IP Library › Patent Application 17693527
Patent Application
App. No. 17/693,527

BEZIMIDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

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Patent No.
US None
App. No.
17/693,527
Abstract

The invention relates to benzimidazole derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

Claims (1068)

1 . (canceled)

2 . The method according to claim 14 , wherein

R 1 is Hal or linear or branched alkyl having 1-10 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 4 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NR 5 SO 2 R 6 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or —CH═CH— groups, and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl, or one of the following structures:

which is unsubstituted or mono-, di- or trisubstituted with R 4

and wherein Q, Y, R 2 , R 3 , R 4 , R 5 and R 6 have the meanings as disclosed in claim 1 , and physiologically acceptable salts, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.

3 . The method according to claim 14 , wherein R 1 is Br or one of the following structures:

which is unsubstituted or mono-, di- or trisubstituted with R 5

and wherein Q, Y, R 2 , R 3 , R 4 , R 5 and R 6 have the meanings as disclosed in claim 1 , and physiologically acceptable salts, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.

4 . The method according to claim 14 , wherein R 2 is one of the following structures:

which is unsubstituted or mono-, di- or trisubstituted with R 5

and wherein Q, Y, R 1 , R 3 , R 4 , R 5 and R 6 have the meanings as disclosed in claim 1 , and physiologically acceptable salts, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.

5 . The method according to claim 1 , wherein

R 3 one of the following structures

and Q, Y, R 1 , R 2 , R 4 , R 5 and R 6 have the meanings as disclosed in claim 1 , and physiologically acceptable salts, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.

6 . The method according to claim 14 , wherein

R 3 is OMe

and Q, Y, R 1 , R 2 , R 4 , R 5 and R 6 have the meanings as disclosed in claim 14 , and physiologically acceptable salts, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.

7 . The method according to claim 14 , wherein the compound of formula I is selected from the group consisting of:

No.

IUPAC-Name

1

7-Methoxy-4-phenyl-1H-benzoimidazol-2-ylamine

2

4-Fluoro-N-(7-methoxy-4-phenyl-1H-benzoimidazol-2-yl)-

benzamide

3

2-Bromo-N-(7-methoxy-4-phenyl-1H-benzoimidazol-2-yl)-

isonicotinamide

4

2-Bromo-N-(4-bromo-7-methoxy-1H-benzoimidazol-2-yl)-

isonicotinamide

5

6-Bromo-N-(7-methoxy-4-phenyl-1H-benzoimidazol-2-yl)-

nicotinamide

6

6-Bromo-N-(4-bromo-7-methoxy-1H-benzoimidazol-2-yl)-

nicotinamide

7

N-(7-Methoxy-4-phenyl-1H-benzoimidazol-2-yl)-2-morpholin-4-yl-

isonicotinamide

8

N-(7-Methoxy-4-phenyl-1H-benzoimidazol-2-yl)-6-morpholin-4-yl-

nicotinamide

9

N′-(7-Methoxy-4-phenyl-1H-benzoimidazol-2-yl)-N,N-dimethyl-

formamidine

10

4-Chloromethyl-N-(7-methoxy-4-phenyl-1H-benzoimidazol-2-yl)-

benzamide

11

4-Ethylaminomethyl-N-(7-methoxy-4-phenyl-1H-benzoimidazol-2-

yl)-benzamide

12

4-Hydroxy-4-methyl-piperidine-1-carboxylic acid (7-methoxy-4-

phenyl-1H-benzoimidazol-2-yl)-amide

13

4-Aminomethyl-N-(7-methoxy-4-phenyl-1H-benzoimidazol-2-yl)-

benzamide

14

4-Cyclohexyl-7-methoxy-1H-benzoimidazol-2-ylamine

15

4-Imidazol-1-ylmethyl-N-(7-methoxy-4-phenyl-1H-benzoimidazol-

2-yl)-benzamide

16

4-Hydroxy-4-methyl-piperidine-1-carboxylic acid (4-cyclohexyl-7-

methoxy-1H-benzoimidazol-2-yl)-amide

17

N-(4-Cyclohexyl-7-methoxy-1H-benzoimidazol-2-yl)-2-morpholin-

4-yl-isonicotinamide

18

7-Methoxy-4-morpholin-4-yl-1H-benzoimidazol-2-ylamine

19

7-Methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-ylamine

20

7-Methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-

ylamine

21

4-hydroxy-N-(7-methoxy-4-morpholino-1H-benzimidazol-2-yl)-4-

methyl-piperidine-1-carboxamide

22

4-Hydroxy-4-methyl-piperidine-1-carboxylic acid [7-methoxy-4-(1-

methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

23

N-(7-Methoxy-4-morpholin-4-yl-1H-benzoimidazol-2-yl)-2-

morpholin-4-yl-isonicotinamide

24

4-Hydroxy-4-methyl-piperidine-1-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

25

4-Methoxy-7-phenyl-3H-imidazo[4,5-c]pyridin-2-ylamine

26

N-[7-Methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-

yl]-2-morpholin-4-yl-isonicotinamide

27

4-Methoxy-7-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-c]pyridin-

2-ylamine

28

4-Methyl-piperidine-1-carboxylic acid (7-methoxy-4-phenyl-1H-

benzoimidazol-2-yl)-amide

29

N-[7-Methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-

6-morpholin-4-yl-nicotinamide

30

2-(3-Hydroxy-3-methyl-pyrrolidin-1-yl)-N-[7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-isonicotinamide

31

3-Hydroxy-3-methyl-pyrrolidine-1-carboxylic acid [7-methoxy-4-

(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

32

4-Hydroxy-4-trifluoromethyl-piperidine-1-carboxylic acid [7-

methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-

amide

33

2-Oxa-7-aza-spiro[3.5]nonane-7-carboxylic acid [7-methoxy-4-(1-

methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

34

4-Difluoromethyl-4-hydroxy-piperidine-1-carboxylic acid [7-

methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-

amide

35

4-Hydroxymethyl-4-methyl-piperidine-1-carboxylic acid [7-

methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-

amide

36

4-Fluoromethyl-4-hydroxy-piperidine-1-carboxylic acid [7-

methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-

amide

37

4-Methoxy-piperidine-1-carboxylic acid [7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

