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US 2025/0084074 A1Published application
Substituted heterocycles as hset inhibitors
AssigneesMerck Patent GmbH, The Institute of Cancer Research, Cancer Research Horizons
InventorsHans-Peter BUCHSTALLER, Daniel KUHN, Ian COLLINS, Thomas MATTHEWS, Jan LANZ, John CALDWELL, Giampiero COLOMBANO
Life of this patent
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Abstract
The invention relates to substituted heterocycles of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
Claims21
Compound of the formula I,
- wherein
- W denotes
- R1 denotes Hal, CN, A, COOR7, CON(R7)2, COA′ or Het1,
- R2 denotes H, Hal, A′,
- R3 denotes
- R4, R8 denote independently of one another H, unbranched or branched alkyl with 1-3 C-atoms,
- R5 denotes H or one or more substituents selected from the group of Hal, A, OH, OCH3, NH2, NHCH3, N(CH3)2 and CH2CN,
- R6 denotes benzoyl, 2-isoquinolinyl or 4-quinazolinyl, which is unsubstituted or one-, two-, or threefold substituted with Hal, A, OH,
- N(R7)2, COOR7, CN, NO2 and/or or Het2,
- A denotes unbranched or branched alkyl or cycloalkyl with 1-10 C-atoms, wherein two adjacent CH— and/or CH2-groups may form a double bond and wherein one or two non-adjacent CH— and/or CH2-groups may be replaced by N-, O- and/or S-atoms and wherein 1-7 H-atoms may be replaced by F or CI,
- A′ denotes unbranched or branched alkyl with 1-4 C-atoms, wherein 1-7 H-atoms may be replaced by F or Cl,
- Het1 denotes oxadiazolyl, which is unsubstituted or substituted with unbranched or branched alkyl with 1-4 C-atoms,
- Het2 denotes oxadiazolyl, tetrazolyl, pyrazolyl or oxazolyl, which unsubstituted or substituted with unbranched or branched alkyl with 1-4 C-atoms,
- R7 denotes H or A,
- Hal denotes F, Cl, Br or I
- and physiologically acceptable salts, derivatives, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.
13 more elements
Compound selected from the group consisting of:
- 1
- Ethyl-4-methyl-2-(3-(3-
- methylbenzamido)propanamido)thiazole-5-
- carboxylate
- 2
- Ethyl-4-methyl-2-(3-(3-(pyrrolidin-1-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 3
- Ethyl-2-(3-(3-(1H-pyrazol-1-yl)benzamido)propanamido)-4-
- methylthiazole-5-carboxylate
- 4
- Ethyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 5
- Ethyl-4-methyl-2-(3-(5,6,7,8-tetrahydronaphthalene-2-
- carboxamido)propanamido)thiazole-5-carboxylate
- 6
- Ethyl-4-methyl-2-(3-(3-(oxazol-5-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 7
- Ethyl-4-methyl-2-(3-(3-
- morpholinobenzamido)propanamido)thiazole-
- 5-carboxylate
- 8
- Ethyl-(S)-2-(2-hydroxy-3-(3-
- methylbenzamido)propanamido)-4-
- methylthiazole-5-carboxylate
- 9
- Ethyl-2-[3-[(3-
- methoxycarbonylbenzoyl)amino]propanoylamino]-4-
- methyl-thiazole-5-carboxylate
- 10
- Ethyl-2-[3-[(3-fluoro-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 11
- Ethyl-2-[3-[(2-fluoro-3-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 12
- Ethyl-2-[3-[(2-chloro-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 13
- Ethyl-2-[3-[(3-chloro-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 14
- Ethyl-2-[3-[(3-methoxycarbonyl-4-methyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 15
- Ethyl-2-[3-[(3-methoxycarbonyl-5-methyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 16
- Ethyl-2-[3-[(3-methoxy-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 17
- Ethyl-2-[3-[(3-cyano-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 18
- Ethyl-2-[3-[(3-bromo-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 19
- Ethyl-2-[3-[(3-ethyl-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 20
- Ethyl-2-[3-[(3-hydroxy-5-methoxycarbonyl-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 21
- Ethyl-4-methyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]-amino]propylamino]thiazole-5-carboxylate
- 22
- Ethyl-2-[3-[[3-methoxycarbonyl-5-[(E)-
- styryl]benzoyl]amino]propanoyl-amino]-4-methyl-thiazole-5-
- carboxylate
- 23
- Ethyl-2-(3-(3-(1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-4-
- methylthiazole-5-carboxylate
- 24
- Ethyl-2-(3-(3-chloro-5-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamido)-
- propanamido)-4-methylthiazole-5-carboxylate
- 25
- Propyl-2-(3-(3-chloro-5-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamido)-
- propanamido)-4-methylthiazole-5-carboxylate
- 26
- Propyl-4-methyl-2-(3-(3-methyl-
