Annelated asaheterocycles including pyrimidine fragment, method of production thereof and pi3k kinase inhibitors

FIELD: medicine; pharmacology.

SUBSTANCE: new annelated asaheterocycles include pyrimidine fragment of general formula I in the form of free bases or pharmaceutically acceptable salts. Compounds of this invention possess properties of PI3 kinase inhibitors. In general formula I X represents oxygen atom or sulphur atom; Z represents oxygen atom, R1 represents hydrogen atom or optionally substituted C1-C6alkyl, or Z represents nitrogen atom together with bound carbon atom forming through Z and R1 optionally substituted annelated imidazoline cycle; R2 represents optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted phenyl, possibly annelated with 5-6-term heterocyclyl containing heteroatoms chosen from oxygen and nitrogen, optionally substituted 5-6-term heterocyclyl containing heteroatoms chosen from nitrogen, oxygen and/or sulphur, possibly annelated with phenyl ring. Invention also concerns method of production of compounds, pharmaceutical compositions and medical products.

EFFECT: effective application for preparation of medical products for oncologic therapy.

14 cl, 3 dwg, 1 tbl, 4 ex

 

The text descriptions are given in facsimile form.

1. Kannelirovannye azaheterocycle, including pyrimidine fragment of General formula I in the form of free bases or pharmaceutically acceptable salts

where X represents an oxygen atom or a sulfur atom;

Z represents an oxygen atom, R1 represents a hydrogen atom or optionally substituted C1-C6alkyl, or

Z represents a nitrogen atom, which, together with the carbon atom to which it is linked, form a through Z, and R1 is optionally substituted annelirovannymi imidazolinones cycle;

R2 is an optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted phenyl, perhaps kannelirovannyh the 5-6-membered heterocyclyl, containing heteroatoms selected from oxygen and nitrogen, optionally substituted 5-6-membered heterocyclyl containing heteroatoms selected from nitrogen, oxygen and/or sulphur, possible annelirovannymi with the phenyl ring.

2. Compounds according to claim 1, which represents a substituted amides of 4-oxo-3,4-dihydrofuro[2,3-b]pyrimidine-5-carboxylic acids of the General formula I.1, substituted amides of 4-oxo-3,4-dihydrothieno[2,3-b]pyrimidine-5-carboxylic acids of the General formula I.2 and substituted amides of 2,3-dihydrofuro[3,2-e]imidazo[1,2-C]pyrimidine-9-carboxylic acids of General formula I.3, or their pharmaceutically acceptable salts

where R1 and R2 have the above meanings; R3a and R3b independently from each other represent a hydrogen atom or lower alkyl.

3. The method of obtaining compounds of General formula I.1, I.2, I.3 according to claim 1 or 2 by the interaction of the corresponding acids of the General formulas F1, F2, H3 with amines of General formula F11 in the presence of condensing reagents

where R1, R2, R3a and R3b have the above values.

4. Inhibitors of PI3 kinases, which are compounds of General formula I according to claim 1.

5. Selek is active inhibitors according to claim 4 isoforms R-alpha PI3 kinase, representing compounds of General formula I according to claim 1.

6. Selective inhibitors according to claim 4 isoforms R-beta PI3 kinases, which are compounds of General formula I according to claim 1.

7. Selective inhibitors according to claim 4 isoforms R-gamma PI3 kinases, which are compounds of General formula I according to claim 1.

8. Selective inhibitors according to claim 4 isoforms R-Delta PI3 kinases, which are compounds of General formula I according to claim 1.

9. Selective inhibitors according to claim 5 isoforms R-alpha PI3 kinase with a mutation in exon 20 (H1047R), which are compounds of General formula I according to claim 1.

10. Compounds of General formula I according to claim 1 as a biologically active agent to obtain drugs for the treatment of cancer.

11. The pharmaceutical composition intended for the treatment of cancer, comprising, as a biologically active principle at least one compound of General formula I according to claim 1, or a compound according to claim 2, or pharmaceutically acceptable salt in an effective amount.

12. The pharmaceutical composition according to claim 11, containing as active principle at least one compound of the General formula I.1, I.2, I.3 according to claim 2 or pharmaceutically acceptable salt in an effective amount.

