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)
- Wood Science & Technology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Zoology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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 (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1553940E (pt) | 2002-07-30 | 2008-05-09 | Wyeth Corp | Formulações parentéricas contendo um hidroxi-éster de rapamicina |
| US7445916B2 (en) * | 2004-04-14 | 2008-11-04 | Wyeth | Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies |
| BRPI0510277A (pt) * | 2004-04-27 | 2007-10-30 | Wyeth Corp | método para marcar especificamente uma rapamicina, rapamicina especificamente marcada, composição, e, kit |
| AR050452A1 (es) * | 2004-08-10 | 2006-10-25 | Wyeth Corp | Derivados de cci-779 |
| TW200736603A (en) * | 2005-12-07 | 2007-10-01 | Wyeth Corp | Methods for preparing crystalline rapamycin and measuring crystallinity of rapamycin compounds using differential scanning calorimetry |
| TW200804399A (en) * | 2005-12-07 | 2008-01-16 | Wyeth Corp | Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate |
| WO2007067565A1 (en) * | 2005-12-07 | 2007-06-14 | Wyeth | Process for the preparation of purified crystalline cci-779 |
| 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 |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414909B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414526B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| 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 |
| US9737640B2 (en) | 2006-11-20 | 2017-08-22 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| TW200845960A (en) * | 2007-04-05 | 2008-12-01 | Wyeth Corp | Wortmannin-rapalog conjugate and uses thereof |
| WO2010024898A2 (en) | 2008-08-29 | 2010-03-04 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| 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 |
| HUE049531T2 (hu) * | 2012-08-16 | 2020-10-28 | Pfizer | Glikokonjugációs eljárások és kompozíciók |
| EP2968281B1 (de) | 2013-03-13 | 2020-08-05 | The Board of Regents of The University of Texas System | Mtor-hemmer zur vorbeugung von darmpolypenwachstum |
| US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
| DK3089737T3 (da) | 2013-12-31 | 2021-12-13 | Rapamycin Holdings Llc | Orale rapamycin-nanopartikelpræparater og anvendelse. |
| EP3624863B1 (de) | 2017-05-15 | 2021-04-14 | C.R. Bard, Inc. | Medizinische vorrichtung mit wirkstofffreisetzender beschichtung und zwischenschicht |
| CN113226389B (zh) | 2018-11-14 | 2022-11-08 | 乐通公司 | 在经改性设备表面上具有药物洗脱涂层的医疗设备 |
| JP7487228B2 (ja) | 2019-04-08 | 2024-05-20 | バード・ペリフェラル・バスキュラー・インコーポレーテッド | 改質されたデバイス表面に薬物溶出コーティングを有する医療用デバイス |
| 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 |
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 |
| US5130307A (en) | 1990-09-28 | 1992-07-14 | American Home Products Corporation | Aminoesters of rapamycin |
| US5378696A (en) | 1990-09-19 | 1995-01-03 | American Home Products Corporation | Rapamycin esters |
| 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 |
| US5233036A (en) | 1990-10-16 | 1993-08-03 | American Home Products Corporation | Rapamycin alkoxyesters |
| US5080899A (en) | 1991-02-22 | 1992-01-14 | American Home Products Corporation | Method of treating pulmonary inflammation |
| US5078999A (en) | 1991-02-22 | 1992-01-07 | American Home Products Corporation | Method of treating systemic lupus erythematosus |
| 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 |
| DE69209183T2 (de) | 1991-06-18 | 1996-08-08 | American Home Prod | Verwendung von Rapamycin zur Behandlung von T-Zellen Lymphom/Leukämie bei Erwachsenen |
| 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 |
| US5302584A (en) | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
| US5480989A (en) | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5434260A (en) | 1992-10-13 | 1995-07-18 | American Home Products Corporation | Carbamates of rapamycin |
| US5480988A (en) | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5411967A (en) | 1992-10-13 | 1995-05-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5489680A (en) | 1992-10-13 | 1996-02-06 | American Home Products Corporation | Carbamates of rapamycin |
| 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 |
| ES2176245T3 (es) | 1993-04-23 | 2002-12-01 | Wyeth Corp | Anticuerpos de ramapicinas de ciclo abierto. |
| 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 |
| US5373014A (en) | 1993-10-08 | 1994-12-13 | American Home Products Corporation | Rapamycin oximes |
| 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 |
| US5385909A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
| US5385910A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Gem-distributed esters of rapamycin |
| US5385908A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered 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 |
| JP2001518784A (ja) | 1997-04-09 | 2001-10-16 | アイソテクニカ，インコーポレイテッド | ラパマイシンの特異的部位に対する抗体の産生方法 |
| 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 |
| RU2339639C2 (ru) | 2003-08-07 | 2008-11-27 | Уайт | Региоселективный синтез cci-779 |
| CA2562952A1 (en) * | 2004-04-14 | 2005-11-10 | Wyeth | Regiospecific synthesis of rapamycin 42-ester derivatives |
| CA2564811A1 (en) | 2004-04-14 | 2005-10-27 | Wyeth | Proline cci-779 (proline-rapamycin 42-ester with 2,2-bis (hydroxymethyl) propionic acid) and two-step enzymatic synthesis of proline cci-779 and cci-779 using microbial lipase |
| US7445916B2 (en) | 2004-04-14 | 2008-11-04 | Wyeth | Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies |
| RU2007103178A (ru) * | 2004-06-30 | 2008-08-10 | Комбинаторкс, Инкорпорейтед (Us) | Способы и реагенты для лечения метаболических нарушений |
-
2005
- 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 JP JP2007508443A patent/JP2007532655A/ja not_active Withdrawn
- 2005-04-12 AU AU2005238432A patent/AU2005238432A1/en not_active Withdrawn
- 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 WO PCT/US2005/012268 patent/WO2005105812A1/en not_active Ceased
- 2005-04-12 AT AT05735488T patent/ATE410431T1/de not_active IP Right Cessation
- 2005-04-12 PL PL05735488T patent/PL1735321T3/pl unknown
- 2005-04-12 CN CNA200580011299XA patent/CN1942478A/zh not_active Withdrawn
- 2005-04-12 MX MXPA06011882A patent/MXPA06011882A/es active IP Right Grant
- 2005-04-12 EP EP05735488A patent/EP1735321B1/de not_active Expired - Lifetime
- 2005-04-12 CA CA002562962A patent/CA2562962A1/en not_active Abandoned
- 2005-04-12 DK DK05735488T patent/DK1735321T3/da active
-
2008
- 2008-09-29 US US12/240,230 patent/US7625726B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1735321A1 (de) | 2006-12-27 |
| PL1735321T3 (pl) | 2009-04-30 |
| ES2313328T3 (es) | 2009-03-01 |
| DK1735321T3 (da) | 2009-01-12 |
| CA2562962A1 (en) | 2005-11-10 |
| US20050234087A1 (en) | 2005-10-20 |
| CN1942478A (zh) | 2007-04-04 |
| DE602005010228D1 (de) | 2008-11-20 |
| BRPI0509810A (pt) | 2007-09-18 |
| US7445916B2 (en) | 2008-11-04 |
| MXPA06011882A (es) | 2006-12-14 |
| EP1735321B1 (de) | 2008-10-08 |
| US20090029426A1 (en) | 2009-01-29 |
| US7625726B2 (en) | 2009-12-01 |
| WO2005105812A1 (en) | 2005-11-10 |
| JP2007532655A (ja) | 2007-11-15 |
| AU2005238432A1 (en) | 2005-11-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |