Granted Patent B2

US 12,344,623 · App. 17/424,568 · Granted Jul 1, 2025

Inventors: Eva-Maria Tanzer Krauel (Billerica, MA); Kai Schiemann (Seeheim-Jugenheim, DE); Alejandro Crespo (West Newton, MA)

Assignee: Domain Therapeutics SA

C07D513/04C07D519/00

Abstract

Claims (490)

1. A compound selected from the group consisting of:

1

(R)-3-Aminomethyl-pyrrolidine-1-carboxylic acid (4-methoxy-

7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide

2

N-{4-methoxy-7-[4-(oxan-4-yloxy)phenyl]-[1,3]thiazolo[4,5-

c]pyridin-2-yl}-8-oxa-2-azaspiro[4.5]decane-2-carboxamide

3

(S)-3-Aminomethyl-pyrrolidine-1-carboxylic acid (4-methoxy-

7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide

4

Cyclopropanecarboxylic acid (6-fluoro-4-methoxy-7-

morpholin-4-yl-thiazolo[4,5-c]pyridin-2-yl)-amide

6

N-(6-Fluoro-4-methoxy-7-morpholin-4-yl-thiazolo[4,5-c]pyridin-

2-yl)-4-(1H-tetrazol-5-yl)-benzamide

7

7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (6-fluoro-4-

methoxy-7-morpholin-4-yl-thiazolo[4,5-c]pyridin-2-yl)-amide

9

N-[7-(1H-indol-6-yl)-4-methoxy-[1,3]thiazolo[4,5-c]pyridin-2-

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

10

(R)-7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (6-fluoro-

4-methoxy-7-morpholin-4-yl-thiazolo[4,5-c]pyridin-2-yl)-amide

11

(5S)-N-[6-fluoro-4-methoxy-7-(morpholin-4-yl)-

[1,3]thiazolo[4,5-c]pyridin-2-yl]-7-oxa-2-azaspiro[4.5]decane-

2-carboxamide

12

(R)-7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (6-fluoro-

4-methoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide

13

(5S)-N-{6-fluoro-4-methoxy-7-phenyl-[1,3]thiazolo[4,5-

c]pyridin-2-yl}-7-oxa-2-azaspiro[4.5]decane-2-carboxamide

14

3-Dimethylaminomethyl-bicyclo[1.1.1]pentane-1-carboxylic

acid (4-methoxy-7-morpholin-4-yl-thiazolo[4,5-c]pyridin-2-yl)-

amide

15

7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-

dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

16

N-[6-fluoro-4-methoxy-7-(morpholin-4-yl)-[1,3]thiazolo[4,5-

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

17

N-[4-methoxy-7-(oxan-4-yl)-[1,3]thiazolo[4,5-c]pyridin-2-yl]-2-

[(2-methoxyethyl)amino]-1,3-thiazole-5-carboxamide

18

(R)-2-Oxa-7-aza-spiro[4.4]nonane-7-carboxylic acid (6-fluoro-

4-methoxy-7-morpholin-4-yl-thiazolo[4,5-c]pyridin-2-yl)-amide

19

(5S)-N-[6-fluoro-4-methoxy-7-(morpholin-4-yl)-

[1,3]thiazolo[4,5-c]pyridin-2-yl]-2-oxa-7-azaspiro[4.4]nonane-

7-carboxamide

20

N-[6-Fluoro-4-methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-

c]pyridin-2-yl]-N′,N′-dimethyl-terephthalamide

21

1-Imidazol-1-ylmethyl-cyclopropanecarboxylic acid [6-fluoro-4-

methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

22

N-[6-fluoro-4-methoxy-7-(oxan-4-yl)-[1,3]thiazolo[4,5-c]pyridin-

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

23

N-[6-fluoro-4-methoxy-7-(oxan-4-yl)-[1,3]thiazolo[4,5-c]pyridin-

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

24

(R)-7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-

dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

25

(S)-7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-

dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

26

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [6-fluoro-4-

methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

27

4-Hydroxy-4-methyl-piperidine-1-carboxylic acid [6-fluoro-7-

(4-fluoro-phenyl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

28

Cyclopropanecarboxylic acid [6-fluoro-4-methoxy-7-

(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

29

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [6-fluoro-7-(4-

fluoro-phenyl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

30

Cyclopropanecarboxylic acid [7-(3-ethylaminomethyl-phenyl)-

4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

31

7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [6-fluoro-4-

methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

32

1H-Imidazole-4-carboxylic acid (6-fluoro-4-methoxy-7-phenyl-

thiazolo[4,5-c]pyridin-2-yl)-amide

33

N-[6-fluoro-4-methoxy-7-(oxan-4-yl)-[1,3]thiazolo[4,5-c]pyridin-

