phenyl group, optionally substituted with one or two group(s), which is(are) selected from halogen atom and trihalogenalkyl group.

EFFECT: compounds can be applied as antihypertensive medication.

15 cl, 18 tbl, 8 dwg, 71 ex

 

The text descriptions are given in facsimile form.

1. Condensed bicyclic compound of the formula [1]:

in which ring A represents a benzene ring having a substituent R1condensed with an adjacent 6-membered heterocyclic ring, and the indicated benzene ring optionally optionally substituted by one or two substituent(s)selected(and) from a halogen atom and C1-8is an alkyl group,
R1represents a C1-8-alkylsulfonamides or C1-8alkylaminocarbonyl group,
R2and R3(a) the same or different and represent a group selected from a hydrogen atom, a C1-8is an alkyl group and from 6 - to 10-membered monocyclic or bicyclic aryl group (specified aryl group optionally is Emesene a halogen atom), (b) United with one another with formation of a carbonyl group, or (c) combined with each other at their ends together with the adjacent carbon atom with the formation of C3-10-cycloalkyl group,
X represents the following group =N-, =C(R4)- or-CH(R4)-,
R4represents a hydrogen atom, a cyano, a halogen atom,
C1-6is an alkyl group, a C2-6-alkenylphenol group, C3-10-cycloalkyl group,
C1-7-alkanoyloxy group, carbamoyl group or a C3-8cycloalkenyl group,
Ar represents a 6 - to 10-membered monocyclic or bicyclic aryl group optionally containing one or more heteroatom(s)selected(s) from sulfur atom, oxygen atom and nitrogen atom (this aryl group optionally substituted by the same or different, one or two substituent(s)selected(s) from a halogen atom, ceanography, C1-8is an alkyl group, trihalogen-C1-8is an alkyl group and C1-8alkoxygroup), and
the dotted line means the presence or absence of a double bond, or its pharmaceutically acceptable salt.

2. The compound according to claim 1, in which R1attached in position 5, 6 or 7 below, the structure of the condensed rings of the General formula [1]:
.

3. Condensed bellicheck the e compound of General formula [I-A]:

in which ring A represents a benzene ring having a substituent R11condensed with an adjacent 6-membered heterocyclic ring, and the indicated benzene ring optionally optionally substituted by one or two substituent(s)selected(and) from a halogen atom and C1-8is an alkyl group,
R11represents a C1-8-alkylsulfonamides or
C1-8-alkylaminocarbonyl group,
R21and R31the same or different, and represent a group selected from (a) hydrogen atom, (b) C1-8is an alkyl group, and (c) from 6 - to 10-membered monocyclic or bicyclic aryl group (this aryl group is optionally substituted by halogen atom), and
Ar1represents a 6 - to 10-membered monocyclic or bicyclic aryl group optionally containing one or more heteroatom(s)selected(s) from sulfur atom, oxygen atom and nitrogen atom (this aryl group optionally substituted by the same or different, one or two substituent(s)selected(s) from a halogen atom, ceanography, C1-8is an alkyl group, trihalogen-C1-8is an alkyl group and C1-8alkoxygroup),
or its pharmaceutically acceptable salt.

4. The compound according to claim 3 in which R11when is outinen in position 7 below, the structure of the condensed rings of the General formula [I-A]:
.

