Substituted sulphamide derivatives

FIELD: chemistry.

SUBSTANCE: invention relates to substituted sulphamide derivatives of formula I: , in which n, m, R1, R2a-c, R3, R4, R5 and R6 are as described in claim 1, in form of a racemate, enantiomers, diastereomers, mixtures of enantiomers or diastereomers or a separate enantiomer or diastereomer, bases and/or salts of physiologically compatible acids. The invention also relates to a method of producing said compounds, a medicinal agent having antagonist action on bradykinin receptor 1 (B1R), containing such compounds, use of such compounds to produce medicinal agents, as well as sulphamide-substituted derivatives selected from a group of compounds given in claim 8.

EFFECT: providing novel compounds which are suitable as pharmacologically active substances in medicinal agents for treating disorders or diseases which are at least partially transmitted through B1R receptors.

13 cl, 581 ex

 

The text descriptions are given in facsimile form.

1. Substituted sulfa derivatives of General formula I

in which
n means 0, 1 or 2;
m denotes 1 or 2;
R1means aryl or heteroaryl selected from the group consisting of phenyl, naphthyl, indolyl, benzofuranyl, benzothiophene, benzoxazole, benzoxadiazole, pyrrolyl, furanyl, thiophenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazothiazole, carbazolyl, dibenzofurane and dibenzothiophene;
R2a-c, R3and R4mean H or with adjacent remnant R2a-c, R3or R4form Besenova group, which is optionally substituted one or more times by stands, methoxy, CF3-, Cl, Br and/or F,
a) R5and R6together form a cyclic group selected from the group consisting of
or
and the basic residue selected from the group including
(i) -N(C1-6-alkyl),
(ii) the balance of the General formula (Aa1)

where a, b and C independently from each other is and can be 0 or 1, provided that when b is 0, a and C are not simultaneously 1;
bridge1-3-once alkyl may be substituted by =O;
and R10selected from the group including




moreover, these residues can be unsubstituted or once substituted in one or more ring members by C1-6-alkyl, F, Cl, or Br;
or R10is

which is unsubstituted, may be substituted one or more times mainly With1-6-alkyl, especially stands or ethyl, F, Cl, Br, C1-6-alkoxy, especially methoxy, or phenyl; or
R10means phenyl, which is substituted by-N(C1-3-alkyl)2or denotes phenyl, which is substituted by pyrrolidinyl, imidazolidinyl, dihydroimidazolium, and the binding can happen in each of the ring members of the phenyl and Deputy
or
R10means a group of the General formula (Aa2)

d is 1 or 2, R13means N or ethyl, R14means phenyl or pyridinyl and R15means morpholinyl or 4-methylpiperazine;
or
b) R5and R6together form a cyclic group selected from the group consisting of
and
and R16represents a group of General formula bb1

and in the formula bb1 (i) a=0, b=1, 2, or 3, and C=0 or (ii) a=0, b=1, 2, or 3, and C=0; and
R18selected from the group consisting of




moreover, these groups can be unsubstituted, singly or multiply substituted by C1-3-alkyl, C1-3-alkoxy, F, Cl, Br, I, CN, CF3N(C1-3-alkyl)2, NH(C1-3-alkyl), N(C1-3-alkyl)(phenyl or phenethyl), benzyl or

all of these alternates equally once or repeatedly can be substituted by F, C, Br, -CN, -CF3With1-3-alkyl; pyrrolidinyl, piperidinyl, 4-methylpiperidine or morpholine;
or R18is heterocyclyl, which is selected from the group consisting of


or
R18is cyclopentyl, cyclohexyl, optionally, one or more annular members once substituted, or C1-3-alkyl optionally substituted one or more times;
or
(C) in the group NR5R6of the General formula I
R5selected from the group consisting of H and C1-6-alkyl selected from methyl, ethyl, propyl and isopropyl, optionally substituted one or more times, and
R6represents a group according to General formula C1

and
a=0, 1, or 2;
b=0, 1, 2, or 3; which
R21is phenyl or naftilos group which may be substituted one or more times by F, Cl, Br, I, CN, C1-3-alkyl,
R22and R23independently of one another denote methyl, ethyl or propyl or isopropyl or NR22R23group together represent an N-heterocycle which is selected from the group consisting of

moreover, these N-heterocycles unsubstituted or can be substituted once in one or more ring members,
or
R6represents a group of General formula C2

and
a=0, 1, 2 or 3;
b=0 or 1, indicating that if b=0, with=0;
with=0, 1, 2, or 3, in which
Y represents phenyl, naphthyl, benzoxadiazole, cyclopentyl, cyclohexyl or cycloheptyl, and
Z is selected from the group consisting of
N(C1-3-alkyl)2;


and R30, R31and R40can represent H, methyl, ethyl, propyl or isopropyl, or Z is selected from the group consisting of




and R32, R33 34selected from H, methyl, ethyl, propyl and isopropyl, or Z is NR24R25group, in which R24and R25independently of one another represent methyl, ethyl, propyl or isopropyl, or Z is-C(=O)-(CH2)d-NR26R27group, and d is 1 or 2 and NR26R27together form a heterocycle selected from

and R35and R36may represent a methyl, ethyl, propyl, or isopropyl,
or
d) in the group NR5R6of the General formula I
R5represents C1-6is alkyl selected from the group consisting of H and methyl, ethyl, propyl and isopropyl, optionally substituted one or more times, and
R6represents a group according to General formula d1

and
a=0, 1, 2, 3 or 4;
b=0 or 1, indicating that if b=0, with=0;
with=0, 1, 2 or 3; and
and J is selected from the group

and K is selected from the group consisting of H, phenyl, naphthyl, pyridinyl, or
e) in the group NR5R6of the General formula I:
R5selected from the group consisting of H, C1-3-alkyl, -(CH2)r-NR28R2 with r=1-3 and R28and R29mean C1-3-alkyl, and
R6-(CH2)r-NR28R29with r=1-3 and R28and R29mean1-3-alkyl, or R6is replaced by N(C1-3-alkyl)(aryl)-s group C1-3is an alkyl group which may be substituted by an aryl group and the aryl mainly means phenyl or naphthyl,
or
f) in the group NR5R6of the General formula I:
R5represents H, methyl, ethyl, propyl, isopropyl, phenyl or benzyl and
R6represents a group of type (C1-3-alkyl)s-X with s=0 or 1 and1-3is an alkyl group may be substituted by pyrrolidinyl, piperidinyl, piperazinil or morpholinyl group, and X is selected from the group consisting of




and R41, R42and R43selected from H, methyl, ethyl, propyl and isopropyl, in the form of the racemate; of the enantiomers, dieste is Omarov, mixtures of the enantiomers or diastereomers or of an individual enantiomer or diastereoisomer; the bases and/or salts of physiologically compatible acids;
where substituted aryl - or heteroaryl residue substituted one or more times by F, Cl, Br, I, CN, NH2, NH-C1-6-alkyl, NH-C1-6-alkyl-HE, N(C1-6alkyl)2N(C1-6-alkyl-OH)2, NH-aryl, N(aryl)2N(C1-6-alkyl)aryl, NO2, SH, S-C1-6-alkyl, HE, O-C1-6-alkyl, O-C1-6alkyl-HE, C(=O)1-6-alkyl, CO2N, CH2SO2-phenyl, CO2-C1-6-alkyl, OCF3, CF3,C1-6-alkyl, pyrrolidinyl, imidazolyl, piperidinyl, morpholinyl, benzyloxy, phenoxy, phenyl, pyridyl, alkylaryl, especially benzyl, tanila or furil,
substituted cycloalkenyl residue or an alkyl residue substituted by F, Cl, Br, I, -CN, NH2, NH-C1-6-alkyl, NH-C1-6-alkyl-HE1-6-alkyl, N(C1-6-alkyl)2N(C1-6-alkyl-OH)2, NO2, SH, S-C1-6-alkyl, S-benzyl, O-C1-6-alkyl, HE, O-C1-6-alkyl-HE, =O, O-benzyl, C(=O)C1-6-alkyl, CO2N, CO2-C1-6-alkyl or benzyl.

2. Substituted sulfa derivative according to claim 1, in which R1means phenyl, naphthyl, benzothiophene, benzoxadiazole is l, thiophenyl, pyridinyl, imidazothiazoles and dibenzofurans, preferably phenyl, naphthyl and benzothiophenes, unsubstituted or singly or multiply substituted mainly by1-3-alkyloxy, C1-6-alkyl, Br, Cl, F, I, CF3, F3HE, SH.

3. Substituted sulfa derivative according to claim 1 or 2, in which R1means phenyl or naphthyl, optionally substituted one or more times by methyl, methoxy, CF3-, CL, Br, and/or F.

4. Substituted sulfa derivative according to claim 1 or 2, in which (CR2a-c)n-group n=1 or 2, mostly 2.

5. Substituted sulfa derivative according to claim 1 or 2, in which m=1.

6. Substituted sulfa derivative according to claim 1, in which
a) formed by NR5R6group, a cyclic group is

and the primary balance is a group of the General formula (Aa1); and i) a=b=c=0, (ii) a=C=0 and b=1, iii) a=b=0 and C=1 or (iv) a=b=1 and C=0;
or basic residue is a group of the General formula (Aa2), and d=1 or 2, mostly 2, and R14is pyridinyl, mostly 3-pyridinyl and R15is morpholinyl, or
b) formed by NR5R6group, a cyclic group is

and R16represents a group of General formula is bb1, in which a=C=0 and b=0, 1, or 2, and R18selected from

in which the phenyl group may be substituted, mainly once substituted by F, Cl or Br, especially F, mostly in the 4th position;
or
(C) in the group NR5R6of the General formula I:
R5selected from the group consisting of H, methyl, ethyl, propyl and isopropyl, mainly methyl, and
R6represents a group according to General formula C2 where a=1 or 2, b=1 and C=0, Y is phenyl or cyclohexyl and Z is pyrrolidinyl or dihydroimidazole.

