Some substituted amides, method of their obtaining and method of their application

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula 2: and to its pharmaceutically acceptable salts and their mixtures, where values of R, M, Q, Z, W, D radicals are described in i.1 of the invention formula. Invention also relates to pharmaceutical compositions, which possess inhibiting activity with respect to Btk, based on formula 2 compounds.

EFFECT: obtained are novel compounds and based on them pharmaceutical compositions which can be applied in medicine for treatment of patients with diseases associated with inhibiting Btk activity and/or B-cell activity.

55 cl, 19 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula 2

or its pharmaceutically acceptable salt, or a mixture, where
R is selected from substituted phenyl selected from monosubstituted phenyl, where the substituents independently selected from lower alkyl, sulfonyl, lower alkyl, substituted by one or more atoms of halogen, lower alkyl, substituted hydroxy, lower alkyl, substituted lower alkoxy, piperidinyl, piperidinyl, substituted hydroxy or lower alkyl, and imidazolyl, pyridyl,
substituted pyridyl selected from monosubstituted of pyridyl, where the substituents independently selected from lower alkyl,
substituted pyrimidinyl selected from monosubstituted of pyrimidinyl, where the substituents independently selected from lower alkyl,
substituted pyrazinyl selected from monosubstituted of pyrazinyl, where the substituents independently selected from lower alkyl,
substituted pyridazinyl selected from monosubstituted of pyridazinyl, where the substituents independently selected from lower alkyl,
4,5,6,7-tetrahydrobenzo[b]thiophene-2-Il,
substituted 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl selected from monosubstituted 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl, where
substituents independently selected from lower alkyl, and
substituted benzo[b]thiophene-2-yl chosen from monogamist the CSOs benzo[b]thiophene-2-yl, where the substituents independently selected from lower alkyl;
M is a covalent bond;
Q is a
,,,,
where R13represents hydrogen,
Z is selected from optionally substituted phenylene and optionally substituted of pyridylimino, where the substituents are selected from lower alkyl and halogen;
W-D is a

where R16selected from hydrogen and lower alkyl, and
D represents-N(H)-B-L-G, where
Selected from phenylene,






and
where
* indicates the point of joining the group-L-G and intermittentindicates the attachment point to the amino group;
X1represents CR31;
X2represents CR31;
X3represents CR31;
R30represents hydrogen;
R31represents hydrogen;
L is selected from C0-C4alkylene, -O-C0-C4alkylene -(C0-C4alkylen)(SO2)- and -(C0-C4alkylen) (=O)-;
G is selected from hydrogen, halogen, hydroxy, alkoxy, nitro, lower alkyl, carbamimidoyl, replaced by morpholinium or-NHCH3, tetrahydropyranyl, -NR7R8where R7and R8independently selected from hydrogen, acyl, substituted tetrahydrofuranyl, pyridinyl, thiazolyl, pyrrolidinyl, -OS2H5and optionally substituted (C1-C6)alkyl, substituted hydroxy; or R7and R8together with the nitrogen atom to which they are bound, form an optionally substituted 5-7-membered nitrogen containing heteroseksualci, which optionally further includes one or two additional heteroatoms selected from N, O and S, and where the substituents are selected from hydroxy, cyano, aminooxy and lower ALK is La.

2. The compound according to claim 1 where Z is selected from orthophenylene, metaphenylene, paraphenylene, orthopaedician, methapyrilene and properidine, each of which is optionally substituted by a group selected from lower alkyl and halogen.

3. The compound according to claim 2, where Z is selected from metaphenylene and metaphenylene substituted by a group selected from lower alkyl and halogen.

4. The compound according to claim 3, where Z is selected from metaphenylene and metaphenylene substituted by a group selected from methyl and halogen.

5. The compound according to claim 1, where the compound of formula 2 has the formula 3

where
R3selected from optionally substituted piperidinyl, tertbutyl and isopropyl;
X is selected from CH and N;
R1and R2independently selected from hydrogen, lower alkyl and halogen, provided that at least one of R1and R2does not represent hydrogen.

6. The compound according to claim 5, where X represents CH.

7. The compound according to claim 5, where X represents N.

8. The compound according to claim 5, where R1and R2independently selected from hydrogen, methyl and fluorine.

9. The connection of claim 8, where R1selected from methyl and fluorine, and R2represents hydrogen.

10. The connection of claim 8, where R1and R2independently selected from methyl and fluorine.

11. The compound according to claim 1, which has the formula 5

where R22denotes hydrogen,
R16selected from hydrogen, lower alkyl.

12. The compound according to claim 1, which has the formula 7

where R22denotes hydrogen,
R4selected from hydrogen, lower alkyl and halogen,
R16selected from hydrogen, lower alkyl.

13. The compound according to claim 1, where a is selected from orthophenylene, metaphenylene, paraphenylene,
and

14. The connection indicated in paragraph 13, where selected from paraphenylene and metaphenylene.

15. The connection 14, where In represents metaphenylene.

16. The connection indicated in paragraph 13, where selected from
and.

17. The compound according to claim 1, where R is selected from 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl and substituted 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl selected from monosubstituted 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl, where the substituents independently selected from lower alkyl.

18. The connection 17, where R is selected from 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl and substituted 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl selected from monosubstituted 4,5,6,7-tetrahydrobenzo[b]thiophene-2-yl, where the Deputy is lower alkyl.

19. Connection p, where R represents a substituted phenyl selected from monosubstituted FeNi is a, where the substituents independently selected from lower alkyl, sulfonyl, lower alkyl, substituted by one or more atoms of halogen, lower alkyl, substituted hydroxy, lower alkyl, substituted lower alkoxy, piperidinyl and imidazolyl.

20. The connection according to claim 19, where R represents a substituted phenyl selected from monosubstituted phenyl, where the substituents independently selected from lower alkyl, piperidinyl, optionally substituted by hydroxy or lower alkyl, and imidazolyl.

21. Connection claim 20, where R is a 4-lower alkylphenyl.

22. Connection item 21, where R is a 4-tertbutylphenyl.

23. Connection item 21, where R is a 4-isopropylphenyl.

24. Connection claim 20, where R is a phenyl, substituted optionally substituted by piperidinyl.

25. The connection section 12, which has the formula 9

where X is selected from N and CH;
U is selected from N and CR41;
R41represents hydrogen;
R5selected from hydrogen, lower alkyl, sulfonyl, lower alkyl, substituted hydroxy, lower alkyl, substituted by one or more atoms of halogen, lower alkyl, substituted hydroxy, and optionally substituted piperidinyl,
R16selected from hydrogen, lower alkyl.

26. The connection 14, where L is selected from the 0-C4alkylene, -O-C0-C4alkylene -(C0-C4alkylen)(SO2)- and -(C0-C4alkylen)(C=O)-.

27. Connection p, where L is selected from -(C=O)-, -CH3-, -CH3(C=O)-, -SO2- , and-CH(CH3) (=O)-.

28. The connection point 24, which has the formula 12

where f is selected from 0, 1 and 2.

29. Connection p, which has the formula 13
.

30. The connection clause 29, where G is-C(O)-(CH2)fattached at the 3-position of the ring.

31. The connection clause 29, where G is-C(O)-(CH2)fattached at the 4-position of the ring.

32. Connection A.25, where G is selected from hydrogen, hydroxy, -NR7R8where R7and R8independently selected from hydrogen, acyl, substituted tetrahydrofuranyl, pyridinyl, thiazolyl, pyrrolidinyl, -OS2H5and optionally substituted (C1-C6)alkyl, substituted hydroxy, or R7and R8together with the nitrogen atom to which they are bound, form an optionally substituted 5-7-membered nitrogen containing heteroseksualci, which optionally further includes one or two additional heteroatoms selected from N, O and S, and where the substituents are selected from hydroxy, cyano, aminooxy and lower alkyl.

33. Connection p, where G is selected from hydrogen, hydroxy, N is melatonine, optionally substituted morpholine-4-yl, optionally substituted piperazine-1-yl and optionally substituted homopiperazin-1-yl.

34. Connection p, where G is selected from hydrogen, morpholine-4-yl, 4-arylpiperazine-1-yl, 4-lower alkylpiperazine-1-yl, 3-oxopiperidin-1-yl, homopiperazin-1-yl and 4-lower alkyl-homopiperazin-1-yl.

