Benzodiapine, the pharmaceutical composition based on them, the method of prevention or treatment gipolipidemicheskoe state

 

The invention relates to benzodiapines General formula I, their derivatives and analogues. Also described pharmaceutical composition on the basis of benzodiapines. Connections are used for the prevention and treatment of such hyperlipidemics States, as a condition associated with atherosclerosis or hypercholesterinemia. 16 C. and 177 C.p. f-crystals, 13 PL.

Description text in facsimile form (see drawings) T T T T T

Claims

1. The compound of formula (I)where q is an integer from 1 to 4; n represents an integer from 0 to 2; R1and R2independently selected from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9R10A-/sup> CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, (polyalkyl)aryl and cycloalkyl optionally contain one or more carbons replaced by O, NR9N+R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C10cycloalkylation; R3and R4independently selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where R9and R10have the previously indicated meanings; or R3and R4together form =O, = NOR11, = S, =NNR11R12, =NR9or =CR11R12where R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, CR>, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that both R3and R4can't be him, NH2or SH, or R11and R12taken together with the nitrogen atom or carbon to which they are attached, form a cyclic ring; R5and R6independently selected from the group consisting of alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl can be substituted by one or more of the group of substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R12A-where And-represents a pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation, the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, P+R7R8R9A-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more of the carbon atoms, which is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene, a R13, R14and R15independently selected from the group consisting of hydrogen, alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, the cycle is of arearelated, where alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-, P(O)R9, phenylene, carbohydrate, amino acid, peptide, or polypeptide, and R13, R14and R15optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R10R11A-S+R9R10A-and C(O)OM, where R16and R17independently selected from the substituents consisting of R9and M; or R14and R15together with the nitrogen atom to which they are attached, form a cyclic ring; R7and R8independently selected from the group consisting of hydrogen and alkyl;
one or more of Rxindependently selected from the group consisting of H, alkyl, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR13OR14N+R9R11R12A-, P+R9R11R12A-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl can be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R10R12A-S+R9R10A-or C(O)OM, where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, hetero is CNY a heterocycle and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM,
SO2NR9R10C(O)OM, PO(OR16R17where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, where in these polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9where Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more group selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13SO, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O) OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-,
provided that both R5and R6can't be HE or SH and, if R is HE, R1, R2, R3, R4, R7and R8can't all be hydrogen; provided that if R5or R6is phenyl, only one of R1or R2is H; provided that when q=1, a Rxrepresents styryl, anilide or anilinoacrolein, only one of R5or R6represents alkyl.

2. Connection on p. 1, where R5and R6independently selected from the group consisting of aryl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl where specified aryl, heteroaryl, Quaternary heterocycle, and Quaternary heteroaryl can be substituted by one or more of the group of substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R1313, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-where the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more of the carbon atoms, which is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene, where the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R9, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle and Quaternary heteroaryl, P(O)R7R8, P+R7R8A-and P(O)(OR7OR8.

3. Connection on p. 2, where R5one or more of Ryindependently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl and heterocycle may be substituted by one or more group substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R137, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, R+R7R8And-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and the heterocycle optionally contains one or more carbon atom that is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene.

4. Connection on p. 3, where R5or R6has the formula (II)

5. Connection on p. 4, where n = 1 or 2.

6. Connection on p. 5, where one of R7or R8represents N and the other of R7or R8represents alkyl.

7. Connection on p. 5, where both R7or R8represent N.

8. Seedio p. 8, where specified, the alkyl is C1-C10alkyl.

10. Connection on p. 8, where R1or R2both represent alkyl.

11. Connection on p. 10, where the specified alkyl is C1-C10alkyl.

12. Connection on p. 11, where the specified alkyl is C2-C7alkyl.

13. Connection on p. 12, where the specified alkyl is C2-C4alkyl.

14. Connection on p. 13, where the specified alkyl is independently selected from the group consisting of ethyl, n-propyl, n-butyl and isobutyl.

15. Connection on p. 8, where R1and R2each represents n-butyl.

16. Connection on p. 8, where one of R1and R2is ethyl and the other of R1and R2represents n-butyl.

17. Connection on p. 15, where q = 1, 2, or 3.

18. Connection on p. 16, where q = 1, 2, or 3.

19. Connection on p. 17, where q = 1 or 2.

20. Connection on p. 19, where q = 1.

21. Connection on p. 18, where q = 1 or 2.

22. Connection on p. 21, where q = 1.

23. Connection on p. 19, where R3and R4independently selected from the group consisting of h, OR9.

24. Connection on p. 21, where R3and R4independently selected from the group consisting of h, OR9.

25. Connection on p. 23, where R9is N.

seeking 7, 8 - or 9-position of the benzene ring of the formula (I).

28. Connection on p. 26, where the specified Rxis a 7-, 8 - or 9-position of the benzene ring of the formula (I).

29. Connection on p. 27, where these Rxare 7 - and 9-position of the benzene ring of the formula (I).

30. Connection on p. 28, where the specified Rxlocated in the 7-position of the benzene ring of the formula (I).

31. Connection on p. 29, where the specified one or more of Rxindependently selected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM and where Rxthe, O2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

32. Connection on p. 30, where the specified Rxselected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R913
N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

33. Connection on p. 31, where the specified one or more of Rxindependently selected from the group consisting of polyester, OR13, NR13R14and N+R9R11R12A-.

34. Connection on p. 32, where the specified Rxselected from the group consisting of polyester, OR13, NR13R14and N+R9R11R12A-.

35. Connection on p. 33, where the specified one or more of Rxindependently selected from the group consisting of OR13and NR13R14.

36. Connection on p. 34, where the specified Rxindependently selected from the group consisting of OR13and NR13R14.

37. Connection on p. 35, where R13and R14each represents methyl.

yindependently is a 3 - or 4-position of the phenyl ring of formula (II).

