JP2012528240A5 - - Google Patents
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- JP2012528240A5 JP2012528240A5 JP2012513256A JP2012513256A JP2012528240A5 JP 2012528240 A5 JP2012528240 A5 JP 2012528240A5 JP 2012513256 A JP2012513256 A JP 2012513256A JP 2012513256 A JP2012513256 A JP 2012513256A JP 2012528240 A5 JP2012528240 A5 JP 2012528240A5
- Authority
- JP
- Japan
- Prior art keywords
- phf
- conjugate
- gly
- cpt
- conjugate according
- Prior art date
- 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.)
- Pending
Links
- 229940127093 camptothecin Drugs 0.000 claims description 46
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 28
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 27
- 229940079593 drug Drugs 0.000 claims description 25
- 239000003814 drug Substances 0.000 claims description 25
- 125000005647 linker group Chemical group 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 20
- 125000004429 atom Chemical group 0.000 claims description 19
- 125000000217 alkyl group Chemical group 0.000 claims description 18
- 125000001142 dicarboxylic acid group Chemical group 0.000 claims description 18
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims description 16
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 14
- 150000001413 amino acids Chemical class 0.000 claims description 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims description 14
- 229930182556 Polyacetal Natural products 0.000 claims description 13
- 229920001855 polyketal Polymers 0.000 claims description 13
- 229920006324 polyoxymethylene Polymers 0.000 claims description 13
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 229940122803 Vinca alkaloid Drugs 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- PAMIQIKDUOTOBW-UHFFFAOYSA-N 1-methylpiperidine Chemical compound CN1CCCCC1 PAMIQIKDUOTOBW-UHFFFAOYSA-N 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 8
- 125000005842 heteroatom Chemical group 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 210000000214 mouth Anatomy 0.000 claims description 8
- 210000003739 neck Anatomy 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 229960001592 paclitaxel Drugs 0.000 claims description 5
- 206010003571 Astrocytoma Diseases 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 206010027406 Mesothelioma Diseases 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 206010039491 Sarcoma Diseases 0.000 claims description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 4
- 125000001931 aliphatic group Chemical group 0.000 claims description 4
- 150000003797 alkaloid derivatives Chemical class 0.000 claims description 4
- 210000000436 anus Anatomy 0.000 claims description 4
- 210000000481 breast Anatomy 0.000 claims description 4
- 210000001072 colon Anatomy 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 210000003238 esophagus Anatomy 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 210000001508 eye Anatomy 0.000 claims description 4
- 210000003128 head Anatomy 0.000 claims description 4
- 201000011066 hemangioma Diseases 0.000 claims description 4
- 210000003734 kidney Anatomy 0.000 claims description 4
- 210000000867 larynx Anatomy 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 210000004185 liver Anatomy 0.000 claims description 4
- 210000004072 lung Anatomy 0.000 claims description 4
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 150000002894 organic compounds Chemical class 0.000 claims description 4
- 210000001672 ovary Anatomy 0.000 claims description 4
- 210000000496 pancreas Anatomy 0.000 claims description 4
- 210000003800 pharynx Anatomy 0.000 claims description 4
- 239000008363 phosphate buffer Substances 0.000 claims description 4
- 210000002307 prostate Anatomy 0.000 claims description 4
- 210000000664 rectum Anatomy 0.000 claims description 4
- 210000002784 stomach Anatomy 0.000 claims description 4
- 210000001550 testis Anatomy 0.000 claims description 4
- 210000003932 urinary bladder Anatomy 0.000 claims description 4