- 5-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 27
- Propyl-1-methyl-3-(3-(3-methyl-
- 5-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-1H-pyrazole-5-carboxylate
- 28
- Propyl-2-(3-(3-cyano-5-
- (trifluoromethyl)benzamido)propanamido)-4-
- methylthiazole-5-carboxylate
- 29
- Propyl-2-(3-(3-(tert-butyl)-5-(methoxycarbonyl)benzamido)-
- propanamido)-4-methylthiazole-5-carboxylate
- 30
- Propyl-2-(3-(3-cyano-5-
- (methoxycarbonyl)benzamido)propanamido)-
- 4-methylthiazole-5-carboxylate
- 31
- N-[3-[(5-tert-butyl-4-methyl-
- thiazol-2-yl)amino]-3-oxo-propyl]-3-
- chloro-5-(5-methyl-1,2,4-oxadiazol-3-yl)benzamide
- 32
- Propyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-yl)-5-
- (trifluoromethyl)benzamido)propanamido)thiazole-
- 5-carboxylate
- 33
- Propyl-2-[3-[(3-methoxycarbonyl-5-nitro-benzoyl)amino]-
- propanoylamino]-4-methyl-thiazole-5-carboxylate
- 34
- Ethyl-4-methyl-2-(3-(3-(3-methyl-1,2,4-oxadiazol-5-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 35
- Cyclopropyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 36
- Ethyl-2-(3-(3-(5-ethyl-1,2,4-oxadiazol-
- 3-yl)benzamido)propanamido)-
- 4-methylthiazole-5-carboxylate
- 37
- Ethyl-4-methyl-2-(3-(3-(5-methyl-
- 1,3,4-oxadiazol-2-yl)benzamido)-
- propanamido)thiazole-5-carboxylate
- 38
- Ethyl-4-methyl-2-(3-(3-(2-methyl-
- 2H-tetrazol-5-yl)benzamido)-
- propanamido)thiazole-5-carboxylate
- 39
- Tert-butyl-4-methyl-2-[3-[[3-(2-
- methyltetrazol-5-yl)benzoyl]amino]-
- propanoylamino]thiazole-5-carboxylate
- 40
- Isopropyl-4-methyl-2-[3-[[3-(2-
- methyltetrazol-5-yl)benzoyl]amino]-
- propanoylamino]thiazole-5-carboxylate
- 41
- N-[3-[(5-tert-butyl-4-methyl-thiazol-
- 2-yl)amino]-3-oxo-propyl]-3-(2-
- methyltetrazol-5-yl)benzamide
- 42
- Ethyl-2-(3-(3-
- (ethoxycarbonyl)benzamido)propanamido)-4-
- methylthiazole-5-carboxylate
- 43
- Ethyl4-methyl-2-(3-(3-methyl-
- 5-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 44
- Propyl-2-(3-(3-(methoxycarbonyl)-
- 5-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-4-methylthiazole-5-carboxylate
- 45
- Ethyl-4-methyl-2-[3-[[7-(5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]propanoylamino]thiazole-5-carboxylate
- 46
- Methyl-4-methyl-2-[3-[[7-(5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]propanoylamino]thiazole-5-carboxylate
- 47
- N-(5-tert-butyl-4-methyl-thiazol-2-yl)-3-[[6-(5-methyl-1,2,4-
- oxadiazol-3-yl)quinazolin-4-yl]amino]propanamide
- 48
- Tert-butyl-4-methyl-2-((1s,3s)-3-
- ((6-(5-methyl-1,2,4-oxadiazol-3-
- yl)quinazolin-4-yl)amino)cyclobutane-1-
- carboxamido)thiazole-5-carboxylate
- 49
- Tert-butyl-4-methyl-2-((1s,3s)-
- N-methyl-3-((6-(5-methyl-1,2,4-
- oxadiazol-3-yl)quinazolin-4-yl)amino)cyclobutane-1-
- carboxamido)thiazole-5-carboxylate
- 50
- N-(5-tert-butyl-4-methyl-thiazol-2-yl)-3-[(7-cyano-1-
- isoquinolyl)amino]-propanamide
- 51
- 3-[(7-cyano-1-isoquinolyl)amino]-
- N-[4-methyl-5-[1-(trifluoromethyl)-
- cyclopropyl]thiazol-2-yl]propanamide
- 52
- 3-[[7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)-1-isoquinolyl]amino]-N-[4-
- methyl-5-[1-(trifluoromethyl)cyclopropyl]thiazol-
- 2-yl]propanamide
- 53
- N-(5-tert-butyl-4-methyl-thiazol-
- 2-yl)-3-[(7-cyano-5-fluoro-1-
- isoquinolyl)amino]propanamide
- 54
- Propyl-4-methyl-2-(3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)propanamido)thiazole-5-carboxylate
- 55
- N-(5-cyanothiazol-2-yl)-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamide
- 56
- 3-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)-N-(1-
- methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)propanamide
- 57
- 3-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)-N-(1-
- methyl-5-pentyl-1H-pyrazol-3-yl)propanamide
- 58
- N-(5-(tert-butyl)-4-methylthiazol-2-
- yl)-3-((7-(5-methyl-2H-tetrazol-2-
- yl)isoquinolin-1-yl)amino)propanamide
- 59
- N-(3-((5-(tert-butyl)-4-methylthiazol-
- 2-yl)amino)-3-oxopropyl)-3-(5-
- methyl-2H-tetrazol-2-yl)benzamide
- 60
- (S)-N-(1-((5-(tert-butyl)-4-methylthiazol-2-yl)amino)-6-
- (methylamino)-1-oxohexan-3-yl)-3-(5-methyl-2H-tetrazol-2-
- yl)benzamide
- 61
- Ethyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-yl)benzamido)-
- propanamido)thiazole-5-carboxylate
- 62
- Methyl-4-methyl-2-(3-(3-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamido)-
- propanamido)thiazole-5-carboxylate
- 63
- Propyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 64
- N-(3-((5-butyl-4-methylthiazol-2-
