JP2009501800A5 - - Google Patents

Info

Publication number

JP2009501800A5

JP2009501800A5 JP2008522908A JP2008522908A JP2009501800A5 JP 2009501800 A5 JP2009501800 A5 JP 2009501800A5 JP 2008522908 A JP2008522908 A JP 2008522908A JP 2008522908 A JP2008522908 A JP 2008522908A JP 2009501800 A5 JP2009501800 A5 JP 2009501800A5

Authority

JP

Japan

Prior art keywords

drug conjugate

alkyl

formula

group

conjugate compound

Prior art date

2006-07-18

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

• Espacenet
• Global Dossier
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• 150000001875 compounds Chemical class 0.000 claims 28
• 239000003814 drug Substances 0.000 claims 27
• 229940079593 drug Drugs 0.000 claims 25
• 239000003446 ligand Substances 0.000 claims 23
• 125000000217 alkyl group Chemical group 0.000 claims 15
• 229910052739 hydrogen Inorganic materials 0.000 claims 12
• 229910052799 carbon Inorganic materials 0.000 claims 11
• 125000000623 heterocyclic group Chemical group 0.000 claims 9
• 206010028980 Neoplasm Diseases 0.000 claims 5
• 125000003118 aryl group Chemical group 0.000 claims 5
• 201000011510 cancer Diseases 0.000 claims 5
• 210000004027 cell Anatomy 0.000 claims 4
• 210000004881 tumor cell Anatomy 0.000 claims 4
• 208000023275 Autoimmune disease Diseases 0.000 claims 3
• 150000003839 salts Chemical class 0.000 claims 3
• 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 2
• AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
• 125000002947 alkylene group Chemical group 0.000 claims 2
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
• 239000003795 chemical substances by application Substances 0.000 claims 2
• 150000008134 glucuronides Chemical group 0.000 claims 2
• 230000002401 inhibitory effect Effects 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 2
• 239000000203 mixture Substances 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 239000012453 solvate Substances 0.000 claims 2
• 125000006850 spacer group Chemical group 0.000 claims 2
• 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 1
• 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 1
• 239000000427 antigen Substances 0.000 claims 1
• 102000036639 antigens Human genes 0.000 claims 1
• 108091007433 antigens Proteins 0.000 claims 1
• 239000011230 binding agent Substances 0.000 claims 1
• 229930195731 calicheamicin Natural products 0.000 claims 1
• HXCHCVDVKSCDHU-LULTVBGHSA-N calicheamicin Chemical compound C1[C@H](OC)[C@@H](NCC)CO[C@H]1O[C@H]1[C@H](O[C@@H]2C\3=C(NC(=O)OC)C(=O)C[C@](C/3=C/CSSSC)(O)C#C\C=C/C#C2)O[C@H](C)[C@@H](NO[C@@H]2O[C@H](C)[C@@H](SC(=O)C=3C(=C(OC)C(O[C@H]4[C@@H]([C@H](OC)[C@@H](O)[C@H](C)O4)O)=C(I)C=3C)OC)[C@@H](O)C2)[C@@H]1O HXCHCVDVKSCDHU-LULTVBGHSA-N 0.000 claims 1
• 125000004093 cyano group Chemical group *C#N 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 229960004679 doxorubicin Drugs 0.000 claims 1
• HKSZLNNOFSGOKW-UHFFFAOYSA-N ent-staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(C)O1 HKSZLNNOFSGOKW-UHFFFAOYSA-N 0.000 claims 1
• 230000012010 growth Effects 0.000 claims 1
• 229910052736 halogen Inorganic materials 0.000 claims 1
• 150000002367 halogens Chemical group 0.000 claims 1
• 150000002431 hydrogen Chemical group 0.000 claims 1
• 239000001257 hydrogen Substances 0.000 claims 1
• 125000005647 linker group Chemical group 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 229910052760 oxygen Inorganic materials 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 229920000642 polymer Polymers 0.000 claims 1
• SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
• HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 claims 1
• CGPUWJWCVCFERF-UHFFFAOYSA-N staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(OC)O1 CGPUWJWCVCFERF-UHFFFAOYSA-N 0.000 claims 1
• 229910052717 sulfur Inorganic materials 0.000 claims 1
• 230000004614 tumor growth Effects 0.000 claims 1
• 0 CC(C(*)C(CCC1)N1C(CC(*)C(*)N(*)C(C(*)(*)NC(C(*)N(C)*)=O)=O)=O)C(N(*)C(C*)C(**)=O)=O Chemical compound CC(C(*)C(CCC1)N1C(CC(*)C(*)N(*)C(C(*)(*)NC(C(*)N(C)*)=O)=O)=O)C(N(*)C(C*)C(**)=O)=O 0.000 description 1