ATE410431T1 - Verfahren zur herstellung von rapamycin-42-estern und fk-506-32-estern mit dicarbonsäure, vorstufen für rapamycinkonjugate und antikörper - Google Patents
Verfahren zur herstellung von rapamycin-42-estern und fk-506-32-estern mit dicarbonsäure, vorstufen für rapamycinkonjugate und antikörperInfo
- Publication number
- ATE410431T1 ATE410431T1 AT05735488T AT05735488T ATE410431T1 AT E410431 T1 ATE410431 T1 AT E410431T1 AT 05735488 T AT05735488 T AT 05735488T AT 05735488 T AT05735488 T AT 05735488T AT E410431 T1 ATE410431 T1 AT E410431T1
- Authority
- AT
- Austria
- Prior art keywords
- esters
- rapamycin
- precursors
- antibodies
- conjugates
- Prior art date
Links
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 title abstract 3
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 title abstract 3
- 229960002930 sirolimus Drugs 0.000 title abstract 3
- 150000002148 esters Chemical class 0.000 title abstract 2
- ZFTFAPZRGNKQPU-UHFFFAOYSA-N dicarbonic acid Chemical compound OC(=O)OC(O)=O ZFTFAPZRGNKQPU-UHFFFAOYSA-N 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 239000002243 precursor Substances 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 102000004882 Lipase Human genes 0.000 abstract 1
- 108090001060 Lipase Proteins 0.000 abstract 1
- 239000004367 Lipase Substances 0.000 abstract 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 abstract 1
- 150000008064 anhydrides Chemical class 0.000 abstract 1
- 230000001588 bifunctional effect Effects 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 150000001991 dicarboxylic acids Chemical class 0.000 abstract 1
- 235000019421 lipase Nutrition 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
- C12P17/188—Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Zoology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Wood Science & Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Microbiology (AREA)
- General Chemical & Material Sciences (AREA)
- Biotechnology (AREA)
- Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56196604P | 2004-04-14 | 2004-04-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE410431T1 true ATE410431T1 (de) | 2008-10-15 |
Family
ID=34965703
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT05735488T ATE410431T1 (de) | 2004-04-14 | 2005-04-12 | Verfahren zur herstellung von rapamycin-42-estern und fk-506-32-estern mit dicarbonsäure, vorstufen für rapamycinkonjugate und antikörper |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7445916B2 (de) |
| EP (1) | EP1735321B1 (de) |
| JP (1) | JP2007532655A (de) |
| CN (1) | CN1942478A (de) |
| AT (1) | ATE410431T1 (de) |
| AU (1) | AU2005238432A1 (de) |
| BR (1) | BRPI0509810A (de) |
| CA (1) | CA2562962A1 (de) |
| DE (1) | DE602005010228D1 (de) |
| DK (1) | DK1735321T3 (de) |
| ES (1) | ES2313328T3 (de) |
| MX (1) | MXPA06011882A (de) |
| PL (1) | PL1735321T3 (de) |
| WO (1) | WO2005105812A1 (de) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR040693A1 (es) | 2002-07-30 | 2005-04-13 | Wyeth Corp | Formulaciones parenterales |
| PL1735321T3 (pl) * | 2004-04-14 | 2009-04-30 | Wyeth Corp | Proces wytwarzania 42-estrów rapamycyny i 32-estrów FK-506 z kwasem dikarboksylowym, prekursory koniugatów rapamycyny oraz przeciwciała |
| CN1946852A (zh) * | 2004-04-27 | 2007-04-11 | 惠氏公司 | 利用雷帕霉素特异性甲基化酶标记雷帕霉素 |
| CA2577011A1 (en) * | 2004-08-10 | 2006-04-13 | Wyeth | Cci-779 derivatives and methods of making same |
| CN101321770A (zh) * | 2005-12-07 | 2008-12-10 | 惠氏公司 | 由雷帕霉素42-酯硼酸酯制备雷帕霉素42-酯的可放大方法 |