38

3-Oxa-9-aza-spiro[5.5]undecane-9-carboxylic acid [7-methoxy-4-

(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

39

4-Methyl-piperidine-1-carboxylic acid [7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

40

4-Hydroxy-piperidine-1-carboxylic acid [7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

41

4-Benzyl-4-hydroxy-piperidine-1-carboxylic acid [7-methoxy-4-(1-

methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

42

N-[4-methoxy-7-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-

c]pyridin-2-yl]-2-(morpholin-4-yl)pyridine-4-carboxamide

43

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-oxa-6-azaspiro[3.4]octane-6-carboxamide

44

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decane-8-carboxamide

45

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1,4-dioxa-8-azaspiro[4.5]decane-8-carboxamide

46

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]morpholine-4-carboxamide

47

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-3-oxo-2,8-diazaspiro[4.5]decane-8-carboxamide

48

4-[(dimethylamino)methyl]-N-[7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-1,3-benzodiazol-2-yl]benzamide

49

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-(methoxymethyl)benzamide

50

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2,4-dioxo-1,3,8-triazaspiro[4.5]decane-8-carboxamide

51

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-oxo-1,8-diazaspiro[4.5]decane-8-carboxamide

52

4-(2-hydroxyethyl)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-

1H-1,3-benzodiazol-2-yl]-1,2,3,6-tetrahydropyridine-1-

carboxamide

53

3-butyl-4-hydroxy-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-

1,3-benzodiazol-2-yl]piperidine-1-carboxamide

54

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-phenoxypiperidine-1-carboxamide

55

4-hydroxy-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-4-(pyridin-3-yl)piperidine-1-carboxamide

56

4-hydroxy-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-3-(2-methylpropyl)piperidine-1-carboxamide

57

N-[4-(2,6-dimethylpyridin-4-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-2-(morpholin-4-yl)pyridine-4-carboxamide

58

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-oxopiperidine-1-carboxamide

59

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]acetamide

60

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxamide

61

3,3-diethyl-1-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]urea

62

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-methyl-5-oxo-1,4,9-triazaspiro[5.5]undecane-9-carboxamide

63

4-fluoro-N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-

yl]benzamide

64

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-6-oxaspiro[2.5]octane-1-carboxamide

65

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-5-{3H-[1,2,3]triazolo[4,5-b]pyridin-3-yloxy}pyrazine-2-

carboxamide

66

(chloromethyl)({2-[(1-{[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-

1H-1,3-benzodiazol-2-yl]carbamoyl}-4-methylpiperidin-4-

yl)oxy]ethyl})dimethylazanium hydrochloride

67

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-7-oxa-2-azaspiro[4.5]decane-2-carboxamide

68

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-8-oxa-2-azaspiro[4.5]decane-2-carboxamide

69

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-oxa-7-azaspiro[4.4]nonane-7-carboxamide

70

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide

71

4-[(1H-imidazol-1-yl)methyl]-N-[7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-1,3-benzodiazol-2-yl]benzamide

72

(lS,2S)-2-bromo-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-

1,3-benzodiazol-2-yl]cyclopropane-1-carboxamide

73

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-5-(2-methoxyethoxy)pyrazine-2-carboxamide

74

4-hydroxy-N-[7-methoxy-4-(pyridin-4-yl)-1H-1,3-benzodiazol-2-yl]-

4-methylpiperidine-1-carboxamide

75

4-benzyl-4-hydroxy-N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-

benzodiazol-2-yl]piperidine-1-carboxamide

76

4-[(1H-imidazol-1-yl)methyl]-N-[7-methoxy-4-(morpholin-4-yl)-1H-

1,3-benzodiazol-2-yl]benzamide

77

N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1-

benzofu ran-5-carboxamide

78

4-hydroxy-N-{7-methoxy-4-[1-(oxan-2-yl)-1H-pyrazol-4-yl]-1H-1,3-

benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

79

4-hydroxy-N-[7-methoxy-4-(1H-pyrazol-4-yl)-1H-1,3-benzodiazol-

2-yl]-4-methylpiperidine-1-carboxamide

80

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-benzofuran-5-carboxamide

81

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-5-(morpholin-4-yl)pyrazine-2-carboxamide

82

4-hydroxy-N-[4-methoxy-7-(1-methyl-1H-pyrazol-4-yl)-3H-

imidazo[4,5-c]pyridin-2-yl]-4-methylpiperidine-1-carboxamide

83

4-benzyl-4-hydroxy-N-[4-methoxy-7-(1-methyl-1H-pyrazol-4-yl)-

3H-imidazo[4,5-c]pyridin-2-yl]piperidine-1-carboxamide

84

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1,2-oxazole-3-carboxamide

85

N-[7-methoxy-4-(pyridin-4-yl)-1H-1,3-benzodiazol-2-yl]-2-oxa-6-

azaspiro[3.4]octane-6-carboxamide

86

1-(1-chloro-3-hydroxypropan-2-yl)-N-[7-methoxy-4-(morpholin-4-

yl)-1H-1,3-benzodiazol-2-yl]-1H-pyrazole-4-carboxamide

87

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-6-(morpholin-4-yl)pyridazine-3-carboxamide

88

4-[(dimethylamino)methyl]-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-

benzodiazol-2-yl]benzamide

89

4-[(dimethylamino)methyl]-N-[7-methoxy-4-(pyridin-4-yl)-1H-1,3-

benzodiazol-2-yl]benzamide

90

4-[(dimethylamino)methyl]-N-[7-methoxy-4-(morpholin-4-yl)-1H-

1,3-benzodiazol-2-yl]benzamide

91

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-6-

(morpholin-4-yl)pyridazine-3-carboxamide

92

4-hydroxy-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-4-(prop-2-yn-1-yl)piperidine-1-carboxamide

93

N4-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-

2-yl]-N1,N1-dimethylbenzene-1,4-dicarboxamide

94

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-(trifluoromethoxy)benzamide

95

2-bromo-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]pyridine-4-carboxamide

96

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-methyl-1,3-oxazole-4-carboxamide

97

4-[(1H-imidazol-1-yl)methyl]-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-

benzodiazol-2-yl]benzamide

98

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1,3-benzoxazole-5-carboxamide