- yl)amino)-3-oxopropyl)-3-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamide
- 65
- Ethyl-4-methyl-2-(3-methyl-3-(3-(5-methyl-1,2,4-oxadiazol-
- 3-yl)benzamido)butanamido)thiazole-5-carboxylate
- 66
- Isopropyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)-propanamido)thiazole-5-carboxylate
- 67
- 2-methoxyethyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-
- 3-yl)benzamido)propanamido)thiazole-5-carboxylate
- 68
- Isobutyl-4-methyl-2-(3-(3-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamido)-
- propanamido)thiazole-5-carboxylate
- 69
- 4-methoxybutyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-
- 3-yl)benzamido)propanamido)thiazole-5-carboxylate
- 70
- Propyl-4-methyl-2-((2-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)ethyl)carbamoyl)thiazole-5-carboxylate
- 71
- Ethyl-1-methyl-3-((2-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)ethyl)carbamoyl)-1H-pyrazole-5-carboxylate
- 72
- Propyl-1-methyl-3-((2-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)ethyl)carbamoyl)-1H-pyrazole-5-carboxylate
- 73
- 1-methyl-3-(3-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)propanamido)-
- N-propyl-1H-pyrazole-5-carboxamide
- 74
- Propyl-4-methyl-2-(methyl(2-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)ethyl)carbamoyl)thiazole-
- 5-carboxylate
- 75
- N-(5-(tert-butyl)-4-methylthiazol-2-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 76
- N-(5-ethyl-1-methyl-1H-pyrazol-3-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 77
- N-(5-(tert-butyl)isoxazol-3-yl)-3-
- ((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamide
- 78
- N-(5-cyclopropylisoxazol-3-yl)-
- 3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamide
- 79
- N-(5-ethylisoxazol-3-yl)-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamide
- 80
- N-(5-(tert-butyl)thiazol-2-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 81
- N-(5-(tert-butyl)-4-ethylthiazol-2-yl)-
- 3-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)propanamide
- 82
- N-(5-(tert-butyl)-1-methyl-1H-
- pyrazol-3-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 83
- N-[5-(3-methoxyoxetan-3-yl)-4-
- methyl-thiazol-2-yl]-3-[[7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)-1-isoquinolyl]amino]propanamide
- 84
- 3-[[7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)-1-isoquinolyl]amino]-N-[4-
- methyl-5-(3-propoxyoxetan-3-yl)thiazol-2-yl]propanamide
- 85
- N,4-dimethyl-2-[3-[[7-(5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]propanoylamino]-
- N-propyl-thiazole-5-carboxamide
- 86
- N-[5-(cyclohexen-1-yl)thiazol-2-yl]-
- 3-[[7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)-1-isoquinolyl]amino]propanamide
- 87
- N-[5-(1-methoxycyclohexyl)thiazol-
- 2-yl]-3-[[7-(5-methyl-1,2,4-
- oxadiazol-3-yl)-1-isoquinolyl]amino]propanamide
- 88
- Ethyl-4-isopropyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]propanoylamino]thiazole-5-carboxylate
- 89
- Tertbutyl-4-methyl-2-(methyl(2-
- ((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)ethyl)carbamoyl)thiazole-
- 5-carboxylate
- 90
- Methyl-4-ethyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]propanoylamino]thiazole-5-carboxylate
- 91
- Ethyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]-
- propanoylamino]-4-(trifluoromethyl)thiazole-5-carboxylate
- 92
- Ethyl-4-ethyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]propanoylamino]thiazole-5-carboxylate
- 93
- N-[3-[[5-[(E)-2-cyclopentylvinyl]-
- 4-methyl-thiazol-2-yl]amino]-3-
- oxo-propyl]-3-(5-methyl-1,2,4-oxadiazol-3-yl)benzamide
- 94
- N-[3-[5-[(E)-3-methoxyprop-1-enyl]-
- 4-methyl-thiazol-2-yl]amino]-3-
- oxo-propyl]-3-(5-methyl-1,2,4-oxadiazol-3-yl)benzamide
- 95
- 3-(5-methyl-1,2,4-oxadiazol-3-yl)-N-[3-[4-methyl-5-(1-
- phenylvinyl)thiazol-2-yl]amino]-3-oxo-propyl]benzamide
- 96
- 3-[[7-(5-methyl-1,2,4-oxadiazol-3-
- yl)-1-isoquinolyl]amino]-N-[5-
- (1,1,2,2,2-pentafluoroethyl)thiazol-
- 2-yl]cyclobutanecarboxamide
- 97
- N-(5-bromo-4-methyl-thiazol-2-yl)-3-
- [[7-(5-methyl-1,2,4-oxadiazol-3-
- yl)-1-isoquinolyl]amino]cyclobutanecarboxamide
- 98
- (1s,3s)-N-(5-(tert-butyl)-4-methylthiazol-
- 2-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamide
- 99
- Propyl-4-methyl-2-((1s,3s)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamido)thiazole-5-carboxylate
- 100
- (1s,3s)-N-(5-(tert-butyl)isoxazol-3-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamide
- 101