40. Connection on p. 32, where one or more of Ryindependently is a 3 - or 4-position of the phenyl ring of formula (II).

41. Connection on p. 39, where t = 1 or 2.

42. Connection on p. 40, where t = 1 or 2.

43. Connection on p. 41, where the specified one or more of Ryindependently selected from the group consisting of alkyl, polyether, fluoride, chloride, bromide, iodide, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

44. Connection on p. 42, where the specified Ryindependently selected from the group consisting of alkyl, polyether, fluoride, chloride, bromide, iodide, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

45. Connection on p. 43, where the specified one or more of Ryindependently selected from the group consisting of alkyl, polyether, fluoride, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO4, where specified Ryindependently selected from the group consisting of alkyl, polyether, fluoride, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

47. Connection on p. 45, where these R13and R14represent alkyl, where alkyl may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

48. Connection on p. 46, where these R9and R10represent alkyl, where alkyl may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

49. Connection on p. 47, where n = 2.

50. Connection on p. 48, where n = 2.

51. Connection on p. 49, where HE stated the group is in the syn-position in a specified structural formula (II).

52. Connection on p. 50, where HE stated the group is in the syn-position in a specified structural formula (II).

53. Connection on p. 51, having the formula

54. Connection on p. 51, having the formula

55. Connection on p. 51, having the formula

58. Connection on p. 52, having the formula

59. Connection on p. 52, having the formula

60. Connection on p. 52, having the formula

61. Connection on p. 52, having the formula

62. Connection on p. 52, having the formula

63. Connection on p. 31, where n = 1.

64. Connection on p. 63, where Ryis N.

65. Connection on p. 64, having the formula

66. Connection on p. 4, where R1and R2independently selected from the group consisting of H and alkyl.

67. Connection on p. 66, where the specified alkyl is C1-C10alkyl.

68. Connection on p. 67, where the specified alkyl is C2-C7alkyl.

69. Connection on p. 68, where the specified alkyl is C2-C4alkyl.

70. Connection on p. 69, where R1and R2independently selected from the group consisting of ethyl, n-propyl, n-butyl and isobutyl.

71. Connection on p. 4, where R3and R4independently selected from the group consisting of h, OR9.

72. Connection on p. 71, where R9is the dust, consisting of h, OR9.

75. Connection on p. 74, where R9is N.

76. Connection on p. 3, where one of R7and R8is N.

77. Connection on p. 76, where both R7and R8represent N.

78. Connection on p. 3, where the specified one or more of Rxindependently selected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SOsOM, SO2NR9R10, PO(ORl6OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR139
N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

79. Connection on p. 78, where the specified one or more of Rxindependently selected from the group consisting of polyester, OR13, NR13R14and N+R9R11R12A-.

80. Connection on p. 79, where the specified one or more of Rxindependently selected from the group consisting of OR13and NR13R14.

81. Connection on p. 80, where R13and R14each represents methyl.

82. Connection on p. 3, where one or more of Ryindependently is a 3 - or 4-position of the phenyl ring of formula (II).

83. Connection on p. 82, where one or more of Ryselected from the group consisting of alkyl, polyether, fluoride, chloride, bromide, iodide, NR9R10and NC(O)R9where the alkyl and polyester can be substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

84. Connection on p. 83, where R9and R10represent alkyl.

85. Connection on p. 84, where ar is R9R10and NC(O)R9.

86. Connection on p. 1, where the specified one or more of Rxindependently selected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14And-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptic>9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

87. Connection on p. 1, where n = 1 or 2.

88. Connection on p. 87, where n = 2.

89. Connection on p. 1, where R1and R2independently selected from the group consisting of H and alkyl.

90. Connection on p. 89, where the specified alkyl is C1-C10alkyl.

91. Connection on p. 90, where the specified alkyl is C2-C7alkyl.

92. Connection on p. 91, where the specified alkyl is C2-C4alkyl.

93. Connection on p. 92, where R1and R2independently selected from the group consisting of ethyl, n-propyl, n-butyl and isobutyl.

94. Connection on p. 1, where R3and R4independently selected from the group consisting of h, OR9.

95. Connection on p. 94, where R9is N.

96. Connection on p. 1, where one of R7and R8is N.

97. Connection on p. 96, where one of R7and R9is N.

98. The compound of formula (III)

where q and r independently represent integers from 0 to 4;
d and e independently represent integers from 0 to 2;
t and u independently represent integers from 0 to 4;kanila, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RWA-, SR9S+R9A-, P+R9R10R11A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, polyalkyl, aryl and cycloalkyl optionally contain one or more carbons replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C1ub>3-C10cycloalkylation;
R3, R3AR4and R4Aindependently selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, NR9R10, SR9, S(O)R9, SO2R9and SO3R9where R9and R10have the previously indicated meanings; or R3and R4together form =O, =NOR11, =S, NNR11R12, =NR9or-CR11R12or R3Aand R4Atogether form =O, =NOR11, =S, =NNR11R12, =NR9or CR11R12where R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9and SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that R3and R4can't HE be both, NH2or SH, or R11and R12taken together with the nitrogen atom or carbon to which they are attached, form a cyclic ring;
And-is pharmaceutically when is independently selected from the group consisting of hydrogen and alkyl;
one or more of Rxand RxAindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13. C(O)NR13R14, R14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, R+R9R11R12And-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10+R9R10A-or C(O)OM, where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, alkyl (Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM, SO2NR9R10C(O)OM, PO(OR16OR17where Rxand RxAone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A - or P(O)R9;Anna from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14With(O)NR13R14With(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-,
R19selected from the group consisting of Alcantara, Alcantara, alcindoro, polyalkylene, alkoxide, polyetherdiol, polyalkoxyalkyl, carbohydrate, amino acid, peptide, polypeptide, where alcander, alkerdeel, alcindor, poly-alcander, alkoxides, polyetherdiol, polyalkoxy, carbohydrate, amino acid, peptide, and polypeptide can optionally contain one or more carbon atom that is replaced by O, NR7N+R7R8, S, SO, SO2S+R7R8PR7, P+R7R8, phenylene, heterocycle, Quaternary heterocycle, Quaternary heteroaryl or aryl, where alcander, alkerdeel, alcindor, polyalkyl who have one or more of the group of deputies, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(or SIG13)Or SIG14S+R13R14A-and N+R9R11R12A-; one or more of Ryand RyAindependently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl and heterocycle may be substituted by one or more group substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-where the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo,
CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, R+R7R8And-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more of the carbon atoms, which is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene. 99. Connection on p. 98, where R1, R1A, R2and R2Aindependently SEL is ezavisimo selected from the group consisting of N and C1-C10the alkyl.