7. Substituted sulfa derivative according to claim 6, in which the group

means

8. Substituted sulfa derivative selected from the group:

1. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfonyl)-pyrrolidin-2-ylethoxy]-N-(4-piperidine-1-ylmethyl-benzyl)-ndimethylacetamide

2. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-N-(4-piperidine-1-ylmethyl-benzyl)-ndimethylacetamide

3. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-N-[4-(4-methyl-piperazine-1-yl)-benzyl]-ndimethylacetamide

4. N-(4-piperidine-1-ylmethyl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

5. 1-[4-(1-methyl-piperidine-4-yl)-piperazine-1-yl]-2-[2-(2,4,6-trimethy the-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-alanon

6. 1-(4-benzyl-[1,4]diazepan-1-yl)-2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-alanon

7. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-N-[4-(4-methyl-piperazine-1-ylmethyl)-benzyl]-ndimethylacetamide

8. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(1-methyl-piperidine-4-yl)-piperazine-1-yl]-alanon

9. 1-(1,4'-bipiperidine-1'-yl)-2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)alanon

10. N-(4-piperidine-1-ylmethyl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

11. N-(4-dimethylaminomethyl-benzyl)-2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

12. N-(1-benzyl-piperidine-3-ylmethyl)-2-[1-(2,4,6-trimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

13. N-[4-(4-methyl-piperazine-1-yl)-benzyl]-2-[1-(2,4,6-trichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

14. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-N-(4-piperidine-1-yl-benzyl)-ndimethylacetamide

15. N-[4-(4-methyl-piperazine-1-ylmethyl)-benzyl]-2-[1-(2,4,6-trichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

16. N-(1-benzyl-piperidine-3-ylmethyl)-2-[1-(3,4-dichloro-phenylsulfonyl)-2,3-dihydro-1H-indole-2-ylethoxy]-ndimethylacetamide

17. 2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(pyrrolidin-1-yl)piperidine-1-yl)alanon

18. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfonyl)-pyrrolidin-ylethoxy]-N-[4-(4-methyl-piperazine-1-yl)-benzyl]-ndimethylacetamide

19. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyrrolidin-1-yl)piperidine-1-yl)alanon

20. 2-((1-(3,4-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

21. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-N-(4-(morpholine-4-yl-benzyl)-ndimethylacetamide

22. 1-[4-(1-methyl-piperidine-4-yl)-piperazine-1-yl]-2-[1-(3-trifluoromethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-alanon

23. 2-((1-(naphthalen-1-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(pyrrolidin-1-yl)piperidine-1-yl)alanon

24. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-N-(4-(morpholine-4-ylmethyl-benzyl)-ndimethylacetamide

25. 1-[4-(3-dimethylamino-propyl)-piperazine-1-yl]-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-alanon

26. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-(4-pyrrolidin-1-yl-piperidine-1-yl)-alanon

27. 1-(2-piperidine-1-ylmethyl-pyrrolidin-1-yl)-2-[1-(2,4,6-trimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-alanon

28. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(4-methyl-piperazine-1-yl)-piperidine-1-yl]-alanon

29. N-[4-(4-methyl-piperazine-1-yl)-benzyl]-2-[1-(2,4,6-trichloro-phenylsulfanyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

30. N-(4-(morpholine-4-ylmethyl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

31. 1-(4-benzyl-[1,4]diazepan-1-yl)-2-[1-(2,4,6-trimethyl-phenylsulfonyl)-Pieper is DIN-2-ylethoxy]-alanon

32. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(1-methyl-piperidine-4-yl)-piperazine-1-yl]-alanon

33. N-[3-(4-methyl-piperazine-1-yl)-benzyl]-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-ndimethylacetamide

34. N-(1-benzyl-piperidine-3-ylmethyl)-2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-ndimethylacetamide

35. N-(4-dimethylaminomethyl-benzyl)-2-[1-(4-methoxy-2,6-dimethyl-phenylsulfonyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

36. 2-((1-(3,4-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

37. N-(4-dimethylaminomethyl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

38. 2-((2-(3,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(pyrrolidin-1-yl)piperidine-1-yl)alanon

39. 1-(4-benzo[1,3]dioxol-5-ylmethyl-piperazine-1-yl)-2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-alanon

40. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfonyl)-pyrrolidin-2-ylethoxy]-N-[4-(4-methyl-piperazine-l-ylmethyl)-benzyl]-ndimethylacetamide

41. N-(1-benzyl-piperidine-3-ylmethyl)-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-ndimethylacetamide

42. 2-((1-(3,4-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperazine-1-yl)alanon

43. 2-[2-(3,4-dichloro-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-N,N-bis-(2-diethylamino-ethyl)-ndimethylacetamide

44. 1-(4-benzo[1,3]dioc the ol-5-ylmethyl-piperazine-1-yl)-2-[1-(3,4-dichloro-phenylsulphonyl)-pyrrolidin-2-ylethoxy]-alanon

45. N-[4-(4-methyl-piperazine-1-ylmethyl)-benzyl]-2-[1-(2,4,6-trichloro-phenylsulfanyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

46. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(2-methoxy-ethyl)-piperazine-1-yl]-alanon

47. N-methyl-N-(2-morpholine-4-yl-1-phenyl-ethyl)-2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-ndimethylacetamide

48. N,N-bis-(2-diethylamino-ethyl)-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-ndimethylacetamide

49. N-(4-(morpholine-4-ylmethyl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

50. N-(3-morpholine-4-yl-benzyl)-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-ndimethylacetamide

51. 2-[2-(2,4-dichloro-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-1-(2-piperidine-1-ylmethyl-pyrrolidin-1-yl)-alanon

52. 2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

53. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(3-methoxy-phenyl)-piperazine-1-yl]-alanon

54. 1-(4-cyclohexylmethyl-piperazine-1-yl)-2-[1-(3,4-dichloro-phenylsulphonyl)-pyrrolidin-2-ylethoxy]-alanon

55. 2-[1-(4-methoxy-2,6-dimethyl-phenylsulfonyl)-pyrrolidin-2-ylethoxy]-N-(4-(morpholine-4-ylmethyl-benzyl)-ndimethylacetamide

56. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-(4-phenyl-piperazine-1-yl)-alanon

57. 1-(4-benzyl-piperidine-1-yl)-2-[1-(3,4-dichloro-phenylsulphonyl)-piperidin the-2-ylethoxy]-alanon

58. 1-[4-(3-dimethylamino-propyl)-piperazine-1-yl]-2-[1-(3-trifluoromethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-alanon

59. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(4-fluoro-phenyl)-piperazine-1-yl]-alanon

60. 2-[1-(4-methoxy-2,6-dimethylbenzenesulfonyl)-pyrrolidin-2-ylethoxy]-N-(4-piperidine-1-yl-benzyl)-ndimethylacetamide

61. N-(4-(morpholine-4-ylmethyl-benzyl)-2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-ndimethylacetamide

62. 2-[1-(3,4-dichloro-phenylsulphonyl)-pyrrolidin-2-ylethoxy]-1-[4-(1-methyl-piperidine-4-yl)-piperazine-1-yl]-alanon

63. 1-[2-(4-dimethylamino-phenyl)-azepin-1-yl]-2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-alanon

64. 2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-1-(2-piperidine-1-ylmethyl-pyrrolidin-1-yl)-alanon

65. 2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-morpholinopropan-1-yl)alanon

66. 1-(3-dimethylamino-pyrrolidin-1-yl)-2-[1-(naphthyl-1-sulfonyl)-piperidine-2-ylethoxy]-alanon

67. 1-(4-benzyl-[1,4]diazepan-1-yl)-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-alanon

68. 1-(4-cyclohexylmethyl-piperazine-1-yl)-2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-alanon

69. 2-((2-(4-methoxybenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

70. N-(1-benzyl-piperidine-3-ylmethyl)-2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-Ilmatar and]ndimethylacetamide

71. N-(4-piperidine-1-yl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

72. 2-((1-(3,4-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperazine-1-yl)alanon

73. N-(4-dimethylaminomethyl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-pyrrolidin-2-ylethoxy]-ndimethylacetamide

74. N-(4-piperidine-1-yl-benzyl)-2-[1-(2,4,6-trichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

75. N-[2-(4-methyl-piperazine-1-yl)-benzyl]-2-[2-(2,4,6-trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-ndimethylacetamide

76. N-(3-piperidine-1-ylmethyl-phenyl)-2-[1-(2,4,6-trimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

77. 1-[4-(3-methoxy-phenyl)-piperazine-1-yl]-2-[1-(2,4,6-trimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-alanon

78. N-(1-benzyl-pyrrolidin-3-yl)-2-[2-(2,4-dichloro-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-N-methyl-ndimethylacetamide

79. 1-(4-benzyl-[1,4]diazepan-1-yl)-2-[2-(2,4-dichloro-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-alanon

80. N-[2-(4-methyl-piperazine-1-yl)-benzyl]-2-[1-(2,4,6-trimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

81. 2-[1-(3,4-dichloro-phenylsulfonyl)-2,3-dihydro-1H-indole-2-ylethoxy]-N-(4-pyrrolidin-1-ylmethyl-benzyl)-ndimethylacetamide

82. 2-[2-(3,4-dichloro-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-1-(2-piperidine-1-ylmethyl-pyrrolidin-1-yl)-alanon

83. N-(4-pyrrolidin-1-ylmethyl-benzyl)-2-[2-(2,4,trimethyl-phenylsulfanyl)-1,2,3,4-tetrahydro-isoquinoline-3-ylethoxy]-ndimethylacetamide

84. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(4-methoxy-phenyl)-piperazine-1-yl]-alanon

85. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(3-dimethylamino-propyl)-piperazine-1-yl]-alanon

86. 2-[1-(3,4-dichloro-phenylsulfanyl)-piperidine-2-ylethoxy]-1-[4-(2-fluoro-phenyl)-piperazine-1-yl]-alanon

87. N-[4-(2-methyl-imidazol-1-yl)-phenyl]-2-[1-(2,4,6-trimethyl-phenylsulfanyl)-piperidine-2-ylethoxy]-ndimethylacetamide

88. 2-[1-(3,4-dichloro-phenylsulphonyl)-pyrrolidin-2-ylethoxy]-1-[4-(3-dimethylamino-propyl)-piperazine-1-yl]-alanon

89. 2-[1-(3,4-dichloro-phenylsulphonyl)-pyrrolidin-2-ylethoxy]-1-(4-phenyl-piperazine-1-yl)-alanon

90. 2-(2-(1-(4-methoxybenzenesulfonyl)piperidine-2-yl)ethoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

91. 2-(2-(1-(4-methoxybenzenesulfonyl)piperidine-2-yl)ethoxy)-1-(4-feiticeira-1-yl)alanon

92. 3-((4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)acetyl)piperazine-1-yl)methyl)benzonitrile hydrochloride

93. 3-((4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)acetyl)piperazine-1-yl)methyl)benzonitrile hydrochloride

94. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)Etalon hydrochloride

95. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

96. 1-(3,4-dihydro-2,6-napthine the h-2(1H)-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)Etalon hydrochloride

97. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

98. 1-(4-(dihydro-1H-pyrido[1,2-a]pyrazin-2(6N,7H,8H,N,an)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

99. 1-(4-(dihydro-1H-pyrido[1,2-a]pyrazin-2(6N,7H,8H,N,an)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)acanon the dihydrochloride

100. 1-(4-(3,4-dihydro-2,6-naphthyridin-2(1H)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

101. tert-butyl 4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)acetyl)piperazine-1-carboxylate

102. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(piperazine-1-yl)Etalon hydrochloride

103. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-(pyridin-4-yl)-1,2,4-oxadiazol-5-yl)piperidine-1-yl)alanon

104. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(tetrahydro-2H-Piran-4-yl)piperazine-1-yl)alanon

105. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylcyclohexyl)piperazine-1-yl)alanon

106. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)acanon the dihydrochloride

107. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-meth is piperidin-4-yl)piperazine-1-yl)alanon

108. 2-((1-(2,6-dichloro-4-(trifluoromethyl)phenylsulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

109. 2-((1-(2-chloro-6-methylphenylsulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

110. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(naphthalen-1-ylsulphonyl)piperidine-2-yl)methoxy)alanon

111. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(naphthalen-2-ylsulphonyl)piperidine-2-yl)methoxy)alanon

112. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)Etalon hydrochloride

113. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(thieno[3,2-d]pyrimidine-4-yl)piperazine-1-yl)alanon

114. 2-((1-(4-chloro-2,5-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

115. 2-((1-(4-chloro-3-(trifluoromethyl)phenylsulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

116. 1-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)acetyl)piperidine-4-one

117. 1-(4-((1H-benzo[d]imidazol-2-yl)methyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

118. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)alanon

119. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(2,4,6-triisopropylphenyl is of IMT)piperidine-2-yl)methoxy)alanon

120. 2-((1-(2,4-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

121. 2-((1-(3-brompheniramine)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

122. 2-((1-(3-brompheniramine)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperazine-1-yl)alanon

123. 2-((1-(4-brompheniramine)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

124. 2-((1-(3-brompheniramine)piperidine-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

125. 2-((1-(4-brompheniramine)piperidine-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

126. 2-((1-(4-brompheniramine)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperazine-1-yl)alanon

127. (S)-2-((2-(4-methoxy-2,6-dimethylbenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

128. 2-((1-(5-chloro-1,3-dimethyl-1H-pyrazole-4-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

129. 2-((1-(6-chloroimidazo[2,1-b]thiazole-5-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

130. 1-(4-fluoro-1,4'-bipiperidine-1'-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

131. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(3-(o-tolyloxy)phenylsulfonyl)piperidine-2-yl)methoxy)alanon

133. (S)-2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-t is traditioinal-3-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

134. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-(trifluoromethyl)cyclohexyl)piperazine-1-yl)alanon

135. (S)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)azetidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

136. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-morpholine-2-(pyridin-3-yl)ethylamino)piperidine-1-yl)alanon

137. 2-((1-(benzo[b]thiophene-3-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

138. 2-((1-(2-chloro-4-(trifluoromethyl)phenylsulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

139. 2-((1-(2-chlorophenylsulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

140. (R)-2-((1-(4-methoxy-2,3,6-trimethylphenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

141. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

142. (S)-2-((2-(4-methoxybenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

143. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(1-(pyridin-4-yl)piperidine-4-yl)ethyl)ndimethylacetamide

144. 1-(4-(5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)method is si)alanon

145. 1-(4-(5,6-dihydro-[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

146. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-carbonyl)piperidine-1-yl)alanon

147. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperazine-1-yl)alanon

148. 2-((1-(4-bromo-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

149. 2-((1-(4-bromo-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

150. 2-((1-(4-bromo-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperazine-1-yl)alanon

151. 2-((1-(5-chloro-3-methylbenzo[b]thiophene-2-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

152. (R)-2-((1-(2-chloro-6-methylphenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

153. 2-((1-(2,5-bis(trifluoromethyl)phenylsulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

154. 2-((1-(7-chlorobenzo[C][1,2,5]oxadiazol-4-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

155. 2-((1-(4-methylnaphthalene-1-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

156.1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(2,4,5-trichlorovinylsilane)piperidine-2-yl)methoxy)acanon the dihydrochloride

157. 2-((1-(2-methylnaphthalene-1-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

158. 2-((1-(5-(dimethylamino)naphthalen-1-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)canondigital

159. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(o-tamilselvan)piperidine-2-yl)methoxy)acanon the dihydrochloride

160. 2-((1-(4-bromo-2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

161. (S)-2-((1-(2-chloro-6-methylphenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)Etalon hydrochloride

162. (S)-2-((1-(2-chloro-6-methylphenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

163. (S)-2-((1-(2-chloro-6-methylphenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)acanon the dihydrochloride

164. 2-(2-(1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)ethoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

165. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridine-3-yloxy)piperidine-1-yl)alanon

166. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(cinoxacin-6-ylmethyl)piperazine-1-yl)alanon

167. (S)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)Pieper is Zin-1-yl)alanon

168. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-(pyrrolidin-1-yl)hinzelin-7-yl)piperazine-1-yl)alanon

169. 2-((1-(4-fluoro-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

170. 2-((1-(2,5-dichlorothiophene-3-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

171. 2-((1-(benzo[b]thiophene-2-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

172. 2-((1-(2,5-dimethylthiophene-3-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

173. 2-((1-(2,3-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

174. 2-((1-(4-methoxynaphthalene-1-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

175. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(quinoline-8-ylsulphonyl)piperidine-2-yl)methoxy)acanon the dihydrochloride

176. 2-((1-(isoquinoline-5-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

177. (R)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

178. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((2-(naphthalen-2-ylsulphonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)is the Thanon the dihydrochloride

179. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(5,6,7,8-tetrahydronaphthalen-2-ylsulphonyl)piperidine-2-yl)methoxy)acanon the dihydrochloride

180. (S)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

181. (S)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)alanon

182. (S)-2-((2-(4-methoxybenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

183. (S)-2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

184. (S)-2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)alanon

185. (S)-2-((2-(4-methoxy-2,6-dimethylbenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)alanon

186. (S)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yloxy)piperidine-1-yl)Etalon hydrochloride

187. (S)-2-((2-(4-methoxy-2,6-dimethylbenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)alanon

188. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-((pyridin-4-yloxy)methyl)piperidine-1-yl)alanon

189. (S)-2-((2-(4-methoxybenzenesulfonyl)-1,2,3,4-then it is carbonated shall raiskinen-3-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)acanon the dihydrochloride

190. (S)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(pyrrolidin-1-yl)ethyl)piperidine-1-yl)Etalon hydrochloride

191. 2-((1-(2-chloronaphthalen-1-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)acanon the dihydrochloride

192. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

193. N-(4-(4,5-dihydro-1H-imidazol-2-yl)benzyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methylacetamide hydrochloride

194. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methyl-N-(2-(4-(pyrrolidin-1-yl)cyclohexyl)ethyl)ndimethylacetamide

195. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(pyrazin-2-yloxy)benzyl)ndimethylacetamide

196. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(pyrazin-2-yloxy)benzyl)ndimethylacetamide

197. 1-(4-((5-chloro-2-phenyl-1H-imidazol-4-yl)methyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

198. 1-(4-((1,5-dimethyl-1H-pyrazole-4-yl)methyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

199. 1-(4-((2-(dimethylamino)pyrimidine-5-yl)methyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

200. 1-(4-(6-fluoro-3,4-dihydroisoquinoline-2(1H)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)Pipa is one-2-yl)methoxy)alanon

201. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperidine-1-yl)alanon

202. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)-1,2,3,4-tetrahydroquinolin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

203. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(naphthalen-2-ylsulphonyl)-1,2,3,4-tetrahydroquinolin-2-yl)methoxy)alanon

204. 2-((1-(4-methoxybenzenesulfonyl)-1,2,3,4-tetrahydroquinolin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

205. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(pyrazin-2-yloxy)benzyl)ndimethylacetamide

206. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(1H-pyrrol[3,4-C]pyridine-2(3H)-yl)alanon

207. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(pyridin-3-yl)morpholine)alanon

208. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(3 -(pyridine-3-ylmethyl)pyrrolidin-1-yl)alanon

209. N-(2-(4-(dimethylamino)cyclohexyl)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methylacetamide

210. 2-((1-(6-methoxynaphthalene-2-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

211. 1-(4-(3,4-dihydropyrrolo[1,2-a]pyrazin-2(1H)-yl)piperidine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

212. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)1-(4-(2-(1-methylpiperidin-4-yl)ethyl)piperazine-1-yl)alanon

213. 2-((1-(3,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroquinolin-2-yl)methoxy)-N-(2-(4-(dimethylamino)cyclohexyl)ethyl)-N-methylacetamide

214. 1-(4-((2-((4-forfinal)(methyl)amino)pyrimidine-5-yl)methyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

215. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(6-(4-methylpiperazin-1-yl)-3,4-dihydroisoquinoline-2(1H)-yl)alanon

216. 2-((1-(3,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroquinolin-2-yl)methoxy)-N-methyl-N-(2-(4-(pyrrolidin-1-yl)cyclohexyl)ethyl)ndimethylacetamide

217. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-3-yl)piperidine-1-yl)alanon

218. N-((S)-1-benzylpyrrolidine-3-yl)-N-methyl-2-((1-(2-(trifluoromethyl)phenylsulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

219. 2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-methylbenzyl)piperazine-1-yl)alanon

220. 2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-penetrtion-2-yl)piperazine-1-yl)alanon

221. 2-(2-(1-(4-methoxybenzenesulfonyl)piperidine-2-yl)ethoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperazine-1-yl)alanon

222. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(5-methyl-1H-benzo[d]imidazol-2-yl)piperidine-1-yl)alanon

223. 1-(2-((4,6-dimethylpyridin-2-yl)methyl)piperidine-1-yl)-2-((2-(mesitylenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)alanon

224. 1-(2-(5-bromopyridin-3-yl)piperidine-1-yl)-2-((1-(3-(reformer)phenylsulfonyl)piperidine-2-yl)methoxy)alanon

225. 1-(1,4'-bipiperidine-1'-yl)-2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)alanon

226. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(pyridine-2-ylmethyl)pyrrolidin-1-yl)alanon

227. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(6-methoxypyridine-3-yl)piperidine-1-yl)alanon

228. 1-(2-((5-ethylpyridine-2-yl)methyl)piperidine-1-yl)-2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)alanon

229. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(2-((3-methylpyridin-2-yl)methyl)piperidine-1-yl)alanon

230. 1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)-2-((1-(naphthene-1-ylsulphonyl)piperidine-2-yl)methoxy)alanon

231. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

232. 2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)alanon

233. 2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

234. 1-(4-(4-sensitiza-2-yl)piperazine-1-yl)-2-((1-(mesitylenesulfonyl)piperidine-2-yl)methoxy)alanon

235. 1-(1,4'-bipiperidine-1'-yl)-2-((1-(naphthene-1-ylsulphonyl)piperidine-2-yl)methoxy)alanon

236. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(3-(pyridin-2-yl)pyrrolidin-1-yl)alanon

237. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(3-(pyridin-3-yl)pyrrolidin-1-yl)alanon

238. 2-((1-(4-methoxy-2,6-di is ethylvanillin)piperidine-2-yl)methoxy)-1-(3-(pyridin-4-yl)pyrrolidin-1-yl)alanon

239. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methyl-N-(2-(pyridin-4-yl)ethyl)ndimethylacetamide

240. 1-(2-((4,6-dimethylpyridin-2-yl)methyl)pyrrolidin-1-yl)-2-((1-(naphthene-1-ylsulphonyl)piperidine-2-yl)methoxy)alanon

241. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methyl-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)ndimethylacetamide

242. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-methylpiperazin-1-yl)alanon

243. N-(2-(1H-indol-3-yl)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

244. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-methylinosine-4-yl)ndimethylacetamide

245. 1-(4-(2-ethoxyethyl)piperazine-1-yl)-2-((2-(mesitylenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)alanon

246. 2-((2-(mesitylenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(2-methoxyethyl)piperazine-1-yl)alanon

247. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(pyridin-2-yl)pyrrolidin-1-yl)alanon

248. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(4-methylpiperazin-1-yl)ethyl)ndimethylacetamide

249. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-morpholine-2-(4-(trifluoromethyl)phenyl)ethyl)ndimethylacetamide

