RU2005114018A - Эпотилон d+фторурацил/гемцитабин - Google Patents
Эпотилон d+фторурацил/гемцитабин Download PDFInfo
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- RU2005114018A RU2005114018A RU2005114018/14A RU2005114018A RU2005114018A RU 2005114018 A RU2005114018 A RU 2005114018A RU 2005114018/14 A RU2005114018/14 A RU 2005114018/14A RU 2005114018 A RU2005114018 A RU 2005114018A RU 2005114018 A RU2005114018 A RU 2005114018A
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- RU
- Russia
- Prior art keywords
- epothilone
- dehydroepotilon
- group
- combination
- epothilones
- Prior art date
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- 229930013356 epothilone Natural products 0.000 claims 10
- 238000000034 method Methods 0.000 claims 9
- 239000002777 nucleoside Substances 0.000 claims 6
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 6
- 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 5
- 150000003883 epothilone derivatives Chemical class 0.000 claims 5
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 4
- XOZIUKBZLSUILX-SDMHVBBESA-N Epothilone D Natural products O=C1[C@H](C)[C@@H](O)[C@@H](C)CCC/C(/C)=C/C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C XOZIUKBZLSUILX-SDMHVBBESA-N 0.000 claims 4
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 4
- XOZIUKBZLSUILX-UHFFFAOYSA-N desoxyepothilone B Natural products O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC(C)=CCC1C(C)=CC1=CSC(C)=N1 XOZIUKBZLSUILX-UHFFFAOYSA-N 0.000 claims 4
- XOZIUKBZLSUILX-GIQCAXHBSA-N epothilone D 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[C@H]1C(\C)=C\C1=CSC(C)=N1 XOZIUKBZLSUILX-GIQCAXHBSA-N 0.000 claims 4
- 229960002949 fluorouracil Drugs 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000003463 hyperproliferative effect Effects 0.000 claims 3
- 229940127073 nucleoside analogue Drugs 0.000 claims 3
- FPVKHBSQESCIEP-UHFFFAOYSA-N (8S)-3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Natural products C1C(O)C(CO)OC1N1C(NC=NCC2O)=C2N=C1 FPVKHBSQESCIEP-UHFFFAOYSA-N 0.000 claims 2
- IDPUKCWIGUEADI-UHFFFAOYSA-N 5-[bis(2-chloroethyl)amino]uracil Chemical compound ClCCN(CCCl)C1=CNC(=O)NC1=O IDPUKCWIGUEADI-UHFFFAOYSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- PTOAARAWEBMLNO-KVQBGUIXSA-N Cladribine Chemical compound C1=NC=2C(N)=NC(Cl)=NC=2N1[C@H]1C[C@H](O)[C@@H](CO)O1 PTOAARAWEBMLNO-KVQBGUIXSA-N 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 2
- QXRSDHAAWVKZLJ-OXZHEXMSSA-N Epothilone B Natural products O=C1[C@H](C)[C@H](O)[C@@H](C)CCC[C@@]2(C)O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C QXRSDHAAWVKZLJ-OXZHEXMSSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229960002436 cladribine Drugs 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 229960000684 cytarabine Drugs 0.000 claims 2
- HESCAJZNRMSMJG-HGYUPSKWSA-N epothilone A Natural products O=C1[C@H](C)[C@H](O)[C@H](C)CCC[C@H]2O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C HESCAJZNRMSMJG-HGYUPSKWSA-N 0.000 claims 2
- QXRSDHAAWVKZLJ-PVYNADRNSA-N epothilone B 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)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 QXRSDHAAWVKZLJ-PVYNADRNSA-N 0.000 claims 2
- GIUYCYHIANZCFB-FJFJXFQQSA-N fludarabine phosphate Chemical compound C1=NC=2C(N)=NC(F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O GIUYCYHIANZCFB-FJFJXFQQSA-N 0.000 claims 2
- 229960005304 fludarabine phosphate Drugs 0.000 claims 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- FPVKHBSQESCIEP-JQCXWYLXSA-N pentostatin Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(N=CNC[C@H]2O)=C2N=C1 FPVKHBSQESCIEP-JQCXWYLXSA-N 0.000 claims 2
- 229960002340 pentostatin Drugs 0.000 claims 2
- -1 phloxuridine Chemical compound 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 229960001055 uracil mustard Drugs 0.000 claims 2
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical compound O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 claims 1
- 229960002756 azacitidine Drugs 0.000 claims 1
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- A61K31/7088—Compounds having three or more nucleosides or nucleotides
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- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Otolaryngology (AREA)
- Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
Claims (14)
1. Способ лечения гиперпролиферативных заболеваний, который включает введение пациенту, нуждающемуся в таком лечении, комбинации одного или нескольких эпотилонов и одного или нескольких аналогов нуклеозидов.