99

3-amino-4-hydroxy-N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-

benzodiazol-2-yl]benzamide

100

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-[(2-oxopyrrolidin-1-yl)methyl]benzamide

101

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2,3-dihydro-1-benzofuran-5-carboxamide

102

4-hydroxy-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-4-

(prop-2-yn-1-yl)piperidine-1-carboxamide

103

4-benzyl-4-hydroxy-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-

benzodiazol-2-yl]piperidine-1-carboxamide

104

2-[(3S)-3-hydroxy-3-methylpyrrolidin-1-yl]-N-[7-methoxy-4-(1-

methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-yl]pyridine-4-

carboxamide

105

2-(4-hydroxy-4-methylpiperidin-1-yl)-N-[7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-yl]pyridine-4-carboxamide

106

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-{2-oxa-7-azaspiro[4.4]nonan-7-yl}pyridine-4-carboxamide

107

2-[(3R)-3-hydroxy-3-methylpyrrolidin-1-yl]-N-[7-methoxy-4-(1-

methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-yl]pyridine-4-

carboxamide

108

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2,3-dihydro-

l-benzofuran-5-carboxamide

109

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-3-(methoxymethyl)pyrrolidine-1-carboxamide

110

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-oxa-7-

azaspiro[4.4]nonane-7-carboxamide

111

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-8-oxa-2-

azaspiro[4.5]decane-2-carboxamide

112

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-hexahydro-

1H-furo[3,4-c]pyrrole-5-carboxamide

113

(5R)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-7-oxa-2-azaspiro[4.5]decane-2-carboxamide

114

(5S)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-7-oxa-2-azaspiro[4.5]decane-2-carboxamide

115

(5S)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-2-oxa-7-azaspiro[4.4]nonane-7-carboxamide

116

(5R)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-2-oxa-7-azaspiro[4.4]nonane-7-carboxamide

117

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-3-

(methoxymethyl)pyrrolidine-1-carboxamide

118

2-(4-hydroxy-4-methylpiperidin-1-yl)-N-[7-methoxy-4-(oxan-4-yl)-

1H-1,3-benzodiazol-2-yl]pyridine-4-carboxamide

119

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-{2-oxa-7-

azaspiro[4.4]nonan-7-yl}pyridine-4-carboxamide

120

2-(4-fluorophenoxy)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-

1H-1,3-benzodiazol-2-yl]-2-methylpropanamide

121

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-hexahydro-1H-furo[3,4-c]pyrrole-5-carboxamide

122

2-(3-hydroxy-3-methylpyrrolidin-1-yl)-N-[7-methoxy-4-(oxan-4-yl)-

1H-1,3-benzodiazol-2-yl]pyridine-4-carboxamide

123

N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-2-oxa-

7-azaspiro[4.4]nonane-7-carboxamide

124

l-{[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]carbamoyl}piperidine-4-carboxylic acid

125

N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-8-oxa-

2-azaspiro[4.5]decane-2-carboxamide

126

N1-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-

2-yl]piperidine-1,4-dicarboxamide

127

4-(diethylamino)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-

1,3-benzodiazol-2-yl]benzamide

128

4-hydroxy-N-{7-methoxy-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-

1H-1,3-benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

129

N-[7-methoxy-4-(pyridin-4-yl)-1H-1,3-benzodiazol-2-yl]-8-oxa-2-

azaspiro[4.5]decane-2-carboxamide

130

2-(1-{[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-

yl]carbamoyl}piperidin-4-yl)acetic acid

131

4-hydroxy-N-[7-methoxy-4-(2-methylphenyl)-1H-1,3-benzodiazol-

2-yl]-4-methylpiperidine-1-carboxamide

132

2-(1-{[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]carbamoyl}piperidin-4-yl)acetic acid

133

N4-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-N1,N1-

dimethylbenzene-1,4-dicarboxamide

134

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-3-(2-methoxyethyl)pyrrolidine-1-carboxamide

135

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-5-(morpholin-4-yl)pyridine-2-carboxamide

136

N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-pyrazole-4-carboxamide

137

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-3-(2-

methoxyethyl)pyrrolidine-1-carboxamide

138

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-4-[(2-

oxopyrrolidin-1-yl)methyl]benzamide

139

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-5-

(morpholin-4-yl)pyridine-2-carboxamide

140

(3R)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-3-(2-methoxyethyl)pyrrolidine-1-carboxamide

141

(3S)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-3-(2-methoxyethyl)pyrrolidine-1-carboxamide

142

2-[(3R)-3-hydroxy-3-methylpyrrolidin-1-yl]-N-[7-methoxy-4-(oxan-

4-yl)-1H-1,3-benzodiazol-2-yl]acetamide

143

2-[(3S)-3-hydroxy-3-methylpyrrolidin-1-yl]-N-[7-methoxy-4-(oxan-

4-yl)-1H-1,3-benzodiazol-2-yl]acetamide

144

N-[4-(4-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-4-

hydroxy-4-methylpiperidine-1-carboxamide

145

tert-butyl 4-(4-{2-[(4-hydroxy-4-methylpiperidine-1-

carbonyl)amino]-4-methoxy-1H-1,3-benzodiazol-7-yl}-1H-pyrazol-

l-yl)piperidine-1-carboxylate

146

4-{[2-amino-7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-1-yl]methyl}benzoic acid

147

(3S)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-3-(methoxymethyl)pyrrolidine-1-carboxamide

148

(3R)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-3-(methoxymethyl)pyrrolidine-1-carboxamide

149

(5S)-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-oxa-7-

azaspiro[4.4]nonane-7-carboxamide

150

(5R)-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-oxa-

7-azaspiro[4.4]nonane-7-carboxamide

151

4-hydroxy-N-{7-metho x y-4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-

1H-1,3-benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

152

N-[7-metho x y-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-[(morpholin-4-yl)methyl]benzamide

153

N-[7-metho x y-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-[(5R)-2-

oxa-7-azaspiro[4.4]nonan-7-yl]pyridine-4-carboxamide

154

N-[7-metho x y-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-[(5S)-2-

oxa-7-azaspiro[4.4]nonan-7-yl]pyridine-4-carboxamide

155

N-[4-(3,6-dihydro-2H-pyran-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-4-hydroxy-4-methylpiperidine-1-carboxamide