101. Connection on p. 100, where the specified alkyl is2-C7alkyl.

102. Connection on p. 101, where R1, R1A, R2and R2Aindependently represent2-C4alkyl.

103. Connection on p. 102, where R1, R1A, R2and R2Aindependently selected from the group consisting of ethyl, n-propyl, n-butyl and isobutyl.

104. Connection on p. 98, where R3, R3AR4and R4Aindependently selected from the group consisting of h, OR9.

105. Connection on p. 104, where R9is N.

106. Connection on p. 98, where R7, R7AR8and R8Arepresent N.

107. Connection on p. 98, where d and e are independently equal to 1 or 2.

108. Connection on p. 107, where d and e are both equal to 2.

109. Connection on p. 98, where one or more of Rxand one or more of RxAindependently selected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, the 9
R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

110. Connection on p. 98, where one or more of Ryand one or more RyAindependently selected from the group consisting of alkyl, polyether, fluoride, chloride, bromide, iodide, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO3R9N+R9R11R12A7N+R7R8, S, SO, SO2S+R7R8PR7, P+R7R8and phenylene.

112. Connection on p. 111, where R19selected from the group consisting of alkoxide and polyalkoxyalkyl, where one or more carbon atoms is optionally replaced by O, NR9N+R9R10, S, SO, SO2S+R9R10PR9, P+R9R10, phenylene, amino acid, peptide, polypeptide, carbohydrate or polyalkyl.

113. Connection on p. 112, where R1, R1AR2and R2Aindependently selected from the group consisting of H and alkyl.

114. Connection on p. 113, where R3, R3AR4and R4Aindependently selected from the group consisting of h, OR9.

115. Connection on p. 114, where R9is N.

116. Connection on p. 115, where R7, R7A, R8and R8Aeach represent N.

117. Connection on p. 116, where d and e are independently equal to 1 or 2.

118. Connection on p. 117, where one or more of Rxand one or more of RxAindependently selected from the group R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

119. Soedineniya of alkyl, polyester, fluoride, chloride, bromide, iodide, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

120. Connection on p. 119, having the formula

PEG = polymer chain glycol with a molecular weight of 3400.

121. The compound of formula (IV)

where q and r independently represent integers from 0 to 3;
d and e independently represent integers from 0 to 2;
t and u independently represent integers from 0 to 5;
R1, R1A, R2and R2Aindependently selected from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9A-, P+R9R10R11 10 where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, polyalkyl, aryl and cycloalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C10cycloalkyl; or R1Aand R2Ataken together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3, R3AR4and R4Aindependently selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, NR9R10, SR9, S(O)R9, SO2R9and SO3R9where R9and R10have the previously indicated meanings; or R3and R4together form =O, =NOR11, =S, =NNR11R12, =NR9or =CR11R12or R3Aand R4Atogether form =O, =NOR119, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that R3and R4both can't imagine HE, NH2or SH, or R11and R12together with the nitrogen atom or carbon to which they are attached, form a cyclic ring;
And-represents a pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation;
R7, R7A, R8and R8Aindependently selected from the group consisting of hydrogen and alkyl;
one or more of Rxand RxAindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, P+R9R11R12A-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R10R12A-S+R9R10A-or C(O)OM, where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, alkyl(Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R2NR9R10, PO(ORl6OR17and C(O)OM, where Rxand RxAone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-; PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9; where Quaternary heterocycle and Quaternary heteroaryl optional
substituted by one or more group selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15/sup>,
R19selected from the group consisting of Alcantara, Alcantara, alcindoro, polyalkylene, alkoxide, polyetherdiol, polyalkoxyalkyl, carbohydrate, amino acid, peptide, polypeptide, where alcander, alkerdeel, alcindor, polyalkanes, alkoxides, polyetherdiol, polyalkoxy, carbohydrate, amino acid, peptide, and polypeptide can optionally contain one or more carbon atoms, which is replaced by O, NR7N+R7R8, S, SO, SO2S+R7R8PR7, P+R7R8, phenylene, heterocycle, Quaternary heterocycle, Quaternary heteroaryl or aryl, where alcander, alkerdeel, alcindor, polyalkanes, alkoxides, polyetherdiol, polyalkoxy, carbohydrate, amino acid, peptide, and polypeptide can be substituted by one or more of the group of substituents selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R5, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R1and N+R9R11R12A-; where the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, R+R7R8And-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more carbon atoms, which is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8And-or phenylene. 122. Connection on p. 121, where R1, R1A, R2and R2Aindependently selected from the group consisting of H and alkyl.

123. Connection on p. 122, where R1, R1A, R2and R2Aindependently selected from the group consisting of N and C11
, R1A, R2and R2Aindependently represent2-C4alkyl.

126. Connection on p. 125, where R1, R1A, R2and R2Aindependently selected from the group consisting of ethyl, n-propyl, n-butyl and isobutyl.