2. Способ по п. 1, в котором один или несколько эпотилонов и один или несколько аналогов нуклеозидов вводятся одновременно.
3. Способ по п. 2, в котором эпотилон выбирают из группы, состоящей из эпотилона B, эпотилона D, 21-гидроксиэпотилона B, 21-гидроксиэпотилона D, 21-аминоэпотилона B, 21-аминоэпотилона D, азаэпотилона B, азаэпотилона D, 9,10-дегидроэпотилона B, 9,10-дегидроэпотилона D, 26-трифтор-9,10-дегидроэпотилона B и 26-трифтор-9,10-дегидроэпотилона D.
4. Способ по п. 2, в котором аналог нуклеозида выбирают из группы, состоящей из азацитидина, кладрибина, цитарабина, флоксуридина, флударабина фосфата, 5-фторурацила, гемцитабина, пентостатина, урамустина и 5'-дезокси-5-фтор-N-[(пентилокси)карбонил]-цитидина.
5. Способ по п. 2, в котором эпотилоном является эпотилон D и аналог нуклеозида выбирают из группы, состоящей из 5-фторурацила и 5'-дезокси-5-фтор-N-[(пентилокси)карбонил]-цитидина.
6. Способ по п. 2, в котором эпотилон используют в дозах от примерно 1 мг/м2 до примерно 200 мг/м2.
7. Способ по п. 1, в котором сначала вводится один или несколько эпотилонов, а затем - один или несколько аналогов нуклеозидов.
8. Способ по п. 1, в котором сначала вводится один или несколько аналогов нуклеозида, а затем - один или несколько эпотилонов.
9. Способ по п. 1, в котором указанной гиперпролиферацией является злокачественная опухоль, выбранная из группы, состоящей из рака толстой кишки, рака молочной железы и немелкоклеточного рака легкого.
10. Комбинация одного и более эпотилонов и одного и более аналогов нуклеозидов для раздельного, одновременного или последовательного применения для лечения гиперпролиферативных заболеваний.
11. Комбинация по п. 10, в которой эпотилон выбирают из группы, состоящей из эпотилона B, эпотилона D, 21-гидроксиэпотилона B, 21-гидроксиэпотилона D, 21-аминоэпотилона B, 21-аминоэпотилона D, азаэпотилона B, азаэпотилона D, 9,10-дегидроэпотилона B, 9,10-дегидроэпотилона D, 26-трифтор-9,10-дегидроэпотилона B и 26-трифтор-9,10-дегидроэпотилона D.
12. Комбинация по п. 10, в которой аналог нуклеозида выбирают из группы, состоящей из азацитидина, кладрибина, цитарабина, флоксуридина, флударабина фосфата, 5-фторурацила, гемцитабина, пентостатина, урамустина и 5'-дезокси-5-фтор-N-[(пентилокси)карбонил]-цитидина.
13. Комбинация по п. 10, в которой эпотилоном является эпотилон D и аналог нуклеозида выбирают из группы, состоящей из 5-фторурацила и 5'-дезокси-5-фтор-N-[(пентилокси)карбонил]-цитидина.