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

34

(R)-7-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [6-fluoro-

4-methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-

yl]-amide

35

(5S)-N-[6-fluoro-4-methoxy-7-(oxan-4-yl)-[1,3]thiazolo[4,5-

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

37

(R)-2-Oxa-7-aza-spiro[4.4]nonane-7-carboxylic acid [6-fluoro-

4-methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-

yl]-amide

38

(5S)-N-[6-fluoro-4-methoxy-7-(oxan-4-yl)-[1,3]thiazolo[4,5-

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

39

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3-amino-

phenyl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

40

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(3-oxo-cyclopent-1-enyl)-thiazolo[4,5-c]pyridin-2-yl]-amide

41

Bicyclo[1.1.1]pentane-1,3-dicarboxylic acid [6-fluoro-4-

methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-

amide (2-hydroxy-ethyl)-methyl-amide

42

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

c]pyridin-2-yl]cyclopropanecarboxamide

43

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

c]pyridin-2-yl]-1H-imidazole-4-carboxamide

44

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

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

45

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

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

46

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(1-acetyl-

1,2,3,6-tetrahydro-pyridin-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-amide

47

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-thiophen-2-yl-thiazolo[4,5-c]pyridin-2-yl)-amide

48

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (7-furan-2-yl-

4-methoxy-thiazolo[4,5-c]pyridin-2-yl)-amide

49

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3-

ethylaminomethyl-phenyl)-4-methoxy-thiazolo[4,5-c]pyridin-2-

yl]-amide

50

N-[6-Fluoro-4-methoxy-7-(tetrahydro-pyran-4-yl)-thiazolo[4,5-

c]pyridin-2-yl]-N′-(2-hydroxy-ethyl)-N′-methyl-terephthalamide

51

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-piperidin-1-yl-thiazolo[4,5-c]pyridin-2-yl)-amide

52

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (7-furan-3-yl-

4-methoxy-thiazolo[4,5-c]pyridin-2-yl)-amide

53

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(4-methyl-piperazin-1-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

54

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(3-methoxy-phenyl)-thiazolo[4,5-c]pyridin-2-yl]-amide

55

N-{6-cyano-4-methoxy-[1,3]thiazolo[4,5-c]pyridin-2-yl}-1-(2-

methoxyethyl)-1H-pyrazole-4-carboxamide

56

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(6-methyl-pyridazin-3-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

57

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (7-azetidin-1-

yl-4-methoxy-thiazolo[4,5-c]pyridin-2-yl)-amide

58

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3-

hydroxy-azetidin-1-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

59

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (7-cyclohex-

1-enyl-4-methoxy-thiazolo[4,5-c]pyridin-2-yl)-amide

60

1H-Imidazole-4-carboxylic acid (4-methoxy-7-phenyl-

thiazolo[4,5-c]pyridin-2-yl)-amide

61

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

[1,3]thiazolo[4,5-c]pyridin-2-yl]-N1,N1-dimethylbenzene-1,4-

dicarboxamide

62

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (7-cyclohexyl-

4-methoxy-thiazolo[4,5-c]pyridin-2-yl)-amide

63

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(4,4-

difluoro-cyclohex-1-enyl)-4-methoxy-thiazolo[4,5-c]pyridin-2-

yl]-amide

64

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-

dihydro-2H-thiopyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-

yl]-amide

65

1H-Imidazole-4-carboxylic acid [7-(3,6-dihydro-2H-pyran-4-yl)-

4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

66

N-[4-methoxy-7-(4-methoxycyclohex-1-en-1-yl)-

[1,3]thiazolo[4,5-c]pyridin-2-yl]-8-oxa-2-azaspiro[4.5]decane-

2-carboxamide

67

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(2-methyl-thiazol-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