5. Condensed bicyclic compound of the formula [I-B]:

in which ring A represents a benzene ring having a substituent R12condensed with an adjacent 6-membered heterocyclic ring, and the indicated benzene ring optionally optionally substituted by one or two substituent(s)selected(and) from a halogen atom and C1-8is an alkyl group,
R12represents a C1-8-alkylsulfonamides or
C1-8-alkylaminocarbonyl group,
R22and R32(a) the same or different and represent a group selected from a hydrogen atom, a C1-8is an alkyl group, (b) combined with each other with the formation of the carbonyl group, or (c) combined with each other at their ends together with the adjacent carbon atom with the formation of C3-10-cycloalkyl group, and
R41represents a hydrogen atom, a cyano, a halogen atom,
C1-6is an alkyl group, a C2-6-alkenylphenol group, C3-10-cycloalkyl group,
C1-7-alkanoyloxy group, carbamoyl group or a C3-8cycloalkenyl group,
Ar2represents a 6 - to 10-membered monocyclic or bicyclic aryl group optionally containing one or more heteroatom(s), you the security(s) from a sulfur atom, oxygen atom and a nitrogen atom (this aryl group optionally substituted by the same or different, one or two substituent(s)selected(s) from a halogen atom, ceanography, C1-8is an alkyl group, trihalogen-C1-8is an alkyl group and C1-8alkoxygroup), and
the dotted line means the presence or absence of a double bond,
or its pharmaceutically acceptable salt.

6. The compound according to claim 5, in which R12attached in position 7 below, the structure of the condensed rings of the General formula [I-B]:

7. The compound of General formula [I-A-a]:

in which R11represents a C1-6-alkylsulfonamides or
C1-6-alkylaminocarbonyl group,
RArepresents a hydrogen atom, halogen atom or C1-6is an alkyl group, one of R23and R33represents a hydrogen atom or a C1-6is an alkyl group and the other represents C1-6is an alkyl group or phenyl group,
Ar11represents a 5 - to 10-membered monocyclic or bicyclic aromatic group (specified cyclic group may contain a heteroatom chosen from sulfur atom and oxygen atom)where the specified aromatic cyclic group optionally replace the s with one or two substituent(s), the selected(s) from a halogen atom, ceanography, C1-6is an alkyl group, trihalogen-C1-6is an alkyl group and C1-6alkoxygroup,
or its pharmaceutically acceptable salt.

8. The compound of General formula [I-b]:

in which R12represents a C1-6-alkylsulfonamides or
C1-6-alkylaminocarbonyl group,
RB, RB2and RB3represent identical or different groups selected from hydrogen atom, halogen atom, and C1-6is an alkyl group,
R24and R34(a) the same or different and represent a hydrogen atom or
C1-6is an alkyl group, (b) combined with each other at their ends together with the adjacent carbon atom with the formation of C3-10-cycloalkyl group, or (c) combined with each other with the formation of the carbonyl group,
R41represents (a) hydrogen atom, (b) cyano, (c) halogen atom, (d) C1-6is an alkyl group, (e) C2-6-alkenylphenol group, (f) C3-10-cycloalkyl group, (g) C2-6-alkanoyloxy group, (h) karbamoilnuyu group or (i)
C3-8-cycloalkenyl group,
Ar21represents a 6-membered aromatic cyclic group, optionally substituted by one or two group(s)selected(s) from a halogen atom, a C1-6-alkyl gr is PPI and trihalogen-C 1-6is an alkyl group (specified cyclic group can contain one or two nitrogen atom as a heteroatom), and the dotted line means the presence or absence of a double bond, or its pharmaceutically acceptable salt.

9. The connection according to claim 7, in which R11represents a
C1-6-alkylsulfonamides,
RArepresents a hydrogen atom, halogen atom or C1-6is an alkyl group, one of R23and R33represents a hydrogen atom or a C1-6is an alkyl group and the other represents C1-6is an alkyl group,
Ar11represents a phenyl group, optionally substituted by one or two group(s), vybranou(s) from a halogen atom and C1-6is an alkyl group.

10. The connection of claim 8, in which R12represents a
C1-6-alkylsulfonamides,
RBrepresents a hydrogen atom or a C1-6is an alkyl group,
RB2and RB3represent a hydrogen atom,
R24and R34the same or different, and represent
C1-6is an alkyl group,
R41represents a hydrogen atom, cyano group, halogen atom or C1-6is an alkyl group,
Ar21represents a phenyl group, optionally substituted by one or two group(s), vybranou(s) and is of a halogen atom, C1-6is an alkyl group and trihalogen-C1-6is an alkyl group.