14. Комбинация по п. 10, в которой гиперпролиферативное заболевание является злокачественной опухолью, выбранной из группы, состоящей из рака толстой кишки, рака молочной железы и немелкоклеточного рака легкого.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41753502P | 2002-10-09 | 2002-10-09 | |
| US60/417,535 | 2002-10-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2005114018A true RU2005114018A (ru) | 2006-01-20 |
Family
ID=32094033
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005114018/14A RU2005114018A (ru) | 2002-10-09 | 2003-10-09 | Эпотилон d+фторурацил/гемцитабин |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20040167097A1 (ru) |
| EP (1) | EP1551378A4 (ru) |
| JP (1) | JP2006504745A (ru) |
| KR (1) | KR20050051688A (ru) |
| CN (1) | CN1297258C (ru) |
| AU (1) | AU2003279923A1 (ru) |
| BR (1) | BR0315169A (ru) |
| CA (1) | CA2499682A1 (ru) |
| MX (1) | MXPA05003706A (ru) |
| RU (1) | RU2005114018A (ru) |
| WO (1) | WO2004032872A2 (ru) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE419239T1 (de) | 2000-10-20 | 2009-01-15 | Eisai R&D Man Co Ltd | Verfahren zur herstellung von 4-phenoxy chinolin derivaten |
| ES2281692T3 (es) | 2002-08-23 | 2007-10-01 | Sloan-Kettering Institute For Cancer Research | Sintesis de epotilones, sus intermediarios, sus analogos y sus usos. |
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| EP1604665B1 (en) | 2003-03-10 | 2011-05-11 | Eisai R&D Management Co., Ltd. | C-kit kinase inhibitor |
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| US20050215604A1 (en) * | 2004-03-26 | 2005-09-29 | Kosan Biosciences, Inc. | Combination therapies with epothilones and carboplatin |
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| CN105264380B (zh) | 2013-05-14 | 2017-09-05 | 卫材R&D管理有限公司 | 用于预测和评价子宫内膜癌受试者对乐伐替尼化合物响应性的生物标志 |
| LT3524595T (lt) | 2014-08-28 | 2022-09-26 | Eisai R&D Management Co., Ltd. | Aukšto grynumo chinolino darinys ir jo gamybos būdas |
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|---|---|---|---|---|
| DE69734362T2 (de) * | 1996-12-03 | 2006-07-20 | Sloan-Kettering Institute For Cancer Research | Synthese von epothilonen, zwischenprodukte dazu, analoga und verwendungen davon |
| US6204388B1 (en) * | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6596875B2 (en) * | 2000-02-07 | 2003-07-22 | James David White | Method for synthesizing epothilones and epothilone analogs |
| ATE254615T1 (de) * | 1999-02-22 | 2003-12-15 | Biotechnolog Forschung Gmbh | C-21 modifizierte epothilone |
| US6291684B1 (en) * | 1999-03-29 | 2001-09-18 | Bristol-Myers Squibb Company | Process for the preparation of aziridinyl epothilones from oxiranyl epothilones |
| CA2369303A1 (en) * | 1999-04-14 | 2000-10-19 | Arthur B. Pardee | Method and composition for the treatment of cancer |
| US6489314B1 (en) * | 2001-04-03 | 2002-12-03 | Kosan Biosciences, Inc. | Epothilone derivatives and methods for making and using the same |
| BRPI0207961B8 (pt) * | 2001-03-14 | 2021-05-25 | Bristol Myers Squibb Co | uso de análogos de epotilona e capecitabina para fabricar medicamento para tratar tumores cancerosos sólidos e kit compreendendo os referidos compostos. |
| TWI287986B (en) * | 2001-12-13 | 2007-10-11 | Novartis Ag | Use of Epothilones for the treatment of the carcinoid syndrome |
| WO2003057217A1 (en) * | 2002-01-14 | 2003-07-17 | Novartis Ag | Combinations comprising epothilones and anti-metabolites |
-
2003
- 2003-10-09 RU RU2005114018/14A patent/RU2005114018A/ru not_active Application Discontinuation
- 2003-10-09 WO PCT/US2003/032148 patent/WO2004032872A2/en not_active Ceased
- 2003-10-09 KR KR1020057006143A patent/KR20050051688A/ko not_active Withdrawn
- 2003-10-09 CN CNB2003801009323A patent/CN1297258C/zh not_active Expired - Fee Related
- 2003-10-09 EP EP03773239A patent/EP1551378A4/en not_active Withdrawn
- 2003-10-09 CA CA002499682A patent/CA2499682A1/en not_active Abandoned
- 2003-10-09 AU AU2003279923A patent/AU2003279923A1/en not_active Abandoned
- 2003-10-09 BR BR0315169-7A patent/BR0315169A/pt not_active IP Right Cessation
- 2003-10-09 JP JP2004543655A patent/JP2006504745A/ja active Pending
- 2003-10-09 MX MXPA05003706A patent/MXPA05003706A/es not_active Application Discontinuation
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2004
- 2004-05-03 US US10/683,203 patent/US20040167097A1/en not_active Abandoned
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| CA2499682A1 (en) | 2004-04-22 |
| WO2004032872A2 (en) | 2004-04-22 |
| BR0315169A (pt) | 2005-08-23 |
| CN1703208A (zh) | 2005-11-30 |
| KR20050051688A (ko) | 2005-06-01 |
| WO2004032872A3 (en) | 2004-11-11 |
| CN1297258C (zh) | 2007-01-31 |
| US20040167097A1 (en) | 2004-08-26 |
| AU2003279923A1 (en) | 2004-05-04 |
| EP1551378A2 (en) | 2005-07-13 |
| MXPA05003706A (es) | 2005-07-01 |
| EP1551378A4 (en) | 2006-09-06 |
| JP2006504745A (ja) | 2006-02-09 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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