JPWO2019124951A5 - - Google Patents

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Publication number

JPWO2019124951A5

JPWO2019124951A5 JP2020535043A JP2020535043A JPWO2019124951A5 JP WO2019124951 A5 JPWO2019124951 A5 JP WO2019124951A5 JP 2020535043 A JP2020535043 A JP 2020535043A JP 2020535043 A JP2020535043 A JP 2020535043A JP WO2019124951 A5 JPWO2019124951 A5 JP WO2019124951A5

Authority

JP

Japan

Prior art keywords

gpcrx

cxcr4

inhibitor

pharmaceutical composition

cancer

Prior art date

2022-09-26

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

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• 239000008194 pharmaceutical composition Substances 0.000 claims description 143
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• 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims description 108
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• 238000003556 assay Methods 0.000 claims description 64
• 230000027425 release of sequestered calcium ion into cytosol Effects 0.000 claims description 60
• -1 FC122 Chemical compound 0.000 claims description 56
• 239000000556 agonist Substances 0.000 claims description 45
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• 239000000523 sample Substances 0.000 claims description 28
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• DYLJVOXRWLXDIG-UHFFFAOYSA-N 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-3-pyrazolyl]-oxomethyl]amino]-2-adamantanecarboxylic acid Chemical compound COC1=CC=CC(OC)=C1C1=CC(C(=O)NC2(C3CC4CC(C3)CC2C4)C(O)=O)=NN1C1=CC=NC2=CC(Cl)=CC=C12 DYLJVOXRWLXDIG-UHFFFAOYSA-N 0.000 claims description 6
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• LGLVVVCSQBZONM-HCCLCSBVSA-N (2r)-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentano Chemical compound NC(N)=NCCC[C@@H](NC(=O)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(N)=O LGLVVVCSQBZONM-HCCLCSBVSA-N 0.000 claims description 4
• WZHKXNSOCOQYQX-FUAFALNISA-N (2s)-6-amino-2-[[(2r)-2-[[(2s)-2-[[(2s)-2-[[(2r)-2-[[(2s)-2-amino-3-(1h-imidazol-5-yl)propanoyl]amino]-3-(1h-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-(1h-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]hexanamide Chemical compound C([C@H](N)C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCCN)C(N)=O)C1=CN=CN1 WZHKXNSOCOQYQX-FUAFALNISA-N 0.000 claims description 4
• QYCXKYOTLRUVFA-MRVPVSSYSA-N (8R)-8-ethyl-4-methyl-2-(2,3,5-trichlorophenyl)-8,9-dihydro-7H-imidazo[2,1-f]purin-5-one Chemical compound CC[C@@H]1Cn2c(N1)c1nc(nc1n(C)c2=O)-c1cc(Cl)cc(Cl)c1Cl QYCXKYOTLRUVFA-MRVPVSSYSA-N 0.000 claims description 4
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• OPUXIXJLNLMIKY-UHFFFAOYSA-N 2-(4-bromophenyl)-4-propyl-8,9-dihydro-7H-imidazo[2,1-f]purin-5-one Chemical compound CCCn1c2nc(nc2c2NCCn2c1=O)-c1ccc(Br)cc1 OPUXIXJLNLMIKY-UHFFFAOYSA-N 0.000 claims description 4
• YSUIQYOGTINQIN-UZFYAQMZSA-N 2-amino-9-[(1S,6R,8R,9S,10R,15R,17R,18R)-8-(6-aminopurin-9-yl)-9,18-difluoro-3,12-dihydroxy-3,12-bis(sulfanylidene)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one Chemical compound NC1=NC2=C(N=CN2[C@@H]2O[C@@H]3COP(S)(=O)O[C@@H]4[C@@H](COP(S)(=O)O[C@@H]2[C@@H]3F)O[C@H]([C@H]4F)N2C=NC3=C2N=CN=C3N)C(=O)N1 YSUIQYOGTINQIN-UZFYAQMZSA-N 0.000 claims description 4
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