127. Connection on p. 125, where R3, R3AR4and R4Aindependently selected from the group consisting of h, OR9.

128. Connection on p. 127, where R9is N.

129. Connection on p. 121, where R7, R7AR8and R8Arepresent N.

130. Connection on p. 121, where d and e are independently equal to 1 or 2.

131. Connection on p. 130, where d and e are both equal to 2.

132. Connection on p. 121, where one or more of Rxand one or more of RxAindependently selected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR14R15N+R9R11R12A-, SR13S+R13R14, CO2R13, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12sup>R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14And-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more carbon atom is optionally replaced by O, NR9N+R9R10And-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

133. Connection on p. 121, where one or more of Ryand one or more RyAindependently selected from the group consisting of alkyl, polyether, fluoride, chloride, bromide, iodide, NR13R14, NR14C(O)R13and OR13where the alkyl and polyester may be further substituted SO3R9N+R9R11R12A-and Quaternary heteroaryl.

134. Connection on p. 121, where R19selected from the group consisting of Alcantara, polyalkylene, alchakov carbon which is replaced by O, NR7N+R7R8, S, SO, SO2S+R7R8PR7, P+R7R8and phenylene.

135. Connection on p. 134, where R19selected from the group consisting of alkoxide and polyalkoxyalkyl, where one or more carbon atoms is optionally replaced by O, NR9N+R9R10, S, SO, SO2S+R9R10PR9, P+R9R10, phenylene, amino acid, peptide, polypeptide, carbohydrate or polyalkyl.

136. Connection on p. 135, where R1, RlA, R2and R2Aindependently selected from the group consisting of H and alkyl.

137. Connection on p. 136, where R3, R3AR4and R4Aindependently selected from the group consisting of h, OR9.

138. Connection on p. 137, where R9is N.

139. Connection on p. 138, where R7, R7AR8and R8Aeach represent N.

140. Connection on p. 139, where d and e are independently equal to 1 or 2.

141. The connection 140 HP, having the formula

PEG=polymer chain glycol with a molecular weight of 3400.

142. The compound of formula (V)

where q independently represents an integer from 0 to 4; u represents an integer from 0 to 5;
R1, R1A, R2and R2Aindependently selected from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9A-, P+R9R10R11A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, polyalkyl, aryl and cycloalkyl optionally contain one or more of the carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, shumilkin) they are attached, form3-C10cycloalkylation or R1Aand R2Ataken together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3, R3AR4and R4Aindependently selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, NR9R10, SR9, S(O)R9, SO3R9and SO3R9where R9and R10have the previously indicated meanings; or R3and R4together form =O, =NOR11, =S, NNR11R12, =NR9or =CR11R12or R3Aand R4Atogether form =O, =NOR11, =S, =NNR11R12, =NR9or =CR11R12where R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that R3and R4both can't be him, NH2or SH, or R11and R12westfleet pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation;
R7, R7AR8and R8Aindependently selected from the group consisting of hydrogen and alkyl;
one or more of Rxand RxAindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, P+R9R11R12A-, amino acids, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl may be further substituted OR9, NR9R10N+R9R11R< is, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, R+R9R11R12A-S+R9R10A-or C(O)OM, where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, alkyl (Quaternary heterocycle and Quaternary heteroaryl may be optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM, SO2NR9R10, PO(OR16OR17and C(O)OM, where RxRxAone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR10A-or P(O)R9; where Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more group selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-,
R19selected from the group consisting of Alcantara, Alcantara, alcindoro, polyalkylene, alkoxide, polyetherdiol, polyalkoxyalkyl, carbohydrate, amino acid, peptide, polypeptide, where alcander, alkerdeel, alcindor, polyalkanes, alkoxides, polyetherdiol, polyalkoxy, carbohydrate, innoculate, peptide and polypeptide optionally contain one or more carbon atom that is replaced by O, NR7N+R7R8, S, SO, SO2S+R7R8PR7, P+R13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-And N+R9R11R12A-;
one or more of Ryand RyAindependently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl and heterocycle can be substituted by one or more of the group of substituents selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, 13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-where the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, P+R7R8A-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more carbon atom that is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A<1, R1A, R2and R2Aindependently selected from the group consisting of H and alkyl.

144. Connection on p. 143, where R1, R1A, R2and R2Aindependently selected from the group consisting of N and C1-C10the alkyl.

145. Connection on p. 144, where the specified alkyl is2-C7alkyl.

146. Connection on p. 145, where R1, R1A, R2and R2Aindependently represent2-C4alkyl.

147. Connection on p. 146, where R1, R1A, R2and R2Aindependently selected from the group consisting of ethyl, n-propyl, n-butyl and isobutyl.

148. Connection on p. 142, where R3, R3A, R4and R4Aindependently selected from the group consisting of h, OR9.

149. Connection on p. 148, where R9is N.

150. Connection on p. 142, where R7, R7A, R8and R8Arepresent N.

151. Connection on p. 142, where d and e are independently equal to 1 or 2.

152. Connection on p. 151, where d and e are both equal to 2.

153. Connection on p. 142, where one or more of Rxand one or more of RxAindependently selected from the group consisting of alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy, polyester, halogen, OR13, NR13R14, NR13NR, NR14C(O)R13and NR14C(O)R13where alkyl, aryl, cycloalkyl, heterocycle, polyalkyl, acyloxy and polyester may be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl, and where in the specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9.

154. Connection on p. 142, where one or more of Ryand one or more RyAindependently selected from the group consisting of alkyl, polyester, probity replaced by the next, SO3R9N+R9R11R12A-and Quaternary heteroaryl.

155. Connection on p. 142, where R19selected from the group consisting of Alcantara, polyalkylene, alkoxide and polyalkoxyalkyl where alcander and polyalkenes can optionally contain one or more carbon atoms, which is replaced by O, NR7N+R7R8, S, SO, SO2S+R7R8PR7, P+R7R8and phenylene.

156. Connection on p. 155, where R19selected from the group consisting of alkoxide and polyalkoxyalkyl, where one or more carbon atoms is optionally replaced by O, NR9N+R9R10, S, SO, SO2S+R9R10PR9, P+R9R10, phenylene, amino acid, peptide, polypeptide, carbohydrate or polyalkyl.