- (1s,3s)-3-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)-
- N-(1-methyl-5-pentyl-1H-pyrazol-3-
- yl)cyclobutane-1-carboxamide
- 102
- (1s,3s)-N-(5-isobutyl-4-methylthiophen-
- 2-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamide
- 103
- (1s,3s)-3-((7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)isoquinolin-1-yl)amino)-
- N-(4-methyl-5-(trifluoromethyl)thiazol-2-yl)cyclobutane-1-
- carboxamide
- 104
- Tert-butyl-4-methyl-2-((1s,3s)-3-
- (3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)cyclobutane-1-carboxamido)thiazole-
- 5-carboxylate
- 105
- Tert-butyl-2-((1s,3s)-3-(3-(1,2,4-oxadiazol-3-yl)benzamido)-
- cyclobutane-1-carboxamido)-4-methylthiazole-5-carboxylate
- 106
- Tert-butyl-4-methyl-2-((1s,3s)-3-
- (3-(5-methyl-1,3,4-oxadiazol-2-
- yl)benzamido)cyclobutane-1-carboxamido)thiazole-
- 5-carboxylate
- 107
- Tert-butyl-4-methyl-2-((1s,3s)-3-(3-(2-methyl-2H-tetrazol-5-
- yl)benzamido)cyclobutane-1-carboxamido)thiazole-
- 5-carboxylate
- 108
- Tert-butyl-2-((1s,3s)-3-((7-
- chloroisoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamido)-4-methylthiazole-5-carboxylate
- 109
- Tert-butyl-4-methyl-2-((1s,3s)-3-((7-
- (trifluoromethyl)isoquinolin-1-
- yl)amino)cyclobutane-1-carboxamido)thiazole-5-carboxylate
- 110
- Tert-butyl-4-methyl-2-[[3-[[7-(5-
- methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]cyclobutanecarbonyl]amino]thiazole-
- 5-carboxylate
- 111
- Tert-butyl-4-methyl-2-[methyl-[3-[[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-
- 1-isoquinolyl]amino]cyclobutanecarbonyl]amino]thiazole-5-
- carboxylate
- 112
- Tert-butyl-4-chloro-2-[[3-[[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]cyclobutanecarbonyl]amino]thiazole-
- 5-carboxylate
- 113
- N-tert-butyl-4-chloro-2-[[3-[[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]cyclobutanecarbonyl]amino]thiazole-5-
- carboxamide
- 114
- [(1R)-2,2,2-trifluoro-1-methyl-ethyl]-
- 4-methyl-2-[[3-[[7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]cyclobutanecarbonyl]amino]-
- thiazole-5-carboxylate
- 115
- [(1S)-2,2,2-trifluoro-1-methyl-ethyl]-4-methyl-2-
- [[3-[7-(5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]cyclobutanecarbonyl]amino]-
- thiazole-5-carboxylate
- 116
- Ethyl-4-(difluoromethyl)-2-[[3-[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]cyclobutanecarbonyl]amino]thiazole-
- 5-carboxylate
- 117
- N-(5-tert-butyl-4-methyl-thiazol-2-yl)-3-[(7-methyl-1-
- isoquinolyl)amino]-cyclobutanecarboxamide
- 118
- 3-(5-methyl-1,2,4-oxadiazol-3-yl)-N-
- (3-((4-methyl-5-(3-methyl-1,2,4-
- oxadiazol-5-yl)thiazol-2-yl)amino)-3-oxopropyl)benzamide
- 119
- 3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)-N-(5-(5-
- propyl-1,2,4-oxadiazol-3-yl)thiazol-2-yl)propanamide
- 120
- Proyl-1-methyl-3-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-1H-pyrazole-5-carboxylate
- 121
- Propyl-4-methyl-2-(N-methyl-3-
- (3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 122
- Cyclopentyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 123
- Hexyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 124
- Cyclohexyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 125
- 4-aminobutyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 126
- 3-(4-methoxyphenyl)propyl-4-methyl-2-(3-(3-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamido)propanamido)thiazole-
- 5-carboxylate
- 127
- 4-(2-methoxyethoxy)butyl-4-methyl-2-(3-(3-(5-methyl-
- 1,2,4-oxadiazol-3-yl)benzamido)propanamido)thiazole-
- 5-carboxylate
- 128
- Methyl-2-methyl-5-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]propanoylamino]pyrazole-3-carboxylate
- 129
- 3-(5-methyl-1,2,4-oxadiazol-3-yl)-N-(3-((4-methyl-5-
- (pentan-2-yl)thiazol-2-yl)amino)-3-oxopropyl)benzamide
- 130
- 4-acetamidobutyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-
- oxadiazol-3-yl)benzamido)propanamido)thiazole-
- 5-carboxylate
- 131
- Propyl-1-methyl-3-(3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)propanamido)-1H-pyrazole-5-carboxylate
- 132
- Tert-butyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 133
- Ethyl-3-methyl-5-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]propanoylamino]thiophene-2-carboxylate
- 134
- Ethyl-4-methyl-2-(3-(3-(5-methyl-1,2,4-
- oxadiazol-3-yl)benzamido)-N-
- propylpropanamido)thiazole-5-carboxylate
- 135
- Ethyl-3-(3-((7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-1-
- yl)amino)propanamido)-1H-pyrazole-5-carboxylate.
