Thieno-(1,3)-oxazine-4-ons possessing inhibiting activity in respect to lipase

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of the formula (1a) or its pharmaceutically acceptable salt, esters or imides where A is a thiophenyl group containing, probably, substitution, the thiophenyl group A containing, probably, substitution with one or several groups as follows: alkyl, halo or arylalkyl, Y is O, S or NR2 where R2 is hydrogen or alkyl group containing 1 to 6 carbon atoms, and R1 is an non-ramified alkyl group containing 6 to 25 carbon atoms, ramified alkyl group containing 6 to 25 carbon atoms, aryl alkyl group where the alkyl group contains 2 to 25 carbon atoms or phenyl group containing substitution with one or several groups as follows: phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR16- phenyl, NR16CO-phenyl or NR16 -phenyl containing, probably, substitution where R16 is hydrogen or alkyl group containing 1 to 4 carbon atoms, the groups phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR-phenyl or NR-phenyl containing, probably, substitution with one or several groups as follows: halo, alkyl, alkylhalo or phenyl group containing substitution with one or several groups or alkyl groups provided the above compound is not 5-methyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on, 6-amyl-2-(4-chlorophenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on or 6-amyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on Invention also relates to method of obtaining compounds of the formula (Ia) or (IIa), to pharmaceutical compound and application, as well as cosmetic technique.

EFFECT: obtaining of new biologically active compounds and pharmaceutical compounds based on them.

27 cl, 4 ex, 1 tbl

 

The text descriptions are given in facsimile form.

1. The use of the compounds of formula (I)

or its pharmaceutically acceptable salt of ester or amide, where a represents a thienyl group, possibly containing the substitution

Y represents O, S or NR2,

a R1represents a substituted or unsubstituted alkyl (possibly containing one or more oxygen atoms), alkenyl, quinil, cycloalkyl, cycloalkenyl, aryl, arylalkyl, restored arylalkyl, arylalkyl, heteroaryl, heteroaromatic, heteroaromatic restored aryl, restored heteroaryl, restored heteroaromatic or contain a substitution derivative of the above groups, and the substituents are independently one or more radicals selected from the following group: halogen, alkyl, galatarasay alkyl, aryl, shall rilastil, heteroaryl, restored heteroaryl, restored heteroallyl, Allakaket, cyano, nitro, -C(O)R4, -CO2R5, -SOR4, -SO2R4, -NR6R7, -OR6, -SR6, -C(O)CX1X2NR6R7, -C(O)N(OR5R6, -C(O)NR5R4, -NR6C(O)R4, -CR6(NH2)CO2R6, -NHCX1X2CO2R6, -N(OH)C(O)NR6R7N(OH)C(O)R4, -NHC(O)NR6R7, -C(O)NHNR6R7, -C(O)N(OR5R6or lipid or steroid (natural or synthetic), provided that the heteroatomic substituent in R1must be separated from ekzoticheskogo heteroatoms by at least two carbon atoms (preferably saturated);

and where R2represents hydrogen or a group as defined above for R1;

R4represents hydrogen, alkyl, alkenyl, quinil, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, heteroaromatic, restored heteroaryl, restored heteroallyl, -OR6, -NHCX1X2CO2R6or-NR6R7or a substituted derivative of any of the above groups;

R5represents hydrogen, alkyl, alkenyl, quinil, cycloalkyl, cycloalkenyl, aryl, arylalkyl heteroaryl, heteroaromatic restored gets roarer or restored heteroaromatic; and R6and R7independently represent hydrogen, alkyl, alkenyl, quinil, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, restored heteroaryl, restored heteroaromatic or -(CH2)n(OR5)mwhere n is from 1 to 12, preferably from 2 to 10, a m is 1-3, or a derivative of any of the above groups containing substitution; and

X1and X2independently represent hydrogen, alkyl, alkenyl, quinil, cycloalkyl, cycloalkenyl, aryl, heteroaryl, arylalkyl, heteroallyl, restored heteroaryl or restored heteroaromatic for the treatment or prevention of obesity or disorders associated with obesity.

2. The use according to claim 1, characterized in that the compound of formula I thienyl group And connected with oxazinone ring in position 2,3 or 3,2 and possibly substituted by one or more of the following groups: hydrogen, hydroxy, halogen, oxo, amino, nitro, cyano, alkyl, aryl, alkylaryl, haloalkyl, alkoxy, aryloxy, alkylthio, alkylamino, aaltio or arylamino, with aaltio, arylamino, aryloxy can be substituted by one or more of the following groups: halo, alkyl, haloalkyl, alkoxy, thioalkyl or aminoalkyl; or the group R12Q, where Q represents O, CO, CONH, NHCO, S, SO, SO2or SO2NH2and R12performance is possessing a hydrogen or the group R 1as defined above; or R1R2N, where R1defined above, and R2represents hydrogen or R1provided that any heteroatomic Deputy in R1and/or R2must be separated from heteroatomic aromatic substituent at least two carbon atoms (preferably saturated).