11. Compound which is selected from the group consisting of:
N-[4-(4-chlorophenyl)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]methanesulfonamide;
N-[4-(4-chloro-2-were)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[4-(4-forfinal)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[4-(4-fluoro-2-were)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]methanesulfonamide;
N-[4-(4-chloro-3-were)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[4-(4-chloro-3-forfinal)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[4-(4-fluoro-3-were)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[4-(4-chloro-2-forfinal)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[5-chloro-4-(4-forfinal)-2,2-dimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[2,2-diethyl-4-(4-forfinal)-2H-1,3-benzoxazin-7-yl]-methanesulfonamide;
N-[2-ethyl-4-(4-forfinal)-2-methyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide; and
N-[4-(4-forfinal)-2,2,5-trimethyl-2H-1,3-benzoxazin-7-yl]-methanesulfonamide,
or its pharmaceutically acceptable salt.

12. Compound which is selected from the group consisting of:
N-[4-(4-forfinal)-2,2,3-trimethyl-2H-chromen-7-yl]methanesulfonamide;
N-[3-cyano-4-(4-forfinal)-2,2-dimethyl-2H-chromen-7-yl]-methanesulfonamide;
N-[3-fluoro-4-(4-forfinal)-2,2-dimethyl-2H-chromen-7-yl]-methanesulfonamide;
N - [4-(4-forfinal)-2,2-dimethyl-3,4-dihydro-2H-chromen-7-yl]-methanesulfonamide;
N-[4-(4-chloro-2-were)-2,2-dimethyl-2H-chromen-7-yl]-methanesulfonamide;
N-[3-cyano-4-(4-forfinal)-2,2-diethyl-2H-chromen-7-yl]-methanesulfonamide;
N-[3-cyano-2,2-dimethyl-4-phenyl-2H-chromen-7-yl]methanesulfonamide;
N-[4-(4-chlorophenyl)-3-cyano-2,2-dimethyl-2H-chromen-7-yl]-methanesulfonamide;
N-[4-(4-chloro-3-were)-3-cyano-2,2-dimethyl-2H-chromen-7-yl]-methanesulfonamide;
N-[4-(4-chloro-3-forfinal)-3-cyano-2,2-dimethyl-2H-chromen-7-yl]-methanesulfonamide;
N-[4-(4-forfinal)-2,2,5-trimethyl-2H-chromen-7-yl]methanesulfonamide; and
N-[3-cyano-4-(4-forfinal)-2,2,5-trimethyl-2H-chromen-7-yl]-methanesulfonamide
or its pharmaceutically acceptable salt.

13. The compound of General formula [ii]:

in which Xarepresents the following group =N - or =C(CN)-,
Rzrepresents a hydrogen atom or halogen atom,
R25and R35represent an alkyl group, and
Ar3represents a phenyl group, optionally substituted by one or two group(s), contractor(s) selected from a halogen atom and trihalogenmethanes group, or its pharmaceutically acceptable salt.

14. Pharmaceutical composition comprising a compound according to any one of claims 1 to 12 or its pharmaceutically acceptable salt as an active ingredient, which is a receptor antagonist mineralocorticoids.