156

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-methyl-1H-1,2,3-triazole-4-carboxamide

157

4-hydroxy-N-{4-methoxy-7-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-1H-

1,3-benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

158

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-5-(2-methoxyethoxy)pyridine-2-carboxamide

159

2-(1-{[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]carbamoyl}piperidin-3-yl)acetic acid

160

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-methyl-1H-pyrazole-4-carboxamide

161

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-(2-methoxyethyl)-1H-pyrazole-4-carboxamide

162

N5-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-

2-yl]-N2,N2-dimethylpyridine-2,5-dicarboxamide

163

4-hydroxy-N-[4-methoxy-1-methyl-7-(1-methyl-1H-pyrazol-4-yl)-

1H-1,3-benzodiazol-2-yl]-4-methylpiperidine-1-carboxamide

164

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-(2-methoxyethyl)-1H-1,2,3-triazole-4-carboxamide

165

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-methyl-1,3-thiazole-5-carboxamide

166

3-cyano-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]propanamide

167

1-(2-Hydroxy-ethyl)-1H-pyrazole-4-carboxylic acid [7-methoxy-4-

(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

168

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-[(4-methylpiperazin-1-yl)methyl]benzamide

169

1-Methyl-1H-pyrazole-4-carboxylic acid [7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

170

5-Methyl-isoxazole-4-carboxylic acid [7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

171

5-Cyclopropyl-isoxazole-4-carboxylic acid [7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

172

1-Cyano-cyclopropanecarboxylic acid [7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

173

Thiazole-5-carboxylic acid [7-methoxy-4-(1-methyl-1H-pyrazol-4-

yl)-1H-benzoimidazol-2-yl]-amide

174

5,6,7,8-Tetrahydro-imidazo[1,2-a]pyridine-3-carboxylic acid [7-

methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-

amide

175

4-(4-Methyl-piperazin-1-yl)-but-2-ynoic acid [7-methoxy-4-(1-

methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

176

4-Hydroxy-but-2-ynoic acid [7-methoxy-4-(1-methyl-1H-pyrazol-4-

yl)-1H-benzoimidazol-2-yl]-amide

177

4-Acetylamino-but-2-ynoic acid [7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

178

4-Dimethylamino-but-2-ynoic acid [7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

179

(S)-3-Methanesulfonyl-pyrrolidine-1-carboxylic acid [7-methoxy-4-

(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

180

(S)-3-Fluoro-pyrrolidine-1-carboxylic acid [7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

181

(S)-3-Cyano-pyrrolidine-1-carboxylic acid [7-methoxy-4-(1-methyl-

1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-amide

182

(R)-3-Dimethylaminomethyl-pyrrolidine-1-carboxylic acid [7-

methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-benzoimidazol-2-yl]-

amide

183

5-Methyl-isoxazole-4-carboxylic acid (7-methoxy-4-morpholin-4-

yl-1H-benzoimidazol-2-yl)-amide

184

N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-1,2,3-triazole-4-carboxamide

185

1-Methyl-1H-[1,2,3]triazole-4-carboxylic acid (7-methoxy-4-

morpholin-4-yl-1H-benzoimidazol-2-yl)-amide

186

Pyridine-2,5-dicarboxylic acid 2-dimethylamide 5-{[7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide}

187

1-(2-Methoxy-ethyl)-1H-pyrazole-4-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

188

N-[7-Methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-

4-morpholin-4-ylmethyl-benzamide

189

N-[7-Methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-

4-(4-methyl-piperazin-1-ylmethyl)-benzamide

190

1-Methyl-1H-pyrazole-4-carboxylic acid [7-methoxy-4-(tetrahydro-

pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

191

5-Methyl-isoxazole-4-carboxylic acid [7-methoxy-4-(tetrahydro-

pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

192

5-Cyclopropyl-isoxazole-4-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

193

1-(2-Methoxy-ethyl)-1H-[1,2,3]triazole-4-carboxylic acid [7-

methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

194

1-Methyl-1H-[1,2,3]triazole-4-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

195

1-Cyano-cyclopropanecarboxylic acid [7-methoxy-4-(tetrahydro-

pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

196

Thiazole-5-carboxylic acid [7-methoxy-4-(tetrahydro-pyran-4-yl)-

1H-benzoimidazol-2-yl]-amide

197

2-Methyl-oxazole-5-carboxylic acid [7-methoxy-4-(tetrahydro-

pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

198

2-Methyl-thiazole-5-carboxylic acid [7-methoxy-4-(tetrahydro-

pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

199

Imidazo[1,2-a]pyridine-3-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

200

5-Amino-2H-[1,2,4]triazole-3-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

201

(S)-3-Methanesulfonyl-pyrrolidine-1-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

202

(S)-3-Fluoro-pyrrolidine-1-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

203

(S)-3-Cyano-pyrrolidine-1-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

204

(R)-3-Dimethylaminomethyl-pyrrolidine-1-carboxylic acid [7-

methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

205

Pyrazolo[1,5-a]pyridine-3-carboxylic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

206

1H-[1,2,4]Triazole-3-carboxylic acid [7-methoxy-4-(tetrahydro-

pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

207

5,6,7,8-Tetrahydro-imidazo[1,2-a]pyridine-3-carboxylic acid [7-

methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

208

2,3-Dimethyl-3H-imidazole-4-sulfonic acid [7-methoxy-4-

(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-amide

209

l-[7-Methoxy-4-(tetrahydro-pyran-4-yl)-1H-benzoimidazol-2-yl]-3-

thiazol-2-ylmethyl-urea

210

N-[7-methoxy-4-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-1,2,3-triazole-4-carboxamide

211

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-1,2,3-triazole-4-carboxamide

212

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-1-methyl-

1H-1,2,3-triazole-4-carboxamide

213

l-cyano-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]cyclopropane-1-carboxamide

214

N5-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-N2,N2-

dimethylpyridine-2,5-dicarboxamide

215

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-2-methyl-1,3-oxazole-5-carboxamide