35. Connection p, which has the formula 15

where R7and R8independently selected from hydrogen and optionally substituted (C1-C6)alkyl; or R7and R8together with the nitrogen atom to which they are bound, form an optionally substituted 5-7-membered nitrogen containing heteroseksualci, which optionally also includes one or two additional heteroatoms selected from N, O and S.

36. The compound according to claim 1, which has the formula 17

where X is selected from N and CH;
R5selected from hydrogen, lower alkyl, sulfonyl, lower alkyl, substituted hydroxy, lower alkyl, substituted by one or more atoms of halogen, lower alkyl, substituted hydroxy, and optionally substituted piperidinyl,
R4selected from hydrogen, optionally substituted lower alkyl, halogen;
R16selected from hydrogen and optionally substituted lower alkyl; and
R22isone hydrogen.

37. The compound according to claim 1, which has the formula 19

where X is selected from N and CH;
R5selected from hydrogen, lower alkyl, sulfonyl, lower alkyl, substituted hydroxy, lower alkyl, substituted by one or more atoms of halogen, lower alkyl, substituted hydroxy, and optionally substituted piperidinyl,
R4selected from hydrogen, optionally substituted lower alkyl, halogen;
R16selected from hydrogen and optionally substituted lower alkyl;
R22represents hydrogen.

38. The compound according to claim 1, which has the value of the IC5010 μm or less in the biochemical analysis of in vitro activity of Btk.

39. Connection § 38, which has a value IC501 μm or less in the biochemical analysis of in vitro activity of Btk.

40. Connection § 39, which has a value IC50of 0.1 μm or less in the biochemical analysis of in vitro activity of Btk.

41. The compound according to claim 1, which has the value of the IC5010 μm or less in the analysis of inhibition of b-cell activity.

42. The connection at paragraph 41, which has a value IC501 μm or less in the analysis of inhibition of b-cell activity.

43. Connection § 42, which has a value IC50500 nm or less in the analysis of inhibition of b-cell activity.

44. The compound according to claim 1, which has the value of the IC50in the analysis of inhibition of T-cell proliferation, at least 3 times greater than the value of the IC50that shows the connection in the analysis of inhibition of b-cell proliferation.

45. Connection item 44, which has a value IC50in the analysis of inhibition of T-cell proliferation, at least 5 times greater than the value of the IC50that shows the connection in the analysis of inhibition of b-cell proliferation.

46. Connection § 45, which has a value IC50in the analysis of inhibition of T-cell proliferation, at least 10 times greater than the value of the IC50that shows the connection in the analysis of inhibition of b-cell proliferation.

47. The compound according to claim 1, which has the value of the IC5010 μm or less in the analysis on the survival of B cells-ALL.