- 136
- 6-hydroxyhexyl-4-methyl-2-(3-(3-
- (5-methyl-1,2,4-oxadiazol-3-yl)-5-
- (trifluoromethyl)benzamido)propanamido)thiazole-
- 5-carboxylate
- 137
- 5-butyl-4-methyl-N-(2-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)ethyl)thiazole-2-carboxamide
- 138
- Cyclopentyl-1-methyl-3-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-
- 1H-pyrazole-5-carboxylate
- 139
- 3-{[3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]formamido}-N-
- [4-methyl-5-(trifluoromethyl)-1,3-thiazol-2-yl]propenamide
- 140
- Ethyl-2-((2-(3-(5-ethyl-1,2,4-oxadiazol-3-yl)benzamido)ethyl)-
- carbamoyl)-4-methylthiazole-5-carboxylate
- 141
- Ethyl-4-methyl-2-((2-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)ethyl)carbamoyl)thiazole-5-carboxylate
- 142
- Ethyl-(R)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)butanamido)thiazole-5-carboxylate
- 143
- Ethyl-(S)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)butanamido)thiazole-5-carboxylate
- 144
- Propyl-2-(2-(4-(3-chloro-5-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)-1-methylpiperidin-4-
- yl)acetamido)-4-methylthiazole-5-
- carboxylate
- 145
- Ethyl-4-methyl-2-(2-methyl-3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 146
- 4-(3-((5-(ethoxycarbonyl)-4-methylthiazol-2-yl)amino)-1-(3-(5-
- methyl-1,2,4-oxadiazol-3-yl)benzamido)-
- 3-oxopropyl)piperidin-1-ium
- 147
- 4-(3-((5-(ethoxycarbonyl)-4-methylthiazol-2-yl)amino)-1-(3-(5-
- methyl-1,2,4-oxadiazol-3-yl)benzamido)-3-oxopropyl)-1-
- methylpiperidin-1-ium
- 148
- Ethyl-2-[[(3R)-4-amino-3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]butanoyl]amino]-4-
- methyl-thiazole-5-carboxylate
- 149
- Ethyl-4-methyl-2-[[(3S,4R)-4-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]pyrrolidine-3-carbonyl]amino]thiazole-5-
- carboxylate;
- 150
- Ethyl-(S)-2-(6-amino-3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)hexanamido)-4-methylthiazole-5-carboxylate
- 151
- Propyl-(S)-2-(6-amino-3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)hexanamido)-4-methylthiazole-5-carboxylate
- 152
- Propyl-4-methyl-2-[[(3S)-6-
- (methylamino)-3-[[3-(5-methyl-1,2,4-
- oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]thiazole-
- 5-carboxylate
- 153
- Propyl-(R)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)-6-(methylamino)hexanamido)thiazole-
- 5-carboxylate
- 154
- Tertbutyl-4-methyl-2-[[(3S)-6-
- (methylamino)-3-[[3-(5-methyl-1,2,4-
- oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]thiazole-
- 5-carboxylate
- 155
- Cyclopentyl-S)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)-6-(methylamino)hexanamido)thiazole-
- 5-carboxylate
- 156
- Isopropyl-(S)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)-6-(methylamino)hexanamido)thiazole-
- 5-carboxylate
- 157
- (S)-N-(1-((5-(tert-butyl)-4-methylthiazol-2-yl)amino)-6-
- (methylamino)-1-oxohexan-3-yl)-3-chloro-5-
- (5-methyl-1,2,4-oxadiazol-3-yl)benzamide
- 158
- Propyl-(S)-2-(6-(dimethylamino)-3-(3-
- (5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)hexanamido)-4-methylthiazole-5-carboxylate
- 159
- Propyl-(S)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)-6-morpholinohexanamido)thiazole-
- 5-carboxylate
- 160
- Propyl-(S)-2-(2-amino-3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-4-methylthiazole-5-carboxylate
- 161
- (S)-N-(2-amino-3-((5-(tert-butyl)-4-ethylthiazol-2-yl)amino)-3-
- oxopropyl)-3-(5-methyl-1,2,4-oxadiazol-3-yl)benzamide
- 162
- Propyl-(S)-2-(5-(dimethylamino)-3-
- (3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)pentanamido)-4-methylthiazole-5-carboxylate
- 163
- Propyl-(S)-2-(6-amino-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)hexanamido)-4-methylthiazole-5-
- carboxylate
- 164
- (S)-6-amino-N-(5-(tert-butyl)-4-
- methylthiazol-2-yl)-3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-yl)amino)hexanamide
- 165
- Cyclopentyl-(S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)-6-
- (methylamino)hexanamido)thiazole-5-
- carboxylate
- 166
- 1,3-difluoropropan-2-yl (S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)-6-(methylamino)-
- hexanamido)thiazole-5-carboxylate
- 167
- Isopropyl-(S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)-6-
- (methylamino)hexanamido)thiazole-5-
- carboxylate
- 168
- Tertbutyl-(S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)-6-
- (methylamino)hexanamido)thiazole-5-
- carboxylate
- 169
- (S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-
- yl)amino)-6-(methylamino)hexanamido)thiazole-5-carboxylic
- 170
- 3,3-difluorocyclopentyl-4-methyl-
- 2-((S)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)-
- 6-(methylamino)hexanamido)-
- thiazole-5-carboxylate
- 171
- (S)-N-(5-(tert-butyl)-4-methylthiazol-
- 2-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)-
- 6-(methylamino)hexanamide
- 172
- Propyl-(S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)-6-