3. The use according to claim 1, wherein the thienyl group may be substituted by one or more of the following groups: hydrogen, lower branched or unbranched alkyl containing from 1 to 20 carbon atoms, cyclic alkyl, containing from 3 to 10 carbon atoms, aryl, haloalkyl or halogen;

Y represents O, S or NR2where R2represents hydrogen or alkyl;

R1represents alkyl or aryl, perhaps, which can be substituted by the following groups: alkyl, haloalkyl, halo, cyano, nitro, OR6, SR6, COR6, CO2R6, NR6, R7or aryl which may be substituted, aryloxy, aaltio, SO-aryl, SO2-aryl-alkylaryl, CO-aryl, CO2-aryl, CONR6-aryl, NR6CO-aryl or NR6-aryl, or substituted derivatives of any of the above groups.

4. The use according to claim 3, wherein R1represents an alkyl group, containing the t 4 to 30 carbon atoms.

5. The use according to claim 1, characterized in that the said compound is a compound of formula II

or its pharmaceutically acceptable salt, ester or amide;

where the group is As defined for formula (I);

Y defined for formula (I);

R20selected from the group comprising OR13, COR13, CO2R13, SR13, SOR13, SO2R13, CONR13R14, NR14C(O)NR13C1-10-alkyl, C1-10-alkoxy, halo-C1-10-alkyl, cyano, halo, aryl, aryl-C1-10-alkyl, heteroaryl or heteroaryl-C1-10-alkyl, where R13and R14independently represent hydrogen, C1-10-alkyl, C2-10alkenyl, C1-10-quinil,3-6-cycloalkyl,3-6-cycloalkenyl, aryl, aryl-C1-10-alkyl, heteroaryl, heteroaryl-C1-10-alkyl, restored heteroaryl or restored heteroaryl-C1-10-alkyl or a derivative of any of the above groups containing substitution.

6. The use according to claim 5, wherein R20represents phenyloxy, phenylthio, SO-phenyl, SO2-phenyl, alkylphenyl, CO-phenyl, CO2-phenyl, CONR13-phenyl, NR13CO-phenyl or NR13is phenyl which may be substituted by one or more of the following groups: halo, alkyl, alcalali alkoxy, aryl, alkylaryl, aryloxy, amino, cyano, hydroxy or heteroaryl.

7. The use according to claim 1, characterized in that the compound used for the treatment of disorders associated with obesity, which constitutes one or more violations of the following groups: hyperlipemia, hyperlipidemia, hyperglycemia (diabetes type II), hypertension, cardiovascular disease, stroke, gastrointestinal disease or gastrointestinal disturbance.

8. The compound of formula (Ia)

or its pharmaceutically acceptable salt, ester or amide,

where a represents tiffaniejoy group, possibly containing the substitution

this teofilina group And may contain a substitution of one or more of the following groups: alkyl, halo, or arylalkyl,

Y represents O, S or NR2where R2represents a hydrogen or alkyl group containing from 1 to 6 carbon atoms,

and R1represents a

unbranched alkyl group containing from 6 to 25 carbon atoms, a branched alkyl group containing from 6 to 25 carbon atoms, arylalkyl group in which the alkyl group contains from 2 to 25 carbon atoms, or

phenyl group containing Zam is the establishment of one or more of the following groups: phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR16-phenyl, NR16CO-phenyl or NR16the phenyl may contain substitution,

where R16represents a hydrogen or alkyl group containing from 1 to 4 carbon atoms,

this group phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR-phenyl or NR-phenyl may contain a substitution of one or more of the following groups: halo, alkyl, alcalali, or

phenyl group containing a substitution of one or more cyano - or accelgroup, provided that the compound is not 5-methyl-2-(4-methoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one, 6-pentyl-2-(4-chlorophenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one or 6-pentyl-2-(4-methoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one.

9. The connection of claim 8, characterized in that it is a compound of formula (IIa)

(IIa) and pharmaceutically acceptable salts, esters and amides;

where the group is As defined for formula (Ia);

Y is defined for formulae (Ia);

a R20represents phenyloxy, phenylthio, SO-phenyl, SO2-phenyl, alkylphenyl, CO-phenyl, CO2-phenyl, CONR6-phenyl, NR6CO-phenyl or NR6-phenyl, possibly containing a substitution of one or more of the following groups: ha is about, cyano, alkyl, alcalali, alkoxy, aryl, alkylaryl, aryloxy, amino, hydroxy or heteroaryl.

10. The compound of formula (IIa) according to claim 8 or 9, selected from the group including

2 phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 Butylochka-4H-thieno-[2,3-d][1,3]oxazin-4-one;

5-methyl-2-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

5,6-dimethyl-2-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

5-phenyl-2-phenylamino-4H-thieno[3,2-d][1,3]oxazin-4-one;

2-(4-(3-triptoreline)phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

5-(1,1-dimethylethyl)-2-phenylamino-4H-thieno[3,2-d][1,3]oxazin-4-one;

6-methyl-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxy)phenylamino-4H-thieno[3,2-d][1,3]oxazin-4-one;

2-(4-phenylmethyl)phenylamino-4H-thieno[2,3-e][1,3]oxazin-4-one;