13. A method of obtaining a pharmaceutical composition according to claim 11 or 12 by mixing the active principle, not only who found themselves at least one compound of General formula I according to claim 1 or its pharmaceutically acceptable salt, with inert fillers and/or solvents.

14. The drug is in the form of tablets, capsules, or injections, placed in pharmaceutically acceptable packing comprising an inhibitor of PI3 kinase according to any one of claims 4 to 9, or pharmaceutical composition according to any one of 11 and 12 in an effective amount.



 

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FIELD: chemistry.

SUBSTANCE: novel compounds are selected from group, consisting of: 4-(2-cyclopropyl-ethyl)-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-fluorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-(2-hydroxymethyl-cyclopropylmethyl)-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopentylmethyl-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-chlorine-4-(3-methyl- 4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-chlorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-(2-cyclopropyl-ethyl)-piperazine-1-carboxylic acid 3-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-fluorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 2-fluorine-4-(3-methyl-4,10-dihudro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 2-fluorine-4-(3-methyl-4,10-dihydro-3H-2,3,4;9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-ethyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 2-chlorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 2-chlorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide and 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-methoxy-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-benzylamide. Invention also relates to pharmaceutical composition and to application of compounds of general formula 1.

EFFECT: obtaining novel biologically active compounds and based on them pharmaceutical composition, possessing antagonistic activity with respect to vasopressin receptors.

60 cl, 153 ex

FIELD: agriculture.

SUBSTANCE: new chemically biologically active compound 3-amino-4,5,6-trimethyl-2-(benzimidazolyl-2)tieno[2,3-b]pyridine of formula 1 revealing growth regulating properties is described.

EFFECT: increasing sugar beet crop yield and sugar content.

1 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted indoles of general formula , where: X stands for -S(O)n-, -C(O)-; A stands for C1-C6alkyl, -(CH2)p-NRaRb; R1, R2, R3 and R4 each is independently selected from group including H, halogen, halogen(C1-C6)alkyl, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, NO2, -NRaRb, phenyl, benzyl and benzyloxy, said phenyl cycles are optionally substituted with substituent, selected from group including C1-C6alkyl, halogen, NO2, halogen(C1-C6)alkyl, C1-C6alkoxy; R5 stands for H, C1-C6alkyl, C1-C6alkoxy, C1-C6alkoxy C1-C6alkyl, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, hydroxyl-(C1-C6)alkyl, hydroxy(C1-C6)alkylamino, halogen, halogen(C1-C6)alkyl-NRaRb, -NRc-( C1-C6)alkylene-NRaRb, or R5 and A together form radical C2-C3alkylene; R6 stands for H, C1-C6alkyl; R' and R" each independently stand for H, C1-C6alkyl; Ra, Rb and Rc each is independently chosen from group including H, C1-C6alkyl, hydroxy(C1-C6)alkyl, C2-C6alkenyl, C3-C6cycloalkyl-(C1-C6)alkyl, or Ra and Rb together with nitrogen atom, to which they are attached, form 5-7 member non-aromatic heterocyclic cycle, optionally containing in cycle O as additional heteroatom; m is equal 1 or 2; n is equal 0, 1 or 2 under condition that, if n is equal 0, R5 does not stand for NRaRb, and p is equal 0, 1 or 2; or their pharmaceutically acceptable salts.

EFFECT: obtaining compounds possessing agonistic activity which allows using them in pharmaceutical composition.

24 cl, 2 tbl, 22 ex

FIELD: chemistry.

SUBSTANCE: claimed invention relates to substituted 3-cyanotiophenacetamides of general formula I , in which R1 and R2 are independently designate (lower) alkyl, or R1 and R2 together with carbon atoms, to which they are bound, including bond between said carbon atoms, form 5-6 member, unsubstituted carbocyclic or 6-member heterocyclic cycle, probably having substitutes, independently selected from group, including (lower) alkyl, alkylsulfonyl and alkoxycarbonyl, R3 is selected from group, which includes (lower) alkyl, unsubstituted aryl, unsubstituted aralkyl and unsubstituted cycloalkyl, R4 - hydrogen, n is zero, or their pharmaceutically acceptable salts. Compounds can be applied for treatment and/or prevention of diseases, associated with antagonistic action on glucagon receptor, such as diabetes. Pharmaceutical composition based on compounds I and their application are also described.