68

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(1-pyridin-3-ylmethyl-1H-pyrazol-4-yl)-thiazolo[4,5-c]pyridin-2-

yl]-amide

69

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(1-pyridin-2-ylmethyl-1H-pyrazol-4-yl)-thiazolo[4,5-c]pyridin-2-

yl]-amide

71

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

c]pyridin-2-yl]-4-(1H-1,2,3-triazol-1-yl)benzamide

72

4-{[7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-[1,3]thiazolo[4,5-

c]pyridin-2-yl]carbamoyl}benzoic acid

73

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (7-

[1,4]dioxan-2-yl-4-methoxy-thiazolo[4,5-c]pyridin-2-yl)-amide

74

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid {7-[1-(2,2-

difluoro-ethyl)-1H-pyrazol-4-yl]-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl}-amide

75

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(1-pyridin-4-ylmethyl-1H-pyrazol-4-yl)-thiazolo[4,5-c]pyridin-2-

yl]-amide

76

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(1-benzyl-

1H-pyrazol-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

79

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(1-

difluoromethyl-1H-pyrazol-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-amide

80

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-

difluoromethoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide

81

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

c]pyridin-2-yl]-2-[(2-methoxyethyl)amino]-1,3-thiazole-5-

carboxamide

82

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

c]pyridin-2-yl]-4-[(1H-imidazol-1-yl)methyl]benzamide

83

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

c]pyridin-2-yl]-4-[(1R)-1-acetamidoethyl]benzamide

84

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid {4-methoxy-

7-[1-(tetrahydro-pyran-2-ylmethyl)-1H-pyrazol-4-yl]-

thiazolo[4,5-c]pyridin-2-yl}-amide

85

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid {4-methoxy-

7-[1-(tetrahydro-pyran-4-ylmethyl)-1H-pyrazol-4-yl]-

thiazolo[4,5-c]pyridin-2-yl}-amide

86

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(1,1-dioxo-

hexahydro-1l6-thiopyran-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-amide

87

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid {4-methoxy-

7-[1-(tetrahydro-pyran-3-ylmethyl)-1H-pyrazol-4-yl]-

thiazolo[4,5-c]pyridin-2-yl}-amide

88

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

c]pyridin-2-yl]-4-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-

yl)piperidine-1-carboxamide

89

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

c]pyridin-2-yl]-1-[4-(2-oxopyrrolidin-1-yl)phenyl]urea

90

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

[1,3]thiazolo[4,5-c]pyridin-2-yl]carbamoyl}amino)phenyl]-2-

(dimethylamino)acetamide

91

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

c]pyridin-2-yl]-4-(2,4-dioxo-1,3-thiazolidin-3-yl)piperidine-1-

carboxamide

92

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

[1,3]thiazolo[4,5-c]pyridin-2-yl]carbamoyl}amino)-2-

methylphenyl]acetamide

93

N4-[7-(3,6-dihydro-2H-pyran-4-yl)-4-hydroxy-[1,3]thiazolo[4,5-

c]pyridin-2-yl]-N1-(2-hydroxyethyl)-N1-methylbenzene-1,4-

dicarboxamide

94

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

c]pyridin-2-yl]-1-[4-(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-

yl)phenyl]urea

95

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

c]pyridin-2-yl]-1-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]urea

96

N1-[7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-

[1,3]thiazolo[4,5-c]pyridin-2-yl]-N4,N4-dimethylpiperidine-1,4-

dicarboxamide

97

[4-(4-Methoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-ylcarbamoyl)-

benzyl]-methyl-carbamic acid methyl ester

98

2,8-Diaza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-dihydro-

2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

99

4-(2,5-Dioxo-pyrrolidin-1-yl)-piperidine-1-carboxylic acid (4-

methoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide

100

4-(2,5-Dioxo-pyrrolidin-1-yl)-piperidine-1-carboxylic acid [7-

(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-

2-yl]-amide

101

Bicyclo[1.1.1]pentane-1,3-dicarboxylic acid (6-fluoro-4-

methoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide (2-

hydroxy-ethyl)-methyl-amide

102

2,7-Diaza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-dihydro-

2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

103

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-{1-[2-(2-methoxy-ethoxy)-ethyl]-1H-pyrazol-4-yl}-

thiazolo[4,5-c]pyridin-2-yl)-amide

104

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-{1-[(R)-1-(tetrahydro-pyran-3-yl)methyl]-1H-pyrazol-4-yl}-