- (methylamino)hexanamido)thiazole-5-
- carboxylate
- 173
- Propyl-(R)-2-(2-amino-3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-4-methylthiazole-5-carboxylate
- 174
- Propyl-(S)-2-(2-amino-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 175
- Propyl-(S)-2-(2-(dimethylamino)-3-
- (3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)-4-methylthiazole-5-carboxylate
- 176
- Propyl-(R)-2-(2-hydroxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 177
- Tertbutyl-(R)-2-(2-hydroxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 178
- Propyl-(S)-2-(2-hydroxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 179
- (S)-2-hydroxy-N-(5-isobutyl-4-
- methylthiazol-2-yl)-3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 180
- Tertbutyl-(S)-2-(2-hydroxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 181
- Tertbutyl-(S)-2-(2-hydroxy-3-((7-(1-methyl-1H-pyrazol-4-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 182
- (S)-2-hydroxy-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-
- yl)amino)-N-(1-methyl-5-(5-propyl-
- 1,2,4-oxadiazol-3-yl)-1H-pyrazol-
- 3-yl)propanamide
- 183
- (S)-2-hydroxy-N-(1-methyl-5-(5-
- propyl-1,2,4-oxadiazol-3-yl)-1H-
- pyrazol-3-yl)-3-((7-methylisoquinolin-
- 1-yl)amino)propanamide
- 184
- Tertbutyl-(R)-2-(2-hydroxy-3-((7-methylisoquinolin-1-
- yl)amino)propanamido)-4-methylthiazole-5-carboxylate
- 185
- Tertbutyl-(S)-2-(2-hydroxy-3-((7-methylisoquinolin-1-
- yl)amino)propanamido)-4-methylthiazole-5-carboxylate
- 186
- Propyl(S)-2-(2-methoxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamido)-4-methylthiazole-5-
- carboxylate
- 187
- (S)-N-(5-(tert-butyl)-4-methylthiazol-
- 2-yl)-2-hydroxy-3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 188
- (S)-2-hydroxy-3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-
- yl)amino)-N-(1-methyl-5-pentyl-1H-pyrazol-
- 3-yl)propanamide
- 189
- (R)-2-hydroxy-3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-
- yl)amino)-N-(1-methyl-5-pentyl-1H-pyrazol-
- 3-yl)propanamide
- 190
- (R)-N-(5-(tert-butyl)-4-methylthiazol-2-yl)-
- 2-hydroxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)propanamide
- 191
- (R)-2-hydroxy-N-(5-isobutyl-4-
- methylthiazol-2-yl)-3-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-yl)amino)propanamide
- 192
- (R)-2-hydroxy-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-
- yl)amino)-N-(4-methyl-5-(1-
- (trifluoromethyl)cyclopropyl)thiazol-2-
- yl)propanamide
- 193
- Tertbutyl-2-[(3S)-4-cyano-3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 194
- Tertbutyl-2-[(3R)-4-cyano-3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 195
- Propan-2-yl-2-[(3S)-4-cyano-3-{[3-(5-methyl-1,2,4-
- oxadiazol-3-yl)phenyl]formamido}butanamido]-4-methyl-
- 1,3-thiazole-5-carboxylate
- 196
- Propan-2-yl-2-[(3R)-4-cyano-3-{[3-(5-methyl-1,2,4-
- oxadiazol-3-yl)phenyl]formamido}butanamido]-4-methyl-
- 1,3-thiazole-5-carboxylate
- 197
- Methyl-2-[(3S)-4-cyano-3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 198
- Methyl-2-[(3R)-4-cyano-3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 199
- Propan-2-yl-2-[(3S)-4-cyano-N-methyl-3-{[3-(5-methyl-1,2,4-
- oxadiazol-3-yl)phenyl]formamido}butanamido]-
- 4-methyl-1,3-thiazole-5-carboxylate
- 200
- Propan-2-yl-2-[(3R)-4-cyano-N-methyl-3-{[3-(5-methyl-
- 1,2,4-oxadiazol-3-yl)phenyl]formamido}butanamido]-
- 4-methyl-1,3-thiazole-5-carboxylate
- 201
- Tertbutyl-2-[(3S)-4-cyano-3-{[3-(1-
- methyl-1H-pyrazol-4-yl)phenyl]-
- formamido}butanamido]-4-methyl-
- 1,3-thiazole-5-carboxylate
- 202
- Tertbutyl-2-[(3R)-4-cyano-3-{[3-(1-methyl-1H-
- pyrazol-4-yl)phenyl]-formamido}butanamido]-4-
- methyl-1,3-thiazole-5-carboxylate
- 203
- Propan-2-yl-2-[(3S)-4-cyano-3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 204
- Propan-2-yl-2-[(3R)-4-cyano-3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 205
- Propan-2-yl-2-[(3S)-4-cyano-N-methyl-
- 3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 206
- Propan-2-yl-2-[(3R)-4-cyano-N-methyl-
- 3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}butanamido]-4-methyl-1,3-thiazole-5-
- carboxylate
- 207
- Propan-2-yl-2-[(3S)-4-cyano-3-[(3-cyanophenyl)formamido]-
- butanamido]-4-methyl-1,3-thiazole-5-carboxylate
- 208
- Propan-2-yl-2-[(3S)-4-cyano-3-[(7-cyanoisoquinolin-1-
- yl)amino]butanamido]-4-methyl-1,3-thiazole-5-carboxylate
- 209
- Propan-2-yl-2-[(3R)-4-cyano-3-[(7-cyanoisoquinolin-1-
- yl)amino]butanamido]-4-methyl-1,3-thiazole-5-carboxylate
- 210
- Propan-2-yl-2-[(3S)-4-cyano-3-{[7-(1-methyl-1H-pyrazol-4-
- yl)isoquinolin-1-yl]amino}butanamido]-
- 4-methyl-1,3-thiazole-5-carboxylate
- 211
- Tertbutyl-2-[(3S)-4-cyano-3-{[6-(1-
- methyl-1H-pyrazol-4-yl)pyridin-2-
- yl]formamido}butanamido]-4-methyl-
- 1,3-thiazole-5-carboxylate
- 212
- Tertbutyl-2-[(3R)-4-cyano-3-{[6-(1-