250. N-(5-(dimethylamino)pentyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

251. N-(2-(2-chlorophenyl)-2-morpholinoethyl)-2-((1-(4-methods the si-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

252. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(4-methoxyphenyl)-2-(pyrrolidin-1-yl)ethyl)ndimethylacetamide

253. 1-(4-(3,5-acid)piperazine-1-yl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)alanon

254. 1-(4-(2-(diisopropylamino)ethyl)piperazine-1-yl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)alanon

255. N-(1-benzylpiperidine-4-yl)-N-temporaril-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide

256. N-(2-morpholino-2-(pyridin-3-yl)ethyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide

257. N-(1-ethyl-1H-pyrazole-5-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

258. N-(isoquinoline-5-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

259. N-(2-(dimethylamino)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

260. N-(3-(2,6-dimethylpiperidin-1-yl)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

261. N-(2-(dimethylamino)-1-phenylethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

262. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)ndimethylacetamide

263. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(4-methylpiperazin-1-yl)-1-phenylethyl)ndimethylacetamide

264. N-(3-morpholinomethyl)-2-((2-(FeNi is sulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)ndimethylacetamide

265. 2-((2-(2,4-dichlorobenzenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-N-(3-morpholinomethyl)ndimethylacetamide

266. 2-((1-(3,4-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(piperidine-1-ylmethyl)morpholine)alanon

267. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

268. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

269. 1-(4-(2-(2,5-dimethyl-1H-pyrrol-1-yl)ethyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

270. 1-(4-(2-(diisopropylamino)ethyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

271. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(2-(pyridin-2-yl)pyrrolidin-1-yl)alanon

272. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(3-(pyridin-3-yl)pyrrolidin-1-yl)alanon

273. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(3-(pyridin-4-yl)pyrrolidin-1-yl)alanon

274. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperazine-1-yl)alanon

275. 2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

276. 2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline the-3-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

277. 2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(2-((6-methylpyridin-2-yl)methyl)piperidine-1-yl)alanon

278. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

279. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

280. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(2,5-dimethyl-1H-pyrrol-1-yl)ethyl)piperazine-1-yl)alanon

281. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(diisopropylamino)ethyl)piperazine-1-yl)alanon

282. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(3-(pyridin-4-yl)pyrrolidin-1-yl)alanon

283. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-4-yl)piperazine-1-yl)alanon

284. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-((6-methylpyridin-2-yl)methyl)piperidine-1-yl)alanon

285. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

286. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

287. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(2,5-dimethyl-1H-pyrrol-1-yl)ethyl)piperazine-1-yl)alanon

288. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-methoxyphenyl)piperazine-1-yl)alanon

289. 1-(4-(4-FPO is phenyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

290. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methoxyphenyl)piperazine-1-yl)alanon

291. 1-(4-isopropylpiperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

292. 2-((2-(mesitylenesulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

293. 2-((1-(3,4-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(pyrrolidin-1-ylmethyl)phenyl)ndimethylacetamide

294. N-(4-(dimethylamino)butyl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

295. 1-(4-ethylpiperazin-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

296. 1-(4-(pyrrolidin-1-yl)piperidine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

297. 1-(4-morpholinopropan-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

298. 1-(1,4'-bipiperidine-1'-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

299. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-(pyrrolidin-1-ylmethyl)benzyl)ndimethylacetamide

300. N-((1-benzylpiperidine-3-yl)methyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

301. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-(4-methylpiperazin-1-yl)phenyl)ndimethylacetamide

302. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-(4-methylpiperazin-yl)benzyl)ndimethylacetamide

303. N-((S)-1-benzylpyrrolidine-3-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-methylacetamide

304. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-methyl-N-(2-morpholino-1-phenylethyl)ndimethylacetamide

305. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(pyridin-2-yl)piperazine-1-yl)alanon

306. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-methoxy)-1-(4-(3-methoxyphenyl)piperazine-1-yl)alanon

307. 1-(4-(4-forfinal)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

308. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methoxyphenyl)piperazine-1-yl)alanon

309. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(pyrimidine-2-yl)piperazine-1-yl)alanon

310. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-feiticeira-1-yl)alanon

311. 1-(4-(5-chloro-2-were)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

312. 2-(4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)acetyl)piperazine-1-yl)nicotinamide

313. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(pyrrolidin-1-ylmethyl)benzyl)ndimethylacetamide

314. N-((1-benzylpiperidine-3-yl)methyl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

315. N-((S)-1-benzylpyrrolidine-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-methylacetamide

316. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-2-yl)piperazine-1-yl)alanon

317. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-methoxyphenyl)piperazine-1-yl)alanon

318. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-forfinal)piperazine-1-yl)alanon

319. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methoxyphenyl)piperazine-1-yl)alanon

320. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-feiticeira-1-yl)alanon

321. 1-(4-(5-chloro-2-were)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

322. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-(pyrrolidin-1-ylmethyl)benzyl)ndimethylacetamide

323. N-((1-benzylpiperidine-3-yl)methyl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

324. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(3-methoxyphenyl)piperazine-1-yl)alanon

325. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methoxyphenyl)piperazine-1-yl)alanon

326. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-feiticeira-1-yl)alanon

327. N-((1-benzylpiperidine-3-yl)methyl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

328. 1-(4-(4-methoxyphenyl)piperazine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

329. 1-(4-feiticeira-1-yl)-2-((1-(2,4,6-trichlo phenylsulfonyl)pyrrolidin-2-yl)methoxy)alanon

330. 1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

331. 1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

332. 1-(4-(2-(2,5-dimethyl-1H-pyrrol-1-yl)ethyl)piperazine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

333. 1-(4-(2-(diisopropylamino)ethyl)piperazine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

334. N-(1-benzylpiperidine-4-yl)-N-cyclopropyl-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

335. 1-(4-(pyridin-4-yl)piperazine-1-yl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)alanon

336. 1-(1,4'-bipiperidine-1'-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

337. 1-(1,4'-bipiperidine-1'-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

338. N-(2-(piperidine-1-yl)ethyl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

339. N-(2-(pyrrolidin-1-yl)ethyl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

340. 1-(4-(3,5-acid)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

341. 1-(4-(2-(diisopropylamino)ethyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

342. N-(1-benzylpiperidine-4-yl)-N-cyclopropyl-2-((1-(4-methoxy-2,6-dimethylphenyl sulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

343. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(pyrrolidin-1-yl)ethyl)ndimethylacetamide

344. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-morpholinopropan)ndimethylacetamide

345. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(pyridine-3-ylmethyl)ndimethylacetamide

346. 1-(4-(3-chlorophenyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

347. 1-(4-(3,4-dimetilfenil)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

348. 1-(4-(3,4-dichlorophenyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

349. 1-(4-(3,4-dichlorobenzyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

350. 1-(4-(4-bromobenzyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

351. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2,4,6-trimethylbenzyl)piperazine-1-yl)alanon

352. 1-(4-(4-Chlorobenzyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

353. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methylbenzyl)piperazine-1-yl)alanon

354. 1-(4-(3-chlorophenyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

355. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)method is si)-1-(4-(3,4-dimetilfenil)piperazine-1-yl)alanon

356. 1-(4-(3,4-dichlorophenyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

357. 1-(4-(3,4-dichlorobenzyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

358. 1-(4-(4-bromobenzyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

359. 1-(4-(4-Chlorobenzyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

360. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methylbenzyl)piperazine-1-yl)alanon

361. N-benzyl-N-(2-(dimethylamino)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

362. 1-(4-benzyl-1,4-diazepan-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

363. 1-((R)-3-(dimethylamino)pyrrolidin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

364. N-((S)-1-benzylpyrrolidine-3-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methylacetamide

365. N-(1-benzylpyrrolidine-3-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

366. N-(3-(1H-imidazol-1-yl)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

367. N-(4-(dimethylamino)benzyl)-N-isopropyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

368. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-meth is l-N-(2-morpholino-1-phenylethyl)ndimethylacetamide

369. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyridin-2-yl)piperazine-1-yl)alanon

370. N-(isoquinoline-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

371. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(1-methyl-1H-benzo[d]imidazol-2-yl)ndimethylacetamide

372. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(pyrimidine-4-yl)ndimethylacetamide

373. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-feiticeira-1-yl)alanon

374. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-((S)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)alanon

375. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-methyl-1,4-diazepan-1-yl)alanon

376. 1-(4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

377. N-benzyl-N-(2-(dimethylamino)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

378. 1-(4-(3,4-dichlorophenyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

379. N-(2-(dimethylamino)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methylacetamide

380. N-(2-(diethylamino)ethyl)-N-ethyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

381. 1-(4-(3,4-dichlorobenzyl)piperazine-1-yl)-2-((1-(-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

382. 1-(4-(4-bromobenzyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

383. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2,4,6-trimethylbenzyl)piperazine-1-yl)alanon

384. 1-(4-(4-Chlorobenzyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

385. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylbenzyl)piperazine-1-yl)alanon

386. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methoxybenzyl)piperazine-1-yl)alanon

387. 1-(4-(2-terbisil)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

388. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-methyl-2-phenylpiperazin-1-yl)alanon

389. 1-(3-(pyridin-3-yl)pyrrolidin-1-yl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)alanon

390. 1-(3-(pyridin-4-yl)pyrrolidin-1-yl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)alanon

391. N-methyl-N-(2-(pyridin-4-yl)ethyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide

392. N-methyl-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide

393. 1-(4-methylpiperazin-1-yl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)alanon

394. N-(pyridine-4-ylmethyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-is)methoxy)ndimethylacetamide

395. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-morpholinopropan-3-yl)ndimethylacetamide

396. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(6-morpholinopropan-3-yl)ndimethylacetamide

397. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(5-methyl-1H-benzo[d]imidazol-2-yl)piperidine-1-yl)alanon

398. 1-(2-(4-(dimethylamino)phenyl)pyrrolidin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

399. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(piperidine-1-ylmethyl)pyrrolidin-1-yl)alanon

400. 1-(2-(4-(dimethylamino)phenyl)azepin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

401. N-(2-(4-benzylpiperazine-1-yl)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

402. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-phenylthiazol-2-yl)piperazine-1-yl)alanon

403. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3,4-dimetilfenil)piperazine-1-yl)alanon

404. 1-(4-(3,4-dichlorophenyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

405. 1-(4-(3,4-dichlorobenzyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

406. 1-(4-(4-bromobenzyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

407. 1-(4-(4-chlorbenzyl)piperazin-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

408. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylbenzyl)piperazine-1-yl)alanon

409. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(pyrrolidin-1-yl)phenyl)ndimethylacetamide

410. 3-(4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)acetyl)piperazine-1-yl)propanenitrile

411. N-(3-(4-benzylpiperazine-1-yl)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

412. N-(3-(4-ethylpiperazin-1-yl)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

413. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(piperidine-1-yl)propyl)ndimethylacetamide

414. N-((1-benzylpyrrolidine-3-yl)methyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

415. N-((1-benzylpiperidine-3-yl)methyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

416. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(5-methyl-1H-pyrazole-1-yl)ethyl)ndimethylacetamide

417. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(2-(1-methyl-1H-benzo[d]imidazol-2-yl)ethyl)phenyl)ndimethylacetamide

418. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(piperidine-1-ylmethyl)phenyl)ndimethylacetamide

419. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(piperidine-1-ylmethyl)phenyl)ndimethylacetamide

420. N-(4-((1H-imidazol-1-is)methyl)phenyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

421. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-((4-methylpiperidin-1-yl)methyl)phenyl)ndimethylacetamide

422. N-((1-benzylpiperidine-3-yl)methyl)-2-((1-(4-methoxybenzenesulfonyl)indolin-2-yl)methoxy)ndimethylacetamide

423. 2-((1-(4-methoxybenzenesulfonyl)indolin-2-yl)methoxy)-N-(3-(piperidine-1-ylmethyl)phenyl)ndimethylacetamide

424. N-(3-(ethyl(phenyl)amino)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

425. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(pyrazin-2-yl)ethyl)ndimethylacetamide

426. N-(1-(1H-pyrazole-1-yl)propan-2-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

427. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(2-methyl-1H-imidazol-1-yl)phenyl)ndimethylacetamide

428. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(piperidine-1-yl)benzyl)ndimethylacetamide

429. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(piperidine-1-yl)phenyl)ndimethylacetamide

430. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(piperidine-1-yl)benzyl)ndimethylacetamide

431. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(4-methylpiperazin-1-yl)phenyl)ndimethylacetamide

432. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(4-methylpiperazin-1-yl)benzyl)ndimethylacetamide

433. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)labels and)-N-(3-(4-methylpiperazin-1-yl)benzyl)ndimethylacetamide

434. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(4-methylpiperazin-1-yl)benzyl)ndimethylacetamide

435. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-morpholinoethyl)ndimethylacetamide

436. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-morpholinomethyl)ndimethylacetamide

437. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-morpholinomethyl)ndimethylacetamide

438. 2-((1-methoxy-2,6-dimethylbenzenesulfonyl)-piperidine-2-yl)methoxy)-N-morpholinoethyl)ndimethylacetamide

439. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-morpholinomethyl)ndimethylacetamide

440. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(piperidine-1-yl)ethyl)ndimethylacetamide

441. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(dimethylamino)butyl)ndimethylacetamide

442. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-forfinal)piperazine-1-yl)alanon

443. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(pyrrolidin-1-yl)piperidine-1-yl)alanon

444. 1-(4-(2-terbisil)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

445. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-methyl-2-phenylpiperazin-1-yl)alanon

446. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-methyl-N-(2-(4-methylpiperazin-1-yl)-1-phenylethyl)ndimethylacetamide

447. 2-((1-(4-methods the si-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(2-(pyridine-2-ylmethyl)pyrrolidin-1-yl)alanon

448. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(2-((6-methylpyridin-2-yl)methyl)pyrrolidin-1-yl)alanon

449. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(2-(pyridine-2-ylmethyl)piperidine-1-yl)alanon

450. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-methyl-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)ndimethylacetamide

451. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(4-methoxybenzyl)piperazine-1-yl)alanon

452. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-(dimethylamino)ethyl)piperazine-1-yl)alanon

453. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(2-(pyridine-4-ylmethyl)piperidine-1-yl)alanon

454. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-terbisil)piperazine-1-yl)alanon

455. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-methyl-2-phenylpiperazin-1-yl)alanon

456. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(pyridine-2-ylmethyl)pyrrolidin-1-yl)alanon

457. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-((4,6-dimethylpyridin-2-yl)methyl)pyrrolidin-1-yl)alanon

458. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-((6-methylpyridin-2-yl)methyl)pyrrolidin-1-yl)alanon

459. N-(2-(pyrrolidin-1-yl)ethyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide

460. 1-(4-benzylpiperazine-1-yl)-2-((1-(4-methoxy-2,6-dim chilenischer)pyrrolidin-2-yl)methoxy)alanon

461. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-phenylpiperazin-1-yl)alanon

462. 1-(4-(benzo[d][1,3]dioxol-5-ylmethyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

463. N-benzyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-methylpyridin-2-yl)ndimethylacetamide

464. N-benzyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(6-methylpyridin-2-yl)ndimethylacetamide

465. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(3-(trifluoromethyl)phenyl)piperazine-1-yl)alanon

466. N-ethyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(pyridine-4-ylmethyl)ndimethylacetamide

467. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-methyl-1,4-diazepan-1-yl)alanon

468. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-yl)alanon

469. 1-(4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

470. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-(2-(1-methyl-1H-benzo[d]imidazol-2-yl)ethyl)phenyl)ndimethylacetamide

471. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(3-(piperidine-1-ylmethyl)phenyl)ndimethylacetamide

472. N-(4-(2-(1H-benzo[d]imidazol-2-yl)ethyl)phenyl)-2-((1-(4-methoxy-2,6-dimethylphenyl the Nile)pyrrolidin-2-yl)methoxy)ndimethylacetamide

473. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(2-(4-methylpiperazin-1-yl)benzyl)ndimethylacetamide

474. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(5-methyl-1H-benzo[d]imidazol-2-yl)piperidine-1-yl)alanon

475. 1-(2-(4-(dimethylamino)phenyl)azepin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

476. 1-((R)-3-(dimethylamino)pyrrolidin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

477. N-(1-benzylpiperidine-4-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

478. 1-(4-benzylpiperazine-1-yl)-2-((1-(2,5-dichlorothiophene-3-ylsulphonyl)pyrrolidin-2-yl)methoxy)alanon

479. 2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-phenylpiperazin-1-yl)alanon

480. 1-(4-benzylpiperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

481. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-(trifluoromethyl)phenyl)piperazine-1-yl)alanon

482. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-ethyl-N-(pyridine-4-ylmethyl)ndimethylacetamide

483. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-methyl-1,4-diazepan-1-yl)alanon

484. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-yl)alanon

485. 1-(4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)piperazine-1-the l)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

486. N-benzyl-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(pyridin-2-yl)ndimethylacetamide

487. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(5-methyl-1H-benzo[d]imidazol-2-yl)piperidine-1-yl)alanon

488. N-(1-benzylpiperidine-4-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

489. N-benzyl-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(2-(dimethylamino)ethyl)ndimethylacetamide

490. 1-(2-((5-ethylpyridine-2-yl)methyl)pyrrolidin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

491. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(2-methoxyphenyl)piperazine-1-yl)alanon

492. 1-(4-(cyclohexylmethyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

493. N-(3-chloro-4-morpholinomethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

494. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(1-methyl-1H-benzo[d]imidazol-5-yl)ndimethylacetamide

495. N-(2-(dimethylamino)-2-(4-(trifluoromethyl)phenyl)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

496. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(2-(pyrrolidin-1-yl)-2-(4-(trifluoromethyl)phenyl)ethyl)ndimethylacetamide

497. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(pyridin-3-yl)pyrrolidin-1-yl)alanon

498. 2-((1-(2,6-dichlorophenols hanil)piperidine-2-yl)methoxy)-1-(4-(2-methoxyphenyl)piperazine-1-yl)alanon

499. 1-(4-(cyclohexylmethyl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

500. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(2-morpholino-1-phenylethyl)ndimethylacetamide

501. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(1-methyl-1H-indazol-6-yl)ndimethylacetamide

502. N-(2-(2-chlorophenyl)-2-(pyrrolidin-1-yl)ethyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

503. 1-(4-(3,5-acid)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

504. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(1-methyl-1H-benzo[d]imidazol-2-yl)ndimethylacetamide

505. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)ndimethylacetamide

506. 3-(4-(2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)acetyl)piperazine-1-yl)propanenitrile

507. N-benzyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-methylpyridin-2-yl)ndimethylacetamide

508. N-benzyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(6-methylpyridin-2-yl)ndimethylacetamide

509. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-(trifluoromethyl)phenyl)piperazine-1-yl)alanon

510. N-ethyl-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(pyridine-4-ylmethyl)ndimethylacetamide

511. 1-(4-(3-chlorophenyl)piperazine-1-yl)-2-((1-(4-methoxy,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

512. 1-(4-(3,4-dimetilfenil)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

513. 2-(4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)acetyl)piperazine-1-yl)nicotinamide

514. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-yl)alanon

515. N-benzyl-2-((1-(2,5-dichlorothiophene-3-ylsulphonyl)piperidine-2-yl)methoxy)-N-(6-methylpyridin-2-yl)ndimethylacetamide

516. 1-(4-(2-forfinal)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

517. 1-(4-ethylpiperazin-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

518. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(pyrrolidin-1-yl)piperidine-1-yl)alanon

519. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-morpholinopropan-1-yl)alanon

520. 1-(1,4'-bipiperidine-1'-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)alanon

521. N-(3-(4-benzylpiperazine-1-yl)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

522. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(3-(piperidine-1-yl)propyl)ndimethylacetamide

523. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-(pyrrolidin-1-yl)butyl)ndimethylacetamide

524. 2-((1-(4-methoxy-2,6-dimethylphenols hanil)piperidine-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

525. N-(3-(1H-benzo[d]imidazol-2-yl)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

526. 1-(4-(benzo[d]thiazol-2-yl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

527. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(2-methyl-1H-imidazol-1-yl)phenyl)ndimethylacetamide

528. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(4-(dimethylamino)phenyl)pyrrolidin-1-yl)alanon

529. 1-(4-benzyl-1,4-diazepan-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

530. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(dimethylamino)benzyl)-N-isopropylacetate

531. 2-(4-(2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)acetyl)-1,4-diazepan-1-yl)nicotinamide

532. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-methyl-N-(2-(piperidine-1-yl)ethyl)ndimethylacetamide

533. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

534. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-1-(2-(2-morpholinoethyl)piperidine-1-yl)alanon

535. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(5-methyl-1H-pyrazole-3-yl)ndimethylacetamide

536. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(5-phenyl-1H-pyrazole-3-yl)ndimethylacetamide

537. N-(3-(4-chlorophenyl)-1H-pyrazole-5-yl)-2-((1-(4-methoxy-2,6-is metilprednisolone)piperidine-2-yl)methoxy)ndimethylacetamide

538. N-(4-(3,4-acid)-1H-pyrazole-5-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

539. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-(thiophene-2-yl)-1H-pyrazole-5-yl)ndimethylacetamide

540. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(5-(2-methoxyphenyl)-1H-pyrazole-3-yl)ndimethylacetamide

541. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(5-(3-methoxyphenyl)-1H-pyrazole-3-yl)ndimethylacetamide

542. N-(5-(3-forfinal)-1H-pyrazole-3-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

543. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(5-(4-methoxyphenyl)-1H-pyrazole-3-yl)ndimethylacetamide

544. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-p-tolyl-1H-pyrazole-5-yl)ndimethylacetamide

545. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-phenyl-1H-pyrazole-5-yl)ndimethylacetamide

546. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)-N-(quinoline-2-yl)ndimethylacetamide

547. 2-((1-(4-methoxybenzenesulfonyl)indolin-2-yl)methoxy)-1-(4-(2-(piperidine-1-yl)ethyl)piperidine-1-yl)alanon