48. The connection of claim 10, where which represents one of the following connections:
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-(morpholine-4-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridines-3-yl}phenyl)benzamide;
4-{5-[3-(4-tert-butylbenzylamine)-2-were]-1-methyl-2-oxo-1,2-dihydropyridines-3-ylamino}benzoic acid;
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridines-3-yl}phenyl)benzamide;
4-tert-butyl-N - (2-methyl-3-{1-methyl-5-[4-(N-methylethanolamine-2-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridin-3-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-([1,4]-oxazepan-4-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridines-3-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{5-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-1-methyl-6-oxo-1,6-dihydropyridines-3-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-(morpholine-4-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridines-3-yl}phenyl)benzamide;
4-{5-[3-(4-tert-butylbenzylamine)-2-were]-1-methyl-2-oxo-1,2-dihydropyridines-3-ylamino}benzoic acid;
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridines-3-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-(N-methylethanolamine-2-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridin-3-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{1-methyl-5-[4-([1,4]oxazepan-4-carbonyl)phenylamino]-6-oxo-1,6-dihydropyridines-3-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{5-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-1-methyl-6-oxo-1,6-dihydropyridines-3-yl}-2-were)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
ethyl Efir-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-metile the Razin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methyl-[1,4]diazepan-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{4-methyl-6-[4-(2-
hydroxyethylmethylcellulose)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-ethyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-ethyl-6-[4-(N-methylethanolamine-2-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(methylcarbamoyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(4-forgenerating)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4,5-dimethyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-Formentera acid;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(methylcarbamoyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-methylp the Nile)benzamide;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(2-hydroxyethylaminomethyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(1H-indazol-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{3-[6-(1H-indazol-5-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)pentamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[3-fluoro-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(1H-imidazol-2-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(4-methanesulfonylaminoethyl)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{4-methyl-6-[4-(3-aminopropylsilyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(1H-imidazol-2-yl)phenylamino]-4-methyl-5-oxo-4,5-dihyd operatin-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(thiomorpholine-4-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ4-thiomorpholine-4-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[4-(1,1-dioxo-N-thiomorpholine-4-
carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(4-sulfhemoglobinemia)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-5-oxo-6-(4-sulfhemoglobinemia)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(1H-tetrazol-5-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
ethyl ester of 4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methyl-[1,4]diazepan-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{4-methyl-6-[4-(2-
hydroxyethylation email)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-ethyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-ethyl-6-[4-(N-methylethanolamine-2-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(methylcarbamoyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(4-forgenerating)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4,5-dimethyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-Formentera acid;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(methylcarbamoyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzo the MFA;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(2-hydroxyethylaminomethyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(1H-indazol-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{3-[6-(1H-indazol-5-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl)phenyl)benzamide;
4-tert-butyl-N-(3-{6-[3-fluoro-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(1H-imidazol-2-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(5-{6-[4-(1H-imidazol-2-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(4-methanesulfonylaminoethyl)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{4-methyl-6-[4-(3-aminopropylsilyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(1H-imidazol-2-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(thiomorpholine-4-carbonyl)phenylamino]-4,5-dihydropyrazol the-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ6-thiomorpholine-4-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[4-(1,1-dioxo-1λ6-thiomorpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(4-sulfhemoglobinemia)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-5-oxo-6-(4-sulfhemoglobinemia)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-methyl-5-[4-methyl-5-oxo-6-(4-sulfhemoglobinemia)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(1H-tetrazol-5-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)phenyl]-4,5-dimethyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(3-{3,4-dimethyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[3-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(N,N-bis-(2-hydroxyethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N,N-bis-(2-hydroxyethyl)aminocarbonyl)phenylamino]-5-about the co-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1H-tetrazol-5-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
morpholine-4-silt ether 4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzosulfimide acid;
N-{3-[6-(1H-benzoimidazol-5-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-(morpholine-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-(2-cyano-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(6-hydroxypyridine-3-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{6-[4-(4-ethylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(3-oxopiperidin-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(1λ6N-methyl-N-(cyanomethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(6-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}pyridine-2-yl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(2-methoxyethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-2-dimethylaminoethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-6-(4-(morpholine-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-oxazol-2-ilfenomeno)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-6-(4-oxazol-2-ilfenomeno)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-{3-[6-(4-imidazol-1-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{2-fluoro-3-[6-(4-imidazol-1-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(N,N-bis-(2-methoxyethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-(3-{6-[4-(4-acetylpiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[4-(4-acetylpiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)-4-tert-butylbenzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(thiomorpholine-4-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(4-hydroxypiperidine-1-
carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-
yl}phenyl)benzamide;
4-bromo-N-(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ6-thiomorpholine-4-carbonyl)phenyl) - Rev. Ino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-(1-hydroxy-1-methylethyl)-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(4-thiomorpholine-4-ilfenomeno)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-{3-[6-(4-imidazol-1-iletilenlerin)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-bromo-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-([1,4]oxazepan-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-forfinal]-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(4-oxopiperidin-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(4-hydroxyethylpiperazine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(2-hydroxymethylpropane-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ6-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(N-(2,2-dimethyl-[1,3]dioxolane-4-and is methyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylthiophene-2-carboxylic acid;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-6-(4-(morpholine-4-ilfenomeno)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(N-(2-(2-hydroxyethoxy)ethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{2-fluoro-3-[6-(4-imidazol-1-iletilenlerin)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-([1,4]oxazepan-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(N-(2,3-dihydroxypropyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-5-oxo-6-(4-thiomorpholine-4-iletilenlerin)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(4-hydroxyethylpiperazine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(2-hydroxymethylpropane-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(1,1-dioxo-1λ4-thiomorpholine-4-phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-methylphe the Il)benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-5-oxo-6-(4-thiomorpholine-4-ilfenomeno)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butylcyclohexanecarboxylic acid(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide;
4-tert-butyl-N-(3-{4-ethyl-5-oxo-6-[4-(1-oxo-1λ4-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}-2-were)benzamide;
4-dimethylamino-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ6-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(4-oxo-4H-pyridin-1-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-isopropyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ4-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-(1-hydroxy-1-methylethyl)-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ6-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-5-oxo-6-(4-pyrrolidin-1 iletilenlerin)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(2-hydroxymethylpropane-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ6-thiomorpholine-4-ylmethyl)phenylamino]-4,5-dihydropyrazine-2-ylphenyl)benzamide;
4-tert-butyl-N-(3-{6-[4-(1,1-dioxo-1λ6-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-N-(2-methoxyethyl)-1λ6-methylaminoacenaphthylene]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(4-methylpiperazin-1λ6-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(4-hydroxypiperidine-1λ6-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo--1λ6-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
4-{6-[3-(4-tert-butylbenzylamine)-2,4-differenl]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(4-methoxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-methyl-N-ethylaminomethyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyrrolidin-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-3-phenylacrylate;
N-(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-3-(3-forfinal)acrylamide;
(2-photo the-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amidase[b]thiophene-2-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amidase[b]thiophene-2-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-bromothiophene-2-carboxylic acid;
(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-bromothiophene-2-carboxylic acid;
N-(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-methylsulfonylbenzoyl;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-methylsulfonylbenzoyl;
4-ethylsulfanyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)lebensform-2-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4,5-dibromothiophene-2-carboxylic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[6-(1-oxo-1N-thiomorpholine-4-yl)-pyridine-3-ylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2,6-debtor-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-cyclopropyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-ylphenyl)benzamide;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(1-oxo-and-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-1N-{3-[6-(3-fluoro-4-thiomorpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-1N-(3-{6-[3-fluoro-4-(1-oxo-1λ6-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
