Derivatives of cyclic amines, the method of inhibiting

 

The invention relates to derivatives of cyclic amines and their use as pharmaceuticals, particularly to a compound represented by the General formula (I), its pharmaceutically acceptable acid additive salts or its pharmaceutically acceptable C1-C6alcaldicios salt, R1-phenyl, C3-8-cycloalkyl, aromatic heterocycle with 1-3 heteroatoms selected from O, S, N, or combinations thereof, and these groups may be condensed with benzene ring or an aromatic heterocyclic group with heteroatoms, selected from O, S or N, or combinations thereof, and may have various substituents. 2 S. and 52 C.p. f-crystals, 52 PL.

Description text in facsimile form (see graphic part),

Claims

1. Derivatives of cyclic amines of the formula (I)their pharmaceutically acceptable acid additive salts or pharmaceutically acceptable With1-C6alkylidyne salt, where R1is a phenyl group, With3-C8cycloalkyl group or aromatic heterocyclic group containing 1 to what toroi phenyl or aromatic heterocyclic group may be condensed with benzene ring or an aromatic heterocyclic group, containing 1-3 heteroatoms selected from the group consisting of oxygen atom, sulfur atom, nitrogen atom, or combinations thereof, with the formation of the condensed rings, while the phenyl group, With3-C8cycloalkyl group, aromatic heterocyclic group or the condensed ring may have one or more substituents from halogen atom, hydroxyl group, ceanography, nitro, carboxyl group, carbamoyl group1-C6alkyl group, a C3-C8cycloalkyl group2-C6alkenylphenol group, C1-C6alkoxygroup, C1-C6allylthiourea,3-C5alkalinous group2-C4accelerometry,1-C3alkylenedioxy, phenyl group, fenoxaprop, phenylthiourea, benzyl group, benzyloxy, benzylamino,2-C7alkanoyloxy group3-C7alkoxycarbonyl group2-C7alkanoyloxy,2-C7alkanolamines,2-C7N-alkylcarboxylic group, C4-C9N-cycloalkylcarbonyl group, C1-C6alkylsulfonyl group3-C8(alkoxy group, 1-pyrrolidinecarbonyl group, the divalent group represented by the formula-NH(C= O)O-, a divalent group represented by the group-NH(C= S)O-, amino, mono(C1-C6alkyl)amino or di(C1-C6alkyl)amino, where the Deputy phenyl group3-C8cycloalkyl group, aromatic heterocyclic group or the condensed ring optionally has one or more substituents from halogen atoms, hydroxyl groups, amino groups, triptorelin group1-C6alkyl group or a C1-C6alkoxygroup; R2is a hydrogen atom, a C1-C6alkyl group, a C1-C7alkoxycarbonyl group, hydroxyl group or phenyl group, where C1-C6alkyl or phenyl group may have one or more substituents of a halogen atom, a hydroxyl group, a C1-C6alkyl group or a C1-C6alkoxygroup, and when j= 0, R2is not a hydroxyl group; j = 0-2; k = 0-2; m = 2-4; n = 0 or 1;
R3is a hydrogen atom or a C1-C6alkyl group, optionally substituted by one or two phenyl groups each of which may have one ILS6alkoxygroup;
R4and R5the same or different from each other and represent a hydrogen atom, hydroxyl group, phenyl group or a C1-C6alkyl group, where C1-C6alkyl group optionally substituted by one or more groups of atoms of halogen, hydroxyl group, ceanography, nitro, carboxyl group, carbamoyl group, mercaptopropyl, a guanidinium moiety,3-C8cycloalkyl group1-C6alkoxygroup, C1-C6allylthiourea, phenyl group, optionally having one or more substituents from halogen atoms, hydroxyl groups, C1-C6alkyl group, a C1-C6alkoxygroup or benzyloxy, fenoxaprop, benzyloxy, benzyloxycarbonyl group2-C7alkanoyloxy group2-C7alkoxycarbonyl group2-C7alkanoyloxy,2-C7alkanolamines,2-C7-N-alkylcarboxylic group2-C7alkylsulfonyl groups, amino groups, mono (C1-C6alkyl) amino, di (C1-C6alkyl) amino group or aromatic heterocycle is nitrogen, or combinations thereof, and optionally condensed with a benzene ring, or R4and R5taken together form a 3-6-membered hydrocarbon cycle;
p = 0 or 1;
q = 0 or 1;
G - group, represents-CO-, -SO2-, -CO-O-, -NR7-CO-, -CO-NR7-, -NH-CO-NH-, -NH-CS-NH-, -NR7-SO2-, -SO2-NR7-, -NH-CO-O - or-O-CO-NH-, where R7that is, an atom of hydrogen or C1-C6alkyl group, or R7taken together with R5represents a C2-C5alkylenes group;
R6is a phenyl group, With3-C8cycloalkyl group3-C8cycloalkenyl group, benzyl group or aromatic heterocyclic group containing 1-3 heteroatoms selected from the group consisting of oxygen atom, sulfur atom, nitrogen atom, or combinations thereof, where the phenyl, benzyl or aromatic heterocyclic group may be condensed with benzene ring or an aromatic heterocyclic group containing 1-3 heteroatoms selected from the group consisting of oxygen atom, sulfur atom, nitrogen atom, or combinations thereof, with the formation of a condensed ring, and the phenyl group3-C8cycloalkyl group3-C8, the ring may have one or more substituents of a halogen atom, hydroxyl group, mercaptopropyl, ceanography, nitro, thiocyanatopropyl, carboxyl group, carbamoyl group, triptorelin group1-C6alkyl group, a C3-C6cycloalkyl group2-C6alkenylphenol group, C1-C6alkoxygroup,3-C8cycloalkylcarbonyl,1-C6allylthiourea, C1-C3alkylenedioxy, phenyl group, fenoxaprop, phenylaminopropyl, benzyl group, bentilee group, phenylsulfinyl group, phenylsulfonyl group, 3-phenylurazole,2-C7alkanoyloxy group2-C7alkoxycarbonyl group2-C7alkanoyloxy,2-C7alkanolamines,2-C7N-alkylcarboxylic group, C1-C6alkylsulfonyl group, phenylcarbamoyl group, and N, N-di (C1-C6alkyl) sulfamoyl groups, amino groups, mono(C1-C6alkyl) amino, di (C1-C6alkyl) amino group, benzylamino, C2-C7(alkoxycarbonyl) amino, C1-C6(alkylsulfonyl) amino group or a bis (C1-C6alkylsulfonyl)amino group, pinoy group, benzyl group, aromatic heterocyclic group or the condensed ring optionally having one or more substituents of a halogen atom, ceanography, hydroxyl group, amino group, triptorelin group, C1-C6alkyl group, a C1-C6alkoxygroup, C1-C6allylthiourea, mono(C1-C6alkyl) amino or di (C1-C6alkyl) amino, provided that when k= 2, m= 2, n= 0, and the phenyl group, R1not substituted C1-C6alkyl group, which is the Deputy phenyl group3-C8cycloalkyl group3-C8cycloalkenyl group, benzyl group, aromatic heterocyclic group or the condensed ring in R6not substituted amino group, and R6not a benzyl group.

2. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I), k= 1 and m= 2.

3. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1 distinguishing the pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I), k= 0, m= 3 and n= 1.

5. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I), k= 1 and m= 3.

6. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I), k= 2 and m= 2.

7. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I) n= 1.

8. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I), k= 1 and m= 4.

9. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I) j= 0.

10. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6/p>11. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I) R2represents a hydrogen atom, R3represents a hydrogen atom and R7represents a hydrogen atom.

12. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (1) Deputy phenyl group3-C8cycloalkyl group, aromatic heterocyclic group or the condensed ring in R1represents one or more groups of atoms of halogen, hydroxyl group, C1-C6alkyl group, a C2-C6alkenylphenol group, C1-C6alkoxygroup, C1-C6allylthiourea,2-C4accelerometry, methylendioxy, N-phenylcarbamoyloxy groups, amino groups, mono(C1-C6alkyl) amino or di (C1-C6alkyl) amino group.

13. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1b>-C8cycloalkyl group3-C8cycloalkenyl group, benzyl group, aromatic heterocyclic group or the condensed ring in R6represents one or more groups of atoms of halogen, nitro, triptorelin group, C1-C6alkyl group, a C1-C6alkoxygroup, phenylsulfonyl group2-C7alkanolamines or amino group.

14. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I) R1represents a phenyl group or isoxazolyl group.

15. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, wherein in the formula (I) R6represents a phenyl group, follow group or thienyl group.

16. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-5-chlorobenzaldehyde salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-4,5-differentail)glycyl} aminomethyl] -1-(4-Chlorobenzyl) piperidine.

18. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-5-trifloromethyl)glycyl} aminomethyl] -1-(4-Chlorobenzyl) piperidine.

19. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-5-trifloromethyl)glycyl} aminomethyl] -1-(4-Chlorobenzyl) piperidine.

20. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-4,5-differentail)glycyl} aminomethyl] -1-(4-bromobenzyl) piperidine.

21. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it made inania, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 1-(3-amino-4-methoxybenzyl)-4-[{ N-(2-amino-4,5-differentail)glycyl} aminomethyl] piperidine.

23. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-4,5-differentail)glycyl} aminomethyl] -1-(4-chloro-3-(methylamino)benzyl) piperidine.

24. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 4-[{ N-(2-amino-5-trifloromethyl)glycyl} aminomethyl] -1-(2-thioxo-2,3-dihydro-1,3-benzoxazol-5-ylmethyl) piperidine.

25. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino} -1-(4-chlorbenzyl) pyrrolidin.

26. The compound, its pharmaceutically acceptable characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] -1-(4-methoxybenzyl) pyrrolidin.

27. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] -1-(3,4-methylenedioxybenzyl) pyrrolidin.

28. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] -1-(2,3-dihydro-1-benzofuran-5-ylmethyl) pyrrolidin.

29. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N - (2-amino-5-trifloromethyl)glycyl} amino] -1-(4-methylthiophenyl) pyrrolidin.

30. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifter the pilot-additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] -1-(4-active compounds) pyrrolidin.

32. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 1-(3-amino-4-methoxybenzyl)-3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] pyrrolidine.

33. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] -1-(4-chloro-3-methylbenzyl) pyrrolidin.

34. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, characterized in that it is a 3-[{ N-(2-amino-5-trifloromethyl)glycyl} amino] -1-(4-hydroxy-3-(methylamino)benzyl) pyrrolidin.

35. The compound, its pharmaceutically acceptable acid additive salt or its pharmaceutically acceptable1-C6alkalidata salt p. 1, atlacatl) pyrrolidin.

36. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell using derivatives of cyclic amines of the formula (I)