2-(4-benzoyl)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2-(4-phenoxy)phenoxy-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-(4-triptoreline)phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-(3-triptoreline)phenoxy)-4H-thieno[3,2-d][1,3]oxazin-4-one;

2-(4-phenylthio)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

5,6-dimethyl-2-(4-phenoxy)phenoxy-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 dodecylamino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-N-dodecyl-N-methylamino-6-methyl-4H-thieno[2,-d][1,3]oxazin-4-one;

2 dodecylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 dodecylthio-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-N-(1-methylethyl)-N-phenylamino)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenylsulfonyl)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenylcarbamoyl)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-(4-chlorophenoxy)-phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-(4-methylphenoxy)-phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-cyanophenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-cyanophenyl)amino-6-propyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-cyanophenyl)amino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-phenylmethyl-2-(4-cyanophenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-cyanophenyl)amino-6-dodecyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2-(4-phenylbutyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(2-chloroethyl)amino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(hept-6-enyl)amino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(5-methoxycarbonylmethyl)amino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 phenylamino-5,6,7,8-tetrahydro-4H-benzothieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxy)phenylamino-4H-thieno-[3,4-d][1,3]oxazin-4-one;

2-(4-(4-triptoreline)phenylamino)-4H-thieno[3,2-d][1,3]oxazin-4-one;

2-(4-cyanophenyl)amino-4H-thieno[3,2-d][1,3]oxazin-4-one;

2-dodecylamino-thieno[3,2-d][1,3]oxazin-4-one;

2-(5-etylhexyl)amino-4H-thieno[3,2-d][1,3]oxazin-4-one;

5-methyl-2-(4-phenoxy)phenylamino-4H-thieno[3,2-d][1,3]oxazin-4-one;

6-propyl-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 hexadecylamine-6-methyl-4H-thieno-[2,3-d][1,3]oxazin-4-one;

6-chloro-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-dodecyl-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-phenylmethyl-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-(4-phenoxybenzamine)-7-oxa-9-thia-1,5-diazafluoren-8-he;

2(5,5,5-tryptophanyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 acotiamide-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 octadecylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 hexadecylamine-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(12-nitratomethyl)-amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(12-vinyldimethyl)-amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(12-(pyrid-2-yl)dodecyl)-amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2 octylamine-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(8-phenylethyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenylsulfinyl)-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxycarbonyl)-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2(4-(4-methoxyphenoxy)-phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

2(4-(4-dimethylaminoethoxy)-phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

2(4-(4-hydroxyphenoxy)-phenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one;

2(3-phenoxy)-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2(2-phenoxy)-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(3-cyanophenyl)amino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-course)amino-6-methyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-AMINOPHENYL)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-hydroxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-ethoxycarbonylphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-trifluoromethyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-N-(4-phenoxy)phenyl-N-ethylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-N-(4-phenoxy)phenyl-N-methylethylamine-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-cyclopropyl-2-(4-phenoxy)-phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxy)phenyl-thio-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxy)phenylamino-6-trifluoromethyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methoxy-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6 phenoxy-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2-(4-methoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one;

2-(4-phenoxy)phenylamino-6-propyl-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-cyano-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-chloro-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2(4-phenoxy)phenylthio-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2-(4-phenoxy)phenoxy-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2-(4-phenoxy)phenoxy-4H-thieno[3,2-d][1,3]oxazin-4-one;

7-methyl-2-(4-phenoxy)phenylamino-4H-thieno[3,4-d][1,3]oxazin-4-one;

5-methyl-2-(4-phenoxy)phenylamino-4H-thieno[3,4-d][1,3]oxazin-4-one;

6-methyl-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one;

6-methyl-2-(3-methylisoxazol-5-yl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one,

or its pharmaceutically acceptable salt, ester or amide.

11. The compound of formula (IIa) according to claim 8, characterized in that a represents a 6-methyl-2-(4-phenoxy)phenylamino-4H-thieno[2,3-d][1,3]oxazin-4-one.

12. The method of obtaining the compounds of formula (Ia) or (IIa), comprising the reaction of cyclization of compounds having the formula (VI)

where a represents tiffaniejoy group, possibly containing the substitution

this teofilina group And may contain a substitution of one or more of the following groups: alkyl, halo, or arylalkyl,

Y represents O, S or NR2where R2represents a hydrogen or alkyl group containing from 1 to 6 carbon atoms,

a R1represents a

unbranched alkyl group containing from 6 to 25 carbon atoms, a branched alkyl group, containing the th from 6 to 25 carbon atoms, arylalkyl group in which the alkyl group contains from 2 to 25 carbon atoms, or

phenyl group containing a substitution of one or more of the following groups: phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR16-phenyl, NR16CO-phenyl or NR16-phenyl, possibly containing the substitution

where R16represents a hydrogen or alkyl group containing from 1 to 4 carbon atoms,

this group phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR-phenyl or NR-phenyl may contain a substitution of one or more of the following groups: halo, alkyl, alcalali, or

phenyl group containing a substitution of one or more cyano - or accelgroup, provided that the compound is not 5-methyl-2-(4-methoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one, 6-pentyl-2-(4-chlorophenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one or 6-pentyl-2-(4-methoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazin-4-one; or R1represents phenyl-R20where R20represents phenyloxy, phenylthio, SO-phenyl, SO2-phenyl, alkylphenyl, CO-phenyl, CO2-phenyl, CONR6-phenyl, NR6CO-phenyl or NR6-phenyl, possibly containing a substitution of one or more of the following groups: halo, cyano, alkyl, alcalali, alkoxy, aryl, alkylaryl,aryloxy, amino, hydroxy or heteroaryl;

and R18represents hydrogen or C1-6-alkyl.