| AR058282A1 (es) * | 2005-12-07 | 2008-01-30 | Wyeth Corp | Forma cristalina purificada de cci-779, un proceso para la preparacion del mismo, un metodo para monitorear la cristalizacion del cci-779, un kit y una composicion farmaceutica que lo comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer. |
| WO2007067566A2 (en) * | 2005-12-07 | 2007-06-14 | Wyeth | Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry |
| CN101394867A (zh) * | 2006-03-07 | 2009-03-25 | 惠氏公司 | 大环内酯类免疫抑制剂的水溶性聚乙二醇结合物的制备方法 |
| US8022188B2 (en) * | 2006-04-24 | 2011-09-20 | Abbott Laboratories | Immunosuppressant binding antibodies and methods of obtaining and using same |
| US8414526B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids |
| US9737640B2 (en) | 2006-11-20 | 2017-08-22 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| US20080276935A1 (en) | 2006-11-20 | 2008-11-13 | Lixiao Wang | Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8430055B2 (en) | 2008-08-29 | 2013-04-30 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| US8414909B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| TW200845960A (en) * | 2007-04-05 | 2008-12-01 | Wyeth Corp | Wortmannin-rapalog conjugate and uses thereof |
| ES2645692T3 (es) | 2008-11-11 | 2017-12-07 | The Board Of Regents,The University Of Texas System | Microcápsulas de rapamicina y su uso para el tratamiento del cáncer |
| US9283211B1 (en) | 2009-11-11 | 2016-03-15 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
| DK2885007T3 (en) * | 2012-08-16 | 2018-12-03 | Pfizer | Methods for glycoconjugation and compositions |
| WO2014160328A1 (en) | 2013-03-13 | 2014-10-02 | The Board Of Regents Of The University Of Texas System | Mtor inhibitors for prevention of intestinal polyp growth |
| EP3089737B1 (de) | 2013-12-31 | 2021-11-03 | Rapamycin Holdings, LLC | Orale rapamycinnanopartikelzubereitungen und verwendung |
| US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
| US20210154372A1 (en) | 2017-05-15 | 2021-05-27 | C.R. Bard, Inc. | Medical device with drug-eluting coating and intermediate layer |
| EP3880266B1 (de) | 2018-11-14 | 2025-05-07 | Lutonix, Inc. | Medizinische vorrichtung mit wirkstofffreisetzender beschichtung auf modifizierter vorrichtungsoberfläche |
| EP3952937A1 (de) | 2019-04-08 | 2022-02-16 | Bard Peripheral Vascular, Inc. | Medizinische vorrichtung mit wirkstofffreisetzender beschichtung auf modifizierter vorrichtungsoberfläche |
| CN118027062B (zh) * | 2023-11-03 | 2025-02-14 | 沈阳药科大学 | 一种雷帕霉素前药及其纳米制剂的制备和应用 |
| GB202415232D0 (en) | 2024-10-16 | 2024-11-27 | Nacamed As | Composition |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US4316885A (en) | 1980-08-25 | 1982-02-23 | Ayerst, Mckenna And Harrison, Inc. | Acyl derivatives of rapamycin |
| US4650803A (en) | 1985-12-06 | 1987-03-17 | University Of Kansas | Prodrugs of rapamycin |
| US5210030A (en) | 1990-06-25 | 1993-05-11 | Merck & Co., Inc. | Process for selectively acylating immunomycin |
| US5023264A (en) | 1990-07-16 | 1991-06-11 | American Home Products Corporation | Rapamycin oximes |
| PT98990A (pt) | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
| US5221670A (en) | 1990-09-19 | 1993-06-22 | American Home Products Corporation | Rapamycin esters |
| US5378696A (en) | 1990-09-19 | 1995-01-03 | American Home Products Corporation | Rapamycin esters |
| US5130307A (en) | 1990-09-28 | 1992-07-14 | American Home Products Corporation | Aminoesters of rapamycin |
| US5233036A (en) | 1990-10-16 | 1993-08-03 | American Home Products Corporation | Rapamycin alkoxyesters |
| US5078999A (en) | 1991-02-22 | 1992-01-07 | American Home Products Corporation | Method of treating systemic lupus erythematosus |