EFFECT: obtaining substituted 3-cyanotiophenacetamides, which can be applied for treatment and/or prevention of diseases, associated with antagonistic action on glucagon receptor, such as diabetes.

22 cl, 23 ex

FIELD: chemistry.

SUBSTANCE: invention refers to compounds of formula I their pharmaceutically acceptable salts and solvate I where X represents O or S; Y and Z mutually independently denote hydrogen or halogen; R1 is hydroxy-C1-C7-alkyl, carboxy, C1-C7-alkyloxycarbonyl, or substitute of formula II R2 is hydrogen, carboxy or alkyloxycarbonyl. Compounds can be used as inhibitors of cytokine or inflammation mediator producing. Intermediate compounds of compounds I and application of compounds 1 are also described.

EFFECT: production of compounds used as inhibitors of cytokine or inflammation mediator producing.

12 cl, 1 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: (I) , in which R1 and R2 independently represent C1-6alkyl, C3-5cycloalkyl C1-3alkyl or C3-6dikloalkyl; Q represents CR4R5, where R4 represents hydrogen; or C1-6alkyl, and R5 represents carbon; Ar represents 5-6-membered aromatic ring system, where heteroatoms can represent up to 2 ring atoms, independently selected from nitrogen and sulphur, notably that this ring system can be substituted by one or more then one substitute, independently selected from C1-4alkyl; Ar2 represents 5-6-membered aromatic ring system containing up to 2 ring atoms, independently selected from nitrogen and sulphur, notably the ring contains at least one heteroatom and can be substituted by one or more then one group, independently selected from C1-4alkyl. The compositions can be used in autoimmune disease modulation. The methods of compounds production, pharmaceutical composition and use of the compounds in the treatment of respiratory disease are described.

EFFECT: production of thienopyrimidindion compounds for autoimmune disease modulation and respiratory disease treatment.

14 cl, 3 ex

FIELD: chemistry, pharmaceuticals.

SUBSTANCE: invention pertains to derivatives of thienopyrimidine with general formula I , where R1 represents C1-4alkyl; R2 represents C1-6alkyl, possibly substituted (1') by a hydroxyl group, (2') C1-4alkoxy, (3') C1-4alkoxycarbonyl, (4') di-C1-4alkylcarbamoil, (5') 5-6-member nitrogen containing heterocyclic group, (6') C1-C4alkylcarbonyl and (7') halogen, 5-6-member nitrogen containing heterocyclic group, phenyl, which can contain a substitute, R3 - C1-4alkyl, R4 - C1-4alkoxy. The compounds have antagonist activity to gonadotropin releasing hormones (GnRH). Description is given of a medicinal preparation based on formula I compounds, used of the compounds in making pharmaceutical compositions and the antagonist effect of the compounds on gonadotropin releasing hormone.

EFFECT: obtaining derivatives of thienopyrimidine with antagonist effect on gonadotropin releasing hormones.

17 cl, 143 ex

FIELD: chemistry, pharmaceuticals.

SUBSTANCE: invention pertains to thienopyrimidine diones with general formula (I), , where R1 and R2 each independently represents C1-6alkyl, C3-5cycloalkylC1-3alkyl or C3-6cycloalkyl; R3 represents a CO-G group, where G is a 5- or 6-member ring, containing a nitrogen atom and a second oxygen heteroatom, adjacent to the nitrogen atom. This ring can be substituted by at least one group, chosen from C1-4alkyl and hydroxyl; Q represents CR4R5, where R4 represents hydrogen or C1-6alkyl, and R5 represents hydrogen; and Ar represents a 5-10-member aromatic ring system, where up to 3 ring atoms can represent heteroatoms, independently chosen from nitrogen and sulphur. This ring system can be substituted with one or more groups. The invention also relates to pharmaceutical salts and solvates of thienopyrimidine diones. Description is also given of the method of obtaining these compounds, pharmaceutical compositions containing them, and their use in therapy, particularly in immunosuppressive therapy.

EFFECT: obtaining thienopyrimidine diones for use in immunosuppressive therapy.

17 cl, 29 ex

New compounds // 2331646

FIELD: chemistry, pharmaceuticals.