157. Connection on p. 156, where R1, R1A, R2and R2Aindependently selected from the group consisting of H and alkyl.

158. Connection on p. 157, where R3, R3A, R4and R4Aindependently selected from the group consisting of h, OR9.

159. Connection on p. 158, where R9is N.

160. Connection on p. 159, where R7, R7A, R8and R8Aeach represents .<"https://img.russianpatents.com/img_data/58/583415.gif">
PEG = polymer chain glycol with a molecular weight of 3400,
163. Pharmaceutical composition comprising antihyperlipidemics effective amount of the compounds of formula (I) under item 1 for oral or rectal administration and pharmaceutically acceptable carrier.

164. Pharmaceutical composition comprising anti-atherosclerotic effective amount of the compounds of formula (I) under item 1 for oral or rectal administration and pharmaceutically acceptable carrier.

165. Pharmaceutical composition comprising antihypercholesterolemic effective amount of the compounds of formula (I) under item 1 for oral or rectal administration and pharmaceutically acceptable carrier.

166. The method of prevention or treatment gipolipidemicheskoe condition, including oral or rectal administration to the needy in this patient the composition of p. 163 in unit dose form.

167. A method of preventing or treating atherosclerotic condition, including oral or rectal administration to the needy in this patient the composition of p. 164 in unit dose form.

168. The method of prevention or treatment of hypercholesterinemia, including oral or rectal administration needs �583416.gif">
where q is an integer from 1 to 4;
n represents an integer from 0 to 2;
R1selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl;
R2selected from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9R10A-, P+R9R10R11A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, (polyalkyl)aryl and cycloalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3and R4independently selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, NR9R10, SR9, S(O)R9, SO2R9and SO3R9where R9and R10have the previously indicated meanings; or R3and R4together form =O, =NR11, =S, =NNR11R12, =NR9or =CR11R12where R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9and SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that R3and R4both are not HE, NH2or SH, or RAlso;
R5and R6independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl can be substituted by one or more of the group of substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO2R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-And-represents a pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation, the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, halo the group, consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R3N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, P+R7R8R9A-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more carbon atoms, which is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene, a R13, R14and R15independently selected from the group consisting of hydrogen, alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where the alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2lot, the peptide or polypeptide, and R13, R14and R15optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10,
PO(OR16OR17, P+R9R10R11A-S+R9R10A-and C(O)OM, where R16and R17independently selected from the substituents consisting of R9and M; or R14and R15taken together with the nitrogen atom to which they are attached, form a cyclic ring;
R7and R8independently selected from the group consisting of hydrogen and alkyl;
one or more of Rxindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R132NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, P+R9R11R12A-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl may be further substituted OR9, NR9R10N+R9R11R12And-, SR9, S(O)R9, SO2R, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A - or C(O)OM and where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, heteroaryl and alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, heteroaryl, alkyl, Quaternary heterocycle, and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R1 is IDA, CONR9R10, SO3R9, SO2OM,
SO2NR9R10, PO(OR16OR17and C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9P+R9R10A-or P(O)R9; where Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more group selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13+
R9R11R12A-,
provided that both R5and R6cannot be hydrogen, HE or SH; provided that if R5or R6represents phenyl, only one of R1or R2is H; provided that when q=1, a Rxrepresents styryl, anilide or anilinoacrolein, only one of R5or R6represents alkyl.

170. The compound of formula (I)

where q is an integer from 1 to 4;
n represents an integer from 0 to 2;
R1and R2independently selected from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9R10A-, P+R9R10R11A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R10A-or phenylene, where R9, R10Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, SR9, S(O)R9, SO2R9, SO3R9and NR9R10;
R4selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, alkenyl, quinil, acyloxy, substituted aryl, anthracene, heterocycle, OR41, NR41R10, SR41, S(O)R41, SO2R41and SO3R9,
or R3and R4together form =NOR42, -NNR11R43, =NR41or =CR11R43,
where R9and R10have the previously indicated meanings; where R11selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkene is NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R41selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, substituted aryl, anthracene, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl, R42selected from the group consisting of alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10and R43selected from the group consisting of C7-C20of alkyl, substituted C7-C20of alkyl, substituted aryl, anthracene, arylalkyl, heterocycle, carboxyethyl, carboalkoxylation, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10and these carboxyethyl, carboalkoxylation and cianelli include7-C20alkyl, or R11and R43together with the nitrogen or carbon to which they>or SH;
R5and R6independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl can be substituted by one or more of the group of substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12And-where R11has the previously indicated meanings, and R12selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, 9
, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have the previously indicated meanings, or R11and R12together with nitrogen atoms or carbon to which they are attached, form a cyclic ring; And-represents a pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation, the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, P+R7R8R9A-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more carbon atoms, which is replaced by O, NR7N+R7R8A-, 13, R14and R15independently selected from the group consisting of hydrogen, alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where the alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbons replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-, P(O)R9, phenylene, carbohydrate, amino acid, peptide, or polypeptide, and R13, R14and R15optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R0, PO(OR16OR17, P+R9R10R11A-S+R9R10A-and C(O)OM, where R16and R17independently selected from the substituents consisting of R9and M; or R14< R8independently selected from the group consisting of hydrogen and alkyl;
one or more of Rxindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, P+R9R11R12A-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl can be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R, SO3R9, oxo, CO2R9,11R12A-S+R9R10A-or C(O)OM and where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, heteroaryl and alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, heteroaryl, alkyl, Quaternary heterocycle, and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM,
SO2NR9R10and C(O)OM and PO(OR16OR17where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, R+R13R14And-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR913, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-,
provided that R5and R6both cannot be hydrogen, HE or SH; provided that if R5or R6represents phenyl, only one of R1or R2is H; provided that when q=1, a Rxrepresents styryl, anilide or anilinoacrolein, only one of R5or R6represents alkyl.

