JP2005527576A5 - - Google Patents
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- Publication number
- JP2005527576A5 JP2005527576A5 JP2003581776A JP2003581776A JP2005527576A5 JP 2005527576 A5 JP2005527576 A5 JP 2005527576A5 JP 2003581776 A JP2003581776 A JP 2003581776A JP 2003581776 A JP2003581776 A JP 2003581776A JP 2005527576 A5 JP2005527576 A5 JP 2005527576A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- pharmaceutically acceptable
- group
- compound
- 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- Withdrawn
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- 229930013356 epothilone Natural products 0.000 claims 24
- -1 epothilone compound Chemical class 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000000547 substituted alkyl group Chemical group 0.000 claims 20
- 239000002253 acid Substances 0.000 claims 14
- 230000003472 neutralizing effect Effects 0.000 claims 14
- 239000000872 buffer Substances 0.000 claims 13
- 239000007788 liquid Substances 0.000 claims 12
- 239000006186 oral dosage form Substances 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 125000002252 acyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000003107 substituted aryl group Chemical group 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 7
- 229940002612 prodrug Drugs 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 2
- 230000015556 catabolic process Effects 0.000 claims 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 2
- 238000006731 degradation reaction Methods 0.000 claims 2
- 150000002118 epoxides Chemical class 0.000 claims 2
- 125000003147 glycosyl group Chemical group 0.000 claims 2
- 229960004543 anhydrous citric acid Drugs 0.000 claims 1
- 229940075564 anhydrous dibasic sodium phosphate Drugs 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 claims 1
- 150000003883 epothilone derivatives Chemical class 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- JCBJVAJGLKENNC-UHFFFAOYSA-N potassium;ethoxymethanedithioic acid Chemical compound [K+].CCOC(S)=S JCBJVAJGLKENNC-UHFFFAOYSA-N 0.000 claims 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims 1
- 229960000999 sodium citrate dihydrate Drugs 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- 0 *c1ncc[s]1 Chemical compound *c1ncc[s]1 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37010402P | 2002-04-04 | 2002-04-04 | |
| PCT/US2003/009984 WO2003084536A1 (en) | 2002-04-04 | 2003-04-01 | Oral administration of epothilones |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005527576A JP2005527576A (ja) | 2005-09-15 |
| JP2005527576A5 true JP2005527576A5 (https=) | 2006-05-25 |
Family
ID=28792029
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003581776A Withdrawn JP2005527576A (ja) | 2002-04-04 | 2003-04-01 | エポチロン化合物の経口投与 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6936628B2 (https=) |
| EP (1) | EP1492529A1 (https=) |
| JP (1) | JP2005527576A (https=) |
| AU (1) | AU2003226189A1 (https=) |
| IS (1) | IS7481A (https=) |
| NO (1) | NO20044452L (https=) |
| PL (1) | PL372773A1 (https=) |
| TW (1) | TW200403994A (https=) |
| WO (1) | WO2003084536A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999001124A1 (en) | 1996-12-03 | 1999-01-14 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US6780620B1 (en) * | 1998-12-23 | 2004-08-24 | Bristol-Myers Squibb Company | Microbial transformation method for the preparation of an epothilone |
| US8618085B2 (en) * | 2000-04-28 | 2013-12-31 | Koasn Biosciences Incorporated | Therapeutic formulations of desoxyepothilones |
| JP4808960B2 (ja) | 2002-05-14 | 2011-11-02 | エフ エム シー コーポレーション | 微結晶質セルロース組成物 |
| TW200400191A (en) * | 2002-05-15 | 2004-01-01 | Bristol Myers Squibb Co | Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives |
| US20050171167A1 (en) * | 2003-11-04 | 2005-08-04 | Haby Thomas A. | Process and formulation containing epothilones and analogs thereof |
| FR2878443B1 (fr) * | 2004-08-03 | 2009-01-16 | Promindus Actions Promotionnel | Composition pharmaceutique, destinee a l'administration par voie orale de principe(s) actif(s) fortement gastro-labile(s et sa preparation |
| AR052142A1 (es) * | 2004-11-18 | 2007-03-07 | Bristol Myers Squibb Co | Perla recubierta enterica que comprende ixabepilona, y preparacion y administracion de la misma |