216

N-[4-(azepan-1-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-4-

hydroxy-4-methylpiperidine-1-carboxamide

217

N-[4-(3-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-4-

hydroxy-4-methylpiperidine-1-carboxamide

218

N-[4-(2-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-4-

hydroxy-4-methylpiperidine-1-carboxamide

219

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1,3-thiazole-5-carboxamide

220

(3R)-3-methanesulfonyl-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-

yl)-1H-1,3-benzodiazol-2-yl]pyrrolidine-1-carboxamide

221

(3S)-3-fluoro-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]pyrrolidine-1-carboxamide

222

4-hydroxy-N-[7-methoxy-4-(1-methyl-6-oxo-1,6-dihydropyridin-3-

yl)-1H-1,3-benzodiazol-2-yl]-4-methylpiperidine-1-carboxamide

223

(3S)-3-(aminomethyl)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-

1H-1,3-benzodiazol-2-yl]pyrrolidine-1-carboxamide

224

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-1-methyl-

1H-pyrazole-4-carboxamide

225

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

226

l-cyano-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-

yl]cyclopropane-1-carboxamide

227

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-methyl-

1,3-thiazole-5-carboxamide

228

3-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-1-[(1,3-

thiazol-2-yl)methyl]urea

229

N-{7-[1-(difluoromethyl)-1H-pyrazol-4-yl]-4-methoxy-1H-1,3-

benzodiazol-2-yl}-4-hydroxy-4-methylpiperidine-1-carboxamide

230

4-hydroxy-N-(4-methoxy-7-{l-[2-(2-methoxyethoxy)ethyl]-1H-

pyrazol-4-yl}-1H-1,3-benzodiazol-2-yl)-4-methylpiperidine-1-

carboxamide

231

4-hydroxy-N-{4-methoxy-7-[1-(pyridin-2-yl)-1H-pyrazol-4-yl]-1H-

1,3-benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

232

N-[7-methoxy-4-(1-propylcyclopropyl)-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-pyrazole-4-carboxamide

233

N-[4-(hexan-3-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-methyl-

1H-pyrazole-4-carboxamide

234

N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-2-methyl-

1,3-oxazole-5-carboxamide

235

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-4-[(4-methylpiperazin-1-yl)methyl]benzamide

236

4-hydroxy-N-{4-methoxy-7-[3-(2-methoxyethoxy)phenyl]-1H-1,3-

benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

237

4-hydroxy-N-(4-methoxy-7-{l-[(pyridin-3-yl)methyl]-1H-pyrazol-4-

yl}-1H-1,3-benzodiazol-2-yl)-4-methylpiperidine-1-carboxamide

238

4-hydroxy-N-{7-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-4-

methoxy-1H-1,3-benzodiazol-2-yl}-4-methylpiperidine-1-

carboxamide

239

N-[4-(3-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-pyrazole-4-carboxamide

240

N4-[4-(3-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-

N1,N1-dimethylbenzene-1,4-dicarboxamide

241

4-hydroxy-N-{4-methoxy-7-[1-(oxolan-3-yl)-1H-pyrazol-4-yl]-1H-

1,3-benzodiazol-2-yl}-4-methylpiperidine-1-carboxamide

242

N4-[4-(2-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-

N1,N1-dimethylbenzene-1,4-dicarboxamide

243

N-[4-(2-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-pyrazole-4-carboxamide

244

N-[4-methoxy-1-methyl-7-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-

benzodiazol-2-yl]-1-methyl-1H-pyrazole-4-carboxamide

245

tert-butyl 3-(4-{2-[(4-hydroxy-4-methylpiperidine-1-

carbonyl)amino]-4-methoxy-1H-1,3-benzodiazol-7-yl}-1H-pyrazol-

1-yl)azetidine-1-carboxylate

246

N-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-5-oxopyrrolidine-3-carboxamide

247

3-[7-methoxy-4-(1-methyl-1H-pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]-1-[(1,3-thiazol-2-yl)methyl]urea

248

4-(2,5-dioxopyrrolidin-1-yl)-N-[7-methoxy-4-(1-methyl-1H-pyrazol-

4-yl)-1H-1,3-benzodiazol-2-yl]benzamide

249

l-[(3R,4S)-4-fluoropyrrolidin-3-yl]-3-[7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-1,3-benzodiazol-2-yl]urea

250

4-(2,5-dioxopyrrolidin-1-yl)-N-[7-methoxy-4-(oxan-4-yl)-1H-1,3-

benzodiazol-2-yl]benzamide

251

tert-butyl (3S,4R)-3-fluoro-4-({[7-methoxy-4-(1-methyl-1H-

pyrazol-4-yl)-1H-1,3-benzodiazol-2-

yl]carbamoyl}amino)pyrrolidine-1-carboxylate

252

N4-[7-methoxy-4-(1,2,3,6-tetrahydropyridin-4-yl)-1H-1,3-

benzodiazol-2-yl]-N1,N1-dimethylbenzene-1,4-dicarboxamide

253

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1H-imidazole-4-

carboxamide

254

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1-methyl-1H-

imidazole-5-carboxamide

255

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-2-methyl-1H-

imidazole-4-carboxamide

256

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1,3-thiazole-5-

carboxamide

257

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-2-methyl-1,3-

thiazole-5-carboxamide

258

2-amino-N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1,3-

thiazole-5-carboxamide

259

N4-[7-methoxy-4-(pyridin-3-yl)-1H-1,3-benzodiazol-2-yl]-N1,N1-

dimethylbenzene-1,4-dicarboxamide

260

N-[7-methoxy-4-(pyridin-3-yl)-1H-1,3-benzodiazol-2-yl]-1-methyl-

1H-pyrazole-4-carboxamide

261

N4-[4-(2,5-dihydrofuran-3-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-N1,N1-dimethylbenzene-1,4-dicarboxamide