thiazolo[4,5-c]pyridin-2-yl)-amide

105

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-{1-[(S)-1-(tetrahydro-pyran-3-yl)methyl]-1H-pyrazol-4-yl}-

thiazolo[4,5-c]pyridin-2-yl)-amide

106

N1-[7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-

[1,3]thiazolo[4,5-c]pyridin-2-yl]piperidine-1,4-dicarboxamide

107

N-[7-(3,6-dihydro-2H-pyran-4-yl)-4-hydroxy-[1,3]thiazolo[4,5-

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

108

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

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

109

4-({4-methoxy-7-phenyl-[1,3]thiazolo[4,5-c]pyridin-2-

yl}carbamoyl)benzoic acid

110

N-{4-methoxy-7-phenyl-[1,3]thiazolo[4,5-c]pyridin-2-yl}-4-(1H-

1,2,3,4-tetrazol-5-yl)benzamide

111

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(4,4-

difluoro-cyclohexyl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

112

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(3-methylamino-phenyl)-thiazolo[4,5-c]pyridin-2-yl]-amide

113

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(5-methyl-thiophen-2-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

114

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(5-methyl-furan-2-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

115

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

[1,3]thiazolo[4,5-c]pyridin-2-yl)carbamoyl]benzoic acid

116

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

c]pyridin-2-yl]-1H-pyrazole-4-carboxamide

117

N-{4-methoxy-7-phenyl-[1,3]thiazolo[4,5-c]pyridin-2-yl}-1H-

pyrazole-4-carboxamide

118

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-{1-[(S)-1-(tetrahydro-pyran-2-yl)methyl]-1H-pyrazol-4-yl}-

thiazolo[4,5-c]pyridin-2-yl)-amide

119

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid (4-methoxy-

7-{1-[(R)-1-(tetrahydro-pyran-2-yl)methyl]-1H-pyrazol-4-yl}-

thiazolo[4,5-c]pyridin-2-yl)-amide

121

(R)-2,7-Diaza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-

dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

122

(S)-2,7-Diaza-spiro[4.5]decane-2-carboxylic acid [7-(3,6-

dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

123

Piperidine-1,4-dicarboxylic acid 4-dimethylamide 1-[(4-

methoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide]

124

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(2-amino-

pyridin-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

125

N-[7-(3,6-Dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-4-(4-methyl-piperazine-1-carbonyl)-benzamide

126

N-[7-(3,6-Dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-N′-(2-piperidin-1-yl-ethyl)-terephthalamide

127

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(2-methylamino-pyridin-4-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

128

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(5-methyl-cyclohex-1-enyl)-thiazolo[4,5-c]pyridin-2-yl]-amide

129

N-[7-(3,6-Dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-4-(4-hydroxy-4-methyl-piperidine-1-carbonyl)-

benzamide

130

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(3-fluoro-5-

methanesulfonylamino-phenyl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-yl]-amide

131

4-(2,5-Dioxo-imidazolidin-1-yl)-piperidine-1-carboxylic acid [7-

(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-

2-yl]-amide

132

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(3-methyl-3,6-dihydro-2H-pyran-4-yl)-thiazolo[4,5-c]pyridin-2-

yl]-amide

133

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(3-trifluoromethyl-piperidin-1-yl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

134

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(3-methoxy-piperidin-1-yl)-thiazolo[4,5-c]pyridin-2-yl]-amide

135

Imidazo[1,2-a]pyridine-3-carboxylic acid [7-(3,6-dihydro-2H-

pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

136

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

(5-oxo-2,5-dihydro-1H-pyrrol-3-yl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

137

4-(2,5-Dioxo-imidazolidin-1-yl)-piperidine-1-carboxylic acid (4-

methoxy-7-phenyl-thiazolo[4,5-c]pyridin-2-yl)-amide

138

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(5-amino-

2-fluoro-pyridin-3-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

139

N-(2-Azetidin-1-yl-ethyl)-N′-[7-(3,6-dihydro-2H-pyran-4-yl)-4-

methoxy-thiazolo[4,5-c]pyridin-2-yl]-terephthalamide

140

2-Pyridin-3-yl-1H-imidazole-4-carboxylic acid [7-(3,6-dihydro-

2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

141

N-{4-methoxy-7-[3-(trifluoromethyl)phenyl]-[1,3]thiazolo[4,5-

c]pyridin-2-yl}-8-oxa-2-azaspiro[4.5]decane-2-carboxamide

142

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(5-amino-

6-fluoro-pyridin-3-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-

amide

143

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [7-(5-amino-

pyridin-3-yl)-4-methoxy-thiazolo[4,5-c]pyridin-2-yl]-amide

144

{4-[7-(3,6-Dihydro-2H-pyran-4-yl)-4-methoxy-thiazolo[4,5-

c]pyridin-2-ylcarbamoyl]-phenyl}-acetic acid

145

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

((S)-3-methyl-cyclohex-1-enyl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