| EP1824458A1 (en) * | 2004-11-18 | 2007-08-29 | Bristol-Myers Squibb Company | Enteric coated bead comprising epothilone or an epothilone analog, and preparation and administration thereof |
| EP1674098A1 (en) * | 2004-12-23 | 2006-06-28 | Schering Aktiengesellschaft | Stable and tolerable parental formulations of highly reactive organic drug substances with low or no solubility in water |
| US20060255258A1 (en) * | 2005-04-11 | 2006-11-16 | Yongdong Wang | Chromatographic and mass spectral date analysis |
| US7879382B2 (en) * | 2005-09-30 | 2011-02-01 | Fmc Corporation | Stabilizers and compositions and products comprising same |
| WO2008057266A2 (en) * | 2006-10-27 | 2008-05-15 | Fmc Corporation | Dry granulation binders, products, and use thereof |
| EP2009114A1 (en) * | 2007-06-29 | 2008-12-31 | Bayer Schering Pharma Aktiengesellschaft | Methods, kits, and compounds for determining responsiveness to treatment of a pathological disorder by epothilones |
| TWI461213B (zh) | 2009-11-05 | 2014-11-21 | Fmc Corp | 作為藥物賦形劑之微晶纖維素及磷酸鈣之組合物 |
| TW201129386A (en) | 2009-11-05 | 2011-09-01 | Fmc Corp | Microcrystalline cellulose and calcium phosphate compositions useful as pharmaceutical excipients |
| CN102665764A (zh) * | 2009-12-22 | 2012-09-12 | Fmc有限公司 | 可用作可再压实药物赋形剂的微晶纤维素和碳酸钙组合物 |
| AU2011255647A1 (en) | 2010-05-18 | 2012-11-15 | Cerulean Pharma Inc. | Compositions and methods for treatment of autoimmune and other diseases |
| BR112014007366B1 (pt) | 2011-10-05 | 2020-09-15 | Dupont Nutrition Usa, Inc | Processo para fabricar uma composição estabilizadora compreendendo extrusão em duas etapas, composição estabilizadora de celulose microcristalina e produto alimentício comestível e suspensão industrial compreendendo a mesma |
| ES2657648T3 (es) | 2011-10-05 | 2018-03-06 | Fmc Corporation | Composición estabilizadora de celulosa microcristalina y carboximetilcelulosa co-reducida, método para elaborarla y usos |
| EP2787837B1 (en) | 2011-12-09 | 2017-03-15 | FMC Corporation | Co-attrited stabilizer composition |
| GB2595203A (en) | 2020-03-03 | 2021-11-24 | Alkaloid Ad Skopje | Formulation |
| CZ2020287A3 (cs) | 2020-05-20 | 2021-12-01 | Mendelova Univerzita V Brně | Způsob přípravy nanokompozitního materiálu na bázi redukovaného grafen oxidu, dusičnanu stříbrného a octanu měďnatého, nanokompozitní materiál, přípravek jej obsahující a jeho použití |
| CN114727995B (zh) * | 2020-09-02 | 2024-06-11 | 北京华昊中天生物医药股份有限公司 | 优替德隆的固体口服制剂 |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4138042C2 (de) | 1991-11-19 | 1993-10-14 | Biotechnolog Forschung Gmbh | Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel |
| US5671397A (en) * | 1993-12-27 | 1997-09-23 | At&T Global Information Solutions Company | Sea-of-cells array of transistors |
| DE19639456A1 (de) | 1996-09-25 | 1998-03-26 | Biotechnolog Forschung Gmbh | Epothilon-Derivate, Herstellung und Mittel |
| DE19542986A1 (de) | 1995-11-17 | 1997-05-22 | Biotechnolog Forschung Gmbh | Epothilon-Derivate und deren Verwendung |
| DK1186606T4 (da) | 1995-11-17 | 2011-12-05 | Biotechnolog Forschung Gmbh | Epothilonderivater, deres fremstilling og anvendelse |
| DE19645361A1 (de) | 1996-08-30 | 1998-04-30 | Ciba Geigy Ag | Zwischenprodukte innerhalb der Totalsynthese von Epothilon A und B, Teil II |
| EP0923583A1 (de) | 1996-08-30 | 1999-06-23 | Novartis AG | Verfahren zur herstellung von epothilonen und zwischenprodukte innerhalb des verfahrens |
| DE19645362A1 (de) | 1996-10-28 | 1998-04-30 | Ciba Geigy Ag | Verfahren zur Herstellung von Epothilon A und B und Derivaten |
| DK1367057T3 (da) | 1996-11-18 | 2009-01-19 | Biotechnolog Forschung Gmbh | Epothiloner E og F |
| US6515016B2 (en) | 1996-12-02 | 2003-02-04 | Angiotech Pharmaceuticals, Inc. | Composition and methods of paclitaxel for treating psoriasis |
| WO1999001124A1 (en) | 1996-12-03 | 1999-01-14 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US6204388B1 (en) | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| 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 |
| DE19701758A1 (de) | 1997-01-20 | 1998-07-23 | Wessjohann Ludgar A Dr | Epothilone-Synthesebausteine |
| PT975638E (pt) | 1997-02-25 | 2002-12-31 | Biotechnolog Forschung Mbh Gbf | Epothilons modificados nas cadeias laterais |
| DE19713970B4 (de) | 1997-04-04 | 2006-08-31 | R&D-Biopharmaceuticals Gmbh | Epothilone-Synthesebausteine II - Prenylderivate |