262

N4-[4-(3,6-dihydro-2H-pyran-4-yl)-5-fluoro-7-methoxy-1H-1,3-

benzodiazol-2-yl]-N1,N1-dimethylbenzene-1,4-dicarboxamide

263

3-{[dimethyl(oxo)-lambda6-sulfanylidene]amino}-N-[7-methoxy-4-

(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]benzamide

264

N-[4-(3,6-dihydro-2H-pyran-4-yl)-5-fluoro-7-methoxy-1H-1,3-

benzodiazol-2-yl]-1-methyl-1H-pyrazole-4-carboxamide

265

N-[7-(3-fluorophenyl)-4-methoxy-1H-1,3-benzodiazol-2-yl]-1H-

imidazole-4-carboxamide

266

N-[4-methoxy-7-(pyridin-4-yl)-1H-1,3-benzodiazol-2-yl]-1H-

imidazole-4-carboxamide

267

N-{4-methoxy-7-[3-(2-methoxyethoxy)phenyl]-1H-1,3-

benzodiazol-2-yl}-1H-imidazole-4-carboxamide

268

N-[4-methoxy-7-(pyridin-3-yl)-1H-1,3-benzodiazol-2-yl]-1H-

imidazole-4-carboxamide

269

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1,3-dimethyl-1H-

pyrazole-4-carboxamide

270

4-hydroxy-N-(7-methoxy-4-{1H-pyrrolo[2,3-b]pyridin-4-yl}-1H-1,3-

benzodiazol-2-yl)-4-methylpiperidine-1-carboxamide

271

4-hydroxy-N-[4-(1H-indazol-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-4-methylpiperidine-1-carboxamide

272

4-hydroxy-N-[4-(1H-indol-6-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-4-methylpiperidine-1-carboxamide

273

4-hydroxy-N-[7-methoxy-4-(1-methyl-1H-indazol-5-yl)-1H-1,3-

benzodiazol-2-yl]-4-methylpiperidine-1-carboxamide

274

4-hydroxy-N-[7-methoxy-4-(3-methyl-1H-indazol-5-yl)-1H-1,3-

benzodiazol-2-yl]-4-methylpiperidine-1-carboxamide

275

4-hydroxy-N-(4-{imidazo[1,2-a]pyridin-7-yl}-7-methoxy-1H-1,3-

benzodiazol-2-yl)-4-methylpiperidine-1-carboxamide

276

(2Z)-2-cyano-3-hydroxy-N-(7-methoxy-4-phenyl-1H-1,3-

benzodiazol-2-yl)but-2-enamide

277

N4-[5-fluoro-7-methoxy-4-(oxan-4-yl)-1H-1,3-benzodiazol-2-yl]-

N1,N1-dimethylbenzene-1,4-dicarboxamide

278

N-(7-methoxy-4-{1H-pyrrolo[2,3-b]pyridin-4-yl}-1H-1,3-

benzodiazol-2-yl)-1-(2-methoxyethyl)-1H-pyrazole-4-carboxamide

279

N-[4-(1H-indazol-4-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

280

N-[4-(1H-indol-6-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

281

N-[7-methoxy-4-(1-methyl-1H-indazol-5-yl)-1H-1,3-benzodiazol-2-

yl]-1-(2-methoxyethyl)-1H-pyrazole-4-carboxamide

282

N-[7-methoxy-4-(3-methyl-1H-indazol-5-yl)-1H-1,3-benzodiazol-2-

yl]-1-(2-methoxyethyl)-1H-pyrazole-4-carboxamide

283

N-[4-(2,3-dihydro-1H-indol-4-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-1-(2-methoxyethyl)-1H-pyrazole-4-carboxamide

284

N2-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-N5,N5-

dimethylpyridine-2,5-dicarboxamide

285

4-(2,5-dioxopyrrolidin-1-yl)-N-(7-methoxy-4-phenyl-1H-1,3-

benzodiazol-2-yl)benzamide

286

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)imidazo[1,2-

a]pyridine-3-carboxamide

287

4,4-difluoro-N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-

yl)piperidine-1-carboxamide

288

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)imidazo[1,2-

b]pyridazine-3-carboxamide

289

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)imidazo[1,2-

a]pyrimidine-3-carboxamide

290

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-2-(pyridin-4-yl)-

1H-imidazole-4-carboxamide

291

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-5H,6H,7H,8H-

imidazo[1,2-a]pyridine-3-carboxamide

292

N-[4-(2,3-dihydro-1H-indol-4-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-4-hydroxy-4-methylpiperidine-1-carboxamide

293

N1-(4-methoxy-7-phenyl-1H-1,3-benzodiazol-2-yl)-N4-

propylbenzene-1,4-dicarboxamide

294

N-(4-methoxy-7-phenyl-1H-1,3-benzodiazol-2-yl)-4-(4-

methylpiperazine-1-carbonyl)benzamide

295

N4-(4-methoxy-7-phenyl-1H-1,3-benzodiazol-2-yl)-N1-(2-

methoxyethyl)-N1-methylbenzene-1,4-dicarboxamide

296

N1-[2-(dimethylamino)ethyl]-N4-(4-methoxy-7-phenyl-1H-1,3-

benzodiazol-2-yl)-N1-methylbenzene-1,4-dicarboxamide

297

N4-(4-methoxy-7-phenyl-1H-1,3-benzodiazol-2-yl)-N1-methyl-N1-

propylbenzene-1,4-dicarboxamide

298

N-(4-methoxy-7-phenyl-1H-1,3-benzodiazol-2-yl)-4-(morpholine-

4-carbonyl)benzamide

299

N-[4-methoxy-7-(2-methylpyridin-4-yl)-1H-1,3-benzodiazol-2-yl]-

1H-imidazole-4-carboxamide

300

N-(5-cyano-7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1-

methyl-1H-pyrazole-4-carboxamide

301

N-(4-{imidazo[1,2-a]pyridin-7-yl}-7-methoxy-1H-1,3-benzodiazol-

2-yl)-1-(2-methoxyethyl)-1H-pyrazole-4-carboxamide

302

N-[4-(1H-indol-5-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

303

4-hydroxy-N-[4-(1H-indol-5-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-4-methylpiperidine-1-carboxamide

304

N-[4-(1H-indol-7-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

305

4-hydroxy-N-[4-(1H-indol-7-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]-4-methylpiperidine-1-carboxamide

