JP2007529455A5 - - Google Patents
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- Publication number
- JP2007529455A5 JP2007529455A5 JP2007503276A JP2007503276A JP2007529455A5 JP 2007529455 A5 JP2007529455 A5 JP 2007529455A5 JP 2007503276 A JP2007503276 A JP 2007503276A JP 2007503276 A JP2007503276 A JP 2007503276A JP 2007529455 A5 JP2007529455 A5 JP 2007529455A5
- Authority
- JP
- Japan
- Prior art keywords
- dione
- dimethyl
- benzimidazol
- tetramethyl
- hydroxy
- 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.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- -1 1,2-Dimethyl-1H-benzimidazol-5-yl Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- IOIXMMLLEZLNPS-BIOQQELPSA-N (1s,3s,10r,11s,12s,16r)-11-hydroxy-8,8,10,12,16-pentamethyl-3-[(e)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione Chemical compound C/C([C@@H]1C[C@@H]2O[C@]2(C)CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)CCC(=O)O1)O)C)=C\C1=CSC(C)=N1 IOIXMMLLEZLNPS-BIOQQELPSA-N 0.000 claims 1
- GEYOFQZSFIWPPK-BQYTYRMFSA-N (1s,3s,10r,11s,12s,16r)-3-(1,2-dimethylbenzimidazol-5-yl)-11-hydroxy-8,8,10,12,16-pentamethyl-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC[C@@]2(C)O[C@H]2C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 GEYOFQZSFIWPPK-BQYTYRMFSA-N 0.000 claims 1
- KSVJJYLXVPYGKF-VQOFAXPZSA-N (1s,5s,6s,7r,10e,14s,16s)-14-(1,2-dimethylbenzimidazol-5-yl)-6-hydroxy-5,7,9,9-tetramethyl-13,17-dioxabicyclo[14.1.0]heptadec-10-ene-8,12-dione Chemical compound O1C(=O)\C=C\C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC[C@@H]2O[C@H]2C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 KSVJJYLXVPYGKF-VQOFAXPZSA-N 0.000 claims 1
- PIUCYHQFEORJGM-CMNJRJKDSA-N (1s,5s,6s,7r,10s,14s,16s)-14-(1,2-dimethylbenzimidazol-5-yl)-6,10-dihydroxy-5,7,9,9-tetramethyl-13,17-dioxabicyclo[14.1.0]heptadecane-8,12-dione Chemical compound O1C(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC[C@@H]2O[C@H]2C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 PIUCYHQFEORJGM-CMNJRJKDSA-N 0.000 claims 1
- PINYKHFDYGYNDE-RFPOXKJFSA-N (1s,5s,6s,7r,14s,16s)-14-(1,2-dimethylbenzimidazol-5-yl)-6-hydroxy-5,7,9,9-tetramethyl-13,17-dioxabicyclo[14.1.0]heptadecane-8,12-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC[C@@H]2O[C@H]2C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 PINYKHFDYGYNDE-RFPOXKJFSA-N 0.000 claims 1
- MNOKJZZTHUGFGO-CCEYBZCHSA-N (3e,7r,8s,9s,13e,16s)-16-(1,2-dimethylbenzimidazol-5-yl)-8-hydroxy-5,5,7,9-tetramethyl-1-oxacyclohexadeca-3,13-diene-2,6-dione Chemical compound O1C(=O)\C=C\C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C=C\C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 MNOKJZZTHUGFGO-CCEYBZCHSA-N 0.000 claims 1
- RJXSMHWBBLJKLY-WPNDJVSTSA-N (4s,7r,8s,9s,13e,16s)-16-(1,2-dimethylbenzimidazol-5-yl)-4,8-dihydroxy-5,5,7,9-tetramethyl-1-oxacyclohexadec-13-ene-2,6-dione Chemical compound O1C(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C=C\C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 RJXSMHWBBLJKLY-WPNDJVSTSA-N 0.000 claims 1
- NAVCAXWTHIGRRQ-HWDUUENNSA-N (7r,8s,9s,13e,16s)-16-(1,2-dimethylbenzimidazol-5-yl)-8-hydroxy-5,5,7,9-tetramethyl-1-oxacyclohexadec-13-ene-2,6-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C=C\C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 NAVCAXWTHIGRRQ-HWDUUENNSA-N 0.000 claims 1