13. The connection of claim 8, intended for the prevention or treatment of obesity or disorders associated with obesity.

14. The connection 13, characterized in that the compound used for the treatment of disorders associated with obesity, which constitutes one or more violations of the following groups: hyperlipemia, hyperlipidemia, hyperglycemia (diabetes type II), hypertension, cardiovascular disease, stroke, gastrointestinal disease or gastrointestinal disturbance.

15. The connection of claim 8, wherein the specified connection is intended for the prevention or treatment of a condition that requires inhibition of the enzyme involved in the metabolism or decomposition of fat.

16. Connection PP-11, characterized in that the specified connection is intended for use to reduce the level of toxins in the body fat.

17. Application connection PP-11, characterized in that the specified connection is intended for introduction into the human or animal.

18. The connection of claim 8, wherein the specified connection is intended for the prevention or treatment of conditions requiring inhibition of the farm is the the preferred course of action which is the catalysis of the hydrolysis of functional groups of ester.

19. The pharmaceutical composition having inhibitory activity against the lipase, phosphatase or esterase containing the connection PP-11 in combination with a pharmaceutically acceptable carrier or diluent.

20. The use of the composition according to claim 19 for preventing or treating obesity or disorders associated with obesity.

21. The use of compounds according to claims 1 to 11 in order to inhibit the enzyme, the preferred course of action which is the catalysis of the hydrolysis of functional groups of ester.

22. Use item 21 for inhibition of the enzyme esterase, phosphoesterase or lipase.

23. Use item 21, in which the inhibition is carried out for control and inhibition of unwanted enzymes in any process or product.

24. Use item 21, in which the inhibition of conduct for prevention of decomposition of the food product that contains fat.

25. The use of compounds according to claims 1 to 11 to reduce the fat content in animals.

26. Cosmetic way to maintain a given weight or cosmetic weight loss, comprising introducing the compound according to claims 1-11.

27. The use of compounds according to claims 1 to 11 to obtain cosmetic compositions containing the surface of the but-active substances, soap or detergents.



 

Same patents:

The invention relates to novel condensed polycyclic heterocyclic compounds of the formula I and the way they are received

The invention relates to new compounds of the formula (I) in which R1represents a group of formula (Ia) or (IB), in which either R7represents an optionally protected hydroxy-group, alloctype, halogen, -OR10where R10represents lower alkyl, optionally protected-O(CH2)mHE, where m = 2 to 4, or-ОСОNН2and R7ais hydrogen, or R7and R7atogether represent oxoprop, R8represents a hydroxy or methoxy group, and R9- hydroxy - or alloctype; R2- hydrogen, alloctype or optionally protected hydroxy-group, and between the two carbon atoms connected by the dotted line, there is a simple or a double bond; R3is methyl, ethyl, n-propyl or allyl; or R4represents hydrogen or a hydroxy-group, and R4ais hydrogen, or R4and R4atogether represent oxoprop; or R5represents a hydroxy-group, and R5ais hydrogen, or R5and R5atogether represent oxoprop; and a represents a group of formula-CH(OR6)-CH2-(CH2)nor-CH= CH-(CH2)n- associated with carbon atom (CH2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): , wherein X represents heteroatom, such as oxygen (O) or sulfur (S) atoms; X and Z mean independently of one another one or some identical or different substitutes bound any available carbon atom and they can represent hydrogen atom or halogen atom; R1 represents a substitute of the formula (II): , wherein R2 and R3 can represent simultaneously or independently of one another hydrogen atom or (C1-C4)-alkyl, or R1 can represent hydrogen, halogen atom, (C1-C7)-alkyl, -CHO, -(CH2)2COOH, -(CH2)2CO2Et, (CH2)mL wherein L means -OH or bromine atom (Br); m represents a whole number from 1 to 3; n represents a whole number from 0 to 3; Q1 and Q2 represent independently of one another oxygen atom or group of the formula: wherein substitutes y1 and y2 represent hydrogen atom, and to their pharmacologically acceptable salts. Also, invention relates to use of these compounds as intermediate substances used in synthesis of novel compounds of dibenzoazulene class, and to their using for preparing drugs.

EFFECT: valuable medicinal properties of compounds.

9 cl, 4 tbl, 13 ex

FIELD: organic chemistry, medicine, pharmacy, chemical technology.