548. 1-(4-(2-(2,5-dimethyl-1H-pyrrol-1-yl)ethyl)piperazine-1-yl)-2-((1-(4-methoxybenzenesulfonyl)indolin-2-yl)methoxy)alanon

549. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-N-(4-(morpholinomethyl)benzyl)ndimethylacetamide

550. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(-(4-(trifluoromethyl)phenyl)piperazine-1-yl)alanon

551. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3,5-dichloropyridine-2-yl)piperazine-1-yl)alanon

552. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-hydroxyethyl)piperazine-1-yl)alanon

553. 1-(4-(benzo[d]thiazol-2-yl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

554. 1-(4-(6-chlorobenzo[d]thiazol-2-yl)piperazine-1-yl)-2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)alanon

555. N-(4-(4-ethylpiperazin-1-yl)phenyl)-2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

556. 2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)-N-(7-morpholines[C][1,2,5]oxadiazol-4-yl)ndimethylacetamide

557. 2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)-N-(3-methyl-4-(2-(piperidine-1-yl)acetamido)phenyl)ndimethylacetamide

558. 2-((1-(4-methoxybenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(2-phenoxyethyl)piperazine-1-yl)alanon

559. 1-(4-(2-(2,5-dimethyl-1H-pyrrol-1-yl)ethyl)piperazine-1-yl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

560. 1-(4-(3-(dimethylamino)propyl)piperazine-1-yl)-2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)alanon

561. N,N-bis(3-(dimethylamino)propyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

562. 2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)E. the anon

563. 2-((2-(4-methoxy-2,3,6-trimethylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-3-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)alanon

564. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(3-(dimethylamino)propyl)piperazine-1-yl)alanon

565. 2-((1-(2,6-dichlorobenzenesulfonyl)piperidine-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

566. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(3-(dimethylamino)propyl)piperazine-1-yl)alanon

567. 2-((1-(2,6-dichlorobenzenesulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

568. 1-(4-benzylpiperazine-1-yl)-2-((1-(4-chloro-2,5-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)alanon

569. 2-((1-(2,6-dichloro-4-(trifluoromethyl)phenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(3-(dimethylamino)propyl)piperazine-1-yl)alanon

570. 2-((1-(2,6-dichloro-4-(trifluoromethyl)phenylsulfonyl)pyrrolidin-2-yl)methoxy)-1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)alanon

571. 1-(4-(1-methylpiperidin-4-yl)piperazine-1-yl)-2-((1-(2-(trifluoromethyl)phenylsulfonyl)piperidine-2-yl)methoxy)alanon

572. 2-((1-(benzo[b]thiophene-3-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-(4-methylpiperazin-1-yl)piperidine-1-yl)alanon

573. 2-((1-(benzo[b]thiophene-3-ylsulphonyl)piperidine-2-yl)methoxy)-1-(4-((1-methylpiperidin-4-yl)methyl)piperazine-1-yl)alanon

574. N-((S)-1-benzylpyrrolidine-3-yl)-2-((1-(2,6-dichloro-4-(trifluoromethyl)phenylsulfonyl)PIP is ridin-2-yl)methoxy)-N-methylacetamide

575. N-(4-(dimethylamino)benzyl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

576. N-(4-(dimethylamino)benzyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)ndimethylacetamide

577. N-(4-(dimethylamino)benzyl)-2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)piperidine-2-yl)methoxy)ndimethylacetamide

578. N-(4-(dimethylamino)benzyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide

579. 2-((1-(4-methoxy-2,6-dimethylbenzenesulfonyl)pyrrolidin-2-yl)methoxy)-N-(4-morpholinomethyl)ndimethylacetamide

580. N-(4-morpholinomethyl)-2-((1-(2,4,6-trichloranisole)pyrrolidin-2-yl)methoxy)ndimethylacetamide

581. N-(4-morpholinomethyl)-2-((1-(2,4,6-trichloranisole)piperidine-2-yl)methoxy)ndimethylacetamide
in the form of the racemate; of the enantiomers, of the diastereomers, mixtures of enantiomers or diastereomers or of an individual enantiomer or diastereoisomer; the bases and/or salts of physiologically compatible acids.

9. The method of obtaining substituted sulfa derivative according to claim 1

moreover, the carboxylic acid of General formula L in the amide formation is subjected to interaction with primary or secondary amines of General formula M, in the presence of dehydrating means, such as sodium sulfate or magnesium sulfate, phosphorus oxide or reagents such as, for example, CDI, DCC, TBTU, EDCI, or in the presence of HOAt or HOBt and an organic base is, for example DIPEA or pyridine, in an organic solvent, such as THF, dichloromethane, diethyl ether, dioxane, DMF or acetonitrile.

10. The drug, which has antagonistic effect on bradykinesia receptor 1 (B1R)containing at least one substituted sulfa derivative according to one of claims 1 to 8, optionally containing suitable additives and/or auxiliary substances.

11. The use of substituted sulfa derivative according to one of claims 1 to 8 to obtain drugs for the treatment of pain, especially acute, neuropathic or chronic pain.

12. The use of substituted sulfa derivative according to one of claims 1 to 8 to obtain drugs for the treatment of pain, especially acute vnutrennostej, neuropathic or chronic pain.

13. The use of substituted sulfa derivative according to one of claims 1 to 8 to obtain drugs for the treatment of migraine, diabetes, respiratory diseases, inflammatory intestinal diseases, neurological diseases, inflammations of the skin, rheumatic diseases, septic shock, reperfusion syndrome, obesity and as an inhibitor of angiogenesis.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are produced new diazepane substituted compounds representing various heterocyclic systems, including condensed, pharmaceutical compositions containing said compounds.

EFFECT: producing the compounds and compositions for preventing and treating neurological and mental disorders and diseases with involved orexin receptors.

13 cl, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I , and pharmaceutically acceptable salts thereof, where L denotes O, S, or CH2; Y denotes N or CH; Z denotes CR3; G denotes CH; R1 denotes a heteroaryl ring of formula , where D1 denotes S, O; D2 denotes N or CR12; D3 denotes CR12; R2 denotes (C6-C10)-aryl; 5-9-member mono- or bicyclic heteroaryl with 1 or 2 heteroatoms independently selected from N or S; a saturated or partially saturated (C3-C7)-cycloalkyl; or a saturated 5-6-member heteocyclyl with 1 heteroatom selected from N, where said aryl, heteroaryl, cycloalkyl and heterocyclyl are optionally substituted with one or two groups independently selected from (C1-C6)-alkyl, F, Cl, Br, CF3, CN, NO2, OR6, C(-O)R6, C(=O)OR6, C(=O)NR6R7, saturated 6-member heterocyclyl with 2 heteroatoms independently selected from N or O, and S(O)2R6, and where said alkyl is optionally substituted with one -OR8 group; R3 denotes H; (C1-C6)-alkyl; (C2-C6)-alkenyl; Cl; Br; OR6; SR6; phenyl; or a 6-member heteroaryl with 1 heteroatom selected from N, where said alkyl and alkenyl are optionally substituted with one group selected from C(=O)OR8, -OR8, -NR8R9; or a saturated 6-member heterocyclyl with 1 heteroatom selected from N or O.

EFFECT: disclosed compounds are used in treating and preventing diseases mediated by insufficient level of glucokinase activity, such as sugar diabetes.

16 cl, 479 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of indole with formula (I) or indole pharmaceutically acceptable salts: where: ring A stands for a benzene or a tiofen ring; R1 stands for a C1-.6 alkyl that may be substituted by one or several groups selected from among -OH, - O-C1-6 alkyl, an amino group that may be substituted by one or two C1-6 alkyls; -O-C1-6 alkyl; a halogen; CN; 5-6-membered cyclic amine; n is equal to 0 - 4 and to 0- 2 if ring A is a benzene or a tiofen ring accordingly; R2 stands for -H, -C1-6 alkyl; R3 stands for H, -C1-6 alkyl that may be substituted by phenyl, C3-6 cycloalkyl; R4 stands for C1-6 alkyl that may be substituted by one or several groups selected from among -OH, -O- C1-6 alkyl, an amino group that may be substituted by one or two C1-6 alkyls and 5-6-membered cyclic amine; C3-6 cycloalkyl, phenyl or-OH; X1 stands for -CH2-, -O-, -S-, -CH(R°)-; X2 stands for -C(RA)(RB)-, -O-; X3 stands for -C(RC)(RD)-; m is equal to 1 - 3; R° stands for -H, or R°, together with R4, form C3-6 alkylene; RA, RB, RC and RD are identical or different and stand for -H, C1-6 alkyl where, in case m is equal to 2 or 3, each RC and R° may be identical or different provided 1- methyl-4a-phenyl-2,3,4,4a,5,9b-hexahydro-1H-indeno [1,2-b] pyridine, 4a-phenyl-2,3,4,4a,5,9b-hexahydro-4aH-indeno [1,2-b] pyridine and 2-(1,2,3,4,5,9b-hexahydro-4aH-indeno [1,2-b] pyridine -4a-yl)-N,N-dimethylethanamine are excluded).

EFFECT: compounds possess antagonistic activity regarding NMDA receptor which enables their usage in pharmaceutical compositions for treatment of Alzheimer disease, vascular dementia, Parkinson disease, chronic depression, attention deficit hyperactivity disorder, migraines etc.