15. The pharmacy is practical composition, including the connection 13 or its pharmaceutically acceptable salt as an active ingredient, which is a receptor antagonist of mineralocorticoids.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of dihydroquinone and dihydronaphthyridinone of formula (I) or to its pharmaceutically acceptable salts, in which X represents group CR11 or N; Y represents group -C(O)R3, oxazolyl or isoxazolyl; Z represents phenyl, pyrrolidinyl, piperidinyl, morpholinyl, tetrahydropyranyl, pyridinyl, pyrimidinyl or pyrazolyl, and is substituted with groups R1 and R2; R1 and R2 each independently represents H, halogen, CN group, C1-6alkyl or group -Y1-Y2-Y3-R8, or R1 and R2 together form group -O(CH2)nO-, where n represents 1 or 2; Y1 represents group -O-, -C(O)-, -C(O)O-, -C(O)NR9-, -NR9C(O), -S-, -SO2- or bond; Y2 represents heterocycloalkylene, C1-6alkylene or bond, where heterocycloalkylene stands for cycloalkylene group, in which one, two carbon atoms are substituted with heteroatoms O or N, where heterocycloalkylene group also contains, at least, two carbon atoms and cycloalkylene represents ; Y3 represents group -O-, -C(O)-, -C(O)O-, -C(O)NR9-, -NR9C(O)-, -SO2- or bond; R8 represents H, C1-6alkyl, C1-6alkoxy, cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, tetrahydropyranyl, or group -NR9R10, where R8, different from H, is optionally substituted with C1-6alkyl, halogen, group -CF3 or group -OH; R9 and R10 each independently represents H or C1-6alkyl; R3 represents OH, C1-6alkyl, C1-6alkoxy, (C1-6alkoxy)-C1-6alkoxy; R4 represents C1-6alkyl, phenyl, cyclopropyl, cyclobutyl, cyclobutyl, cyclohexyl, tetrahydropyranyl or tetrahydrothiophene 1,1 -dioxide, and is optionally substituted with C1-6alkyl, hydroxyl group, C1-6alkoxy, halogen, nitro group, amino group, cyano group or halo-lower alkyl; R5 and R6 each independently represents H, halogen, C1-6alkyl, group -CF3, C1-6alkoxy; R7 represents H; R11 represents H. Invention also re4lates to pharmaceutical composition based on formula (I) compound.

EFFECT: obtained are novel dihydroquinone and dihydronaphthyridinone derivatives, useful for treatment of disease mediated by JNK kinase.

9 cl, 4 tbl, 38 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula , where A, Q, R1, R2, R3, R4, R5' are represented in i.1 of the formula, as well as to its hydrates, solvates and pharmaceutically acceptable salts, Also described are application of said compound and pharmaceutical composition, including such compound, for treatment of disease condition in mammals, which is sensitive to action of antagonists of vasopressin V1a, V1b or V2 receptors.

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20 cl, 13 ex, 1 dwg

FIELD: medicine.

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8 cl, 4 tbl, 3 dwg, 7 ex

FIELD: medicine, pharmaceutics.

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10 cl, 9 ex, 17 tbl

FIELD: medicine, pharmaceutics.

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EFFECT: compounds show Hsp90 inhibitory activity that enables using them for treating the diseases caused by abnormal cell growth in mammals.

26 cl, 8 dwg, 2 tbl, 82 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pyridine-3-yl derivatives of formula (I)

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EFFECT: there are produced and described new compounds which are especially active as immunomodulatory agents.

18 cl, 92 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I):

, where: R=NO2, or and Het denotes an azolyl radical selected from nitroazolyl and tetrazolyl radicals; except 3- and nitro-4-(4-nitro-1,2,3-triazol-1-yl)furazan. The invention also describes a method of producing a compound of formula I and an energy composition based on said compounds.

EFFECT: compounds have high energy characteristics, low sensitivity and high thermal stability.

11 cl, 7 ex, 3 tbl, 2 dwg

FIELD: chemistry.

SUBSTANCE: invention describes isoxazolines of formula (I), in which A denotes C or N; R denotes C1-4 haloalkyl; X denotes identical or different halogens or C1-4 haloalkyl; l equals 0, 1 or 2; Y denotes halogen or C1-4 alkyl, C1-4alkoxy, C1-4haloalkyl, cyano, nitro, amino, C1-4 alkylcarbonylamino, benzoylamino or C1-4 alkoxycarbonylamino; m equals 1 or 1; and G denotes any group selected from heterocyclic groups given in the description, and a method of producing said compounds and use as insecticides for controlling the population of harmful insects or arthropods.