4-tert-butyl-N-(3-{6-[4-(4-methoxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(4-methanesulfonylaminoethyl-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-fluoro-3-{6-[4-(4-methanesulfonylaminoethyl-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4-tert-butylcyclohexanecarboxylic acid;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-(morpholine-4-ilfenomeno)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(ethylmethylamino)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(ethylmethylamino)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-meth is l-6-(2-morpholine-4-espiridion-4-ylamino)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1N-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide benzo[b]thiophene-2-carboxylic acid;
N-(3-{6-[4-(4-acetylpiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)-4-tert-butylbenzamide;
N-(3-{6-[4-(4-acetylpiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
4-tert-butyl-N-{3-[6-(4-hydroxyethylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-1N-(3-{6-[4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(4-piperidine-1-ilfenomeno)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-1N-{2-methyl-3-[4-methyl-5-oxo-6-(4-pyridin-4-ilfenomeno)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-fluoro-3-[4-methyl-6-(4-methylaminomethyl)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(3-ethyl-1-methyluridine)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)benzamide;
4-tert-butyl-N-{3-[6-(3-hydroxyethylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{6-[4-(3-hydroxypyrrolidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(4-pyridine-3-ilfenomeno)-4,5-dihydropyrazol--yl]phenyl}benzamide;
4-tert-butyl-N-[2-fluoro-3-(6-{4-[(methysulfonylmethane)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)phenyl]benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxypyridine-3-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
amide 1-(4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)piperidine-4-carboxylic acid;
4-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)N-methylbenzamide;
N-(3-{6-[4-(4-acetyl-[1,4]diazepan-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
4-tert-butyl-N-(3-{6-[4-(4-methanesulfonyl-[1,4]diazepan-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-ethyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
amide 1-(4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)piperidine-3-carboxylic acid;
amide 1-(4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)pyrrolidin-2-carboxylic acid;
4-tert-butyl-1N-{2-methyl-3-[4-methyl-5-oxo-6-(pyridine-4-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(1,1-dioxo-1λ6-thiomorpholine-4-phenylamino]-4-ethyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;br/> 4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(1-oxypyridine-3-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(1-oxypyridine-4-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-(3-{6-[4-(1,4-dioxa-8 azaspiro[4,5]Dec-8-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(4-carbamidomethylation)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{4-cyclopropyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(3-dimethylaminomethylene)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(pyridine-4-ylmethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(pyridine-3-ylmethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
6-tert-butyl-N-(3-{6-[4-(1,1-dioxo-1λ4-thiomorpholine-4-phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxypyridine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(1-ethyl-2-oxo-1,2-dihydropyridines-4-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{4-cyano-6-[4-(morpholine-4-carbonyl)Fe is ylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(piperidine-4-yl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(3-morpholine-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl] phenyl}benzamide;
(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ4-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide 5,6,7,8-tetrahydronaphthalen-2-carboxylic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(1-ethylpiperazin-4-yl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(4-hydroxyphenylazo)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(3-nitrophenylamino)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-{3-[6-(4-methanesulfonamido)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-{3-[6-(3-aminophenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(piperidine-4-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(3-hydroxytyramine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(2-pyridin-4-retil)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(2-methylthiazole-4-yl)phenylamino]-5-OK, what about the-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(2-morpholine-4-ylethoxy)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1N-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1N-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide 6-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-N-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)-4-piperidine-1-ylbenzene;
6-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-(morpholine-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(3-AMINOPHENYL)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-(3-{6-[4-(4-aminopiperidin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
4-tert-butyl-N-(3-{6-[4-(1-ethylpiperazin-4-yloxy)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
N-{3-[6-(benzothiazol-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
N-(3-{6-[4-(2-aminopyridine-4-ylethoxy)phenylamino]-4-methyl-5-oxo-4,5-digidropiridina-2-yl}-2-were)-4-tert-butylbenzamide;
4-tert-butyl-N-[3-(6-{4-[4-(2-hydroxyethyl)piperazine-1-carbonyl]phenylamino}-4-methyl-5-oxo-4,5-dihydro shall irisin-2-yl)-2-were]benzamide;
4-tert-butyl-N-{3-[6-(2,3-dihydrobenzo[1,4]dioxin-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(2-fluoro-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(2-morpholine-4-ylacetic)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1λ4-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide 5-tert-butylpyridinium-2-carboxylic acid;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-piperidine-1-ylbenzene;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-piperidine-1-ylbenzene;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyridine-4-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyridine-4-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
4-tert-butyl-N-[3-(6-{4-[4-(2-hydroxyethyl)piperazine]-1-yl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
6-tert-butyl-N-[3-(6-{4-[4-(2-hydroxyethyl)piperazine-1-yl]phenylamino}-4-methyl-5-oxo-4,5-di is itoperates-2-yl)-2-were]nicotinamide;
N-{3-[6-(3-aminophenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-6-tert-butylnitrone;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 3,4,5,6-tetrahydro-2N-[1,2']bipyridinyl-5'-carboxylic acid;
N-{3-[6-(2-aminopyridine-4-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N,N-bis-(2-methoxyethyl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylpyridinium-2-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylpyridinium-2-carboxylic acid;
4-iodine-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-{3-[6-(3-benzylaminopurine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(2-morpholine-4-ylethoxy)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(tetrahydropyran-4-yl)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-[2-methyl-3-(4-methyl-5-oxo-6-{4-[(tetrahydropyran-4-ylamino)methyl]phenylamino}-4,5-dihydropyrazol-2-yl)phenyl]be same;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-pyrrolidin-1-ylbenzene;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-2-carboxylic acid;
4-tert-butyl-N-(3-{6-[3-(cyclohexanecarbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
N-{3-[6-(3-amino-4-forgenerating)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5,6-dihydro-4H-cyclopent[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[1-(2-morpholine-4-retil)-2-oxo-1,2-dihydropyridines-4-ylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-(2-methyl-3-{4-methyl-6-[4-(1-methylpiperidin-4-yloxy)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-piperidine-1-ylbenzene;
6-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-(3-{6-[4-(4-ethylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
6-tert-butyl-N-[3-(6-{4-[4-(2-hydroxyethyl)piperazine-1-carbonyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]nicotinamide;
4-(6-{3-[(6-tert-butylpyridinium-3-carbonyl)amino]-2-were}-4-methyl-3-the CSR-3,4-dihydropyrazine-2-ylamino)benzoic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide benzo[b]thiophene-5-carboxylic acid;
6-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methyl-[1,4]diazepan-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[3-(pyridine-3-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[3-(pyridine-3-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4,4-DIMETHYLPROPANE-7-carboxylic acid;
6-tert-butyl-N-(3-{6-[4-(2-hydroxymethylpropane-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
6-tert-butyl-N-(2-fluoro-3-{6-[4-(2-hydroxymethylpropane-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[3-(pyridine-4-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[3-(pyridine-4-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-(3-{6-[4-(2-hydroxymethylpropane-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
6-tert-butyl-N-(2-fluoro-3-{6-[4-(2-hydroxymethylpropane-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)shall nicotinamide;
6-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(4-methyl-[1,4]diazepan-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-(3-{6-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
6-tert-butyl-N-(2-fluoro-3-{6-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-nitrophenylamino)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
N-{3-[6-(4-aminophenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
N-(3-{6-[4-(4-aminopiperidin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-6-tert-butylnitrone;
4-(6-{3-[(6-tert-butylpyridinium-3-carbonyl)amino]-2-forfinal}-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino)benzoic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyridine-3-ylethoxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyridine-3-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyridine-3-yloxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(piperazine-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-[2-fluoro-3-(6-{4-[4-(2-hydroxyethyl)piperazine-1-yl]phenyl is Mino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)phenyl]nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-yl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[4-(4-ethylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(N-(hydroxy)aminocarbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-{3-[6-(3-aminophenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-piperidine-1-ylbenzene;
6-tert-butyl-N-[3-(6-{4-[(2-hydroxyethyl)methylcarbamoyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]nicotinamide;
6-tert-butyl-N-(3-{6-[4-(cyanomethylation)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(3-oxopiperidin-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
N-(3-{6-[4-(4-ethylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-piperidine-1-ylbenzene;
6-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-yl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-(3-{6-[4-(4-ethylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
N-{2-methyl-3-[4-methyl-6-(4-(morpholine-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}-4-piperidine-1-ylbenzene;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(N-(1-aminoacridine))phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(3-cyclopropanemethylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(3-piperidine-1-iletilenlerin)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-[3-(6-{3-[(cyanomethylene)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
amide 1-(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzyl)piperidine-4-carboxylic acid;