| US5080899A (en) | 1991-02-22 | 1992-01-14 | American Home Products Corporation | Method of treating pulmonary inflammation |
| US5120842A (en) | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5100883A (en) | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
| US5118678A (en) | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5118667A (en) | 1991-05-03 | 1992-06-02 | Celtrix Pharmaceuticals, Inc. | Bone growth factors and inhibitors of bone resorption for promoting bone formation |
| US5130507A (en) * | 1991-05-23 | 1992-07-14 | Eaton Corporation | Capacitive switch assembly |
| DK0525960T3 (da) | 1991-06-18 | 1996-04-15 | American Home Prod | Anvendelse af rapamycin til behandling af T-celle leukæmi/lymfon |
| US5162333A (en) | 1991-09-11 | 1992-11-10 | American Home Products Corporation | Aminodiesters of rapamycin |
| US5177203A (en) | 1992-03-05 | 1993-01-05 | American Home Products Corporation | Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents |
| US5256790A (en) | 1992-08-13 | 1993-10-26 | American Home Products Corporation | 27-hydroxyrapamycin and derivatives thereof |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5434260A (en) | 1992-10-13 | 1995-07-18 | American Home Products Corporation | Carbamates of rapamycin |
| US5480989A (en) | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5302584A (en) | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
| US5489680A (en) | 1992-10-13 | 1996-02-06 | American Home Products Corporation | Carbamates of rapamycin |
| US5411967A (en) | 1992-10-13 | 1995-05-02 | American Home Products Corporation | Carbamates of rapamycin |
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| US5262423A (en) | 1992-10-29 | 1993-11-16 | American Home Products Corporation | Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents |
| US5258389A (en) | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| US5260300A (en) | 1992-11-19 | 1993-11-09 | American Home Products Corporation | Rapamycin carbonate esters as immuno-suppressant agents |
| US5252579A (en) | 1993-02-16 | 1993-10-12 | American Home Products Corporation | Macrocyclic immunomodulators |
| GB9307491D0 (en) | 1993-04-08 | 1993-06-02 | Sandoz Ltd | Organic compounds |
| US5504091A (en) | 1993-04-23 | 1996-04-02 | American Home Products Corporation | Biotin esters of rapamycin |
| ES2295093T3 (es) | 1993-04-23 | 2008-04-16 | Wyeth | Conjugados y anticuerpos de rapamicina. |
| WO1994025072A1 (en) | 1993-04-23 | 1994-11-10 | American Home Products Corporation | Rapamycin conjugates and antibodies |
| GB2281294A (en) | 1993-08-23 | 1995-03-01 | Fujisawa Pharmaceutical Co | Process for producing half esters of the macrolide FK506 |
| US5378836A (en) | 1993-10-08 | 1995-01-03 | American Home Products Corporation | Rapamycin oximes and hydrazones |
| US5391730A (en) | 1993-10-08 | 1995-02-21 | American Home Products Corporation | Phosphorylcarbamates of rapamycin and oxime derivatives thereof |
| US5373014A (en) | 1993-10-08 | 1994-12-13 | American Home Products Corporation | Rapamycin oximes |
| US5385908A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered esters of rapamycin |
| US5385910A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Gem-distributed esters of rapamycin |
| US5385909A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
| US5389639A (en) | 1993-12-29 | 1995-02-14 | American Home Products Company | Amino alkanoic esters of rapamycin |
| US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| US5463048A (en) | 1994-06-14 | 1995-10-31 | American Home Products Corporation | Rapamycin amidino carbamates |