SUBSTANCE: invention pertains to thienopyridazinones with formula , where R1 represents C1-6alkyl, or C3-6cycloalkyl, R2 represents C1-6alkyl; R3 represents a CO-G group, where G is a 5-member ring, containing a nitrogen atom and a second heteroatom, chosen from oxygen, adjacent to the nitrogen atom, and can be substituted with groups in quantity of up to 2, chosen from hydroxyl and C1-4alkyl; Q represents CR5R6, where R5 and R6 - hydrogen, and R4 represents a 5-10-member mono- or bi-cyclic aromatic ring system, containing 2 heteroatoms, independently chosen from nitrogen. This ring system can be substituted. The invention also relates to pharmaceutical salts and solvates of thienopyridazinones. Description is also given of the method of obtaining these compounds, pharmaceutical compositions containing them, and their use in therapy, particularly in the modulation of autoimmune disease.

EFFECT: obtaining thienopyridazinones for use in modulation of autoimmune disease.

12 cl, 17 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the novel form of the crystalline clopidogrel naphthalenesulfonate with formula Ia: for which the powder X-ray diffraction scanning reveals the principal peaks with the I/I0 values more than 10% at 2θ=6.7, 8.2, 8.5, 12.4, 13.0, 13.5, 16.8, 17.2, 18.9, 19.6, 20.2, 21.2, 22.3, 22.9, 23.2, 23.6, 24.7, 25.0, 25.3, 25.8, 27.0, 27.5, 28.0, 28.6, 32.1, 32.5, 34.7. and monohydrate crystalline clopidogrel 1,5-naphthalenesulfonate with formula (Ib) for which the powder X-ray diffraction scanning reveals the principal peaks with the I/I0 values more than 10% at 2θ=7.6, 9.7, 10.7, 11.0, 12.1, 13.6, 14.2, 15.3, 16.6, 17.0, 18.1, 18.5, 19.8, 21.5, 22.2, 23.0, 23.5, 24.3, 24.8, 25.7, 26.4, 26.9, 27.3, 28.4, 29.0, as well as to the method of their production and to their pharmaceutical composition.

EFFECT: increased stability of compounds.

10 cl, 8 dwg, 9 tbl, 4 ex

FIELD: organic chemistry, medicine, oncology, pharmacy.

SUBSTANCE: invention relates to novel polycyclic compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, cycle A, cycles B, X, Y and Z have values given in the invention claims and in description of the claim, and to their pharmaceutically acceptable salts also. Proposed compound possess an antitumor activity and can be used in treatment of oncological diseases. Also, invention relates to a pharmaceutical composition based on these compounds.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

23 cl, 1 tbl, 57 ex

FIELD: organic synthesis.

SUBSTANCE: invention relates to synthesis of camptotecin analogues from 2'-amino-5'-hydroxypropiophnone corresponding to AB ring portion of camptotecin structure and tricyclic ketone converted into CDE ring portion in camptotecin structure. Preparation of 2'-amino-5'-hydroxypropiophnone comprises following steps: (1) preparing compound (b) by mixing compound (a), benzylation agent, and a base followed by stirring mixture obtained in solvent on heating under reflux; (2) preparing compound (c) by dropwise adding Grignard reagent to compound (b) under an inert gas atmosphere; (3) preparing compound (d) by mixing compound (c) with an oxidant and stirring resulting mixture; and (4) preparing compound (e) via catalytic reduction of compound (d) (see scheme 1 below). Intermediate compounds (c') and (d') are described. Also described is a method for preparing tricyclic ketone to provide efficient complete synthesis of camptotecin serving as starting compound for irinotecan hydrochloride and a various types of camptotecin derivatives as well as for stable preparation of camptotecin and its derivatives. Scheme 1: .

EFFECT: expanded synthetic possibilities in camptotecin derivatives series.

5 cl, 17 tbl, 33 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to triheterocyclic compound of the formula (I): wherein X represents carbon atom; Y represents carbon or nitrogen atom; W represents carbon or nitrogen atom; U represents -CR2, and Z represents -CR2 or nitrogen atom; ring A represents (C5-C6)-cycloalkyl ring or 5-membered heterocyclic ring comprising one nitrogen, oxygen or sulfur atom; R1 represents alkyl, alkenyl, alkynyl, -NR4R5, -OR6 and others; R3 represents phenyl ring substituted with 1-3 substitutes or pyridyl or 1,3-dioxoindanyl ring substituted with 1-2 substitutes, and its pharmaceutically acceptable salts and pharmaceutical composition containing thereof as an active component. Also, invention relates to derivatives of pyrazolopyrimidine and derivatives of pyrrolopyrimidine. Compounds of the formula (I) show antagonistic activity with respect to corticotropin-releasing factor receptors. The compound can be used in treatment and/or prophylaxis of depression, anxiety state, disorders in food intake, post-traumatic stress, ulcerous disease, irritable bowel syndrome, Alzheimer's disease, abuse in drugs using or alcoholic syndrome dependence.