- methyl-1H-pyrazol-4-yl)pyridin-2-
- yl]formamido}butanamido]-4-methyl-
- 1,3-thiazole-5-carboxylate
- 213
- Propan-2-yl-2-[(3S)-4-cyano-3-{[6-(1-methyl-1H-pyrazol-4-
- yl)pyridin-2-yl]formamido}butanamido]-4-
- methyl-1,3-thiazole-5-carboxylate
- 214
- Propan-2-yl-2-[(3R)-4-cyano-3-{[6-(1-methyl-1H-pyrazol-4-
- yl)pyridin-2-yl]formamido}butanamido]-4-methyl-
- 1,3-thiazole-5-carboxylate
- 215
- Ethyl-4-methyl-2-(3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}pentanamido)-
- 1,3-thiazole-5-carboxylate
- 216
- (3R)-4-{[5-(methoxycarbonyl)-4-
- methyl-1,3-thiazol-2-yl]carbamoyl}-
- 3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}butanoic
- 217
- (3S)-4-{[5-(methoxycarbonyl)-4-methyl-1,3-thiazol-2-
- yl](methyl)carbamoyl}-3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}butanoic
- 218
- Tertbutyl-2-((1s,3s)-N-ethyl-3-
- ((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)cyclobutanecarboxamido)-
- 4-methylthiazole-5-carboxylate
- 219
- Ethyl-4-methyl-2-(N-methyl-3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)propanamido)thiazole-5-carboxylate
- 220
- Propyl-4-methyl-2-(((1s,3s)-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)cyclobutyl)carbamoyl)thiazole-5-
- carboxylate
- 221
- (1r,3r)-N-(5-(tert-butyl)-4-methylthiazol-2-yl)-
- 1-hydroxy-3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)cyclobutane-1-
- carboxamide
- 222
- Tertbutyl-2-((1s,3s)-1-fluoro-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamido)-4-methylthiazole-5-carboxylate
- 223
- Tertbutyl-2-((1r,3r)-1-fluoro-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-
- 1-carboxamido)-4-methylthiazole-5-carboxylate
- 224
- Tertbutyl-4-methyl-2-((1s,3s)-1-methyl-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)cyclobutane-1-
- carboxamido)thiazole-5-carboxylate
- 225
- Tertbutyl-4-methyl-2-[[(3R)-3-[[7-(5-
- methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]pyrrolidine-1-carbonyl]amino]thiazole-5-
- carboxylate
- 226
- Tertbutyl-4-methyl-2-[[(3S)-3-[[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]pyrrolidine-1-carbonyl]amino]thiazole-5-
- carboxylate
- 227
- Tertbutyl-4-methyl-2-[methyl-[(3S)-
- 3-[[7-(5-methyl-1,2,4-oxadiazol-
- 3-yl)-1-isoquinolyl]amino]pyrrolidine-
- 1-carbonyl]amino]thiazole-5-
- carboxylate
- 228
- Tertbutyl-4-methyl-2-[[3-[[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]azetidine-1-carbonyl]amino]thiazole-
- 5-carboxylate
- 229
- Tertbutyl-4-methyl-2-[methyl-[3-[[3-
- (5-methyl-1,2,4-oxadiazol-3-
- yl)benzoyl]amino]azetidine-1-carbonyl]amino]thiazole-
- 5-carboxylate
- 230
- Tertbutyl-4-methyl-2-[[3-[[7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)-1-isoquinolyl]amino]azetidine-
- 1-carbonyl]amino]thiazole-5-carboxylate
- 231
- Tertbutyl-4-methyl-2-[methyl-[3-[[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-
- 1-isoquinolyl]aminoJazetidine-1-carbonyl]amino]thiazole-5-
- carboxylate
- 232
- N-(5-(tert-butyl)-4-methylthiazol-2-yl)-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)azetidine-
- 1-carboxamide
- 233
- Propyl-2-(3-(3-chloro-5-(5-methyl-1,2,4-
- oxadiazol-3-yl)benzamido)-
- N-methylpropanamido)-4-methylthiazole-5-carboxylate
- 234
- Propyl-4-methyl-2-((2S,4S)-1-methyl-
- 4-(3-(5-methyl-1,2,4-oxadiazol-
- 3-yl)benzamido)pyrrolidine-2-carboxamido)thiazole-
- 5-carboxylate.
- 235
- Propyl-4-methyl-2-((2R,4R)-1-methyl-
- 4-(3-(5-methyl-1,2,4-oxadiazol-
- 3-yl)benzamido)pyrrolidine-2-carboxamido)thiazole-
- 5-carboxylate
- 236
- (2S,4S)-N-(5-(tert-butyl)-4-methylthiazol-2-yl)-1-methyl-
- 4-((7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)pyrrolidine-2-carboxamide
- 237
- Propyl-4-methyl-2-((2S,4S)-1-methyl-4-((7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-yl)amino)pyrrolidine-
- 2-carboxamido)thiazole-5-carboxylate
- 238
- (2S,4S)-1-methyl-4-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)-N-(1-methyl-5-pentyl-1H-
- pyrazol-3-yl)pyrrolidine-2-carboxamide
- 239
- Propyl-4-methyl-2-((2S,4S)-4-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)pyrrolidine-
- 2-carboxamido)thiazole-5-carboxylate
- 240
- Propyl-(S)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)pyrrolidine-1-carbonyl)thiazole-5-carboxylate
- 241
- Propyl-(R)-4-methyl-2-(3-(3-(5-methyl-1,2,4-oxadiazol-3-
- yl)benzamido)pyrrolidine-1-carbonyl)thiazole-5-carboxylate
- 242
- Propyl-4-methyl-2-[(3S)-3-[[3-(2-methyltetrazol-5-
- yl)benzoyl]amino]pyrrolidine-1-carbonyl]thiazole-
- 5-carboxylate
- 243
- Propyl-(S)-4-methyl-2-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidine-1-carbonyl)thiazole-5-
- carboxylate
- 244
- Propyl-(R)-4-methyl-2-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidine-1-carbonyl)thiazole-5-
- carboxylate
- 245
- Propyl-(S)-1-methyl-3-(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidine-1-carbonyl)-
- 1H-pyrazole-5-carboxylate
- 246