306

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1-methyl-1H-

pyrazole-4-carboxamide

307

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

308

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-2-methyl-1,3-

oxazole-5-carboxamide

309

N4-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-N1,N1-

dimethylbenzene-1,4-dicarboxamide

310

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-8-oxa-2-

azaspiro[4.5]decane-2-carboxamide

311

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-4-[(2-

oxopyrrolidin-1-yl)methyl]benzamide

312

N1-(2-hydroxyethyl)-N4-(4-methoxy-7-phenyl-1H-1,3-benzodiazol-

2-yl)benzene-1,4-dicarboxamide

313

N4-[7-methoxy-4-(1,4-oxazepan-4-yl)-1H-1,3-benzodiazol-2-yl]-

N1,N1-dimethylbenzene-1,4-dicarboxamide

314

N-[4-(3,6-dihydro-2H-pyran-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]cyclopropanecarboxamide

315

N-[7-methoxy-4-(pyridin-3-yl)-1H-1,3-benzodiazol-2-

yl]cyclopropanecarboxamide

316

N4-[4-(4-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-

N1,N1-dimethylbenzene-1,4-dicarboxamide

317

4-(2,5-dioxopyrrolidin-1-yl)-N-[4-(4-fluorophenyl)-7-methoxy-1H-

1,3-benzodiazol-2-yl]benzamide

318

N-[4-(4-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-pyrazole-4-carboxamide

319

N4-[4-(2,6-dimethoxypyridin-3-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-N1,N1-dimethylbenzene-1,4-dicarboxamide

320

N-[4-(2,6-dimethoxypyridin-3-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]cyclopropanecarboxamide

321

N-[7-methoxy-4-(pyridin-3-yl)-1H-1,3-benzodiazol-2-yl]-2-methyl-

1,3-oxazole-5-carboxamide

322

N-[4-(2,5-dihydrofuran-3-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-

2-methyl-1,3-oxazole-5-carboxamide

323

N-[4-(4-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-2-

methyl-1,3-oxazole-5-carboxamide

324

N4-[4-(3,6-dihydro-2H-pyran-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-N1,N1-dimethylbenzene-1,4-dicarboxamide

325

N-[4-(3,6-dihydro-2H-pyran-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-1-methyl-1H-pyrazole-4-carboxamide

326

(4-{2-[(4-hydroxy-4-methylpiperidine-1-carbonyl)amino]-7-

methoxy-1H-1,3-benzodiazol-4-yl}morpholin-2-yl)methyl

carbamate

327

(1-{2-[(4-hydroxy-4-methylpiperidine-1-carbonyl)amino]-7-

methoxy-1H-1,3-benzodiazol-4-yl}piperidin-3-yl)methyl cyanate

328

(1-{2-[(4-hydroxy-4-methylpiperidine-1-carbonyl)amino]-7-

methoxy-1H-1,3-benzodiazol-4-yl}piperidin-3-yl)methyl

carbamate

329

N-(7-methoxy-4-phenyl-1H-1,3-benzodiazol-2-yl)-2-oxa-8-

azaspiro[4.5]decane-8-carboxamide

330

N-[4-(1H-indol-6-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1H-

imidazole-4-carboxamide

331

N-[4-(1H-indol-6-yl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-1-

methyl-1H-pyrazole-4-carboxamide

332

N-[4-(4-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-8-oxa-

2-azaspiro[4.5]decane-2-carboxamide

333

N-[4-(3,6-dihydro-2H-pyran-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-8-oxa-2-azaspiro[4.5]decane-2-carboxamide

334

N-[4-(3,6-dihydro-2H-pyran-4-yl)-7-methoxy-1H-1,3-benzodiazol-

2-yl]-4-[(2-oxopyrrolidin-1-yl)methyl]benzamide

335

N-[4-(4-fluorophenyl)-7-methoxy-1H-1,3-benzodiazol-2-yl]-4-[(2-

oxopyrrolidin-1-yl)methyl]benzamide

336

N-[4-(1H-indol-6-yl)-7-methoxy-1H-1,3-benzodiazol-2-

yl]cyclopropanecarboxamide

and physiologically acceptable salts, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.

8 . (canceled)

9 . (canceled)

10 . (canceled)

11 . (canceled)

12 . (canceled)

13 . (canceled)

14 . A method for the treatment and/or prophylaxis of physiological and/or pathophysiological states in a host in need thereof, comprising administering to said host an effective amount of a medicament comprising at least one compound of the formula I,

wherein

Q, Y are independently of one another CH or N,

R 1 is Hal or linear or branched alkyl having 1-10 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 4 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NR 5 SO 2 R 6 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or —CH═CH— groups, and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl, or mono- or bicyclic cyclic alkyl having 3-7 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 4 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NR 5 SO 2 R 6 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or by —CH═CH— groups and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl, or mono- or bicyclic heteroaryl, heterocyclyl, aryl or cyclic alkylaryl, containing 3 to 14 carbon atoms and 0-4 heteroatoms, independently selected from N, O and S, which is unsubstituted or mono-, di- or trisubstituted by R 4 ,

R 2 is linear or branched alkyl having 1-10 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 4 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NR 5 SO 2 R 6 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or —CH═CH— groups, and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl, or cyclic alkyl having 3-7 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 4 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NR 5 SO 2 R 6 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or by —CH═CH— groups and/or, in addition, 1-11 H atoms may be replaced by F and/or Cl, or mono- or bicyclic heteroaryl, heterocyclyl, aryl or cyclic alkylaryl, containing 3 to 14 carbon atoms and 0-4 heteroatoms, independently selected from N, O and S, which is unsubstituted or mono-, di- or trisubstituted by R 4 ,

R 3 is linear or branched alkyl or O-alkyl having 1-6 C atoms or cyclic alkyl having 3-6 C atoms, which is unsubstituted or mono-, di- or trisubstituted by H, ═S, ═NH, ═O, OH, cyclic alkyl having 3-6 C atoms, COOH, Hal, NH 2 , SO 2 CH 3 , SO 2 NH 2 , CN, CONH 2 , NHCOCH 3 , NHCONH 2 or NO 2 ,