| WO1998047891A1 (de) | 1997-04-18 | 1998-10-29 | Studiengesellschaft Kohle Mbh | Selektive olefinmetathese von bi- oder polyfunktionellen substraten in komprimiertem kohlendioxid als reaktionsmedium |
| DE19720312A1 (de) | 1997-05-15 | 1998-11-19 | Hoechst Ag | Zubereitung mit erhöhter in vivo Verträglichkeit |
| DE19821954A1 (de) | 1997-05-15 | 1998-11-19 | Biotechnolog Forschung Gmbh | Verfahren zur Herstellung eines Epothilon-Derivats |
| DE19726627A1 (de) | 1997-06-17 | 1998-12-24 | Schering Ag | Zwischenprodukte, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Epothilon |
| US6605599B1 (en) | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
| US6384230B1 (en) | 1997-07-16 | 2002-05-07 | Schering Aktiengesellschaft | Thiazole derivatives, method for their production and use |
| ES2290993T3 (es) | 1997-08-09 | 2008-02-16 | Bayer Schering Pharma Aktiengesellschaft | Nuevos derivados de epotilona, proceso para su produccion y su utilizacion farmaceutica. |
| US6365749B1 (en) | 1997-12-04 | 2002-04-02 | Bristol-Myers Squibb Company | Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs |
| SK287775B6 (sk) | 1998-02-05 | 2011-09-05 | Novartis Ag | Farmaceutická formulácia obsahujúca epothilon, infúzny roztok a použitie farmaceutickej formulácie |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| DE69927790T2 (de) | 1998-02-25 | 2006-07-20 | Sloan-Kettering Institute For Cancer Research | Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen |
| 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 |
| US6399638B1 (en) | 1998-04-21 | 2002-06-04 | Bristol-Myers Squibb Company | 12,13-modified epothilone derivatives |
| WO2000000485A1 (de) | 1998-06-30 | 2000-01-06 | Schering Aktiengesellschaft | Epothilon-derivate, verfahren zu deren herstellung, zwischenprodukte und ihre pharmazeutische verwendung |
| NZ511722A (en) | 1998-11-20 | 2004-05-28 | Kosan Biosciences Inc | Recombinant methods and materials for producing epothilone and epothilone derivatives |
| CN1122668C (zh) | 1998-12-22 | 2003-10-01 | 诺瓦提斯公司 | 环氧噻酮衍生物，其制备方法及其药物组合物 |
| HK1040739A1 (zh) | 1998-12-23 | 2002-06-21 | Bristol-Myers Squibb Company | 微生物转形方法，用以制造epothilone |
| US6780620B1 (en) | 1998-12-23 | 2004-08-24 | Bristol-Myers Squibb Company | Microbial transformation method for the preparation of an epothilone |
| YU59001A (sh) | 1999-02-18 | 2005-07-19 | Schering Ag. | 16-halogen-epotilon-derivati, postupak za njihovo dobijanje i njihova farmaceutska primena |
| BR0008379A (pt) * | 1999-02-22 | 2002-09-24 | Biotechnolog Forschung Gmbh | Epotilonas modificadas em c-21 |
| US6211412B1 (en) | 1999-03-29 | 2001-04-03 | The University Of Kansas | Synthesis of epothilones |
| AR023792A1 (es) | 1999-04-30 | 2002-09-04 | Bayer Schering Pharma Ag | Derivados 6-alquenilo- y 6-alquinilo-epotilona, los procedimientos para prepararlos y su empleo en productos farmaceuticos |
| US6518421B1 (en) | 2000-03-20 | 2003-02-11 | Bristol-Myers Squibb Company | Process for the preparation of epothilone analogs |
| NZ526871A (en) * | 2001-01-25 | 2006-01-27 | Bristol Myers Squibb Co | Pharmaceutical dosage forms of epothilones for oral administration |
| PL363363A1 (en) | 2001-02-20 | 2004-11-15 | Bristol-Myers Squibb Company | Epothilone derivatives for the treatment of refractory tumors |
| BR0207487A (pt) | 2001-02-20 | 2004-08-10 | Brystol Myers Squibb Company | Método de tratamento de tumores em mamìferos e uso de compostos de epotilona |
| WO2002072085A1 (en) | 2001-03-14 | 2002-09-19 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
| TW200303202A (en) | 2002-02-15 | 2003-09-01 | Bristol Myers Squibb Co | Method of preparation of 21-amino epothilone derivatives |
-
2003
- 2003-03-28 TW TW092107147A patent/TW200403994A/zh unknown
- 2003-04-01 EP EP03746097A patent/EP1492529A1/en not_active Withdrawn
- 2003-04-01 WO PCT/US2003/009984 patent/WO2003084536A1/en not_active Ceased
- 2003-04-01 JP JP2003581776A patent/JP2005527576A/ja not_active Withdrawn
- 2003-04-01 AU AU2003226189A patent/AU2003226189A1/en not_active Abandoned
- 2003-04-01 US US10/404,324 patent/US6936628B2/en not_active Expired - Fee Related
- 2003-04-01 PL PL03372773A patent/PL372773A1/xx not_active Application Discontinuation
-
2004
- 2004-09-30 IS IS7481A patent/IS7481A/is unknown
- 2004-10-19 NO NO20044452A patent/NO20044452L/no not_active Application Discontinuation
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