18 cl, 40 tbl, 84 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of formula (I) or to their pharmaceutically acceptable salts, in which X is selected from group, consisting of-C(R1)2-, -O-, -S-, -S(O2)-, -NR1-; each R1 is independently selected from group consisting of H and alkyl; each of R2, R3 and R4 is independently selected from group consisting of (1) H, (2) alkyl, (3) -OR5, (4) alkylene-OR5, (5) -alkylene-R6, (6) -C(O)O-alkyl, (7) - alkylene-C(O)O-alkyl, (8) -alkylene-R8, (9) -NHR5, (10) -N(R5)2, (11) alkenyl, (12) -NH-R8, (13) -NH-CH(C(O)O(C1-C6)alkyl)-alkylene-O-alkyleneR6, (14)-NHCH(C(O)O(C1-C6)aalkyl)-alkylene-OH, (15) -NH-C(O)-alkenyl and (16) -N(C1-C6alkyl)C(O)-alkenyl; or R2 and R3 or R2 and R4 or R3 and R4 together with atoms with which they are bound, form condensed 3-7-member cycloalkyl or heterocycloalkyl ring, which represents non-aromatic monocyclic ring system, which contains in ring from about 5 to about 7 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen or oxygen, and said condensed cycloalkyl or heterocycloalkyl ring is not substituted or is substituted with one or several groups L3 ; and on condition that if X represents -O-, and m equals 1, then, at least, one of R2, R3 or R4 is not H; each R5 is independently selected from group consisting of (1) H, (2) (C1-C6)alkyl, (3) hydroxy-substituted alkyl, (4) R6, (5) R7, (6) -C(O)-(C1-C6)alkyl, (7) -C(O)-(C1-C6)halogenalkyl, (8) -C(O)-R6, (9) -C(O)-R7, (10) -C(O)NH-(C1-C6)alkyl, (11) -C(O)N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (12) -S(O)2-(C1-C6)alkyl, (13) -S(O)2-(C1-C6)halogenalkyl, (14) -S(O)2-R6, (15) -S(O)2-R7, (16) -S(O)2-R8, (17) -alkylene-C(O)-(C1-C6)alkyl, (18) -alkylene-C(O)-(C1-C6)halogen-alkyl, (19) -alkylene-C(O)-R6, (20) -alkylene-C(O)-R7, (21) -alkylene-S(O)2-(C1-C6)alkyl, (22) -alkylene-S(O)2-(C1-C6)halogenalkyl, (23) -alkylene-S(O)2-R6, (24) -alkylene-S(O)2-R7, (25) -alkylene-S(O)2-R8, (26) -alkylene-NHC(O)-(C1-C6)alkyl, (27) -alkylene-NHC(O)-(C1-C6)halogenalkyl, (28) alkylene-NHC(O)-R6, (29) -alkylene-NHC(O)-R7, (30) -alkylene-NHS(O)2-(C1-C6)alkyl, (31) -alkylene-NHS(O)2-(C1-C6)halogenalkyl, (32) -alkylene-NHS(O)2-R6, (33) -alkylene-NHS(O)2-R7, (34) -alkylene-N(alkyl)C(O)-(C1-C6)alkyl, (35) -alkylene-N(alkyl)C(O)-(C1-C6)halogenalkyl, (36) -alkylene-N(alkyl)C(O)-R6, (37) -alkylene-N(alkyl)C(O)-R7, (38) -alkylene-N(alkyl)S(O)2-(C1-Ce)alkyl, (39) -alkylene-N(alkyl)S(O)2-(C1-C6)halogen-alkyl, (40)-alkylene-N(alkyl)S(O)2-R6, (41) -alkylene-N(alkyl)S(O)2-R7, (42) -alkylene-C(O)-NH-(C1-C6)alkyl, (43) -alkylene-C(O)-NHR6, (44) -alkylene-C(O)-NHR7, (45) -alkylene-S(O)2NH-(C1-C6)alkyl, (46) -alkylene-S(O)2NH-R6, (47) -alkylene-S(O)2NH-R7 , (48) -alkylene-C(O)-N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (49) -alkylene-C(O)-N(alkyl)-R6, (50) -alkylene-C(O)-N(alkylene)-R7, (51) -alkylene-S(O)2N((C1-C6)alkyl)2, in which each alkyl group is selected independently, (52) -alkylene-S(O)2N(alkyl)-R6, (53) -alkylene-S(O)2N(alkyl)-R7, (54) -alkylene-OH, (55) -alkylene-OC(O)-NH-alkyl, (56) -alkylene-OC(O)NH-R8, (57) -alkylene-CN, (58) -R8, (59) -alkylene-SH, (60) -alkylene-S(O)2-NH-R8, (61) -alkylene-S(O)2-alkylene-R6, (62) substituted with halogen alkylene, (63) -C(O)OR8, (64) -C(O)O(C1-C6)alkyl, (65) -C(O)R8, (66) -C(O)-alkylene-O-(C1-C6)alkyl, (67) -C(O)NH2, (68) -alkylene-O-(C1-C6)alkyl, (69) -alkylene-R8, (70) -S(O)2-halogen(C1-C6)alkyl, (71) hydroxy-substituted halogen(C1-C6)alkyl, (72) -alkylene-NH2, (73) -alkylene-NH-S(O)2-R8, (74) -alkylene-NH-C(O)-R8, (75) -alkylene-NH-C(O)O-(C1-C6)alkyl, (76) -alkylene-O-C(O)-(C1-C6)alkyl, (77) -alkylene-O-S(O)2-(C1-C6)alkyl, (78) -alkylene-R6 , (79) -alkylene-R7, (80) -alkylene-NH-C(O)NH-(C1-C6)alkyl, (81) -alkylene-N(S(O)2 halogen(C1-C6)alkyl)2, and each -S(O)2 halogen(C1-C6)alkyl fragment is selected independently, (82) -alkylene-N((C1-C6)alkyl)S(O)2-R8 , (83) -alkylene-OC(O)-N(alkyl)2, and each alkyl is selected independently, (84) -alkylene-NH-(C1-C6)alkyl, (85) -C(O)-alkylene-C(O)O-(C1-C6)alkyl, (86) -C(O)-C(O)-O-(C1-C6)alkyl, (87) -C(O)-alkylene-R6, (88) -C(O)-NH-R8, (89) -C(O)-NH-R6, (90) -C(O)-NH-alkylene-R6, (91) -C(O)-alkylene-NH-S(O)2-halogen(C1-C6)alkyl, (92) -C(O)-alkylene-NH-C(O)-O-(C1-C6)alkyl, (93) -C(O)-alkylene-NH2, (94) -C(O)-alkylene-NH-S(O)2-R8, (95) -C(O)-alkylene-NH-S(O)2-(C1-C6)alkyl, (96) -C(O)-alkylene-NH-C(O)-(C1-C6)alkyl, (97) -C(O)-alkylene-N(S(O)2(C1-C6)alkyl)2, and each -S(O)2(C1-C6)alkyl fragment is elected independently, (98) -C(O)-alkylene-NH-C(O)-NH-(C1-C6)alkyl, (99) -alkylene-O-R6, (100) -alkylene-R7, (101) -C(O)OH, (102) -alkylene-N(S(O)2(C1-C6)alkyl)2, (103) -alkylene-C(O)-O-(C1-C6)alkyl, (104) halogenalkyl, (105) halogen, (106) -alkylene-C(O)-NH2, (107) =N-O-(C1-C6)alkyl, (108) =N-O-alkylene-R6, (109) =N-O-alkenyl, (110) -N-O-R6, (111) =N-NH-S(O)2-R6, (112) alkenyl, (113) =R8, (114) -O-C(O)-R9, (115) -O-C(O)-(C1-C6)alkyl, (116)-CN, R6 is selected from group consisting of unsubstituted (C6-C14)aryl, (C6-C14)aryl, substituted with one or several groups L1, unsubstituted (C5-C14)heteroaryl and (C5-C14)heteroaryl, which represents aromatic monocyclic or bicyclic system, which contains in ring from about 5 to about 9 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen, oxygen or sulphur, one or in combination, substituted with one or several groups L1; R7 is selected from group consisting of unsubstituted heterocycloalkyl and heterocycloalkyl which represents non-aromatic monocyclic system, which contains in ring from about 4 to about 6 atoms, and one or several atoms in ring system represent atom of element, different from carbon, for instance, nitrogen, oxygen substituted with one or several groups L2; R8 is selected from group consisting of unsubstituted cycloalkyl and cycloalkyl substituted with one or several groups L2; A8 is selected from group consisting of (a) unsubstituted aryl, (b) aryl substituted with one or several groups L1; each group L1 is independently selected fron group consisting of halogen, alkyl, -CN, -CF3, -O-(C1-C6)alkyl, -O-(halogen(C1-C6)alkyl), -alkylen-OH (-CH2OH); each group L2 is independently selected from group consisting of (a) -OH, (b) alkyl, (c) alkyl substituted with one or several groups -OH and (d) piperidyl; each group L3 is independently selected from group consisting of -CN, =O, R5 , -OR5 ; =N-R5 and -N(R5)2; n equals 0, 1, 2 or 3; and m equals 0, 1 or 2; and on condition that in composition of substituent -OR5 fragment R5 and oxygen atom, which it is bound with, do not form group -O-O-; and on condition that in composition of substituents -OR5, =N-R5 and -NHR5 R5 are not -CH2OH, -CH2NH2, -CH2NH-alkyl, -CH2NH-aryl or -C(O)OH. Invention also relates to pharmaceutical composition, as well as to application of one or several compounds by one of ii. 1-125.

EFFECT: obtaining novel biologically active compounds possessing properties of γ-secretase inhibitor.

127 cl, 447 ex, 94 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to azabenzothiophenyl compounds of formula I

and salts thereof, where: Z1 denotes CR1; Z2 denotes N; Z3 denotes CR3; Z4 denotes CR4; R1, R3 and R4 are independently selected from H or halogen; W denotes , R5 and R6 denote H; X1 denotes -OR11; X2 denotes phenyl which is optionally substituted with one or two groups selected from halogen or (C1-C3)alkylsulphanyl; R11 denotes (C1-C12) alkyl, substituted by one or two groups independently selected from - (CR19R20)nOR16; n equals 0; R16 denotes H, (C1-C12) alkyl or (C2-C8) alkenyl. The invention also relates to a pharmaceutical composition based on said compounds, which can be used in medicine for treating hyperproliferative disorders.

EFFECT: high efficiency of using said compounds.

11 cl, 12 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formulae

and ,

which can be used to inhibit lipid kinase, including PI3K, and treat lipid kinase-mediated disorders. Values of radicals are given in claim 1.

EFFECT: improved properties of the compound.

11 cl, 2 tbl, 7 ex

Antiviral compound // 2441010

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds or their pharmaceutically acceptable salts where the compound has formula (I). The compounds have the properties of hepatitis C virus (HCV) replication inhibition and can be used for treating HCV-infection. In formula (I) B represents heterocyclyl selected from thieno, thiazolo, pyrazolo, pyrido and pyrimidogroup with B being optionally substituted by one or more R18, A represents phenyl which is optionally substituted by one or more R18; each W1 and W2 are independently selected from N or C(R33); Z represents -NH-; each R10 and R33 containing of hydrogen; X is selected from a group consisting of -Ls-O-, -Ls-S-; R22 means hydrogen or phenyl optionally substituted by one or more R26 ; Y is selected from a group consisting of -Ls-O-, -Ls-S-; -Ls-C(O)- and -Ls-NH(SO)2-; R50 represents -L1-A1, where L1 represents a bond, and A1 is selected from a group consisting of carbocyclyl where carbocyclyl represents phenyl or C3-C6carbocyclyl, banzimidazolyl and C1-C6alkyl optionally substituted by phenyl where A1 is optionally substituted by one or more R30 ; the substitute values are specified in the patent claim.

EFFECT: preparing the compounds exhibiting the properties of hepatitis C virus replication inhibition.

17 cl, 8 dwg, 255 ex

FIELD: chemistry.

SUBSTANCE: method is realised by treating a compound of formula

with boronic acid or ether thereof of formula

,

in which two OR15 groups together with the boron atom with which they are bonded form a pinacolato boronate ester group in the presence of a Pd catalyst. The invention relates to a method of producing a pharmaceutically acceptable salt of thieno[3,2-d]pyrimidine of formula

.

The invention also relates to a pharmaceutical composition, having phosphatidyl inositol-3-kinase inhibitor activity, containing thieno[3,2-d]pyrimidine of formula (I) as an active ingredient, a method of preparing said composition and use of thieno[3,2-d]pyrimidine of formula (I) or pharmaceutically acceptable salt thereof in producing a medicinal agent for inhibiting phosphatidyl inositol-3-kinase.

EFFECT: use of the derivative as a phosphatidyl inositol-3-kinase inhibitor.