146

8-Oxa-2-aza-spiro[4.5]decane-2-carboxylic acid [4-methoxy-7-

((R)-3-methyl-cyclohex-1-enyl)-thiazolo[4,5-c]pyridin-2-yl]-

amide

or a physiologically acceptable salt or stereoisomer thereof.

2. A pharmaceutical composition comprising at least one compound according to claim 1 or a physiologically acceptable salt or stereoisomer thereof, and one or more excipients and/or adjuvants.

3. The pharmaceutical composition according to claim 2 , further comprising at least one further pharmaceutically active compound.

4. A process for preparing the pharmaceutical composition according to claim 2 , comprising bringing said at least one compound or a physiologically acceptable salt or stereoisomer thereof into a dosage form together with one or more solid, liquid or semi-liquid excipients or adjuvants.

5. A method for treating rheumatoid arthritis, cancer or an infectious disease, comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition according to claim 2 .

6. A method for treating cancer, comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition according to claim 2 .

7. A method for treating cancer, which 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 or 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, comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition according to claim 2 .

8. A method for treating an infectious disease, which is

i. a virally induced infectious disease which is caused by a retrovirus, hepadnavirus, herpesvirus, flaviviridae and/or adenovirus, wherein the retrovirus is a lentivirus or oncoretrovirus, wherein the lentivirus is selected from the group consisting of HIV-1, HIV-2, FIV, BIV, SIVs, SHIV, CAEV, VMV and EIAV and the oncoretrovirus is selected from the group consisting of HTLV-I, HTLV-II and BLV, the hepadnavirus is selected from the group consisting of HBV, GSHV and WHV, the herpesivirus is selected from the group consisting of HSV I, HSV II, EBV, VZV, HCMV and HHV 8 and the flaviviridae is selected from the group consisting of HCV, West nile and Yellow Fever,

ii. a bacterial infectious disease which is caused by Gram-positive bacteria, wherein the Gram-positive bacteria is selected from the group consisting of methicillin-susceptible and methicillin-resistant staphylococci, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus , coagulase-negative staphylococci, glycopeptides-intermediate susceptible Staphylococcus aureus , penicillin-susceptible and penicillin-resistant streptococci, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus avium, Streptococcus bovis, Streptococcus lactis, Streptococcus sanguis , Streptococci Group C, Streptococci Group G, viridans streptococci, enterococci, vancomycin susceptible and vancomycin-resistant strains, Enterococcus faecalis, Enterococcus faecium, Clostridium difficile, Listeria monocytogenes, Corynebacterium jeikeium, Chlamydia spp, C. pneumoniae and Mycobacterium tuberculosis,

iii. a bacterial infectious disease which is caused by Gram-negative bacteria, wherein the Gram-negative bacteria is selected from the group consisting of the Genus Enterobacteriacae, Escherichia spp., Escherichia coli, Klebsiella spp., Enterobacter spp., Citrobacter spp., Serratia spp., Proteus spp., Providencia spp., Salmonella spp., Shigella spp., the genus Pseudomonas, P. aeruginosa, Moraxella spp., M. catarrhalis, Haemophilus spp. and Neisseria spp.,

iv. an infectious disease induced by intracellular active parasites selected from the group consisting of phylum Apicomplexa, Sarcomastigophora, Trypanosoma, Plasmodia, Leishmania, Babesia, Theileria, Cryptosporidia, Sacrocystida, Amoebia, Coccidia and Trichomonadia,

said method comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition according to claim 2 .

9. A kit comprising separate packs of

a) an effective amount of the compound according to claim 1 or a physiologically acceptable salt or stereoisomer thereof, and

b) a further pharmaceutically active compound.

Assignments (6)

Priority Claims (1)

Continuity (1)

References Cited (29)