EFFECT: high efficiency of using said compounds.

11 cl, 28 ex, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a compound with formula (I): where the values of radicals Q, R1, R2, R3, R4, X and Y are as specified in Clause 1 of the patent claim or to a pharmaceutically acceptable salt of such compound or a compound ether hydrolysed in vivo provided such compound is not: {(3S)-1-[5-(adamantan-1-ylcarbamoyl)pyridine-2-yl] piperidine-3-yl} acetic acid or {(3S)-1-[5-(cyclohexylcarbamoyl)-6-(piperazine-1-yl) pyridine-2-yl] piperidine-3-yl} acetic acid or a pharmaceutically acceptable salt thereof or a compound ether hydrolysed in vivo. Additionally, the invention relates to a pharmaceutical composition containing a compound with formula I for treatment of metabolic syndrome, Type II diabetes, adiposity etc and to application of such compound with formula I for manufacture of a medication to be applied for causing an inhibition effect with regard to 11βHSD1 with a homoiothermal animal.

EFFECT: produced and described is a new compound possessing inhibition activity with regard to Type 1 human 11-β-hydroxisteroiddehydrohenase enzyme (11βHSD1).

15 cl, 187 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: this invention relates to new compounds with formula (I) possessing the properties of mGLuR2 antagonists, to their obtainment methods, their application for production of medicines for prevention and treatment of disorders wherein mGLuR2 plays the activation role (in particular - central nervous system disorders). In formula (I) either any of X and Y represents N while the other represents CH or each of X and Y represents N; A represents aryl representing phenyl or 5- or 6-membered heteroaryl containing in the cycle 1-3 atoms selected from among nitrogen, oxygen or sulphur, the heteroaryl selected from among amidazolyl, [1,2,4] oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4] triazolyl, tiazolyl and pyrimidinyl, each of them substitutable by C1-6-alkyl; B represents H, cyano or represents a possibly substituted aryl selected from among phenyl or possibly substituted by 5- or 6-membered heteroaryl containing in the cycle 1-3 atoms selected from among nitrogen, oxygen or sulphur where the substitutes are selected from the group consisting of nitro, C1-6-alkyl, possibly substituted hydroxy, NRaRb where Ra and Rb independently represent H, C1-6-alkyl etc. R1 represents H, a halogen atom, C1-6-alkyl, possibly substituted hydroxy, C1-6-alcoxy, C1-6-halogenoalkyl, C3-6-cycloalkyl represents H cyano, a halogen atom, C1-6-halogenoalkyl, C1-6-alcoxy, C1-6-halogenoalcoxi-, C1-6-alkyl or C3-6-cycloalkyl R3 represents a halogen atom, H, C1-6-alcoxy, C1-6-halogenoalkyl, C1-6-alkyl, C3-6-cycloalkyl, C1-6-halogenoalcoxy R4 reprsents H or halogeno.

EFFECT: creation of new compounds of formula (I) possessing mGLuR2 antagonist properties.

104 cl, 465 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: in the given invention, there is offered a method for preparing a compound of formula , where Y is specified of CH3, CH2OH, CH2CH2OH, CH2Br and Br; involving the stages: (1) reaction of the compound of formula where OX represents hydroxy or O-M+ where M+ represents cation chosen of Li+, Na+ and K+ and Y is such as specified above; with trans-cynnamaldehyde , with a secondary amine compound added; then (2) acid treatment of a product from the previous stage to prepare a compound of formula (I). The aforesaid method can be used for preparing tolterodine and fezoterodine which are effective in treating the hyperactive urinary bladder. There are also declared compounds of formulae V, VI and VII.

EFFECT: development of the effective method for preparing the compound.