171. The compound of formula (I)

where q is an integer from 1 to 4;
n represents an integer from 0 to 2;
R1and R2independently selected from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9R10A-, P+R9R10R11A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, (polyalkyl)aryl and cycloalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3and R4independently selected from the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, NR9R10, the tion; or R3and R4together form = O, =NOR11, =S, =NNR11R12, =NR9or =CR11R12where R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that R3and R4both can't be him, NH2or SH, or R11and R12together with nitrogen atoms or carbon to which they are attached, form a cyclic ring;
R5selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, alkenyl, quinil, substituted aryl, anthracene, cycloalkyl, heterocycle containing at least one heteroatom phosphorus, Quaternary heterocycle, OR51, SR51, S(O)R51, SO2R51and SO3R9where the specified R5replaced With1-C20alkyl and substituted aryl substituents independently include one or more group will replace/sub>the quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, oxo, OR52, NR52R14, SR52, S(O)R52, SO2R52, SO3R13, NR13OR14, NR13NR14R15, CO2R52, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-N+R51R11R12A-and where specified R5With7-C20alkyl, alkenyl, quinil, anthracene, cycloalkyl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl (substituents) may be substituted by one or more group substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R< P(OR13OR14S+R13R14A-and N+R9R11R12A-; R6selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where the specified R6alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl (substituents) may be substituted by one or more of the group of substituents, independently selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-And-represents a pharmaceutically acceptable anion and M predstavljali, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, P+R7R8R9A-and P(O)(OR7OR8and where specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle optionally can have one or more carbon atom that is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene, and R9has these values, R51selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, replaced aryl, anthracene, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl, R52selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, polyalkenes of heteroaryl and Quaternary heteroallyl, and R13, R14and R15independently selected from the group consisting of hydrogen, alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where the alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-, P(O)R9, phenylene, carbohydrate, amino acid, peptide, or polypeptide, and R13, R14, R15and R52optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R10R11A-S+R9R10A-and C(O)OM, where R16and R17independently selected from the substituents consisting of R;
R7and R8independently selected from the group consisting of hydrogen and alkyl;
one or more of Rxindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, P+R13R14R15A-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl can be further substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R, SO3R9, oxo, CO+R9R11R12A-S+R9R10A-or C(O)OM and where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, heteroaryl and alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, heteroaryl, alkyl, Quaternary heterocycle, and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12And-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM,
SO2NR9R10C(O)OM and PO(OR16OR17where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9Aheteroaryl optionally substituted by one or more group substituents, selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-,
provided that, if R6is HE, R1, R2, R3, R4, R7and R8can't all be hydrogen; provided that if R5or R6represents phenyl, only one of R1or R2is H; provided that when q=1, a Rxrepresents styryl, anilide or anilinoacrolein, only one of R5or R6represents alkyl.

172. The compound of formula (I)

where q is an integer from 1 to 4;
n represents an integer from 0 to 2;
R1and R2independently selected from the group consisting of H, alkyl, alkenyl, quinil, Galkina, where alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9R10A-, P+R9R10A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, (polyalkyl)aryl and cycloalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3and R4independently selected from the group consisting of H, alkyl, alkenyl, quinil, ACI is up> where R9and R10have the previously indicated meanings; or R3and R4together form =O, =NOR11, =S, =NNR11Rl2, =NR9or =CR11R12where R11and R12independently selected from the group consisting of H, alkyl,
alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO3R9, SO2R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that R3and R4both can't be him, NH2or SH, or R11and R12together with nitrogen atoms or carbon to which they are attached, form a cyclic ring;
R5and R6independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, and Quaternary heteroaryl can be substituted by one or more of the group of substituents, independently selected from groupola, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-, A-represents a pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation, the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary heteroaryl, P(O)R7R8, P+R7R8R9A-and P(O)(OR7OR8and where specified and shall keep one or more carbon atoms, which is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene, a R13, R14and R15independently selected from the group consisting of hydrogen, alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where the alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-, P(O)R9, phenylene, carbohydrate,
amino acid, peptide, or polypeptide, and R13, R14and R15optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17independently selected from the substituents consisting of R9and M; or R14and R15together with the nitrogen atom to which they are attached, form a cyclic ring;
R7selected from the group consisting of hydrogen and alkyl;
R8is alkyl;
one or more of Rxindependently selected from the group consisting of H, alkyl, alkenyl, quinil, polyalkyl, acyloxy, aryl, arylalkyl, halogen, haloalkyl, cycloalkyl, heterocycle, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R10R12A-, P+R9R11R12A-, amino acid, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle >2
A-, SR9, S(O)R9, SO2R, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM and where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, heteroaryl and alkyl, where acyl, arylethoxysilanes, arylalkyl, heterocycle, heteroaryl, alkyl, Quaternary heterocycle, and Quaternary heteroaryl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO2R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM, SO2NR9R10C(O)OM, PO(ORl6OR17where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, and the/sup> N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9; where Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more group selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13R14S+R13R14A-and N+R9R11R12A-,
provided that both R5and R6cannot be hydrogen, HE or SH; provided that if R5or R6represents phenylene, only one of R1or R2is H; provided that when q=1, a Rxrepresents styryl, anilide or anilinoacrolein, only one of R5or R6represents alkyl.