- PVDJHOFZNQMBSV-GANQCTJWSA-N (7r,8s,9s,13z,16s)-16-(1,2-dimethylbenzimidazol-5-yl)-8-hydroxy-5,5,7,9,13-pentamethyl-1-oxacyclohexadec-13-ene-2,6-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C(C)=C/C[C@H]1C1=CC=C(N(C)C(C)=N2)C2=C1 PVDJHOFZNQMBSV-GANQCTJWSA-N 0.000 claims 1
- OFFMAOLMRZZNAE-CHZUWRTOSA-N (7r,8s,9s,13z,16s)-8-hydroxy-5,5,7,9,13-pentamethyl-16-[(e)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-1-oxacyclohexadec-13-ene-2,6-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C(C)=C/C[C@H]1C(\C)=C\C1=CSC(C)=N1 OFFMAOLMRZZNAE-CHZUWRTOSA-N 0.000 claims 1
- PIUCYHQFEORJGM-UHFFFAOYSA-N 14-(1,2-dimethylbenzimidazol-5-yl)-6,10-dihydroxy-5,7,9,9-tetramethyl-13,17-dioxabicyclo[14.1.0]heptadecane-8,12-dione Chemical compound O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC2OC2CC1C1=CC=C(N(C)C(C)=N2)C2=C1 PIUCYHQFEORJGM-UHFFFAOYSA-N 0.000 claims 1
- BNEVSCPIBMLZGL-UHFFFAOYSA-N 14-(1,2-dimethylbenzimidazol-5-yl)-6,10-dihydroxy-5,7,9,9-tetramethyl-13-oxabicyclo[14.1.0]heptadecane-8,12-dione Chemical compound O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC2CC2CC1C1=CC=C(N(C)C(C)=N2)C2=C1 BNEVSCPIBMLZGL-UHFFFAOYSA-N 0.000 claims 1
- PINYKHFDYGYNDE-UHFFFAOYSA-N 14-(1,2-dimethylbenzimidazol-5-yl)-6-hydroxy-5,7,9,9-tetramethyl-13,17-dioxabicyclo[14.1.0]heptadecane-8,12-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)C(C)C(O)C(C)CCCC2OC2CC1C1=CC=C(N(C)C(C)=N2)C2=C1 PINYKHFDYGYNDE-UHFFFAOYSA-N 0.000 claims 1
- RJXSMHWBBLJKLY-UHFFFAOYSA-N 16-(1,2-dimethylbenzimidazol-5-yl)-4,8-dihydroxy-5,5,7,9-tetramethyl-1-oxacyclohexadec-13-ene-2,6-dione Chemical compound O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC=CCC1C1=CC=C(N(C)C(C)=N2)C2=C1 RJXSMHWBBLJKLY-UHFFFAOYSA-N 0.000 claims 1
- NAVCAXWTHIGRRQ-UHFFFAOYSA-N 16-(1,2-dimethylbenzimidazol-5-yl)-8-hydroxy-5,5,7,9-tetramethyl-1-oxacyclohexadec-13-ene-2,6-dione Chemical compound O1C(=O)CCC(C)(C)C(=O)C(C)C(O)C(C)CCCC=CCC1C1=CC=C(N(C)C(C)=N2)C2=C1 NAVCAXWTHIGRRQ-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 238000006798 ring closing metathesis reaction Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 0 CC(*)=Cc1c[s]c(C)n1 Chemical compound CC(*)=Cc1c[s]c(C)n1 0.000 description 2
- QGRVWTDNWKSQPX-UHFFFAOYSA-N CC(C)(C)C(NC)SC=C Chemical compound CC(C)(C)C(NC)SC=C QGRVWTDNWKSQPX-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0405898.8A GB0405898D0 (en) | 2004-03-16 | 2004-03-16 | Organic compounds |
| PCT/EP2005/002756 WO2005090335A1 (en) | 2004-03-16 | 2005-03-15 | Epothilone derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007529455A JP2007529455A (ja) | 2007-10-25 |
| JP2007529455A5 true JP2007529455A5 (enExample) | 2008-05-01 |
Family
ID=32117793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007503276A Withdrawn JP2007529455A (ja) | 2004-03-16 | 2005-03-15 | エポチロン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US7825141B2 (enExample) |
| EP (3) | EP1730138A1 (enExample) |
| JP (1) | JP2007529455A (enExample) |
| KR (1) | KR20070006773A (enExample) |
| CN (2) | CN101805328A (enExample) |
| AU (1) | AU2005223325B2 (enExample) |
| BR (1) | BRPI0508874A (enExample) |
| CA (1) | CA2556915A1 (enExample) |