4-tert-butyl-N-{3-[6-(3-{[(2-hydroxyethyl)methylamino]methyl}phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-[3-(6-{3-[(2-hydroxyethylamino)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-(3-{6-[3-(4-hydroxypiperidine-1-ylmethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[3-(2-hydroxymethylpropane-4-ylmethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
(4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-2-carboxylic acid;
(4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-3-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydrospiro the Jn-2-yl}phenyl)amide 3,4,5,6-tetrahydro-2N-[1,3']bipyridinyl-6'-carboxylic acid;
6-tert-butyl-N-(2-fluoro-3-{4-methyl-5-oxo-6-[4-(piperazine-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
N-(3-{6-[4-(1,1-dioxo-and-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-piperidine-1-ylbenzene;
6-tert-butyl-N-(3-{6-[4-(1,1-dioxo-1λ4-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)nicotinamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amid-tert-butylpyridinium-5-carboxylic acid;
6-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(pyridine-3-ylethoxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)nicotinamide;
N-(3-{6-[4-(4-aminopiperidin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)-6-tert-butylnitrone;
6-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylpiperazine-2-carboxylic acid;
6-tert-butyl-N-(2-fluoro-3-{6-[4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
N-(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-yl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-piperidine-1-ylbenzene;
N-(3-{6-[4-(4-ethylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-methylpheni is)-4-piperidine-1-ylbenzene;
6-tert-butyl-N-(2-fluoro-3-{4-methyl-6-[4-(4-methylpiperazin-1-yl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)nicotinamide;
6-tert-butyl-N-(3-{6-[4-(4-ethylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)nicotinamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(4-oxopiperidin-1-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
N-(3-{6-[4-(3-aminopropylsilyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)-6-tert-butylnitrone;
N-(3-{6-[4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-piperidine-1-ylbenzene;
6-tert-butyl-N-(3-{6-[4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were)nicotinamide;
4-azepin-1-yl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-fluoro-3-{6-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylpyridinium-2-carboxylic acid;
N-{3-[5-(3-aminophenylamino)-1-methyl-6-oxo-1,6-dihydropyridines-3-yl]-2-were}-4-tert-butylbenzamide;
(3-{5-[3-(4-tert-butylbenzylamine)-2-were]-1-methyl-2-oxo-1,2-dihydropyridines-3-ylamino}phenyl)literarymaven-2-carboxylic acid;
4-tert-butyl-N-{3-[1,4-dimethyl-5-(4-(morpholine-4-yl)phenylamino)-6-oxo-1,6-dihydropyridines-3-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{5-[4-(1,1-d is oxo-1N-thiomorpholine-4-yl)phenylamino]-1-methyl-6-oxo-1,6-dihydropyridines-3-yl}-2-were)benzamide;
6-tert-butyl-N-(3-{6-[4-(carbamoylmethyluridine)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
6-tert-butyl-N-{3-[6-(4-hydroxycarbamoyl)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}nicotinamide;
(3-{6-[4-(4-ethylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpyridinium-2-carboxylic acid;
N-(3-{6-[4-(4-aminopiperidin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
4-{6-[3-(4-(1-piperidinyl)benzoylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzohydroxamic acid;
(3-{6-[4-(1,1-dioxo-1N-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpyridinium-2-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylpiperazine-2-carboxylic acid;
(3-{6-[4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpyridinium-2-carboxylic acid;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-(4-methylpiperidin-1-yl)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(5-methyl-1H-pyrazole-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
(3-{6-[4-(2-hydroxymethylpropane-4-yl)phenylamino]-4-IU the Il-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpyridinium-2-carboxylic acid;
N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(3-oxopiperidin-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)-4-piperidine-1-ylbenzene;
4-(1-piperidinyl)-N-(3-{4-methyl-6-[4-(2-hydroxyethylaminomethyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(1H-pyrazole-3-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
N-(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)isonicotinamide;
(3-{6-[4-(1,1-dioxo-1N-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpiperazine-2-carboxylic acid;
(3-{6-[3-(4-tert-butylbenzylamine)-2-forfinal]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-2-carboxylic acid;
(3-{6-[4-(carbamoylmethyluridine)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpyridinium-2-carboxylic acid;
(3-{6-[4-(carbamoylmethyluridine)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-(3-methylpiperidin-1-yl)benzamide;
N-{3-[6-(3-acetylaminophenol)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-3-carboxylic acid;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)amitiza-4-carboxylic acid;
ethyl ester of(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)carbamino acid;
4-tert-butyl-N-(3-{6-[3-(2-methoxyethylamine)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-tert-butylpyridinium-2-carboxylic acid;
4-(isopropylethylene)-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(2-methyl-3-{6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-1N-(3-{6-[4-(1,1-dioxo-1λ4-thiomorpholine-4-ylmethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
N-[2-methyl-3-(4-methyl-5-oxo-6-{4-[(tetrahydropyran-4-ylamino)methyl]phenylamino}-4,5-dihydropyrazol-2-yl)phenyl]-4-piperidine-1-ylbenzene;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-ylmethyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[4-(4-ethylpiperazin-1-ylmethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(4-{[(2-hydroxyethyl)methylamino]methyl}phenylamino)-4-methyl-5-oxo-4,5-Digi operatin-2-yl]-2-were}benzamide;
N-[3-(6-{4-[4-(2-hydroxyethyl)piperazine-1-carbonyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]-4-piperidine-1-ylbenzene;
amide 1-(4-{4-methyl-6-[2-methyl-3-(4-piperidine-1-albenzaalbenza)phenyl]-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)piperidine-4-carboxylic acid;
(3-{6-[4-(4-aminopiperidin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-tert-butylpiperazine-2-carboxylic acid;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-(4-methylpiperazin-1-ylmethyl)benzamide;
4-tert-butyl-N-[2-fluoro-3-(4-methyl-6-{3-[2-(4-methylpiperazin-1-yl)acetylamino]phenylamino}-5-oxo-4,5-dihydropyrazine-2-yl)phenyl]benzamide;
N-{3-[6-(3-aminophenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-forfinal}-4-tert-butylbenzamide;
N-{3-[6-(3-aminophenylamino)-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
(2-methyl-3-{4-methyl-5-oxo-6-[4-(piperazine-1-carbonyl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide 5-tert-butylpyridinium-2-carboxylic acid;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-2-carboxylic acid;
[3-(6-{2-methyl-3-[(4,5,6,7-tetrahydrobenzo[b]thiophene-2-carbonyl)amino]phenyl}-3-oxo-3,4-dihydropyrazine-2-ylamino)phenyl]literarymaven-2-carboxylic acid;
(5-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-ox is -3,4-dihydropyrazine-2-ylamino}-2-forfinal)literarymaven-2-carboxylic acid;
3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl ether acetic acid;
N-(2-methyl-3-{6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-piperidine-1-ylbenzene;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-2-ylethoxy)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amid-tert-butylpiperazine-3-carboxylic acid;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-imidazol-1-yl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[3-(3-methoxypropylamine)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)ameture-2-carboxylic acid;
6-tert-butyl-N-(3-{6-[4-(1,1-dioxo-and-thiomorpholine-4-yl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)nicotinamide;
4-tert-butyl-N-[3-(6-{4-[2-(4-ethylpiperazin-1-yl)ethoxy]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
tetrahydrofuran-3-silt ether(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)ka is benovoy acid;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)literarymaven-2-carboxylic acid;
N-{3-[6-(5-aminopyridine-3-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-{3-[6-(1H-indol-5-ylamino)-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)ameerally-2-carboxylic acid;
4-tert-butyl-N-(3-{6-[3-(2-hydroxyacetylamino)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-[3-(6-cyclopropylamino-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-[3-(6-hydroxy-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-(3-{6-[3-(2-ethoxyacetylene)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
N-{3-[6-(3-amino-4-methylphenylimino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-(3-{6-[4-(4-hydroxyethylpiperazine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[3-(2-hydroxy-2-methylpropionamide)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)amid tragedian-4-carboxylic acid;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(4-thiomorpholine-4-iletilenlerin)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-(4-hydroxypiperidine-1-yl)-1N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-{3-[6-(3-amino-4-chlorpheniramine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-(2-methylpiperidin-1-yl)benzamide;
(3-{6-[4-(1,1-dioxo-1λ4-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-{3-[6-(3-dimethylaminopropylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(piperidine-4-ylethoxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
4-tert-butyl-N-[3-(6-{4-[(2-hydroxyethylamino)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
phenyl ether(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)carbamino acid;
4-tert-butyl-N-{3-[6-(4-cyclopropanemethylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}be same;
4-tert-butyl-N-[3-(6-{4-[(carbamoylmethyl)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-(4-methoxypiperidine-l-yl)-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-(3-{6-[3-(2-aminoethylamino)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
(3-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)imidazolidin-2-carboxylic acid;
(5-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-were)literarymaven-2-carboxylic acid;
4-tert-butyl-N-(3-{6-[4-(4-hydroxy-4-methylpiperidin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
1-methyl-3-[4-(morpholine-4-carbonyl)phenylamino]-5-(2-phenylbenzoxazole-7-yl)-1H-pyrazin-2-he;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(1-methylpiperidin-2-ylethoxy)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
5-[2-(4-methoxyphenyl)benzooxazol-7-yl]-1-methyl-3-[4-(morpholine-4-carbonyl)phenylamino]-1H-pyrazin-2-he;
4-tert-butyl-N-{3-[6-(1H-indol-5-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-{3-[6-(3-aminoethylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-(3-{6-[4-(1-ethylpiperazin-4-ylethoxy)penilai what about]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(1-pyridine-4-ylmethyl-1H-indole-6-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-furan-2-yl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-(2-methoxy-1,1-dimethylethyl)N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[4-(4-hydroxy-4-methylpiperidin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{6-[4-(4-hydroxy-4-methylpiperidin-1-ylmethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
{3-[6-(3-aminophenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}amide 6-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-hydroxybenzoic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)-3-nitrophenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-ethyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4 azetidin-1-yl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-3-methoxy-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)Fenelon is but]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-methoxybenzoic acid;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 1,4,4-trimethyl-1,2,3,4-tetrahydroquinolin-7-carboxylic acid;
4-(1-methoxy-1-methylethyl)-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-(2,2-dimethylpropionic)N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-(3-{6-[3-methoxy-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-methoxy-N-(3-methoxypropyl)benzamide;
