TW200806670A - Inhibitors of checkpoint kinases - Google Patents

Info

Publication number

TW200806670A

TW200806670A TW096113500A TW96113500A TW200806670A TW 200806670 A TW200806670 A TW 200806670A TW 096113500 A TW096113500 A TW 096113500A TW 96113500 A TW96113500 A TW 96113500A TW 200806670 A TW200806670 A TW 200806670A

Authority

TW

Taiwan

Prior art keywords

isoquinoline

triazolium

group

alkyl

ketone

Prior art date

2006-04-25

Links

• Espacenet
• Global Dossier
• Discuss

• 239000003112 inhibitor Substances 0.000 title description 67
• 108091000080 Phosphotransferase Proteins 0.000 title description 7
• 102000020233 phosphotransferase Human genes 0.000 title description 7
• 150000001875 compounds Chemical class 0.000 claims abstract description 239
• 206010028980 Neoplasm Diseases 0.000 claims abstract description 58
• 201000011510 cancer Diseases 0.000 claims abstract description 45
• 238000011282 treatment Methods 0.000 claims abstract description 45
• 125000001425 triazolyl group Chemical group 0.000 claims description 268
• OUQVKRKGTAUJQA-UHFFFAOYSA-N n-[(1-chloro-4-hydroxyisoquinolin-3-yl)carbonyl]glycine Chemical compound C1=CC=CC2=C(O)C(C(=O)NCC(=O)O)=NC(Cl)=C21 OUQVKRKGTAUJQA-UHFFFAOYSA-N 0.000 claims description 238
• -1 Ci-C10 alkyl Chemical group 0.000 claims description 143
• 125000000217 alkyl group Chemical group 0.000 claims description 126
• 125000000623 heterocyclic group Chemical group 0.000 claims description 108
• 125000003118 aryl group Chemical group 0.000 claims description 106
• 125000001424 substituent group Chemical group 0.000 claims description 78
• HKOOXMFOFWEVGF-UHFFFAOYSA-N phenylhydrazine Chemical compound NNC1=CC=CC=C1 HKOOXMFOFWEVGF-UHFFFAOYSA-N 0.000 claims description 74
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 71
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 70
• AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 70
• 125000003342 alkenyl group Chemical group 0.000 claims description 56
• OAKJQQAXSVQMHS-UHFFFAOYSA-N hydrazine group Chemical group NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 54
• 150000003839 salts Chemical class 0.000 claims description 54
• 150000002576 ketones Chemical class 0.000 claims description 44
• 125000000304 alkynyl group Chemical group 0.000 claims description 43
• 239000003814 drug Substances 0.000 claims description 43
• 229910052757 nitrogen Inorganic materials 0.000 claims description 42
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• 150000002367 halogens Chemical class 0.000 claims description 35
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 33
• GYPOFOQUZZUVQL-UHFFFAOYSA-N 2h-isoquinolin-3-one Chemical compound C1=CC=C2C=NC(O)=CC2=C1 GYPOFOQUZZUVQL-UHFFFAOYSA-N 0.000 claims description 32
• 239000007789 gas Substances 0.000 claims description 32
• 125000002950 monocyclic group Chemical group 0.000 claims description 31
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• 125000005842 heteroatom Chemical group 0.000 claims description 22
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• XBZYWSMVVKYHQN-MYPRUECHSA-N (4as,6as,6br,8ar,9r,10s,12ar,12br,14bs)-10-hydroxy-2,2,6a,6b,9,12a-hexamethyl-9-[(sulfooxy)methyl]-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-icosahydropicene-4a-carboxylic acid Chemical compound C1C[C@H](O)[C@@](C)(COS(O)(=O)=O)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C XBZYWSMVVKYHQN-MYPRUECHSA-N 0.000 claims description 5
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