- 210000004291 uterus Anatomy 0.000 claims description 4
- IICQZTQZQSBHBY-HWKANZROSA-N (e)-non-2-ene Chemical compound CCCCCC\C=C\C IICQZTQZQSBHBY-HWKANZROSA-N 0.000 claims description 3
- IICQZTQZQSBHBY-UHFFFAOYSA-N 2t-nonene Natural products CCCCCCC=CC IICQZTQZQSBHBY-UHFFFAOYSA-N 0.000 claims description 3
- CEVCTNCUIVEQOY-UHFFFAOYSA-N Fumagillol Natural products O1C(CC=C(C)C)C1(C)C1C(OC)C(O)CCC21CO2 CEVCTNCUIVEQOY-UHFFFAOYSA-N 0.000 claims description 2
- 150000001414 amino alcohols Chemical class 0.000 claims description 2
- 125000005365 aminothiol group Chemical class 0.000 claims description 2
- 230000001588 bifunctional effect Effects 0.000 claims description 2
- 150000004985 diamines Chemical class 0.000 claims description 2
- CEVCTNCUIVEQOY-STXHBLNNSA-N fumagillol Chemical compound C([C@@H](O)[C@H](C1[C@]2(C)[C@H](O2)CC=C(C)C)OC)C[C@@]21CO2 CEVCTNCUIVEQOY-STXHBLNNSA-N 0.000 claims description 2
- 239000000178 monomer Substances 0.000 claims description 2
- 150000003335 secondary amines Chemical class 0.000 claims description 2
- 150000003512 tertiary amines Chemical class 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 9
- 229920001307 poly(hydroxymethylethylene hydroxymethyl formal) Polymers 0.000 claims 5
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- -1 2-nonen-2-yl Chemical group 0.000 claims 1
- 229930190064 illudin Natural products 0.000 claims 1
- 238000000034 method Methods 0.000 description 10
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 description 2
- 125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 description 2
- 239000000872 buffer Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18192609P | 2009-05-28 | 2009-05-28 | |
| US61/181,926 | 2009-05-28 | ||
| PCT/US2010/036413 WO2010138719A1 (en) | 2009-05-28 | 2010-05-27 | Polyal drug conjugates comprising variable rate-releasing linkers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012528240A JP2012528240A (ja) | 2012-11-12 |
| JP2012528240A5 true JP2012528240A5 (enExample) | 2013-05-30 |
Family
ID=43220947
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012513256A Pending JP2012528240A (ja) | 2009-05-28 | 2010-05-27 | 可変速度放出リンカーを含むポリアル−薬物コンジュゲート |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8524214B2 (enExample) |
| EP (1) | EP2435053B1 (enExample) |
| JP (1) | JP2012528240A (enExample) |
| KR (1) | KR20120057588A (enExample) |
| CN (1) | CN102448469A (enExample) |
| AR (1) | AR078510A1 (enExample) |
| AU (1) | AU2010254013A1 (enExample) |
| CA (1) | CA2762877A1 (enExample) |
| IL (1) | IL216325A0 (enExample) |
| TW (1) | TW201102089A (enExample) |
| WO (1) | WO2010138719A1 (enExample) |
Families Citing this family (82)
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| CA2935077C (en) | 2013-12-27 | 2022-03-15 | Geoffrey C. Winters | Sulfonamide-containing linkage systems for drug conjugates |
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| WO2009121564A1 (en) * | 2008-03-31 | 2009-10-08 | Freie Universität Berlin | Drug conjugates with polyglycerols |
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2010
- 2010-05-27 US US12/789,047 patent/US8524214B2/en not_active Expired - Fee Related
- 2010-05-27 EP EP10781215.8A patent/EP2435053B1/en not_active Not-in-force
- 2010-05-27 AU AU2010254013A patent/AU2010254013A1/en not_active Abandoned
- 2010-05-27 WO PCT/US2010/036413 patent/WO2010138719A1/en not_active Ceased
- 2010-05-27 CA CA2762877A patent/CA2762877A1/en not_active Abandoned
- 2010-05-27 JP JP2012513256A patent/JP2012528240A/ja active Pending
- 2010-05-27 CN CN2010800236442A patent/CN102448469A/zh active Pending
- 2010-05-27 KR KR1020117031373A patent/KR20120057588A/ko not_active Withdrawn
- 2010-05-28 TW TW099117180A patent/TW201102089A/zh unknown
- 2010-05-28 AR ARP100101862A patent/AR078510A1/es not_active Application Discontinuation
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2011
- 2011-11-13 IL IL216325A patent/IL216325A0/en unknown