25 cl, 19 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel chromane derivatives of formula I: or their pharmaceutically acceptable salts, where: m equals 0 or 1; p equals 2; q equals 2; Ar is phenyl which is possibly substituted with a halogen atom; each R1 is independently a halogen; R2 is ; n equals 1 or 2; each of R3 and R4 is independently hydrogen or C1-12-alkyl; each of R5 and R6 is independently hydrogen or C1-12-alkyl; and each of R7 and R8 is independently hydrogen or C1-12-alkyl; or one of R7 and R8 is hydrogen and the other is a 5- or 6-member heterocyclyl containing one nitrogen atom, or R7 and R8 together with the nitrogen atom with which they are bonded can form an amidinyl group, a urea group, a guanidinyl group or a pyrrolidine ring which is possibly substituted with an amine group.

EFFECT: obtaining novel chromane derivatives and pharmaceutical compositions having 5-HT6 and/or 5-HT2a receptor modulator activity.

22 cl, 11 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention refers to novel method of obtaining [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyrane-2-methanol] racemate of the formula (I) (nebivolol) and its pharmaceutically acceptable salts , involving stages indicated in the claim, and to intermediate compounds and methods of obtainment thereof.

EFFECT: improved method.

106 cl, 12 tbl, 20 ex

FIELD: chemistry.

SUBSTANCE: invention refers to novel aminoalkyl-and amodialkylbenzopyran derivatives of the general formula (I): (a), where (a) group is a substitute in 6 or 7 position, where R is mono- or bicyclic (C6-C10)-aryl radical optionally substituted with one or two substitutes selected out of linear or ramified (C1-C5)-alkyls, linear or ramified (C1-C5)-alkoxy, hydroxy, halogen and trifluoromethyl; m is zero or integer 1-3; n, p, R1 and R2 are as indicated in the description, and both R3 and R4 are hydrogen or both are oxygen: and to pharmaceutically acceptable salts thereof.

EFFECT: selective reversible MAO-B inhibitors in vitro and in vivo, applicable as medicines for prevention and treatment of degenerative central nervous system disorders.

13 cl, 24 ex

FIELD: chemistry.

SUBSTANCE: invention relates to an improved method of producing 2H-1-benzopyran-2-methanol-α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-[2R*[R*[R*(S*)]]]], i.e. a nebivolol base of formula (IX), or its hydrochloride salt

as well as to a method of producing an intermediate compound - benzylated nebivolol of formula (VIII),

EFFECT: invention also relates to a pharmaceutical composition with antihypertensive action without using a wetting agent, and to a tablet containing this pharmaceutical composition.

21 cl, 20 tbl, 21 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of derivative of aminobenzopyrane of the formula (2): Method involves reduction of nitro-group in derivative of 2,2-dimethyl-2H-1-benzopyrane of the formula (1): with hydrazine in the presence of a metallic catalyst. Invention provides high selectivity of the process with respect to olefin bonds and simple treatment that results to small waste and doesn't effect on reactor.

EFFECT: improved method of synthesis.

2 tbl

FIELD: organic chemistry, heterocyclic compounds, medicine, pharmacy.

SUBSTANCE: invention relates to new biologically active heterocyclic retinoid compounds. Invention describes retinoid compounds corresponding to the formula (I): or their pharmaceutically acceptable salts, solvates or hydrates wherein n means a whole number from 0 to 2; A represents optionally substituted phenyl; B represents oxygen (O), sulfur (S) atom or -NR6 wherein R6 represents hydrogen atom or alkyl; Y represents -OR7 wherein R7 represents hydrogen atom, alkyl, optionally substituted phenyl, aralkyl wherein aryl fragment means optionally substituted phenyl, cycloalkyl or cycloalkylalkyl; Z represents -C(R101)2-, -R102C=CR102-, -C≡C-, -C(R103)2S-, -C(O)O- or -C(O)NR10- wherein each among R10, R101, R102 and R103 represents independently hydrogen atom or alkyl; R1 and R2 represent independently hydrogen atom or alkyl; R3 represents hydrogen atom or alkyl; R4 and R5 represent independently hydrogen atom, (C1-C8)-alkyl or arylalkyl wherein aryl fragment means optionally substituted phenyl. Also, invention describes methods for preparing retinoid compounds, a pharmaceutical composition based on thereof and a method for treatment and/or prophylaxis of respiratory ways obstructive disease, cancer or dermatological disturbance or disorder. Invention provides preparing new compounds possessing useful biological properties.