its pharmaceutically acceptable acid additive salts or its pharmaceutically acceptable C1-C6alcaldicios salt,
where R1is a phenyl group, With3-C8cycloalkyl group, or an aromatic heterocyclic group containing 1-3 heteroatoms selected from the group consisting of oxygen atom, sulfur atom, nitrogen atom, or combinations thereof, in which phenyl or aromatic heterocyclic group may be condensed with benzene ring or an aromatic heterocyclic group containing 1-3 heteroatoms selected from the group consisting of oxygen atom, sulfur atom, nitrogen atom, or combinations thereof, with the formation of the condensed rings, while the phenyl group, With3-C8cycloalkyl group, aromatic heterocyclic group or the condensed ring may have one or more substituents from halogen atom, hydroxyl group, ceanography, nitro, carboxyl group, carbamoyl group,group, With1-C6alkoxygroup, C1-C6allylthiourea,3-C5alkalinous group2-C4accelerometry, C1-C3alkylenedioxy, phenyl group, fenoxaprop, phenylthiourea, benzyl group, benzyloxy, benzylamino,2-C7alkanoyloxy group2-C7alkoxycarbonyl group, C2-C7alkanoyloxy,2-C7alkanolamines,2-C7N-alkylcarboxylic group4-C9N-cycloalkylcarbonyl group, C1-C6alkylsulfonyl group3-C8(alkoxycarbonyl) methyl group, N-phenylcarbamoyloxy group, piperidinylcarbonyl group, morpholinylcarbonyl group, 1-pyrrolidinecarbonyl groups, amino groups, mono (C1-C6alkyl) amino or di (C1-C6alkyl)amino, where the Deputy phenyl group3-C8cycloalkyl group, aromatic heterocyclic group or the condensed ring optionally has one or more substituents from halogen atom, hydroxyl group, amino group, triptorelin group1-C6alkyl group or a C1<>alkoxycarbonyl group, hydroxyl group or phenyl group, where C1-C6alkyl or phenyl group may have one or more substituents of a halogen atom, a hydroxyl group, a C1-C6alkyl group or a C1-C6alkoxygroup, and when j= 0, R2is not a hydroxyl group;
j = 0-2;
k = 0-2;
m = 2-4;
n = 0 or 1;
R3is a hydrogen atom or a C1-C6alkyl group, optionally substituted by one or two phenyl groups each of which may have one or more substituents from halogen atom, hydroxyl group,1-C6alkyl group, a C1-C6alkoxygroup;
R4and R5the same or different from each other and represent a hydrogen atom, hydroxyl group, phenyl group or a C1-C6alkyl group, where C1-C6alkyl group optionally has one or more substituents from halogen atom, hydroxyl group, ceanography, nitro, carboxyl group, carbamoyl group, mercaptopropyl, a guanidinium moiety,3-C8cycloalkyl group, C1-C6alkoxygroup, C1-C6allylthiourea, With1-C6alkyl group, a C1-C6alkoxygroup or benzyloxy, fenoxaprop, benzyloxy, benzyloxycarbonyl group2-C7alkanoyloxy group2-C7alkoxycarbonyl group2-C7; alkanoyloxy,2-C7alkanolamines,2-C7-N-alkylcarboxylic group2-C7alkylsulfonyl groups, amino groups, mono (C1-C6alkyl) amino, di (C1-C6alkyl) amino group or aromatic heterocyclic group containing 1-3 heteroatoms selected from the group consisting of oxygen atom, sulfur atom, nitrogen atom, or combinations thereof, and optionally condensed with a benzene ring, or R4and R5taken together form a 3-6 membered hydrocarbon cycle;
p = 0 or 1;
q = 0 or 1;
G - group, represents-CO-, -SO2-, -CO-O-, -NR7-CO-, -CO-NR7-, -NH-CO-NH-, -NH-CS-NH-, -NR7-SO2-, -SO2-NR7-, -NH-CO-O - or-O-CO-NH-, where R7is a hydrogen atom or a C1-C6alkyl group, or R7taken together with R5represents a C2-C5alkylenes group;
R6is a phenyl group, With33-C8cycloalkyl group3-C8cycloalkenyl group, benzyl group, aromatic heterocyclic group or the condensed ring may have one or more substituents from halogen atom, hydroxyl group, mercaptopropyl, ceanography, nitro, thiocyanatopropyl, carboxyl group, carbamoyl group, triptorelin group, C1-C6alkyl group, a C3-C6cycloalkyl group2-C6alkenylphenol group, C1-C6alkoxygroup,3-C8cycloalkane group, C1-C6allylthiourea, C1-C3alkylenedioxy, phenyl group, fenoxaprop, phenylaminopropyl, benzyl group, bentilee the ilen group, With2-C7alkoxycarbonyl group2-C7alkanoyloxy,2-C7alkanolamines,2-C7N-alkylcarboxylic group, C1-C6alkylsulfonyl group, phenylcarbamoyl group, a N, N-di (C1-C6alkyl) sulfamoyl groups, amino groups, mono (C1-C6alkyl) amino, di (C1-C6alkyl) amino group, benzylamino,2-C7(alkoxycarbonyl) amino group, (C1-C6alkylsulfonyl) amino group or bis C1-C6(alkylsulfonyl)amino group, and the Deputy phenyl group3-C8cycloalkyl group3-C8cycloalkenyl group, benzyl group, aromatic heterocyclic group or the condensed ring optionally has one or more substituents of a halogen atom, ceanography, hydroxyl group, amino group, triptorelin group, C1-C6alkyl group, a C1-C6alkoxygroup, C1-C6allylthiourea, mono (C1-C6alkyl) amino or di (C1-C6alkyl) amino group.

37. Method of inhibiting the binding of a chemokine to the receptor of target cells and/elevazione of the chemokine to the receptor of the target cell and/or its action on a target cell by p. 37, characterized in that in formula (I) n= 0.

39. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein k= 0, m= 3 and n= 1 in the above formula (I).

40. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I), k= 1 and m= 3.

41. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I), k= 2 and m= 2.

42. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell under item 41, wherein in the formula (I) n= 1.

43. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I), k= 1 and m= 4.

44. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I) j= 0.

45. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I) p= 0, q= 0 and G is a group-NR2is a hydrogen atom, R3is a hydrogen atom and R7is a hydrogen atom.

47. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I) Deputy phenyl group3-C8cycloalkyl group, aromatic heterocyclic group or the condensed ring in R1represents one or more substituents of a halogen atom, a hydroxyl group, a C1-C6alkyl group, a C2-C6alkenylphenol group, C1-C6alkoxygroup, C1-C6allylthiourea, C2-C4accelerometry, methylendioxy, N-phenylcarbamoyloxy groups, amino groups, mono(C1-C6alkyl) amino or di (C1-C6alkyl) amino group.

48. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I) Deputy phenyl group3-C8cycloalkyl group3-C8cycloalkenyl group, benzyl group, aromatic heterocyclic group or condensed the school group, C1-C6alkyl group, a C1-C6alkoxygroup, phenylsulfonyl group2-C7alkanolamines or amino group.

49. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I) R1is a phenyl group or isoxazolidine group.

50. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell by p. 36, wherein in the formula (I) R6is a phenyl group, furilla group or thienyl group.

51. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell under item 36, wherein the chemokine is MIP-1.
52. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell under item 36, wherein the chemokine is MCP-1.

53. Method of inhibiting the binding of a chemokine to the receptor of the target cell and/or its action on a target cell under item 36, wherein the chemokine receptor CCR1 is.

54. Method of inhibiting the binding of a chemokine to the receptor cells-mission is

Priority items:
18.11.1997 - on all counts, except for the PP. 24 and 28;
17.11.1998 - p. 24;
06.04.1998 - p. 28.

 

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< / BR>
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The invention relates to new derivatives of spirobiindane General formula (I), where R1represents a phenyl group which may be optionally substituted by 1-3 substituents selected from halogen atoms, lower alkyl groups, halogenized alkyl groups, lower alkoxygroup, lower alkoxycarbonyl groups, hydroxyl groups, lower aliphatic acylamino, cyano groups, or a 5 - or 6-membered heterocyclic group containing 1-3 oxygen atom, sulfur and/or nitrogen, which may be optionally condensed with a phenyl group; R2represents a phenyl group which is substituted by 1-3 fluorine atoms or chlorine; a represents a carbonyl group; represents a simple bond; D represents an oxygen atom or sulfur; E represents C1-4Allenova group;represents a group of formula (II), where G represents C5-8alonovoa ring, which is substituted by hydroxyl group; Ar represents a phenyl ring; n represents the integer 1 or 2, or a pharmacologically acceptable salt

The invention relates to new derivatives of benzoxazinone General formula (I), where R1means N or carboxyethyl, R2represents hydrogen or alkyl, and R3is a different derivatively of amino acids, dipeptides and hydrazones acid groups, respectively, their conjugates with active substances, such as residues from a number of penicillin

The invention relates to new imidazole derivative of General formula (1), where n1is an integer from 1 to 3, a represents hydrogen, linear or branched C1-C10-alkyl, which may be optionally substituted C3-C7-cycloalkyl or lower alkoxy, or a radical selected from the group shown in the formula of the invention, Y represents a radical selected from the group described in the claims, or to his new pharmaceutically acceptable salts

The invention relates to new derivatives of piperidineacetate-2-it General formula I, where R1and R2each independently from each other represents an unsubstituted or once substituted phenyl residues, substituents which may be OA, Hal, NH2, OTHER3; R3denotes-CO-alkyl, where alkyl has 1 to 7 carbon atoms; And indicates WITH1-C6alkyl; Hal denotes F, CL, Br or J

The invention relates to new compounds of the formula (I), where R1is (C3-C7)cycloalkyl group or a 3-7-membered saturated heterocyclic group containing 1 or 2 heteroatoms selected from nitrogen, oxygen, or sulfur, which may be optionally substituted by oxopropoxy; R2- aryl group, which optionally can be substituted by 1-3 halogen atoms; And a is methylene or carbonyl group; a simple bond; D is oxygen atom or sulfur; G is - (C1-C4)alkylenes group; L is a group of the formula-C(R4)(R5)-, where R4and R5defined in the claims, Z is two hydrogen atoms or an oxygen atom, n = 0 or 1, or its pharmaceutically acceptable salts, esters, Quaternary amines or hydrates

The invention relates to new N-phenylamine and N-pyridylamine derivative of the formula I

< / BR>
in which X denotes O or S;

R1and R2which may be identical or different, denote hydrogen, (C1-C6)alkyl or (C3-C8)cycloalkyl or R1and R2together with the carbon atom to which they are attached, form a (C3-C8)cycloalkyl;

R3means (C6-C12)aryl, optionally substituted by one or more radicals Y, which may be the same or different;

Y represents halogen;

R4and R5represent hydrogen;

Ar denotes one of the following groups or WITH:

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T represents hydrogen or (C1-C6)alkyl;

T3and T4which may be identical or different, denote (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)allylthiourea;

R6and R7each denotes hydrogen or R6and R7together represent a bond;

Z denotes either (I) the divalent group-CHR9- in which the R11-, in which R10and R11together they form a bond that Z represents the group-CH=CH-, or R10and R11that may be the same or different, have the meanings indicated above for R9or (III) a divalent group-CHR12-CHR13-CH2-, in which R12and R13together they form a bond, Z represents-CH=CH-CH2-, or R12and R13that may be the same or different, have the meanings indicated above for R9,

as well as their additive salts with pharmaceutically acceptable acids or bases, and method of production thereof, pharmaceutical compositions and drug manifesting gipolipedimecescoe and antiatherosclerotic action based on them
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