SUBSTANCE: invention relates to novel substituted esters of 1,2,3,7-tetrahydropyrrolo[3,2-f][1,3]benzoxazin-5-carboxylic acids of the general formula (1): or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and/or hydrates possessing the antiviral effect. In compounds of the general formula (1) each R1 and R4 represents independently of one another a substitutes of amino group chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and possibly an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R2 represents alkyl substitute chosen from hydrogen atom, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl or cycloalkyl; R5 represents a substitute of cyclic system chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and optionally an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R6 represents a substitute of cyclic system chosen from hydrogen atom, halogen atom, cyano group, optionally substituted aryl or optionally substituted and optionally annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides. Also, invention relates to methods for treatment, drugs and pharmaceutical compositions using compounds of this invention. Proposed compounds can be used as active components of drugs used in treatment of such diseases as infectious hepatitis, human immunodeficiency, atypical pneumonia and avian influenza.

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

22 cl, 3 tbl, 6 dwg, 7 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods for synthesis and preparing.

35 cl, 16 sch, 13 tbl, 43 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to compounds of general formula 1 (G1 is group of general formulae 2 G1 is group of general formulae ; meanings of the rest substituents are as described in specification) or pharmaceutically acceptable salts thereof and use thereof in srug production. Said compounds are useful in treatment of male and female sexual disorders.

EFFECT: new oxytocin antagonists.

30 cl, 177 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to compounds of general formula I and pharmaceutically acceptable salt thereof, wherein R1, R3, R4, R5, and R10 are independently H, halogen, C1-C4-alkyl, etc.; R2 is H, halogen, NO2, etc.; R6 is H, C1-C6-alkyl, C1-C6-alkoxy-substituted C1-C4-alkyl, etc.; R7 is H, C1-C4-alkyl or C2-C4-alkenyl, optionally substituted with halogen; R8 and R9 are H, R11 and R12; meanings of the rest substituents are as define in specification.

EFFECT: new compounds with value biological properties and useful as drug having activity in relates to progesterone receptor.

15 cl, 3 tbl, 80 ex

FIELD: organic chemistry.

SUBSTANCE: invention relates to new method for production of E-2-aroylmethylene-1-phenyl-1,2,3,4-tetrahydroquinazolin-4-ones of general formula I wherein R represents H, methyl, Cl. Claimed method includes interaction of 5-aryl-2,3-dihydro-2,3-furandiones with N-phenylanthranyl acid amide in medium of inert aprotic solvent (preferably benzene) followed by isolation of target products. Process is carried out preferably at 79-80°C. Claimed compounds have fluorescent properties and are useful in labeling and copying agents, intermediates for synthesis of new heterocyclic compounds, etc.

EFFECT: new fluorescent compounds.

3 cl, 1 dwg, 3 ex

FIELD: organic chemistry, antibacterial agents.

SUBSTANCE: invention relates to an agent used against acid-resistant microorganisms containing derivative of pyridone carboxylic acid as an active component, its pharmaceutically acceptable salt or its hydrate that elicits high antibacterial activity against Mycobacterium tuberculosis and atypical acid-resistant microorganisms. Invention describes agent used against acid-resistant microorganisms containing compound represented by the following formula (I) its salt or its hydrate as an active component wherein R1 represents cyclic alkyl group comprising 3-6 carbon atoms that can comprise substitute(s) chosen from halogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom; A1 represents incomplete structure represented by the formula (2): wherein X2 represents halogen atom, alkyl group comprising 1-6 carbon atoms or alkoxy-group comprising 1-6 carbon atoms; A1, A2 and A3 form incomplete structure of the formula: in common with carbon atoms combined with them; X1 represents halogen atom; Y represents hydrogen atom; Z represents phenylpiperazine substitute. Invention provides synthesis of pyridone carboxylic acid eliciting high antibacterial activity against Mycobacterium tuberculosis and atypical acid-resistant microorganisms in combination with good pharmacokinetics indices and safety.

EFFECT: valuable biological property of agent.

10 cl, 9 tbl, 10 ex

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to a synthetic quinolone agent that is effective as medicinal agents, veterinary preparations, drugs used in fishing industry or as antibacterial preserving agents. Invention describes compound represented by the following general formula (I): as its separate isomers or their mixture, its salt and their hydrates wherein R1 represents cyclic alkyl group comprising 3-6 carbon atoms that can comprise a substitute chosen from halogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom; R4 represents hydrogen atom, amino-group, hydroxyl group; A represents nitrogen atom or part of structure as given in the invention claim; each R5 and R6 represents independently alkyl group comprising 1-6 carbon atoms or hydrogen atom; n means a whole number 1 or 2. Also, invention describes antibacterial agent and therapeutic agent based on compounds of the formula (I) used in treatment of infectious disease, a method for preparing antibacterial agent, a method for preparing a medicinal agent used in treatment of infectious disease and using compound of the formula (I) for preparing an antibacterial agent and using compound of the formula (I) for preparing a medicinal agent used in treatment of infectious disease. Invention provides novel compounds possessing useful biological properties.

EFFECT: improved preparing method of agents, valuable medicinal properties of compounds and agents.

35 cl, 2 tbl, 15 ex

FIELD: chemistry of heterocyclic compounds, antibacterial agents.