N-{3-[6-(3-acryloylmorpholine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-{3-[6-(1H-indol-4-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-[3-(6-{4-[(2-methoxyethylamine)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-{3-[6-(4-ethylaminomethyl)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{3-[6-(4-diethylaminoethylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-[3-(6-{4-[(isop is Obermeilen)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(2-methylpiperidin-1-ylmethyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-[2-methyl-3-(4-methyl-5-oxo-6-{4-[2-(tetrahydropyran-4-ylamino)ethyl]phenylamino}-4,5-dihydropyrazol-2-yl)phenyl]benzamide;
5-amino-2-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-N-cyclopropylbenzene;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 5-amino-benzo[b]thiophene-2-carboxylic acid;
2-amino-N-{3-[6-(benzothiazol-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-piperidine-1-ylbenzene;
4-tert-butyl-N-[3-(6-{2-[(2-hydroxyethyl)methylamino]-pyridine-4-ylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-(3-{6-[3-methoxy-4-(4-methylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-N-(2-hydroxyethyl)-2-methoxy-N-methylbenzamide;
4-tert-butyl-N-(3-{6-[3-methoxy-4-(piperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
N-{3-[6-(3-amino-4-morpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
N-{3-[6-(4-amino-2-piperidine-1-iletilenlerin)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-methylphe the yl}-4-tert-butylbenzamide;
(4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzylamino)acetic acid;
4-tert-butyl-N-[3-(6-{4-[(cyclopropylamino)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
N-{3-[6-(3-amino-4-thiomorpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-5-oxo-6-[4-(piperidine-3-ylethoxy)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)benzamide;
N-(3-{6-[3-amino-4-(1,1-dioxo-1λ4-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(piperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-5-oxo-6-(1,2,3,4-tetrahydroisoquinoline-6-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}benzamide;
4-tert-butyl-N-[3-(6-{4-[2-(4-ethylpiperazin-1-yl)ethyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-[3-(6-{4-[2-(2-hydroxyethylamino)ethyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-{3-[6-(4-{2-[(2-hydroxyethyl)methylamino]ethyl}phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-(3-{6-[4-(2-diethylaminoethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
2-Amin is-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-N-(2-hydroxyethyl)N-methylbenzamide;
4-[2-(2-methoxyethoxy)-1,1-dimethylethyl]N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-(3-methoxypiperidine-1-yl)N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-{3-[6-(4-hydroxymethyl-3-methoxybenzylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{3-[6-(1H-indol-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-(3-{6-[3-amino-4-(4-methylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(4-ethylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}N-(2-dimethylaminoethyl)benzamide;
4-tert-butyl-N-{2-methyl-3-[6-(4-(morpholine-4-yl-3-nitrophenylamino)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-(morpholine-4-yl-3-nitrophenylamino)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
N-{3-[6-(3-amino-4-morpholine-4-ilfenomeno)-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}N-(2-diethylaminoethyl)benzamide;
4-tert-butyl-N-(3-{4-this is l-6-[4-(phenylcarbamoyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-(3-{4-ethyl-6-[4-(2-methylphenylcarbinol)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)benzamide;
4-tert-butyl-N-{3-[6-(4-cyclopropylamino-3-methoxybenzylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{3-[6-(4-cyclopropylamino-3-methoxybenzylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
4-tert-butyl-N-{3-[6-(3-{2-[(2-hydroxyethyl)methylamino]ethyl}phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-(3-{6-[3-amino-4-(1-oxo-1λ4-thiomorpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
4-(1-methylcyclohexyl)-N-(2-ethyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-{3-[6-(4-{[bis-(2-hydroxyethyl)amino]methyl}phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-[3-(6-{3-[2-(2-hydroxyethylamino)ethyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[3-(2-morpholine-4-retil)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
4-tert-butyl-N-[3-(6-{3-[2-(1,1-dioxo-1λ4-thiomorpholine-4-yl)ethyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]benzamide;
4-tert-butyl-N-[3-(6-{3-[2-(4-ethylpiperazin-1-yl)ethyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyran the h-2-yl)-2-were]benzamide;
N-{3-[6-(3-{2-[bis-(2-hydroxyethyl)amino]ethyl}phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-tert-butyl-N-{3-[6-(3,4-dihydro-2H-benzo[1,4]oxazin-6-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-(3-{6-[4-(4-aminomethyl-4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}benzoic acid;
5-(3-amino-2-were)-1-methyl-3-(4-(morpholine-4-yl-3-nitrophenylamino)-1H-pyrazin-2-he;
{3-[6-(3-amino-4-morpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}amide 5-tert-butylpyridinium-2-carboxylic acid;,
{3-[6-(3-amino-4-morpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-{3-[6-(3-amino-4-morpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-piperidine-1-ylbenzene;
N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)-4-methylsulfonylbenzoyl;
N-{3-[6-(3-amino-4-cyclopropanemethylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-methyl-4,5,6,7-tetrahydro what Enzo[b]thiophene-2-carboxylic acid;
N-(3-{6-[3-amino-4-(thiomorpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-N-pyridin-3-ylbenzene;
N-(5-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-N-(2-methoxyethyl)-N-methylbenzamide;
(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)aminothiophenol-2-carboxylic acid;
N-(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-6-tert-butylnitrone;
N-{3-[6-(2-aminoindan-5-ylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)-4-tert-butylbenzamide;
N-{3-[6-(3-amino-4-methoxybenzylamine)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(1-oxo-1λ4-thiomorpholine-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3N-{6-[3-amino-4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzo the ID;
N-(3-{6-[3-amino-4-(4-ethylpiperazin-1-ylmethyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
amide 1-(2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)piperidine-4-carboxylic acid;
N-{3-[6-(3-amino-4-morpholine-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-forfinal}-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(4-ethylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[4-(4-aminomethyl-4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[4-(1,1-inocsa-1λ4-thiomorpholine-4-yl)phenylamino]-4-methyl-3-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-pentabromoethylbenzene;
{2-methyl-3-[4-methyl-6-(4-(morpholine-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-{3-[6-(3-amino-4-[1,4]oxazepan-4-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
(3-{6-[3-amino-4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thio is ene-2-carboxylic acid;
N-[3-(6-{3-amino-4-[4-(2-hydroxyethyl)piperazine-1-yl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]-4-tert-butylbenzamide;
4-tert-butyl-N-{3-[6-(3-methoxy-4-morpholine-4-iletilenlerin)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-(3-{6-[3-amino-4-(4-hydroxy-4-methylpiperidin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(2-morpholine-4-ylethoxy)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-[3-(6-{3-amino-4-[(2-methoxyethyl)methylamino]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]-4-tert-butylbenzamide;
methyl Efir-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-methylbenzoic acid;
4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}-2-methylbenzoic acid;
(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-forfinal)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-1N-{2-methyl-3-[4-methyl-6-(3-methyl-4-morpholine-4-ilfenomeno)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
[2-methyl-3-(4-methyl-5-oxo-6-{4-[(tetrahydropyran-4-ylamino)methyl]phenylamino}-4,5-dihydropyrazol-2-yl)phenyl]amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-[1,4]oxazepan-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
{3-[6-(4-hydroxyethylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
[3-(6-{4-[(carbamoylmethyl)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
1-(2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)-4-hydroxypyridine;
N-[3-(6-{3-amino-4-[(2-hydroxyethyl)methylamino]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-piperidine-1-ylbenzene;
N-(3-{6-[3-amino-4-(4-methylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
(2-methyl-3-{4-methyl-5-oxo-6-[4-(1-oxo-1N-thiomorpholine-4-yl)phenylamino]-4,5-dihydropyrazol-2-yl}phenyl)amide 5,6,7,8-tetrahydronaphthalen-2-carboxylic acid;
(2-methyl-3-{4-methyl-6-[4-(4-methylpiperazin-1-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
[2-methyl-3-(4-methyl-5-oxo-6-{4-[(tetrahydropyran-4-ylamino)methyl]phenylamino}-4,5-dihydropyrazol-2-yl)phenyl]amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-{2-methyl-3-[4-methyl-6-(4-[1,4]oxazepan-4-iletilenlerin)-5-oxo-4,5-dihydropyrazine-2-yl]phenyl}benzamide;
{3-[6-(4-hydroxyethylamino)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
[3-(6-{4-[(carbamoylmethyl)methyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 5-methyl-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(4-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
1-(2-amino-4-{6-[3-(4-tert-butylbenzylamine)-2-were]-4-methyl-3-oxo-3,4-dihydropyrazine-2-ylamino}phenyl)-4-hydroxypyridine;
N-[3-(6-3-amino-4-[(2-hydroxyethyl)methylamino]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-piperidine-1-ylbenzene;
N-(3-{6-[3-amino-4-(4-methylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
(3-{6-[3-amino-4-(4-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-(3-{6-[3-amino-4-(3-hydroxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(3-hydroxypyrrolidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N - {3-[6-(3-amino-4-piperidine-1-ilfenomeno)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}-4-tert-butylbenzamide;
4-(2-hydroxy-1,1-dimethylethyl)N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
amide 1-[2-amino-4-(4-methyl-6-{2-methyl-3-[(4,5,6,7-tetrahydrobenzo[b]thiophene-2-carbonyl)amino]phenyl}-3-oxo-3,4-dihydropyrazine-2-ylamino)benzoyl]piperidine-4-carboxylic acid;
(3-{6-[3-amino-4-(3-hydroxypyrrolidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(4-ethylpiperazin-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,7 tetrahydrobenzo[b]thiophene-2-carboxylic acid;
(3-{6-[3-amino-4-(3-hydroxypiperidine-1-carbonyl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
N-(3-{6-[3-amino-4-(4-methyl-[1,4]diazepan-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(2-hydroxymethylpropane-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(4-hydroxyethylpiperazine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
amide 1-[2-amino-4-(4-methyl-6-{2-methyl-3-[(4,5,6,7-tetrahydrobenzo[b]thiophene-2-carbonyl)amino]phenyl}-3-oxo-3,4-dihydropyrazine-2-ylamino)phenyl]piperidine-4-carboxylic acid;
(3-{6-[3-amino-4-(2-hydroxymethylpropane-4-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
[3-(6-{3-amino-4-[(2-hydroxyethyl)methylcarbamoyl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[3-nitro-4-(pyridine-3-yloxy)phenylamino]-5-oxo-4,5-dihydropyrazine-2-yl}phenyl)benzamide;
N-[3-(6-{3-amino-4-[4-(2-hydroxyethyl)piperidine-1-yl]phenylamino}-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl)-2-were]-4-tert-butylbenzamide;
{2-methyl-3-[4-methyl-5-oxo-6-(pyridine-3-ylamino)-4,5-d is getoperation-2-yl]phenyl}amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid;
4-tert-butyl-N-{3-[6-(3-fluoro-4-morpholine-4-iletilenlerin)-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl]-2-were}benzamide;
N-(3-{6-[3-amino-4-(4-methoxypiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(4-cyanopiperidine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
amide 1-[2-amino-4-(4-methyl-6-{2-methyl-3-[(4,5,6,7-tetrahydrobenzo[b]thiophene-2-carbonyl)amino]phenyl}-3-oxo-3,4-dihydropyrazine-2-ylamino)phenyl]piperidine-3-carboxylic acid;
N-(3-{6-[3-amino-4-(3-hydroxyethylpiperazine-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
N-(3-{6-[3-amino-4-(3-methylpiperazin-1-yl)phenylamino]-4-methyl-5-oxo-4,5-dihydropyrazine-2-yl}-2-were)-4-tert-butylbenzamide;
{2-methyl-3-[4-methyl-5-oxo-6-(pyridine-4-ylamino)-4,5-dihydropyrazol-2-yl]phenyl}amide 4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxylic acid.