| GB (1) | GB0405898D0 (enExample) |
| RU (1) | RU2006136089A (enExample) |
| WO (1) | WO2005090335A1 (enExample) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102007016046A1 (de) * | 2007-03-30 | 2008-10-23 | Bayer Schering Pharma Aktiengesellschaft | Verfahren zur Herstellung von Epothilonderivaten durch selektive katalytische Epoxidierung |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1440973A3 (de) | 1995-11-17 | 2004-10-20 | Gesellschaft für biotechnologische Forschung mbH (GBF) | Epothilonderivate, Herstellung und Mittel |
| DE19751027A1 (de) | 1996-11-20 | 1998-05-28 | Degussa | Arylsubstituierte aminoacylierte Phosphonsäuren und deren Halbester |
| US6441186B1 (en) | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
| US6380394B1 (en) * | 1996-12-13 | 2002-04-30 | The Scripps Research Institute | Epothilone analogs |
| IL135590A (en) | 1997-12-04 | 2003-09-17 | Bristol Myers Squibb Co | Process for the reduction of oxiranyl epothilones to olefinic epothilones |
| FR2775187B1 (fr) | 1998-02-25 | 2003-02-21 | Novartis Ag | Utilisation de l'epothilone b pour la fabrication d'une preparation pharmaceutique antiproliferative et d'une composition comprenant l'epothilone b comme agent antiproliferatif in vivo |
| DE19856128A1 (de) | 1998-12-04 | 2000-06-15 | Volkswagen Ag | Verfahren und Einrichtung zum Lesen von Navigationsdaten |
| AU2795000A (en) * | 1998-12-22 | 2000-07-12 | Novartis Ag | Epothilone derivatives and their use as antitumor agents |
| SK287200B6 (sk) | 1999-02-22 | 2010-03-08 | Gesellschaft Fuer Biotechnologische Forschung Mbh (Gbf) | C-21 modifikované epotilóny, spôsob ich prípravy, farmaceutický prostriedok s ich obsahom a použitie |
| BR0212107A (pt) | 2001-08-23 | 2004-08-24 | Novartis Ag | Análogos da ciclopropil e da ciclobutil epotilona |
| DK1483251T3 (da) | 2002-03-12 | 2010-04-12 | Bristol Myers Squibb Co | C3-cyano-epothilon-derivater |
| AU2003266961A1 (en) | 2002-08-02 | 2004-02-25 | Novartis Ag | Epothilone derivatives |
-
2004
- 2004-03-16 GB GBGB0405898.8A patent/GB0405898D0/en not_active Ceased
-
2005
- 2005-03-15 EP EP05716085A patent/EP1730138A1/en not_active Withdrawn
- 2005-03-15 CN CN201010150615A patent/CN101805328A/zh active Pending
- 2005-03-15 EP EP10180401A patent/EP2301940A1/en not_active Withdrawn
- 2005-03-15 CA CA002556915A patent/CA2556915A1/en not_active Abandoned
- 2005-03-15 CN CN2005800069311A patent/CN1926133B/zh not_active Expired - Fee Related
- 2005-03-15 KR KR1020067018936A patent/KR20070006773A/ko not_active Withdrawn
- 2005-03-15 WO PCT/EP2005/002756 patent/WO2005090335A1/en not_active Ceased
- 2005-03-15 RU RU2006136089/04A patent/RU2006136089A/ru not_active Application Discontinuation
- 2005-03-15 JP JP2007503276A patent/JP2007529455A/ja not_active Withdrawn
- 2005-03-15 EP EP10160012A patent/EP2213670A3/en not_active Withdrawn
- 2005-03-15 BR BRPI0508874-7A patent/BRPI0508874A/pt not_active IP Right Cessation
- 2005-03-15 US US10/591,921 patent/US7825141B2/en not_active Expired - Fee Related
- 2005-03-15 AU AU2005223325A patent/AU2005223325B2/en not_active Ceased
-
2010
- 2010-09-21 US US12/886,819 patent/US20110009459A1/en not_active Abandoned
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