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

28 cl, 10 tbl, 16 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention concerns to applying RARγ agonist for preparing a medicinal agent comprising one or some such agonists and designated for treatment of emphysema wherein RARγ agonist is taken among compounds of the formula (I):

wherein R1 means residue of the formula:

or , or , or ; R2 means (C2-C8)-alkanoyl, (C2-C8)-alkyl, (C2-C8)-alkenyl, (C2-C8)-alkynyl or group -OCH2R3 wherein R3 means hydrogen atom, (C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-alkynyl; each among R4-R9 means independently of one another hydrogen atom or (C1-C6)-alkyl; or R8 and R9 mean in common (CRaRb)n wherein Ra and Rb mean independently of one another hydrogen atom or (C1-C6)-alkyl; n = 1, 2 or 3; R4-R7 have above given values; R10 means carboxyl, (C1-C6)-alkoxycarbonyl or mono- or di-(C1-C6)-alkylcarbamoyl; and their pharmaceutically acceptable salts; or among compounds of the formula (VI):

wherein R1 means C(O)R6 or CH2OH (wherein R6 means hydroxy-group or (C1-C6)-alkoxy-group); R2 means hydrogen atom, (C1-C15)-alkyl, (C1-C6)-alkoxy-group or cycloaliphatic group; R3 means hydrogen atom, hydroxy-group, (C1-C6)-alkyl, dihydroxy-(C1-C6)-alkyl, (C1-C10)-alkoxy-group or cycloaliphatic group; R4 and R5 mean independently of one another hydrogen atom, hydroxy-group, (C1-C6)-alkyl, (C1-C6)-alkoxy-group; or among compound of the formula (VIII):

. Invention provides applying agonists eliciting the selective effect with respect to RARγ, for preparing a medicinal agent comprising one or some such agonists designated for emphysema treatment.

EFFECT: valuable medicinal properties of compounds.

4 cl, 5 tbl, 3 ex

The invention relates to a derivative chromane formula I

in which R1denotes acyl with 1 to 6 carbon atoms, R2, R3, R4represent hydrogen, X represents N,N or O, as well as their enantiomers and their salts, and methods for their preparation

FIELD: chemistry.

SUBSTANCE: invention relates to use of tetrahydrobenzoxazines

in which substitute R1 denotes a hydrocarbyl residue having 1-3000 carbon atoms, and substitutes R2, R3, R4 and R5 independently denote hydrogen atoms, hydroxyl groups or hydrocarbyl residues, having 1-3000 carbon atoms, respectively, and in which substitutes R3 and R4 or R4 and R5 with a partial structure -O-CH2-NR7-CH2-, bonded to the benzene ring, can also form a second tetrahydrooxazine ring, where R7 denotes hydrocarbyl residues having 1-3000 carbon atoms, provided that at least one of substitutes R1, R2, R3, R4, R5 or R7 are polyisobutenyl, having 3000 carbon atoms and the rest of the substitutes from the group R1, R2, R3, R4, R5 or R7, if they denote hydrocarbyl residues, have 1-20 carbon atoms, respectively, as anti-oxidants for stabilising mineral oil and fuel products against the effect of light, oxygen and heat. The invention also describes jet fuel and jet fuel additive concentrate containing tetrahydrobenzoxazine of formula (I).

EFFECT: preparation of stabilisers having improved stabilisation of nonliving organic material, particularly jet fuel against the effect of light, oxygen and heat.

9 cl, 14 ex

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