| US5491231A (en) | 1994-11-28 | 1996-02-13 | American Home Products Corporation | Hindered N-oxide esters of rapamycin |
| US5563145A (en) | 1994-12-07 | 1996-10-08 | American Home Products Corporation | Rapamycin 42-oximes and hydroxylamines |
| US6261813B1 (en) | 1995-09-11 | 2001-07-17 | Albany Molecular Research, Inc. | Two step enzymatic acylation |
| US5780462A (en) | 1995-12-27 | 1998-07-14 | American Home Products Corporation | Water soluble rapamycin esters |
| CA2286311A1 (en) | 1997-04-09 | 1998-10-15 | Isotechnika, Inc. | Method for production of antibodies to specific sites of rapamycin |
| US6277983B1 (en) | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| US7153983B2 (en) * | 2002-03-25 | 2006-12-26 | Council Of Scientific And Industrial Research | Chemo-enzymatic process for the preparation of opticaly enriched β-benzyl-γ-butyrolactones |
| US6745478B2 (en) | 2002-07-18 | 2004-06-08 | Delillo Dominick D. | Multi-purpose work knife |
| JP4227649B2 (ja) | 2003-08-07 | 2009-02-18 | ワイス | Ｃｃｉ−７７９の位置選択的合成 |
| PL1735321T3 (pl) * | 2004-04-14 | 2009-04-30 | Wyeth Corp | Proces wytwarzania 42-estrów rapamycyny i 32-estrów FK-506 z kwasem dikarboksylowym, prekursory koniugatów rapamycyny oraz przeciwciała |
| MXPA06011883A (es) * | 2004-04-14 | 2006-12-14 | Wyeth Corp | 42-ester de prolina-rapamicina con acido 2,2-bis(hidroximetil)propionico y sintesis enzimatica de dos etapas de 42-ester de prolina-rapamicina con acido 2,2-bis(hidroximetil)propionico y 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionic |
| JP4224115B2 (ja) * | 2004-04-14 | 2009-02-12 | ワイス | ラパマイシン４２−エステル誘導体の位置特異的合成 |
| JP2008505176A (ja) * | 2004-06-30 | 2008-02-21 | コンビナトアールエックス インコーポレーティッド | 代謝障害を治療するための方法および試薬 |
-
2005
- 2005-04-12 PL PL05735488T patent/PL1735321T3/pl unknown
- 2005-04-12 BR BRPI0509810-6A patent/BRPI0509810A/pt not_active IP Right Cessation
- 2005-04-12 ES ES05735488T patent/ES2313328T3/es not_active Expired - Lifetime
- 2005-04-12 EP EP05735488A patent/EP1735321B1/de not_active Expired - Lifetime
- 2005-04-12 WO PCT/US2005/012268 patent/WO2005105812A1/en not_active Ceased
- 2005-04-12 AU AU2005238432A patent/AU2005238432A1/en not_active Withdrawn
- 2005-04-12 MX MXPA06011882A patent/MXPA06011882A/es active IP Right Grant
- 2005-04-12 CA CA002562962A patent/CA2562962A1/en not_active Abandoned
- 2005-04-12 DK DK05735488T patent/DK1735321T3/da active
- 2005-04-12 JP JP2007508443A patent/JP2007532655A/ja not_active Withdrawn
- 2005-04-12 US US11/104,349 patent/US7445916B2/en not_active Expired - Lifetime
- 2005-04-12 DE DE602005010228T patent/DE602005010228D1/de not_active Expired - Fee Related
- 2005-04-12 CN CNA200580011299XA patent/CN1942478A/zh not_active Withdrawn
- 2005-04-12 AT AT05735488T patent/ATE410431T1/de not_active IP Right Cessation
-
2008
- 2008-09-29 US US12/240,230 patent/US7625726B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0509810A (pt) | 2007-09-18 |
| US20050234087A1 (en) | 2005-10-20 |
| WO2005105812A1 (en) | 2005-11-10 |
| EP1735321B1 (de) | 2008-10-08 |
| US20090029426A1 (en) | 2009-01-29 |
| DK1735321T3 (da) | 2009-01-12 |
| AU2005238432A1 (en) | 2005-11-10 |
| PL1735321T3 (pl) | 2009-04-30 |
| US7625726B2 (en) | 2009-12-01 |
| DE602005010228D1 (de) | 2008-11-20 |
| MXPA06011882A (es) | 2006-12-14 |
| US7445916B2 (en) | 2008-11-04 |
| CA2562962A1 (en) | 2005-11-10 |
| JP2007532655A (ja) | 2007-11-15 |
| EP1735321A1 (de) | 2006-12-27 |
| ES2313328T3 (es) | 2009-03-01 |
| CN1942478A (zh) | 2007-04-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |