TWI341728B - Combinations comprising epothilones and anti-metabolites - Google Patents
Combinations comprising epothilones and anti-metabolites Download PDFInfo
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- TWI341728B TWI341728B TW092100606A TW92100606A TWI341728B TW I341728 B TWI341728 B TW I341728B TW 092100606 A TW092100606 A TW 092100606A TW 92100606 A TW92100606 A TW 92100606A TW I341728 B TWI341728 B TW I341728B
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- treatment
- combination
- epothilone
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- pharmaceutically acceptable
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- 230000000340 anti-metabolite Effects 0.000 title description 10
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- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 239000002831 pharmacologic agent Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 208000026435 phlegm Diseases 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 238000002601 radiography Methods 0.000 description 1
- 206010038038 rectal cancer Diseases 0.000 description 1
- 201000001275 rectum cancer Diseases 0.000 description 1
- 238000005932 reductive alkylation reaction Methods 0.000 description 1
- 230000003014 reinforcing effect Effects 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 201000000849 skin cancer Diseases 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- UOCLRXFKRLRMKV-UHFFFAOYSA-N trolnitrate phosphate Chemical compound OP(O)(O)=O.OP(O)(O)=O.[O-][N+](=O)OCCN(CCO[N+]([O-])=O)CCO[N+]([O-])=O UOCLRXFKRLRMKV-UHFFFAOYSA-N 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 229940045136 urea Drugs 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 206010046885 vaginal cancer Diseases 0.000 description 1
- 208000013139 vaginal neoplasm Diseases 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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|---|---|---|---|
| US34862202P | 2002-01-14 | 2002-01-14 | |
| US41617302P | 2002-10-04 | 2002-10-04 |
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| TW200306185A TW200306185A (en) | 2003-11-16 |
| TWI341728B true TWI341728B (en) | 2011-05-11 |
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|---|---|---|---|
| TW092100606A TWI341728B (en) | 2002-01-14 | 2003-01-13 | Combinations comprising epothilones and anti-metabolites |
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| EP (2) | EP1469847A1 (enExample) |
| JP (1) | JP2005513167A (enExample) |
| KR (1) | KR20040078123A (enExample) |
| CN (1) | CN1615136A (enExample) |
| AU (1) | AU2003235761A1 (enExample) |
| BR (1) | BR0306861A (enExample) |
| CA (1) | CA2471509A1 (enExample) |
| IL (1) | IL162595A0 (enExample) |
| MX (1) | MXPA04006822A (enExample) |
| NO (1) | NO20043279L (enExample) |
| NZ (1) | NZ533940A (enExample) |
| PL (1) | PL369670A1 (enExample) |
| RU (1) | RU2346686C2 (enExample) |
| TW (1) | TWI341728B (enExample) |
| WO (1) | WO2003057217A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6204388B1 (en) | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6242469B1 (en) | 1996-12-03 | 2001-06-05 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| CA2440555A1 (en) | 2001-03-14 | 2002-09-19 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
| WO2002074042A2 (en) * | 2001-03-19 | 2002-09-26 | Novartis Ag | Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative |
| BR0315169A (pt) * | 2002-10-09 | 2005-08-23 | Kosan Biosciences Inc | Referência cruzada a pedidos de patente relacionados |
| BRPI0414043A (pt) * | 2003-09-02 | 2006-10-24 | Novartis Ag | tratamento de cáncer com epotilonas |
| US20050171167A1 (en) | 2003-11-04 | 2005-08-04 | Haby Thomas A. | Process and formulation containing epothilones and analogs thereof |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| US20090099103A1 (en) * | 2006-04-05 | 2009-04-16 | Novartis Ag. | Combinations of therapeutic agents for treating cancer |
| CN101415409B (zh) * | 2006-04-05 | 2012-12-05 | 诺瓦提斯公司 | 用于治疗癌症的治疗剂的组合 |
| WO2011146638A1 (en) | 2010-05-18 | 2011-11-24 | Cerulean Pharma Inc. | Compositions and methods for treatment of autoimmune and other diseases |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2802005A (en) | 1957-08-06 | S-eluorourace | ||
| US2705727A (en) | 1952-07-10 | 1955-04-05 | Du Pont | Synthesis of ureas |
| US2933498A (en) | 1954-12-28 | 1960-04-19 | Burroughs Wellcome Co | 7-aminothiazolo-(5,4-d) pyrimidine |
| US3116282A (en) | 1960-04-27 | 1963-12-31 | Upjohn Co | Pyrimidine nucleosides and process |
| US4393064A (en) | 1976-03-05 | 1983-07-12 | Sri International | Process and composition for treatment of leukemia and process for preparing the same |
| US4357324A (en) | 1981-02-24 | 1982-11-02 | The United States Of America As Represented By The Department Of Health And Human Services | Prodrug derivatives of 9β-D-arabinofuranosyl-2-fluoroadenine |
| US4760135A (en) | 1984-09-06 | 1988-07-26 | University Of Kentucky Research Foundation | Phloretin and phlorizin derivative containing compounds |