SUBSTANCE: invention relates to agent used against acid-resistant microorganisms. Invention describes agent against acid-resistant microorganisms containing as an active component the compound represented by the general formula (1) or its hydrate wherein R2 represents hydrogen atom; R3 represents hydrogen atom; A1, A2 and A3 form incomplete structure of the formula: wherein A1 represent incomplete structure of the formula: wherein X2 and above described R1 can be combined to form six-membered cyclic structure comprising part of the parent nucleus wherein formed ring can comprise oxygen atom and, except for, can comprise alkyl group having 1-6 carbon atoms as a substitute; X1 represents halogen atom, hydrogen atom or amino-group; Y represents hydrogen atom; Z represents incomplete structure of the formula: . Agent elicits high antibacterial activity of broad spectrum and possesses good pharmacokinetics and safety also.

EFFECT: improved and valuable properties of agent.

3 cl, 9 tbl, 10 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel lactam compounds of the formula (I) or their pharmaceutically acceptable salts wherein A means phenyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl; R2, R3 and R4 can be similar or different and mean independently of one another hydrogen atom (H), halogen atom, -OH, (C1-C6)-alkyl, (C1-C6)-alkoxy-group, -NH2, -NO2, -CF3, phenyl that can comprise substitute(s), benzyloxy-group that can comprise substitute(s), pnehylvinyl, and one among R2, R3 and R4 means -CF3-O- and others mean H; B means phenyl that can comprises substitute(s), monocyclic aliphatic (C3-C8)-ring, dihydropyrane ring; -X- and -Y- xan be similar or different and they mean independently -O-, -NH-, -NR5-, -S-; Z means -CH2-, -NH-; W means -NR1-, -CR8R9- wherein R1 means H; R8 and R9 are similar or different and mean H; wherein R5 represents a linear alkyl group that can comprise substitute(s), (C1-C8)-linear or branched alkoxycarbonyl group, acyl group chosen from formyl group, acyl group comprising (C1-C6)-alkyl, (C1-C6)-alkenyl or (C1-C6)-alkynyl group that can comprise substitute(s), carbamoyl group comprising (C1-C6)-alkyl group at nitrogen atom that can comprise substitutes, sulfonyl group comprising (C1-C6)-alkyl group at sulfur atom that can comprise substitute(s); each among a, b and c represents position of carbon atom under condition that: (i) substitute(s) is chosen from the group comprising halogen atom, -OH, (C1-C6)-alkyl, mercapto-group, (C1-C6)-alkoxy-group, -NO2, -COOH, -CF3, phenyl, -NH2, (C1-C8)-linear or branched alkoxycarbonyl group, (C1-C8)-linear or branched acyl group, (C1-C8)-linear or branched acyloxy-group; (ii) when B represents benzene ring, each among -X- and -Y- represents -NH-, -Z- represents -CH2- and -W- represents -NH- then R2, R3 and R4 can not mean phenyl group, 4-bromophenyl group, 4-hydroxyphenyl group, 4-methoxyphenyl group, 2-hydroxyphenyl group, 3,4-dimethoxyphenyl group or 3-methoxy-4-hydroxyphenyl group. Compounds of the formula (I) show the enhanced capacity for transport of sugar and can be used in pharmaceutical compositions for prophylaxis and/or treatment of diabetes mellitus and diabetic nephropathy.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

19 cl, 21 tbl, 54 ex

FIELD: medicine; pharmacology.

SUBSTANCE: invention relates to the novel compounds with formula (I) and their pharmaceutically acceptable salts. The compounds of this invention has the properties of the NPY receptor antagonists and can be used fortreatment of such diseases as arthritis, diabetes, malnutrition, obesity. In general formula (I) , R1 means phenyl or 6-term nitrogen-containing heteroaryl, where in at least one of two meta-positions each phenyl group or 6-term nitrogen-containing heteroaryl group is substituted by group R5; R2 means hydrogen; R3 means C3-C6cycloalkyl, naphthyl, phenyl or 5-6-term heteroaryl, containing N or S as heteroatoms, where in at least one of two ortho-positions each group of C3-C6 cycloalkyl, naphthyl, phenyl or 5-6-term heteroaryl, containing N or S as heteroatoms, substituted by group R6; R4 means hydrogen, C1-C6alkyl; R5 means hydrogen, cyano, trifluoromethyl, C1-C6alkyl-SO2-, amino-SO2-, halogen, C1-C6alcoxy, C1-C6alkylcarbonil or aminocarbonil; R6 means hydrogen, halogen, cyano, nitro, trifluoromethyl, C1-C6 alkyl, C1-C6 alcoxy or hydroxy, provided, one R5 group, and R6 doesn't mean hydrogen.

EFFECT: described compounds and based on them pharmaceutical agents are efficient in treatment and prevention of above listed diseases.

19 cl, 2 tbl, 2 dwg, 130 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to drugs and concerns a liquid food composition showing pH value above 6, viscosity value less 600 mPa x s at the shift rate value 100 s-1 and temperature 20°C and wherein viscosity value is at least 125% of the above given viscosity value at pH less 5 and temperature 37°C. Proposed composition comprises the following components: (a) at least 0.05 wt.-% of pectin with the methoxylation degree from 2 to 50, and/or alginate; (b) at least 0.005 wt.-% of calcium, and (c) at least 0.1 wt.-% of nondigestable oligosaccharide with polymerization degree in the range from 2 to 60 and chosen from group consisting of fructans, fructooligosaccharides, nondigestable dextrins, galactooligosaccharides, xylooligosaccharides, soybean oligosaccharides, arabinooligosaccharides and their mixtures, and from 50 to 98 wt.-% of water. Also, invention discloses using this composition in a method for prophylaxis or treatment of excessive weight, and in a method for treatment or prophylaxis of diabetes mellitus of type II in mammals. Invention provides increasing bioavailability of calcium and elevating viscosity of the food composition at low pH value.