173. The compound of formula (I)
the performance is chosen from the group consisting of H, alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl, where the alkyl, alkenyl, quinil, haloalkyl, alkylaryl, arylalkyl, alkoxy, alkoxyalkyl, dialkylamino, alkylthio, (polyalkyl)aryl and cycloalkyl optionally substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R10RwA-, SR9S+R9R10A-, P+R9R10R11A-, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where alkyl, alkenyl, quinil, alkylaryl, alkoxy, alkoxyalkyl, (polyalkyl)aryl and cycloalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-, P+R9R10A-or phenylene, where R9, R10and Rwindependently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; or R1and R2taken together with the carbon to which the group consisting of H, alkyl, alkenyl, quinil, acyloxy, aryl, heterocycle, OR9, NR9R10, SR9, S(O)R9, SO2R9and SO2R9where R9and R10have the previously indicated meanings; or R3and R4together form =O, =NOR11, =S, =NNR11R12, =NR9or CR11R12where R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R, SO3R, CO2R, CN, halogen, oxo and CONR9R10where R9and R10have these values, provided that both R3and R4can't be him, NH2or SH, or R11and R12taken together with the nitrogen atoms or carbon to which they are attached, form a cyclic ring,
R5and R6independently selected from the group consisting of N alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, Quaternary heterocycle, OR9, SR9, S(O)R9, SO2R9and SO3R9where alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, chiabrando independently from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary, heteroaryl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R13, SO3R13, NR13OR14, NR13NR14R15, NO2, CO2R13, CN, OM, SO2OHM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-And-represents a pharmaceutically acceptable anion, and M represents a pharmaceutically acceptable cation, the specified alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can be further substituted by one or more group substituents selected from the group consisting of OR7, NR7R8, SR7, S(O)R7, SO2R7, SO3R7, CO2R7, CN, oxo, CONR7R8N+R7R8R9A-, alkyl, alkenyl, quinil, aryl, cycloalkyl, heterocycle, arylalkyl, Quaternary heterocycle, Quaternary g is th alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl and heterocycle can optionally contain one or more carbon atom that is replaced by O, NR7N+R7R8A-, S, SO, SO2S+R7A-PR7, P(O)R7, P+R7R8A-or phenylene, and R13, R14and R15independently selected from the group consisting of hydrogen, alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where the alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-, P(O)R9, phenylene, carbohydrate,
amino acid, peptide, or polypeptide, and R13, R14and R15optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12And-, SR9, S(O)R9SO9
R10, PO(OR16OR17, P+R9R10R11A-S+R9R10A-and C(O)OM, where R16and R17independently selected from the substituents consisting of R9and M; or R14and R15together with the nitrogen atom to which they are attached, form a cyclic ring;
R7and R8independently selected from the group consisting of hydrogen and alkyl; and one or more of Rxsubstituents selected from the group consisting of C7-C20of alkyl, C7-C20alkenyl,7-C20the quinil, substituted C1-C20of alkyl, substituted C2-C20alkenyl, substituted C2-C20the quinil, polyalkyl, acyloxy, aryl, arylalkyl, haloalkyl, including7-C20alkyl, cycloalkyl, heterocycle, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR61, NR61R14, SR61, S(O)R61, S(O)2R61, SO3R61S+R13R14A-, NR61OR14, NR13NR14R15, CO2R62, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR63, S(O)nNR18/sup>R12A-, amino acid, peptide, polypeptide, and carbohydrate, where R18selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, heteroaryl and alkyl, where R61selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, polyalkyl, substituted aryl, anthracene, arylalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where R62selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, alkenyl, quinil, polyalkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic, where R63selected from the group consisting of acyl, arylalkanolamine, arylalkyl, heterocycle, heteroaryl,7-C20of alkyl and substituted C1-C20of alkyl, and where R64selected from the group consisting of C7-C20of alkyl, substituted C1-C20of alkyl, substituted aryl, anthracene, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl;
additional Rxdeputies are badila, halogen, haloalkyl, cycloalkyl, heterocycle, heteroaryl, polyether, Quaternary heterocycle, Quaternary heteroaryl, OR13, NR13R14, SR13, S(O)R13, S(O)2R13, SO3R13S+R13R14A-, NR13OR14, NR13NR14R5, NO2, CO2R13, CN, OM, SO2OM, SO2NR13R14, NR14C(O)R13C(O)NR13R14, NR14C(O)R13C(O)OM, COR13, OR18, S(O)nNR18, NR13R18, NR18OR14N+R9R11R12A-, R+R9R11R2A-, amino acids, peptide, polypeptide, and carbohydrate, where the alkyl, alkenyl, quinil, cycloalkyl, aryl, polyalkyl, heterocycle, aryloxy, arylalkyl, haloalkyl, polyether, Quaternary heterocycle, and Quaternary heteroaryl can be optionally substituted OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R11R12A-S+R9R10A-or C(O)OM, where acyl, arylalkenes the tion substituted by one or more Deputy selected from the group consisting of OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO3R9, SO2OM, SO2NR9R10, PO(OR16OR17and C(O)OM, where Rxone or more of the carbon atoms is optionally replaced by O, NR13N+R13R14A-, S, SO, SO2S+R13A-PR13, P(O)R13, P+R13R14A-, phenylene, amino acid, peptide, polypeptide, carbohydrate, polyether, or polyalkyl where specified polyalkyl, phenylene, amino acid, peptide, polypeptide, and carbohydrate, one or more of the carbon atoms is optionally replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-or P(O)R9; where Quaternary heterocycle and Quaternary heteroaryl optionally substituted by one or more group selected from the group consisting of alkyl, alkenyl, quinil, polyalkyl, polyester, aryl, haloalkyl, cycloalkyl, heterocycle, arylalkyl, halogen, oxo, OR13, NR13R14, SR13, S(O)R13, SO2R2OM, SO2NR13R14C(O)NR13R14C(O)OM, COR13, P(O)R13R14, P+R13R14R15A-P(OR13OR14S+R13R14A-and N+R9R11R12A-,
provided that both R5and R6cannot be hydrogen, HE or SH, and if R5is HE, R1, R2, R3, R4, R7and R8can't all be hydrogen; provided that if R5or R6represents phenyl, only one of R1or R2is H; provided that when q=1, a Rxrepresents styryl, anilide or anilinoacrolein, only one of R5or R6represents alkyl.