| DE3587500T2 (de) | 1984-12-04 | 1993-12-16 | Lilly Co Eli | Tumorbehandlung bei Säugetieren. |
| DE3773716D1 (de) | 1986-03-24 | 1991-11-21 | Nippon Kayaku Kk | Verfahren zur herstellung von monosodiumsalz und dessen monohydrat von 1-beta-d-arabinofuranosylcytosin-5'stearylphosphat und diese enthaltende pharmazeutische zusammensetzung. |
| EP0443028B1 (en) * | 1989-01-05 | 1993-09-29 | Otsuka Pharmaceutical Co., Ltd. | Non-injection carcinostatic agent for suppressing occurrence of inflammation due to 5-fluorouracil and method for curing cancer |
| KR0148589B1 (ko) | 1991-05-27 | 1998-11-02 | 고바야시 유끼오 | 항종양 효과의 상승 및 종양의 치료를 위한 조성물 및 키트 |
| DE4138042C2 (de) | 1991-11-19 | 1993-10-14 | Biotechnolog Forschung Gmbh | Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel |
| AU671491B2 (en) | 1992-12-18 | 1996-08-29 | F. Hoffmann-La Roche Ag | N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines |
| NZ334821A (en) | 1996-08-30 | 2000-12-22 | Novartis Ag | Method for producing epothilones |
| CN100344627C (zh) | 1996-11-18 | 2007-10-24 | 生物技术研究有限公司(Gbf) | 埃坡霉素c、其制备方法以及作为细胞抑制剂和植物保护剂的应用 |
| 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 |
| US6605599B1 (en) | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
| EP1052974B1 (en) | 1998-02-05 | 2009-05-20 | Novartis AG | Pharmaceutical formulation containing epothilone |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| US6302838B1 (en) * | 1998-02-25 | 2001-10-16 | Novartis Ag | Cancer treatment with epothilones |
| ATE307123T1 (de) | 1998-02-25 | 2005-11-15 | Sloan Kettering Inst Cancer | 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 |
| EP1135470A2 (en) | 1998-11-20 | 2001-09-26 | Kosan Biosciences, Inc. | Recombinant methods and materials for producing epothilone and epothilone derivatives |
| EP1140944B1 (en) * | 1998-12-22 | 2003-08-27 | Novartis AG | Epothilone derivatives and their use as antitumor agents |
| ATE254615T1 (de) * | 1999-02-22 | 2003-12-15 | Biotechnolog Forschung Gmbh | C-21 modifizierte epothilone |
| JP2002541200A (ja) * | 1999-04-14 | 2002-12-03 | デイナ−ファーバー キャンサー インスティチュート,インコーポレイテッド | 癌の処置のための方法および組成物 |
| GB9918429D0 (en) * | 1999-08-04 | 1999-10-06 | Novartis Ag | Organic compounds |
| AU2001266583A1 (en) * | 2000-05-26 | 2001-12-11 | Kosan Biosciences, Inc. | Epothilone derivatives and methods for making and using the same |
| CA2440555A1 (en) * | 2001-03-14 | 2002-09-19 | Bristol-Myers Squibb Company | Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases |
| TWI287986B (en) * | 2001-12-13 | 2007-10-11 | Novartis Ag | Use of Epothilones for the treatment of the carcinoid syndrome |
-
2003
- 2003-01-13 MX MXPA04006822A patent/MXPA04006822A/es active IP Right Grant
- 2003-01-13 KR KR10-2004-7010853A patent/KR20040078123A/ko not_active Ceased
- 2003-01-13 WO PCT/EP2003/000232 patent/WO2003057217A1/en not_active Ceased
- 2003-01-13 EP EP20030729249 patent/EP1469847A1/en not_active Ceased
- 2003-01-13 CN CNA03802215XA patent/CN1615136A/zh active Pending
- 2003-01-13 PL PL03369670A patent/PL369670A1/xx unknown
- 2003-01-13 JP JP2003557575A patent/JP2005513167A/ja not_active Ceased
- 2003-01-13 RU RU2004124943/15A patent/RU2346686C2/ru not_active IP Right Cessation
- 2003-01-13 IL IL16259503A patent/IL162595A0/xx unknown
- 2003-01-13 NZ NZ533940A patent/NZ533940A/en not_active IP Right Cessation
- 2003-01-13 AU AU2003235761A patent/AU2003235761A1/en not_active Abandoned
- 2003-01-13 CA CA002471509A patent/CA2471509A1/en not_active Abandoned
- 2003-01-13 BR BR0306861-7A patent/BR0306861A/pt not_active Application Discontinuation
- 2003-01-13 US US10/501,207 patent/US20060089327A1/en not_active Abandoned
- 2003-01-13 EP EP08169239A patent/EP2030618A3/en not_active Withdrawn
- 2003-01-13 TW TW092100606A patent/TWI341728B/zh not_active IP Right Cessation
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2004
- 2004-08-05 NO NO20043279A patent/NO20043279L/no not_active Application Discontinuation
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2009
- 2009-08-12 US US12/539,891 patent/US20090298791A1/en not_active Abandoned
-
2010
- 2010-12-13 US US12/966,575 patent/US20110082101A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2003057217A1 (en) | 2003-07-17 |
| KR20040078123A (ko) | 2004-09-08 |
| US20090298791A1 (en) | 2009-12-03 |
| US20110082101A1 (en) | 2011-04-07 |
| PL369670A1 (en) | 2005-05-02 |
| AU2003235761A1 (en) | 2003-07-24 |
| RU2004124943A (ru) | 2005-08-10 |
| CN1615136A (zh) | 2005-05-11 |
| TW200306185A (en) | 2003-11-16 |
| JP2005513167A (ja) | 2005-05-12 |
| IL162595A0 (en) | 2005-11-20 |
| CA2471509A1 (en) | 2003-07-17 |
| RU2346686C2 (ru) | 2009-02-20 |
| MXPA04006822A (es) | 2004-12-08 |
| BR0306861A (pt) | 2004-11-03 |
| US20060089327A1 (en) | 2006-04-27 |
| NO20043279L (no) | 2004-08-05 |
| EP2030618A2 (en) | 2009-03-04 |
| NZ533940A (en) | 2007-06-29 |
| EP2030618A3 (en) | 2009-03-11 |
| EP1469847A1 (en) | 2004-10-27 |
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| MM4A | Annulment or lapse of patent due to non-payment of fees |