- (S)-(5-(tert-butyl)-4-methylthiazol-2-yl)(3-
- ((7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)pyrrolidin-1-yl)methanone
- 247
- (S)-(5-cyclopropyl-1-methyl-1H-pyrazol-
- 3-yl)(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidin-1-yl)methanone
- 248
- (S)-(3-((7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-1-
- yl)amino)pyrrolidin-1-yl)(1-methyl-5-phenyl-1H-pyrazol-3-
- yl)methanone
- 249
- (S)-(5-isopropyl-1-methyl-1H-pyrazol-3-yl)(3-
- ((7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl)amino)pyrrolidin-1-yl)methanone
- 250
- S)-(1H-imidazol-5-yl)(3-((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidin-1-yl)methanone
- 251
- (5-methylisoxazol-3-yl)-[(3S)-3-[[7-
- (5-methyl-1,2,4-oxadiazol-3-yl)-1-
- isoquinolyl]amino]pyrrolidin-1-yl]methanone
- 252
- (1-Tert-butylpyrazol-4-yl)-[(3S)-3-
- [[7-(5-methyl-1,2,4-oxadiazol-3-
- yl)-1-isoquinolyl]amino]pyrrolidin-1-yl]methanone
- 253
- (S)-(5-isopropyl-1H-pyrazol-3-yl)(3-
- ((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidin-1-yl)methanone
- 254
- (S)-(5-(tert-butyl)-1H-pyrazol-3-yl)(3-
- ((7-(5-methyl-1,2,4-oxadiazol-3-
- yl)isoquinolin-1-yl)amino)pyrrolidin-1-yl)methanone
- 255
- Propyl-4-methyl-2-((2S,3R)-2-methyl-3-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)pyrrolidine-1-
- carbonyl)thiazole-5-carboxylate
- 256
- Tertbutyl-2-((3R,4R)-3-fluoro-4-((7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-yl)amino)pyrrolidine-1-
- carbonyl)-4-methylthiazole-5-carboxylate
- 257
- Propyl-2-methyl-4-(3-{[7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl]amino}propanamido)-1H-imidazole-1-carboxylate
- 258
- Propan-2-yl-2-methyl-4-(3-{[7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-
- yl]amino}propanamido)-1H-imidazole-1-carboxylate
- 259
- Ethyl-2-methyl-4-(3-{[7-(5-methyl-
- 1,2,4-oxadiazol-3-yl)isoquinolin-1-
- yl]amino}propanamido)-1H-imidazole-1-carboxylate
- 260
- Propyl-4-(3-{[7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl]amino}propanamido)-1H-imidazole-1-carboxylate
- 261
- Ethyl-2-methyl-4-(3-{[7-(1-methyl-
- 1H-pyrazol-4-yl)isoquinolin-1-
- yl]amino}propanamido)-1H-imidazole-1-carboxylate
- 262
- Propyl-2-methyl-4-(3-{[7-(1-methyl-
- 1H-pyrazol-4-yl)isoquinolin-1-
- yl]amino}propanamido)-1H-imidazole-1-carboxylate
- 263
- Propyl-2-methyl-4-(3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}propanamido)-
- 1H-imidazole-1-carboxylate
- 264
- Propan-2-yl-2-methyl-4-(3-{[3-(5-methyl-1,2,4-
- oxadiazol-3-yl)phenyl]formamido}propanamido)-
- 1H-imidazole-1-carboxylate
- 265
- Ethyl-2-methyl-4-(3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}propanamido)-
- 1H-imidazole-1-carboxylate
- 266
- Propyl-4-(3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}propanamido)-
- 1H-imidazole-1-carboxylate
- 267
- Propyl-4-[(2S)-2-hydroxy-3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}propanamido]-2-methyl-
- 1H-imidazole-1-carboxylate
- 268
- Propyl-4-[(2R)-2-hydroxy-3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}propanamido]-2-methyl-
- 1H-imidazole-1-carboxylate
- 269
- Propan-2-yl-4-[(2S)-2-hydroxy-3-{[3-(1-methyl-1H-
- pyrazol-4-yl)phenyl]formamido}propanamido]-2-
- methyl-1H-imidazole-1-carboxylate
- 270
- Propan-2-yl4-[(2R)-2-hydroxy-3-{[3-(1-methyl-1H-
- pyrazol-4-yl)phenyl]formamido}propanamido]-2-
- methyl-1H-imidazole-1-carboxylate
- 271
- Ethyl-4-[(2S)-2-hydroxy-3-{[3-(1-methyl-1H-pyrazol-4-
- yl)phenyl]formamido}propanamido]-2-methyl-
- 1H-imidazole-1-carboxylate
- 272
- Tertbutyl-4-(3-{[7-(5-methyl-1,2,4-
- oxadiazol-3-yl)isoquinolin-1-
- yl]amino}propanamido)-1H-pyrazole-1-carboxylate
- 273
- Propyl-4-(3-{[7-(5-methyl-1,2,4-oxadiazol-3-yl)isoquinolin-
- 1-yl]amino}propanamido)-1H-pyrazole-1-carboxylate
- 274
- Tertbutyl-4-(3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}propanamido)-
- 1H-pyrazole-1-carboxylate
- 275
- Propyl-4-(3-{[3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}propanamido)-1H-pyrazole-
- 1-carboxylate
- 276
- Propyl-4-methyl-2-(3-{[6-(5-methyl-
- 1,2,4-oxadiazol-3-yl)pyridin-2-
- yl]formamido}propanamido)-1,3-thiazole-5-carboxylate
- 277
- Tertbuyl-4-methyl-2-(3-{[6-(5-methyl-
- 1,2,4-oxadiazol-3-yl)pyridin-2-
- yl]formamido}propanamido)-1,3-thiazole-5-carboxylate
- 278
- Propan-2-yl-4-methyl-2-(3-{[6-(5-methyl-1,2,4-oxadiazol-3-
- yl)pyridin-2-yl]formamido}propanamido)-
- 1,3-thiazole-5-carboxylate
- 279
- Tertbutyl-2-(3-{[2-fluoro-3-(5-methyl-1,2,4-oxadiazol-3-
- yl)phenyl]formamido}propanamido)-4-methyl-1,3-thiazole-5-
- carboxylate
- 280
- Propyl-4-methyl-2-[3-[(7-methyl-1-
- isoquinolyl)amino]propanoyl-
- amino]thiazole-5-carboxylate
- and physiologically acceptable salts, derivatives, solvates, prodrugs and stereoisomers thereof, including mixtures thereof in all ratios.
1,096 more elements
(canceled)
Dependencies are inferred from the claim text.