R 4 is H, R 5 , ═S, ═NR 5 , =0, OH, COOH, Hal, NH 2 , SO 2 CH 3 , SO 2 NH 2 , CN, CONH 2 , NHCOCH 3 , NHCONH 2 , NO 2 , or linear or branched alkyl having 1-10 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 5 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NR 5 SO 2 R 6 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or —CH═CH— groups, and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl, or mono- or bicyclic cyclic alkyl having 3-7 C atoms which is unsubstituted or mono-, di- or trisubstituted by R 5 and in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —NRSO 2 R 4 —, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or by —CH═CH— groups and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl, or mono- or bicyclic heteroaryl, heterocyclyl, aryl or cyclic alkylaryl, containing 3 to 14 carbon atoms and 0-4 heteroatoms, independently selected from N, O and S, which is unsubstituted or mono-, di- or trisubstituted by R 5 ,

R 5 , R 6 are independently of one another selected from the group consisting of H, ═S, ═NH, ═O, OH, COOH, Hal, NH 2 , SO 2 CH 3 , SO 2 NH 2 , CN, CONH 2 , NHCOCH 3 , NHCONH 2 , NO 2 and linear or branched alkyl having 1-10 C atoms in which 1-4 C atoms may be replaced, independently of one another, by O, S, SO, SO 2 , NH, NCH 3 , —OCO—, —NHCONH—, —NHCO—, —COO—, —CONH—, —NCH 3 CO—, —CONCH 3 —, —C≡C— groups and/or —CH═CH— groups, and/or, in addition, 1-10 H atoms may be replaced by F and/or Cl,

Hal is F, C, Br, or I,

and/or one of its physiologically acceptable salts, derivatives, solvates, prodrugs and stereoisomers, including mixtures thereof in all ratios.

15 . The method according to claim 14 , wherein the physiological states are hyperproliferative or infectious diseases or disorders.

16 . The method according to claim 15 , wherein the hyperproliferative disease or disorder is cancer.

17 . The method according to claim 16 , wherein the cancer is acute or chronic lymphocytic leukemia, acute granulocytic leukemia, adrenal cortex cancer, bladder cancer, brain cancer, breast cancer, cervical cancer, cervical hyperplasia, cervical cancer, chorio cancer, chronic granulocytic leukemia, chronic lymphocytic leukemia, colon cancer, endometrial cancer, esophageal cancer, essential thrombocytosis, genitourinary carcinoma, glioma, glioblastoma, hairy cell leukemia, head and neck carcinoma, Hodgkin's disease, Kaposi's sarcoma, lung carcinoma, lymphoma, malignant carcinoid carcinoma, malignant hypercalcemia, malignant melanoma, malignant pancreatic insulinoma, medullary thyroid carcinoma, melanoma, multiple myeloma, mycosis fungoides, myeloid and lymphocytic leukemia, neuroblastoma, non-Hodgkin's lymphoma, non-small cell lung cancer, osteogenic sarcoma, ovarian carcinoma, pancreatic carcinoma, polycythemia vera, primary brain carcinoma, primary macroglobulinemia, prostatic cancer, renal cell cancer, rhabdomyosarcoma, skin cancer, small-cell lung cancer, soft-tissue sarcoma, squamous cell cancer, stomach cancer, testicular cancer, thyroid cancer or Wilms' tumor.

18 . The method according to claim 15 , wherein the hyperproliferative disease or disorder is selected from the group consisting of age-related macular degeneration, Crohn's disease, cirrhosis, chronic inflammatory-related disorders, proliferative diabetic retinopathy, proliferative vitreoretinopathy, retinopathy of prematurity, granulomatosis, immune hyperproliferation associated with organ or tissue transplantation an immunoproliferative disease or disorder that is inflammatory bowel disease, psoriasis, rheumatoid arthritis, systemic lupus erythematosus (SLE), vascular hyperproliferation secondary to retinal hypoxia or vasculitis.

19 . The method according to claim 15 , wherein the infectious disease or disorder is

a) virally induced infectious diseases which are caused by retroviruses, hepadnaviruses, herpesviruses, flaviviridae and/or adenoviruses wherein the retroviruses are lentiviruses or oncoretroviruses, wherein the lentivirus is HIV-1, HIV-2, FIV, BIV, SIVs, SHIV, CAEV, VMV or EIAV and the oncoretrovirus HTLV-I, HTLV-II or BLV, the hepadnavirus is HBV, GSHV or WHV, the herpesivirus is HSV I, HSV II, EBV, VZV, HCMV or HHV 8 and the flaviviridae is HCV, West nile or Yellow Fever,

b) bacterial infectious diseases which are caused by Gram-positive bacteria wherein the Gram-positive bacteria are of methicillin-susceptible or methicillin-resistant staphylococci that are Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus , or coagulase-negative staphylococci, glycopeptides-intermediate susceptible Staphylococcus aureus (GISA), penicillin-susceptible or penicillin-resistant streptococci that are Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus avium, Streptococcus bovis, Streptococcus lactis, Streptococcus sanguis or Streptococci Group C (GCS), Streptococci Group G (GGS) or viridans streptococci, enterococci that are vancomycin susceptible or vancomycin-resistant strains that are Enterococcus faecalis or Enterococcus faecium, Clostridium difficile, Listeria monocytogenes, Corynebacterium jeikeium, Chlamydia spp or Mycobacterium tuberculosis,

c) bacterial infectious diseases which are caused by Gram-negative bacteria wherein the Gram-negative bacteria are of the Genus Enterobacteriacae, Klebsiella spp., Enterobacter spp., Citrobacter spp., Serratia spp., Proteus spp., Providencia spp., Salmonella spp., Shigella spp., the genus Pseudomonas, Moraxella spp. Haemophilus spp. or Neisseria spp.,

d) infectious diseases induced by intracellular active parasites of phylum Apicomplexa, or Sarcomastigophora that are Trypanosoma, Plasmodia, Leishmania, Babesia or Theileria , Cryptosporidia, Sacrocystida, Amoebia, Coccidia or Trichomonadia.

20 . (canceled)

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 15, 2025
From: MERCK PATENT GMBH; MERCK HEALTHCARE KGAA
To: DOMAIN THERAPEUTICS
Reel/Frame 072033/0504 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 14, 2022
From: TANZER, EVA-MARIA; SCHIEMANN, KAI; KLEIN, MARKUS
To: MERCK PATENT GMBH
Reel/Frame 059595/0477 →