49. Pharmaceutical composition having inhibitory activity against Btk, comprising at least one compound according to claim 1 and at least one pharmaceutically acceptable carrier, adjuvant or excipient.

50. The pharmaceutical composition according to § 49, which is an injectable fluid, an aerosol, cream, gel, tablet, pill, capsule, syrup, ophthalmic solution or transdermal place is IRL.

51. Packaged pharmaceutical composition, comprising a pharmaceutical composition according to § 49 and instructions sufficient for applying the composition to treat a patient suffering from psoriasis.

52. The method of treatment of the patient with disease of psoriasis, including introduction to the patient an effective amount of a compound according to claim 1.

53. The method according to paragraph 52, where the patient is selected from cats and dogs.

54. The method according to paragraph 52, where the effective amount of the specified at least one compound is administered intravenously, intramuscularly, or parenteral.

55. The method according to paragraph 52, where the effective amount of the compounds administered orally.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: in formula I' , R denotes -(C=Q)R2a, CN or Y; Y denotes phenyl, or ; Q denotes O; R2a denotes phenyl, OR5 or N(R5)2; R1 denotes H; Z denotes a bond; R3 and R4 denotes H, halogen, C1-6alkoxy, N(R5)2 or Um-V, where m equals 0 or 1; V denotes H, phenyl, 5-6-member heteroaryl containing up to two nitrogen atoms, 5-6-member heterocyclyl containing up to two heteroatoms selected from N or O, or C1-6aliphatic group; U denotes a C1-6alkylidene chain, where up to two methylene links of the chain may be substituted with -CO2-, -C(O)-, -C(O)NH-, -C(O)NR5; R5 denotes H, C0-6alkykphenyl or C1-6aliphatic group, or two R5 groups, taken together with an atom to which they are bonded are optionally bonded to form a 5-7-member heterocyclic ring containing 1-2 heteroatoms selected from N, O or S; JY is selected from N(R9)2, SR9, OR9, halogen, CN, COOR9, -X-OH, phenyl, -X-phenyl, 5-6-member heteroaryl containing up to two nitrogen atoms, -X-(5-6-member heteroaryl containing up to two nitrogen atoms) or X; X denotes a C1-12aliphatic group; R9 denotes H, C1-6aliphatic group, phenyl, C3-6cycloaliphatic group, 4-6-member heterocyclyl containing up to 2 nitrogen atoms. Invention also relates to a pharmaceutical composition and a method of inhibiting Tec or c-Met kinase activity.

EFFECT: high inhibiting activity towards Tec or c-Met kinase.

16 cl, 11 tbl, 20 ex

FIELD: chemistry.

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

EFFECT: high effectiveness of the compounds.

40 cl, 8 dwg, 18 tbl, 84 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: described are new compounds of general formula (I): het-X-AB (I) where het is pentamerous N-heteroaryl, additionally containing one O, S or N atom as a heteroatom with heteroaryl with additional O atom being condensed with a benzene ring, or hexamerous N-heteroaryl; X means S; and where N-atom of N- heteroaryl residue and an X group are separated by one carbon atom; AB means 1,2,3-triazolo[4,5-d] pyrimidine-7-yl radical of general formula (II): where R3 is C1-8alkyl, phenyl, benzyl optionally substituted; R5-H, C1-8alkyl or phenyl.

EFFECT: production of new compounds for preparing a pharmaceutical composition either effective for treating cardiovascular, cancer, autoimmune diseases, stroke, neurodegenerative diseases, cystic fibrosis, or used in antithrombotic therapy.

9 cl, 11 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel 5,7-diamino-substituted pyrazolo[1,5-a]pyrimidines selected from specific compounds, e.g. those given below, which have cyclin-dependent kinase inhibiting properties, such as CDK2. The compounds can be used to treat diseases and conditions associated with CDK, such as proliferative diseases, leukaemia.

.

EFFECT: more effective use of the compounds.

12 cl, 87 tbl, 1057 ex

FIELD: chemistry.

SUBSTANCE: invention describes novel benzotriazole UV ray absorbers of general formula (I): (values of radicals are given in the description), having an absorption spectrum which is shifted towards the long-wave region with considerable optical density to 410-420 nm, as well as a UV radiation stable composition which contains novel UV ray absorbers, and use of the novel compounds as UV radiation stabilisers when applying coating on automobiles.

EFFECT: improved composition.

9 cl, 6 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention describes novel polymorphic modification N-{5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-N-methyl-acetamide, methods of its obtaining, its application as medication, its application for preparation of medication and pharmaceutical compositions, including novel polymorphic modification.

EFFECT: obtaining novel polymorphic modification for preparation of medication and pharmaceutical compositions.

30 cl, 2 tbl, 24 ex, 7 dwg

FIELD: chemistry.

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

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

20 cl, 5 dwg, 193 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel acetylenyl-pyrazole-pyrimidine derivatives of general formula (I), having mGluR2 (metabotropic glutamate receptor) antogonist properties). In compounds of general formula (I): either E and J denote N, G denotes C and L denotes N, M denotes CH, or M denotes N, L denotes CH; or L and G denote N, E denotes C, and J and M denote CH; or J, G and L denote N, E denotes C, and M denotes CH; or E and L denote N, J and M denote CH, and G denotes C; R1 denotes H, halogen, CF3, CHF2 or C1-6alkyl; R2 denotes H, halogen, C1-6-alkyl, C1-6-alkoxy, CF3 or CHF2, wherein R1=R2≠H; R3 denotes H; -C(CH3)2OH; linear C1-4-alkyl or C3-4-cycloalkyl, which are possibly substituted with one or more substitutes selected from a group comprising 1-3 F and 1-2 OH; A is selected from a group comprising phenyl or a 5- or 6-member heteroaryl having in the ring 1-2 heteroatoms selected from nitrogen, sulphur or nitrogen and sulphur in the 5-member ring, and 1-2 nitrogen atoms i the 6-member ring, and possibly substituted with 1-3 Ra; Ra denotes halogen; hydroxy; cyano; CF3; NReRf; C1-C6-alkyl, possibly substituted amino or hydroxy; ; C1-6-alkoxy; C3-4-cycloalkyl; CO-NRbRc, SO2-NRbRc; or SO2-Rd-; Rb and RC can be identical or different and are selected from a group comprising H; normal or branched C1-6-alkyl, possibly substituted with one or more substitutes selected from a group comprising F, cyano, hydroxy, C1-6-alkoxy, -NH-C(O)-O-C1-6-alkyl, amino, (C1-6-alkyl)amino, di(C1-6-alkyl)amino, heterocycloalkyl having 6 ring atoms, from which 1-2 heteroatoms are selected from nitrogen or nitrogen and oxygen, or a 6-member heteroaryl with one nitrogen heteroatom in the ring; or a 6-membeer heteroaryl with one nitrogen heteroatom in the ring; or Rb and Rc, together with the nitrogen atom with which they are bonded, can form a heterocyclic ring having 6 members in the ring, from which 1-2 atoms are selected from nitrogen and/or oxygen, and which can be substituted with C1-6-alkyl; Rd denotes OH or C1-6-alkyl; Re and Rf denote H, C1-6-alkyl, possibly substituted hydroxy, -C(O)- C1-6-alkyl; S(O)2-C1-6-alkyl.

EFFECT: compounds can be used in preparing medicinal agents for treating central nervous system (CNS) disorders, such as Huntington's chorea, amyotrophic lateral sclerosis, dementia caused by AIDS, parkinsonism etc.

55 cl, 6 dwg, 321 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of the 2,9-disubstituted imidazo[1,2-a]benzimidazole family, specifically to water-soluble salts of 9-aminoethyl-substituted 2-(4-fluorophenyl)imidazo[1,2-a]benzimidazole of general formula I:

,

where NR2 = pyrrolidine-, piperidine-, morpholine-; Y=HBr, H2SO4, (CH2COOH)2 and [CH(OH)COOH]2; n=1, 2.

EFFECT: novel compounds have analgesic action.

2 cl, 2 tbl, 15 ex

Pyrazolepyrimidines // 2412186

FIELD: chemistry.

SUBSTANCE: compounds can be used to treat tumourous diseases, such as solid tumours, breast, lung, large intestine or prostate gland tumours. In compounds of formula

: R1 is selected from a group comprising: (a) saturated cyclic radical containing 3-8 ring atoms, from which 1-3 atoms are N atoms, which can contain up to four substitutes independently selected from a group comprising: (i) lower alkyl; and (ii) CO2R3, OR7 or S(O)nR8; (b) C6-C10aryl, which can contain up to four substitutes independently selected from a group comprising: (i) S(O)nR8, lower alkyl; OR7 and halogen; (c) C3-C8cycloalkyl, which can be substituted with NR5R6; and (d) lower alkyl, which can be substituted: (i) OR7, NR5R6; R2 is selected from a group comprising: (i) H; (ii) lower alkyl; (iii) C6-C10aryl which can be substituted with a halogen, lower alkyl, lower alkoxy group; R3 is selected from a group comprising: (i) H; (ii) lower alkyl; (iv) C3-C8cycloalkyl; R5 and R6 are independently selected from a group comprising: (i) H; (ii) lower alkyl; (iii) C3-C8cycloalkyl; (v) SO2R3; and (vi) CO2R3; R7 is selected from a group comprising H and lower alkyl; R8 is selected from a group comprising: (iii) NR5R6; (iv) lower alkyl; and n equals 1 or 2.