174. The compound of formula (I)

where q=1 or 2;
n=2;
R1and R2each represents alkyl;
R3represents hydroxy;
R4and R6represent hydrogen;
R5has the formula (II)

where t represents an integer from 0 to 5;
one or more of Ryindependently selected from the group consisting of OR13, NR13R14and SR13; R13and R14independently selected from the group consisting of alkyl, alkene is, everting of heteroaryl and Quaternary heteroalkyl; where these R13and R14alkyl, alkenyl, quinil, arylalkyl, heterocycle and polyalkyl optionally contain one or more carbon atoms, which is replaced by O, NR9N+R9R10A-, S, SO, SO2S+R9A-PR9, P+R9R10A-, P(O)R9, phenylene, carbohydrate, amino acid, peptide or polypeptide; the specified R13and R14polyalkyl, arylalkyl, heterocycle, heteroaryl, Quaternary heterocycle, Quaternary heteroaryl and Quaternary heteroaromatic optionally substituted by one or more group selected from the group consisting of sulfoalkyl, Quaternary heterocycle, Quaternary heteroaryl, OR9, NR9R10N+R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo,
CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R10R11A-,
S+R9R10A-and C(O)OM; and these R13and R14alkyl, alkenyl, quinil, aryl and cycloalkyl substituted by one or more group selected from the group sotr>+
R9R11R12A-, SR9, S(O)R9, SO2R9, SO3R9, oxo, CO2R9CN, halogen, CONR9R10, SO2OM, SO2NR9R10, PO(OR16OR17, P+R9R10R11A-S+R9R10A-and C(O)OM; and R9and R10independently selected from the group consisting of H, alkyl, alkenyl, quinil, cycloalkyl, aryl, acyl, heterocycle, ammonioalkyl, alkylammonium and arylalkyl; R11and R12independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo and CONR9R10where R9and R10have the previously indicated meanings; or R11and R12together with nitrogen atoms or carbon to which they are attached, form a cyclic ring; or R16and R17independently selected from the substituents constituting R9and M, where M represents a pharmaceutically acceptable cation;
R7and R8represent hydrogen;<.

175. Connection on p. 174, where R1and R2each represents n-butyl.

176. Connection on p. 175, where Ryis OR13, a R13has specified in paragraph 174.

177. Connection on p. 176, where one or more Rxindependently selected from methoxy and dimethylamino.

178. Connection on p. 176, where Rxis dimethylamino.

179. Connection on p. 176, where t=1; Ryis para-OR13; and R13has specified in paragraph 174.

180. Connection on p. 176, where t=1; Ryis meta OR13; and R13has specified in paragraph 174.

181. Connection p. 176 4R, 5R configuration.

182. Connection p. 177, where R13selected from the group consisting of alkyl, arylalkyl and Quaternary heteroaromatic; specified R13arylalkyl and Quaternary heteroaromatic optionally substituted by one or more group selected from Quaternary heterocycle, Quaternary heteroaryl, NR9R10and CONR9R10; specified R13alkyl group substituted by one or more group selected from Quaternary heterocycle, Quaternary heteroaryl, NR9R10and CONR9R10; and R9and R10represent hydrogen.

183 is made by steam-OR13; and R13has specified in paragraph 182.

185. Connection on p. 182, where t=1; Ryis meta OR13; and R13has specified in paragraph 182.

186. Connection on p. 182, which has 4R, 5R configuration.

187. Connection on p. 174 with the structural formula

188. Connection on p. 174 with the structural formula

189. Connection on p. 1 of General formula (I)

where q is an integer from 1 to 4;
n is an integer from 0 to 2;
R1and R2each independently selected from the group consisting of H, alkyl, or R1and R2together with the carbon atom to which they are attached, form a3-C10cycloalkylation;
R3and R4each independently selected from the group consisting of N, OR9or R3and R4together form =O;
R5and R6each independently selected from the group consisting of alkyl and aryl, where alkyl and aryl can be substituted by one or more group substituents independently selected from the group consisting of haloalkyl, Quaternary heterocycle, halogen, OR13, NR13R14, NO2; and where specified, the alkyl and the aryl may, N. the/sup> and heterocycle;
R7and R8each independently selected from the group consisting of hydrogen and alkyl;
one or more Rxeach independently selected from the group consisting of H, alkyl, halogen, heterocycle, representing a saturated monocyclic carbocycle, in which one or two carbon atoms may be replaced by N or O, NR13OR14, OR13, NR13R14, SR13, NO2, NR14C(O)R13OR18N+R9R11R12A-where Rxone or more carbon atom, optionally substituted O, N+R13R14A-provided that if R5or R6are phenyl, only one of R1or R2represents H; R9is hydrogen or alkyl; R11and R12is independently selected from the group consisting of H, alkyl, alkenyl, quinil, aryl, arylalkyl, alkenylacyl, alkenylacyl, heterocycle, carboxyethyl, carboalkoxylation, cycloalkyl, cyanoalanine, OR9, NR9R10, SR9, S(O)R9, SO2R9, SO3R9, CO2R9CN, halogen, oxo, and CONR9R10where R9and R10previously defined, and provided that R3and R4can't for the formation of a cyclic ring; R13and R14each independently selected from hydrogen, alkyl, arylalkyl; R18- alkyl; and-is a pharmaceutically acceptable anion.

190. Connection on p. 169, where these R1and R2are alkilani, R3is HE, R4and R5are H, R6substituted aryl, R7and R8are N and n = 2.

191. Connection on p. 98, where R19represents alcander, which optionally may contain one or more carbon atoms, substituted on oxygen.

192. Connection on p. 121, where R19represents alcander, which optionally may contain one or more carbon atoms, substituted on oxygen.

193. Connection on p. 142, where R19represents alcander, which optionally may contain one or more carbon atoms, substituted on oxygen.

Priority items:
11.03.1996 on PP.53-62, 65 and 182-188;
11.03.1997 on PP.1-52, 63, 64, 66-181 and 189-193.

 

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< / BR>
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