JP2018531287A5 - - Google Patents

Info

Publication number

JP2018531287A5

JP2018531287A5 JP2018537732A JP2018537732A JP2018531287A5 JP 2018531287 A5 JP2018531287 A5 JP 2018531287A5 JP 2018537732 A JP2018537732 A JP 2018537732A JP 2018537732 A JP2018537732 A JP 2018537732A JP 2018531287 A5 JP2018531287 A5 JP 2018531287A5

Authority

JP

Japan

Prior art keywords

compound

nhco

formula

conh

pharmaceutically acceptable

Prior art date

2016-10-07

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

Links

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• 150000001875 compounds Chemical class 0.000 claims description 125
• 150000003839 salts Chemical class 0.000 claims description 50
• 108091008104 nucleic acid aptamers Proteins 0.000 claims description 28
• ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims description 24
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 24
• YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims description 16
• 125000006850 spacer group Chemical group 0.000 claims description 16
• YJTKZCDBKVTVBY-UHFFFAOYSA-N 1,3-Diphenylbenzene Chemical group C1=CC=CC=C1C1=CC=CC(C=2C=CC=CC=2)=C1 YJTKZCDBKVTVBY-UHFFFAOYSA-N 0.000 claims description 12
• 235000010290 biphenyl Nutrition 0.000 claims description 12
• 239000004305 biphenyl Substances 0.000 claims description 12
• 229960002685 biotin Drugs 0.000 claims description 8
• 235000020958 biotin Nutrition 0.000 claims description 8
• 239000011616 biotin Substances 0.000 claims description 8
• 238000000034 method Methods 0.000 claims description 6
• 206010028980 Neoplasm Diseases 0.000 claims description 5
• 201000011510 cancer Diseases 0.000 claims description 5
• 201000010099 disease Diseases 0.000 claims description 5
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
• 239000012678 infectious agent Substances 0.000 claims description 5
• 230000001404 mediated effect Effects 0.000 claims description 5
• 125000003277 amino group Chemical group 0.000 claims description 4
• 150000001720 carbohydrates Chemical class 0.000 claims description 4
• 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 4
• KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical compound O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims description 4
• 238000004519 manufacturing process Methods 0.000 claims description 3
• GUBGYTABKSRVRQ-WWZHPTPQSA-N 4-O-β-D-Galactopyranosyl-D-galactopyranose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-WWZHPTPQSA-N 0.000 claims description 2
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 2
• 238000006243 chemical reaction Methods 0.000 claims description 2
• 238000010511 deprotection reaction Methods 0.000 claims description 2
• 239000003814 drug Substances 0.000 claims description 2
• 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 2
• 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 2
• 230000002949 hemolytic effect Effects 0.000 claims description 2
• YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical group FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 2
• 229950006780 n-acetylglucosamine Drugs 0.000 claims description 2
• 239000008194 pharmaceutical composition Substances 0.000 claims description 2
• 108090000623 proteins and genes Proteins 0.000 claims description 2
• 102000004169 proteins and genes Human genes 0.000 claims description 2
• KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 2
• 229960002317 succinimide Drugs 0.000 claims description 2
• 230000001225 therapeutic effect Effects 0.000 claims description 2
• 238000002560 therapeutic procedure Methods 0.000 claims description 2
• 239000003183 carcinogenic agent Substances 0.000 claims 1
• 239000000126 substance Substances 0.000 description 9
• JVERXSWAVSISQC-UHFFFAOYSA-N C=C=C[IH]CC(CN)CF Chemical compound C=C=C[IH]CC(CN)CF JVERXSWAVSISQC-UHFFFAOYSA-N 0.000 description 1
• 241000191967 Staphylococcus aureus Species 0.000 description 1
• 210000004027 cell Anatomy 0.000 description 1
• MHMNJMPURVTYEJ-UHFFFAOYSA-N fluorescein-5-isothiocyanate Chemical compound O1C(=O)C2=CC(N=C=S)=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 MHMNJMPURVTYEJ-UHFFFAOYSA-N 0.000 description 1
• 239000000203 mixture Substances 0.000 description 1