EFFECT: improved and valuable properties of composition.

18 cl, 9 tbl, 5 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): and their pharmaceutically acceptable salts and esters wherein R1 means phenyl, naphthyl, 5-6-membered heterocyclyl comprising oxygen (O), nitrogen (N) or sulfur atom (S) as heteroatoms and wherein phenyl, naphthyl and heterocyclyl are optionally substituted with 1-3 substitutes chosen from halogen atom, (C1-C6)-alkyl, (C1-C6)-alkoxy, halogen-(C1-C6)-alkyl, halogen-(C1-C6)-alkoxy, nitro; di-(C1-C6)-alkylamino or (C1-C6)-alkoxy groups; R2 means hydrogen atom; R3 means (C1-C6)-alkyl or trifluoromethyl; A1 means C-R3 or nitrogen atom; A2 means piperidine or pyrrolidine wherein nitrogen atom in piperidine or pyrrolidine ring is added to A3 wherein A3 means -S(O)2- or -C(O)-; n = 0, 1 or 2. Also, invention relates to a pharmaceutical composition based on compounds proposed by the invention. Proposed compounds possess properties of NPY receptors antagonists and can be used in treatment arthritis, diabetes mellitus, nutrition disorders, obesity and others.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

16 cl, 1 tbl, 1 dwg, 26 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): wherein R1 means hydrogen atom (H) or (C1-C8)-alkyl; R2 means (C1-C8)-alkyl, -CH2-O-(C1-C8)-alkyl, -OH or -CH2OH; R2a means H; or R2 and R2a for in common -CH2-CH2-; R3 means halogen atom, perhalogenalkyl, -CN, -SR5, -NHR5, -N(R5)2, aryl or heteroaryl wherein indicated aryl can comprise optionally up to two substitutes chosen from (C1-C8)-alkyl, halogen atom, perhalogenalkyl and alkoxy-group, and indicated heteroaryl can comprise optionally up to two substitutes chosen from halogen atom and (C1-C8)-alkyl; R4 means H, halogen atom, perhalogenalkyl, -CN, -OR5, -SR5, -NHR5, -N(R5)2, -OH, aryl or heteroaryl wherein indicated aryl can comprise optionally up to two substitutes chosen from (C1-C8)-alkyl, halogen atom, perhalogenalkyl and alkoxy-group, and indicated heteroaryl can comprise optionally up to two substitutes chosen from halogen atom and (C1-C8)-alkyl; or R3 and R in common with atoms to which they are added can form 5- or 6-membered heterocyclic ring comprising one oxygen atom (O); each R5 means independently (C1-C8)-alkyl, (C2-C8)-alkenyl, aryl, heteroaryl, arylalkyl, alheteroarylalkyl, perhalogenalkyl or allyl; R6 means H or (C1-C8)-alkyl, or their pharmaceutically acceptable salts, solvates or hydrates under condition that if R6 differs from H then R4 can't mean H; if R1 and R2 mean methyl and R4 means H then R3 can't -NHR5 or -N(R5)2; if R1 and R2 mean methyl and R4 means H then R3 can't imidazole, substituted imidazole or imidazole derivative. Also, invention relates to a pharmaceutical composition used for modulation of 5-HT2C receptors, a method for modulation of 5-HT2C receptors, a method for prophylaxis or treatment of disorders of the central nervous system and obesity, a method for reducing food consumption in mammals, a method for inducing the satisfying sense in mammals and to a method for preparing the composition. Invention provides synthesis of novel compounds possessing useful biological properties and preparing pharmaceutical composition based on thereof.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

70 cl, 1 tbl, 57 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to compounds inhibiting activity of hormone-sensitive lipase and represented by structure of the formula: (XXXXIVa)