EFFECT: capacity to inhibit activity of cyclin-dependant kinase.

FIELD: chemistry.

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

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

27 cl, 160 ex, 2 tbl

FIELD: chemistry.

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

EFFECT: high efficiency of using the composition.

24 cl, 1 dwg, 64 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) or (II) or pharmaceutically acceptable salts thereof, in which X is or ; Y is H; Z is -C(O)-; R1 and R3 each independently denotes H or (C1-C4) alkyl; R2 and R4 each independently denotes , , or ; R5 denotes H or (C1-C6) alkyl; R8 and R9 each independently denote (C1-C6) alkyl; and Q is H.

EFFECT: possibility of use in stimulating the growth hormone in a subject based on the said compounds.

49 cl, 2 tbl, 57 ex

Aromatic compound // 2416608

FIELD: chemistry.

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

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

62 cl, 2717 ex, 432 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds described by formula in which radical and symbol values are specified in the patent claim, and their pharmaceutically acceptable salts. These compounds inhibit tompomyosine-related kinases (Trk), and can find application in treating a malignant growth, such as breast cancer, rectal cancer and prostate cancer. Also, the invention relates to a method for producing these compounds, a based pharmaceutical composition and to methods of application thereof.

EFFECT: preparation of the pharmaceutical composition which can find application in treating a malignant growth.

18 cl, 134 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I), where R2 denotes H, [(C1-C6) alkylene]0-1-R'; R3 denotes H; R4 denotes H, halogen or (C1-C6) alkyl; R5 denotes H or halogen; R6 denotes H, (C1-C8) alkyl, R', (C1-C6) alkylene-R'; R7 and R8 independently denote H, halogen, (C1-C6) alkyl, O-(C1-C6) alkyl, R'; R9 denotes (C1-C6)alkyl; n equals 0 or 1; L denotes O or O-(C1-C6)alkylene; where R' denotes (C3-C8) cycloalkyl; (C5-C10)heterocyclyl, which denotes an aromatic or saturated mono- or bicyclic ring system which, besides a carbon atom, includes one or more heteroatoms such as nitrogen, oxygen and sulphur atoms; or (C6-C10) aryl; where in the heterocyclyl is unsubstituted or substituted with (C1-C6)alkyl, and the aryl is unsubstituted or substituted with a halogen, (C1-C4)alkyl, -O-(C1-C4)alkyl, SO2- (C1-C4) alkyl or N[(C1-C4) alkyl]2; and where in groups R4, R6 and R7 the alkyl can be halogenised in one or more positions; or pharmaceutically acceptable salts and/or stereo isomer forms thereof. The invention also relates to use of formula (I) compounds, as well as a medicinal agent.

EFFECT: obtaining novel biologically active compounds having Rho-kinase inhibiting activity.

21 cl, 320 ex, 3 tbl

FIELD: chemistry.

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

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

20 cl, 5 dwg, 193 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula [I-D1] or pharmaceutically acceptable salt thereof,

,

where each symbol is defined in the claim. The invention also relates to pharmaceutical compositions containing said compound and having HCV polymerase inhibiting activity.

EFFECT: disclosed compound exhibits anti-HCV activity, based on HCV polymerase inhibiting activity and is useful as an agent for preventing and treating hepatitis C.

32 cl, 497 tbl, 1129 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula 1, its pharmaceutically acceptable salts and stereoisomers: $ (1), where: R1 means H, amidino, C1-C4-alkyl amidino, C1-C4alkanoylamidino, C1-C10-alkyl, C3-C7-cycloalkyl, C6-C10-aryl, 6-members heterocycle with O atom, 5-members heterocycle with two N atoms, 6-members heteroaryl with one or two N atoms, 5-members heteroaryl with two heteroatoms, one of which is N, and the other is S, C1-C6-alkylcarbonyl, C3-C7-cycloalkylcarbonyl, C1-C4-alkoxycarbonyl, C6-C10-aryl-C1-C4-alkoxycarbonyl, -SO2-C1-C4-alkyl, -C(O)-N(R6)(R7) or -C(S)-N(R6)(R7); and, R6, R7 means H, C1-C6-alkyl, C3-C7-cycloalkyl; alkyl, cycloalkyl, heterocycle, aryl or heteroaryl are unsubstituted or substituted; R2 means C6-C10-aryl which is unsubstituted or mono- or disubstituted; R3 means H, CN, C1-C6-alkyl, C3-C7-cycloalkyl, C2-C6-alkenyl, monocyclic 5-members heterocycle with N and O, monocyclic 5-members heteroaryl with two heteroatoms, one of which is N, and the other is O or S, C(O)-R8 or -C(S)-R8; and R8 means OH, C1-C4-alkyl, C1-C4-alkyloxy or N(R9)(R10); R9, R10 mean N, C1-C6-alkyl, C3-C7-cycloalkyl, C1-C4-alkyloxy, phenyl or 5-members heteroaryl with two heteroatoms, one of which is N, and the other is S, 6-members heteroaryl with N; R9, R10 together with N whereto attached can form a single 4-6-members ring which can include in addition O or S; and alkyl, cycloalkyl, heterocycle, phenyl or heteroaryl are unsubstituted or substituted. R4 means C3-C8-cycloalkyl, C6-C10-aryl, 5-members heteroaryl with two heteroatoms, one of which is N, and the other is S, 6-members heteroaryl with N, 6-members heterocycle with O, and C6-C10-aryl or heteroaryl are unsubstituted or mono- or polysubstituted. R5 means N, C1-C6-alkyl, -C(O)-R11, C1-C6-alkylsulphonyl, C6-C10-arylsulphonyl, -(CH2)p-C6-C10-aryl, -(CH2)p-heteroaryl or -(CH2)p-C3-C8-cycloalkyl where heteroaryl means 5-members heteroaryl with O or with N or with S which can contain in addition N. p is equal to 1 or 2; R11 means C1-C10-alkyl, C1-C6-alkenyl, C3-C8-cycloalkyl, C3-C8-cycloalkenyl, NH2, C1-C4alkylamino, (C1-C4-alkyl)(C1-C4-alkyl)amino, C6-C10-aryl, 5-members heteroaryl with N or with O or with 8 which can contain in addition N, 6-members heterocycle with N and O, 5- or 6-members heterocycle with O, and alkyl is unsubstituted or substituted with one substitute. Aryl, heteroaryl, cycloalkyl, cycloalkenyl or heterocycle are unsubstituted or mono- or disubstituted.

EFFECT: compounds are melanocortin receptor agonists so presented to be used in a pharmaceutical composition for treatment and prevention of obesity, diabetes, inflammation, erectile dysfunction.

19 cl, 18 tbl

FIELD: chemistry.

SUBSTANCE: described are novel derivatives of genera formula (1) (where A denotes an oxygen or sulphur atom, -CH2- or -NH- group; R1 denotes C1-6alkyl group, possibly substituted ; R1A denotes a hydrogen atom or a C1-6 alkyl group; or these two radicals together with a carbon atom to which they are bonded form a cyclic C3-6 alkyl group; R2 denotes a C1-6 alkyl group or a C3-6 cycloalkyl group; R3 denotes an aryl group or a heteroaryl group, which can be substituted; R4 denotes a hydrogen atom; R5 denotes C1-6 alkyl group, aryl or heteroaryl group, which can be substituted), a pharmaceutical composition containing said derivatives and intermediate compounds. Said compounds (1) can inhibit bonding between SIP and its receptor Edg-1 (SIP1).

EFFECT: possibility of use in medicine.

18 cl, 2 tbl, 28 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) or (II) or pharmaceutically acceptable salts thereof, in which X is or ; Y is H; Z is -C(O)-; R1 and R3 each independently denotes H or (C1-C4) alkyl; R2 and R4 each independently denotes , , or ; R5 denotes H or (C1-C6) alkyl; R8 and R9 each independently denote (C1-C6) alkyl; and Q is H.

EFFECT: possibility of use in stimulating the growth hormone in a subject based on the said compounds.

49 cl, 2 tbl, 57 ex

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