11 cl, 13 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formulae and including their stereoisomers, as well as pharmaceutically acceptable salt, where X denotes O or S; R1 is selected from H, F, CI, Br, I, CN, -CR14R15-NR16R17, -CR14R15-NHR10, -(CR14R15)NR10R11, -(CR14R15)nNR12C(=Y)R10, -(CR14R15)nNR12S(O)2R10, -(CR14R15)mOR10, -(CR14R15)nS(O)2R10, -C(OR10)R11R14, -C(R14)=CR18R19, -C(=Y)OR10, -C(=Y)NR10R11, -C(=Y)NR12OR10, -C(=O)NR12S(O)2R10, -C(=O)NR12(CR14R15)mNR10R11, -NHR12, -NR12C(=Y)R10, -S(O)2R10, -S(O)2NR10R11, C2-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C4 carbocyclyl, piperidinyl, thiopyranyl, phenyl or C5-C6 heteroaryl; R2 is selected from H, C2-C12 alkyl and thiazolyl; R3 denotes a condensed bicyclic heteroaryl selected from indazole, indole, benzoimidazole, pyrrolopyridine, imidazopyridine and quinoline; R10, R11 and R12 independently denote H, C2-C12 alkyl, C3 carbocyclyl, heterocyclyl selected from pyrrolidine, morpholine and piperazine, phenyl or heteroaryl selected from pyrazole, pyridine, benzothiophene; or R10 and R11 together with a nitrogen atom with which they are bonded possibly form a saturated C3-C6 heterocyclic ring, possibly containing one additional ring atom selected from N or O, where said heterocyclic ring is possibly substituted with one or more groups independently selected from oxo, (CH2)mOR10, NR10R11, SO2R10, C(=O)R10, NR12S(O)R11, C(=Y)NR10R11, C1-C12 alkyl and heterocyclyl selected from pyrrolidine; R14 and R15 are independently selected from H or C1-C12 alkyl; R16 and R17 independently denote H or phenyl; R18 and R19 together with a carbon atom with which they are bonded form a C3-C20 heterocyclic ring, where said alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, phenyl, heteroaryl, piperidinyl and condensed bicyclic heteroaryl possibly substituted with one or more groups independently selected from F, CI, Br, I, CF3, -C(=Y)R10, -C(=Y)OR10, oxo, R10, -C(=Y)NR10R11, -(CR14R15)nNR10R11, -NR10R11, -NR12C(=Y)R10, -NR12C(=Y)NR10R11, -NR12SO2R10, OR10, SR10, -S(O)2R10, -S(O)2NR10R11, possibly substituted with carbocyclyl, selected from cyclopropyl, possibly substituted heterocyclyl selected from piperazine, possibly substituted with alkyl and alkylsulphonyl, pyrrolidine, morpholine, piperdine, possibly substituted CH3, phenyl and possibly substituted heteroaryl selected from imidazole and triazole; Y denotes O; m equals 0, 1 or 2; n equals 1 and t equals 2. The invention also relates to a pharmaceutical composition which modulates lipid kinase activity, based on said compounds.

EFFECT: obtaining novel compounds and a composition based on said compounds, which can be used to treat lipid kinase-mediated diseases, for example, cancer.

48 cl, 2 tbl, 372 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for producing prasugrel hydrochloride which involves the following stages: (i) chlorination of a compound described by formula (III) by addition of an chlorinating agent, optionally drop-by-drop, in a solvent; (ii) reaction of the prepared compound of formula (IV) and a compound described by general formula (V) where R means a protective group for hydroxyl, or its salt in a solvent in the presence of a base; (iii) acetylation of the prepared compound described by general formula (II) by reaction with an acetylation agent in a solvent in the presence of a base and an acetylation catalyst; and (iv) addition of hydrochloric acid, optionally drop-by-drop, to the prepared compound described by formula (I) in a solvent to produce prasugrel hydrochloride described by formula (1a), and differs by the fact that at the stage (i) temperature during addition of the chlorinating agent, optionally drop-by-drop, ranges within -20°C to 5°C, and reaction temperature after addition of the chlorinating agent, optionally drop-by-drop, ranges within -20°C to 5°C. The invention also concerns a product containing prasugrel hydrochloride and CATP in an amount no more than 0.3 %, to the pharmaceutical composition suitable for prevention or treatment of thrombosis or embolism on the basis of the specified product.

EFFECT: production of low-CATP prasugrel hydrochloride.

31 cl, 3 dwg, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are produced new diazepane substituted compounds representing various heterocyclic systems, including condensed, pharmaceutical compositions containing said compounds.

EFFECT: producing the compounds and compositions for preventing and treating neurological and mental disorders and diseases with involved orexin receptors.

13 cl, 1 tbl

New compounds // 2458920

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula or to its pharmaceutically acceptable salts wherein -A-(R1)a means a group; -B-(R2)b means a group specified in the patent claim 1, R3 means hydrogen; X means CH2 or O; and Y means CH2. Also, the invention refers to a pharmaceutical composition exhibiting FGFR inhibitor activity on the basis of the declared compound.

EFFECT: there are produced new compounds and based pharmaceutical composition which can find application in medicine for preparing a cancer drug.

8 cl, 1 tbl, 180 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: pyrazolo[1,5-a]-pyrimidine compounds according to the invention are specified in a group consisting of: N-{2-fluor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-ethylmethanesulphonamide; {2-fluor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-chlor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-chlor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-fluor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-methanesulphonamide, N-{2-chlor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-methanesulphonamide, N-{2-methyl-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-methoxy-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2,4-difluor-5-[3-(thiophene_2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide and N-{5-fluor-2-methoxy-3-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide.

EFFECT: preparing pyrazolo[1,5-a]pyrimidine compounds, their pharmaceutically acceptable salts and hydrates showing an ability to inhibit GABAA receptors, and applicable for treating and preventing anxiety, epilepsy and sleeping disorders, including insomnia, as well as for inducing a sedative-hypnotic, analgesic and sleeping effects and myorelaxation.

14 cl, 6 tbl, 4 dwg, 22 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described new compounds of general formula (I):

in the form of a separate stereoisomer or mixed stereoisomers or in the form of its pharmaceutically acceptable salt wherein R1 is indazolyl or substituted indazolyl; R6 is C6aryl or C6-12aryl substituted by halogen, hydroxy, cyano and C1-6alkoxy; or C6heterocyclyl containing 1-2 heteroatoms specified in nitrogen or oxygen; each X2 and X3 independently mean hydrogen, hydroxy or phosphate.

EFFECT: prepared compounds may be used for preparing a drug preparation for treating or preventing cancer, particularly acute myeloid leukemia.

6 cl, 6 tbl, 8 ex, 4 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I , and pharmaceutically acceptable salts thereof, where L denotes O, S, or CH2; Y denotes N or CH; Z denotes CR3; G denotes CH; R1 denotes a heteroaryl ring of formula , where D1 denotes S, O; D2 denotes N or CR12; D3 denotes CR12; R2 denotes (C6-C10)-aryl; 5-9-member mono- or bicyclic heteroaryl with 1 or 2 heteroatoms independently selected from N or S; a saturated or partially saturated (C3-C7)-cycloalkyl; or a saturated 5-6-member heteocyclyl with 1 heteroatom selected from N, where said aryl, heteroaryl, cycloalkyl and heterocyclyl are optionally substituted with one or two groups independently selected from (C1-C6)-alkyl, F, Cl, Br, CF3, CN, NO2, OR6, C(-O)R6, C(=O)OR6, C(=O)NR6R7, saturated 6-member heterocyclyl with 2 heteroatoms independently selected from N or O, and S(O)2R6, and where said alkyl is optionally substituted with one -OR8 group; R3 denotes H; (C1-C6)-alkyl; (C2-C6)-alkenyl; Cl; Br; OR6; SR6; phenyl; or a 6-member heteroaryl with 1 heteroatom selected from N, where said alkyl and alkenyl are optionally substituted with one group selected from C(=O)OR8, -OR8, -NR8R9; or a saturated 6-member heterocyclyl with 1 heteroatom selected from N or O.

EFFECT: disclosed compounds are used in treating and preventing diseases mediated by insufficient level of glucokinase activity, such as sugar diabetes.

16 cl, 479 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present patent claim discloses sulphonyl-substituted compounds of formula QUIN which are used for the purpose of a method for producing a macrocyclic compound of formula (I)

EFFECT: compounds of formula (I) are effective active agents for treating Hepatitis C viral (HCV) infection.

8 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 4-amino-3-arylamino-6-arylpyrazolol[3.4-d]-pyrimidine derivatives showing antiviral activity. In formula I: the groups A and B independently represent phenyl, naphthyl, pyridyl, quinolyl, pyrazinyl, pyrimidyl, pyrazolyl, triazinyl, imidazolyl, furanyl, thienyl, and in each of these groups one to three hydrogen atoms can be independently substituted by the radical R1; R1 can be NO2, CN, CONR22, COOR2, CHO, CONH2, halogen, saturated or unsaturated, linear or branched alkyl with a number of atoms in the chain 1 to 7, saturated or unsaturated, linear or branched alkanole with a number of atoms in the chain 1 to 8, OR2, SR2, NR22, SO2NR32, di- or trifluoromethyl, phenyl; R2 represents hydrogen, CF3, and linear or branched alkyl with a number of atoms in the chain 1 to 7; the radical R3 represents H, benzyl, or linear or branched alkyl with a number of atoms in the chain 1 to 7; the radicals R4 and R5 represent hydrogen.

EFFECT: developing the method for preparing the compound of formula (I) and applying the compounds of the present invention as a biological agent exhibiting antiviral activity, eg for treating picornavirus infections.

9 cl, 6 ex, 1 dwg

FIELD: chemistry.

SUBSTANCE: described are novel benzotriazole UV-absorbers, having absorption spectrum shifted towards the long-wave side with considerable absorption in the region up to 410-420 nm, having general formulae (a)-(k) (structural formula and values of radicals are given in the description), composition which is stabilised with respect to UV radiation and containing novel UV-absorbers, and use of the novel compounds as UV light stabilisers for organic materials.

EFFECT: obtaining novel benzotriazole UV-absorbers, having absorption spectrum shifted towards the long-wave side.

13 cl, 23 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: described is a novel compound - 6-(2'-amino-2'-carboxyethylthio)-2-methylthio-4-pivaloyloxy-methyl-1,2,4-triazolo[5,1-c] 1,2,4-triazin-7(4H)-one of formula having antiviral action and low toxicity.

EFFECT: compound can be used in medicine.

1 cl, 1 ex, 3 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and synthesis of heterocyclic compounds - 5,6-dihydro-7H-pyrrolo[1,2-d][1,4]benzodiazepin-6-one derivatives of formula 1a-e by boiling 2-amino-N-(2-furan-2-yl-phenyl)-acetamides in a mixture of glacial acetic acid and concentrated hydrochloric acid with subsequent treatment with sodium bicarbonate while boiling.

EFFECT: method is characterised by simple execution.

2 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention describes the pyrrolo- and thiazolopyridinium compounds and their pharmaceutically acceptable salts covered by general structural formula I: wherein the values A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are those as presented in cl.1, and a pharmaceutical composition based on the given compound for inhibition of hypoxia-inducible factor (HIF) hydroxylase activity.

EFFECT: there are produced and described new compounds able to modulate hypoxia-inducible factor (HIF) stability and/or activity.

29 cl, 178 ex

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