EFFECT: valuable medicinal properties of compounds and pharmaceutical agent.

7 cl, 1 dwg, 24 ex

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

SUBSTANCE: invention relates to new substituted pyrido[4',3':5,6]pyrano[2,3-d]pyrimidines of the general formula (1): or (2): or their pharmaceutically acceptable salts, N-oxides or hydrate possessing physiologically active properties, in particular, eliciting ability to induce apoptosis in tumor cells causing their death. In the general formula (1) or (2) X represents sulfur or oxygen atom; Y represents sulfur atom, group -SO, group -SO2, group -NH or group -NR6; R1 represents aryl, substituted aryl, heteroaryl; R2 and R5 represent hydrogen atom, alkyl, allyl, substituted benzyl, group -CH2-C(O)R3, group -CH2-C(O)NR3R4 wherein R3, R4 and R6 represent inert substitute. Also, invention relates to new combinatory libraries for search compound-leaders and candidates for medicinal compounds preparing by screening the combinatory libraries.

EFFECT: valuable medicinal properties of compounds.

9 cl, 1 tbl, 9 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a new substance eliciting an antiviral and antibacterial activity that is based on derivatives of 2,8-dithioxo-1H-pyrano[2,3-d;6,5-d']dipyrimidine and their 10-aza-analogues. This substance comprises derivative of indicated group of the general formula: A1*M: wherein X is taken among the group: oxygen atom (O), NH, N-alkyl; R1 is taken among the group: hydrogen atom (H), OH, chlorine atom (Cl), O-alkyl, NH2, NH-alkyl, NH-Ar, N-(alkyl)2, SH, S-alkyl; R2 is taken among the group: unsubstituted or substituted phenyl, naphthyl, thienyl; R3 is taken among the group: hydrogen atom (H), chlorine atom (Cl), O-alkyl, NH2, NH-alkyl, S-dihydroxypyrimidinyl; M is absent or taken among the group: cation Na, K, Li, ammonium or any other pharmacologically acceptable cation; or complex of pharmacologically acceptable cation (see above) with anion of one of derivatives of A1 (variants R1-R3 are given above). Invention provides preparing new compounds eliciting an antiviral and antibacterial activity.

EFFECT: valuable medicinal properties of substance.

17 cl, 7 tbl, 16 ex

The invention relates to a method for producing a condensed polycyclic alkaloids of General formula I, including new, including phase cyclization of azometynoylid General formula II, where a is optionally substituted aryl, Z is oxygen, n = 1, Y is optionally substituted aryl, W and X together with the nitrogen atoms and the carbon to which they are attached, form a saturated or unsaturated nitrogen-containing heterocyclic group, possibly substituted and possibly condensed with aryl, carbocyclic or heterocyclic group

The invention relates to novel condensed pyrrolo (2,3-C)carbazole-6-Onam represented by the General formulas (I) and (II)

The invention relates to new derivatives of 5H-pyrano[2,3-d:6,5-d']dipyrimidine General formula I possess anti-microbial, antiviral and immunomodulatory effects

FIELD: chemistry.

SUBSTANCE: claimed are novel pyrazole derivatives of formula II or its pharmaceutically acceptable salts, where C ring is selected from phenyl or pyridinyl ring and R2, R2', Rx and Ry are such as said in given description. C ring has ortho-substituent and is optionally substituted in non-ortho positions. R2 and R2' , optionally taken with their intermediate atoms, form condensed ring system, such s indazole ring, and Rx and Ry, optionally taken together with their intermediate atoms, form condensed ring system, such a quinazoline ring.

EFFECT: possibility to use compositions as inhibitors of protein kinases as inhibitors GSK-3 and other kinases and apply them for protein kinase-mediated diseases.

41 cl, 8 tbl, 423 ex

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