and the formula (XXXXIVb): wherein R1ap and R2ap are chosen independently from (C1-C6)-alkyl, aryl wherein each (C1-C6)-alkyl and aryl can be substituted optionally with one or some substitutes chosen independently from halogen atom, (C1-C6)-alkyl under condition that if R1ap and R2ap are similar then they are not methyl or ethyl, and wherein between substitutes R1ap and R2ap can be a covalent bond optionally, and wherein R5ap, R6ap and R7ap are chosen independently from hydrogen atom and fluorine atom (F), and R4ap is chosen from hydrogen atom, sulfanyl, halogen atom, amino-, nitro-group, (C1-C6)-alkyl, heteroaryl, (C3-C8)-heterocyclyl wherein each among sulfanyl, amino-group, (C1-C6)-alkyl, heteroaryl, (C3-C8)-heterocyclyl can be substituted optionally with one or some substitutes chosen independently from hydroxy-, oxo-group, halogen atom, (C1-C6)-alkyl, aryl, heteroaryl wherein each among (C1-C6)-alkyl, aryl, heteroaryl can be substituted optionally with one or some substituted chosen independently from oxo-group, halogen atom, amino-group, (C1-C6)-alkyl, (C3-C8)-heterocyclyl wherein each among amino-group, (C1-C6)-alkyl, (C3-C8)_heterocyclyl can be substituted optionally with one or some substitutes chosen independently from oxo-group, (C1-C6)-alkyl wherein (C1-C6)-alkyl can be substituted optionally with one or some substitutes chosen independently from oxo-group under condition that R4ap is not methyl. Also, invention relates to a pharmaceutical composition and using these compounds for preparing a medicinal agent used for inhibition of lipolytic activity of hormone-sensitive lipase. Invention describes compounds that can be useful in treatment and prophylaxis of clinical disorders wherein decrease of activity of hormone-sensitive lipase is desirable.

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

8 cl, 1 tbl, 602 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of glucopyranosyloxypyrazole of the general formula: wherein R means hydrogen atom, lower alkyl, acyl, alkoxycarbonyl, acyloxymethyl or alkoxycarbonyloxymethyl; one of Q and T represents a group of the general formula: wherein P means hydrogen atom, lower acyl or alkoxycarbonyl but other radical means lower alkyl or halogen(lower alkyl); R2 means hydrogen atom, lower alkyl, alkoxy-, alkylthio-group, halogen(lower)alkyl) or halogen atom under condition that P doesn't represent hydrogen atom when R means hydrogen atom or lower alkyl. Also, invention relates to pharmaceutically acceptable salts of these compounds, pharmaceutical compositions used for prophylaxis of renal glucose re-absorption and eliciting the inhibitory activity with respect to human SGLT2, pharmaceutical combinations that are used for prophylaxis or treatment of diseases associated with hyperglycemia.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

36 cl, 1 dwg, 6 tbl, 48 ex

FIELD: organic chemistry, medicine, endocrinology.

SUBSTANCE: invention relates to novel compounds representing C-glycoside derivatives and their salts of the formula: wherein ring A represents (1) benzene ring; (2) five- or six-membered monocyclic heteroaryl ring comprising 1, 2 or 4 heteroatoms chosen from nitrogen (N) and sulfur (S) atoms but with exception of tetrazoles, or (3) unsaturated nine-membered bicyclic heterocycle comprising 1 heteroatom representing oxygen atom (O); ring B represents (1) unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (2) saturated or unsaturated five- or six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (3) unsaturated nine-membered bicyclic carbocycle, or (4) benzene ring; X represents a bond or lower alkylene wherein values for ring A, ring B and X correlate so manner that (1) when ring A represents benzene ring then ring B is not benzene ring, or (2) when ring A represents benzene ring and ring B represents unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O and comprising benzene ring or unsaturated nine-membered bicyclic carbocycle comprising benzene ring then X is bound to ring B in moiety distinct from benzene ring comprised in ring B; each among R1-R4 represents separately hydrogen atom, -C(=O)-lower alkyl or lower alkylene-aryl; each R5-R11 represents separately hydrogen atom, lower alkyl, halogen atom, -OH, =O, -NH2, halogen-substituted lower alkyl-sulfonyl, phenyl, saturated six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N and O, lower alkylene-OH, lower alkyl, -COOH, -CN, -C(=O)-O-lower alkyl, -O-lower alkyl, -O-cycloalkyl, -O-lower alkylene-OH, -O-lower alkylene-O-lower alkyl, -O-lower alkylene-COOH, -O-lower alkylene-C(=O)-O-lower alkyl, -O-lower alkylene-C(=O)-NH2, -O-lower alkylene-C(=O)-N-(lower alkyl)2, -O-lower alkylene-CH(OH)-CH2(OH), -O-lower alkylene-NH, -O-lower alkylene-NH-lower alkyl, -O-lower alkylene-N-(lower alkyl)2, -O-lower alkylene-NH-C(=O)-lower alkyl, -NH-lower alkyl, -N-(lower alkyl)2, -NH-lower alkylene-OH or NH-C(=O)-lower alkyl. Indicated derivatives can be used as inhibitor of co-transporter of Na+-glucose and especially as a therapeutic and/or prophylactic agent in diabetes mellitus, such as insulin-dependent diabetes mellitus (diabetes mellitus 1 type) and non-insulin-dependent diabetes mellitus (diabetes mellitus 2 type), and in diseases associated with diabetes mellitus, such as insulin-resistant diseases and obesity.

EFFECT: valuable medicinal properties of compounds.

11 cl, 41 tbl, 243 ex

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to Ginkgo biloba extracts useful for stimulating of muscle mass building up at the cost of fat mass in patients which are treated with diet or drugs. Claimed extract contains specific amounts of flavoneglycosides, ginkolides A, B, C, and J, bilobalide, proanthocyanidines and alkylphenol-like compounds and is useful in production of drug for stimulating of muscle mass building up at the cost of fat mass in patients which are treated with diet or drugs.

EFFECT: extract of high effectiveness.

4 cl

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