PE20071000A1 - Metodos para la preparacion de rapamicina cristalina y para la medicion de la cristalinidad de los compuestos de rapamicina utilizando calorimetria diferencial de barrido - Google Patents
Metodos para la preparacion de rapamicina cristalina y para la medicion de la cristalinidad de los compuestos de rapamicina utilizando calorimetria diferencial de barridoInfo
- Publication number
- PE20071000A1 PE20071000A1 PE2006001569A PE2006001569A PE20071000A1 PE 20071000 A1 PE20071000 A1 PE 20071000A1 PE 2006001569 A PE2006001569 A PE 2006001569A PE 2006001569 A PE2006001569 A PE 2006001569A PE 20071000 A1 PE20071000 A1 PE 20071000A1
- Authority
- PE
- Peru
- Prior art keywords
- rapamycin
- differential scanning
- scanning calorimetry
- crystallinity
- crystal
- 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 5
- 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 5
- 229960002930 sirolimus Drugs 0.000 title abstract 5
- 238000000113 differential scanning calorimetry Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 238000005259 measurement Methods 0.000 title 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 abstract 3
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[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 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 abstract 2
- 239000002245 particle Substances 0.000 abstract 2
- 229960000235 temsirolimus Drugs 0.000 abstract 2
- -1 RAPAMYCIN COMPOUND Chemical class 0.000 abstract 1
- 230000004927 fusion Effects 0.000 abstract 1
- 238000010438 heat treatment Methods 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
- QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N25/00—Investigating or analyzing materials by the use of thermal means
- G01N25/20—Investigating or analyzing materials by the use of thermal means by investigating the development of heat, i.e. calorimetry, e.g. by measuring specific heat, by measuring thermal conductivity
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- C07D498/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N25/00—Investigating or analyzing materials by the use of thermal means
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N25/00—Investigating or analyzing materials by the use of thermal means
- G01N25/20—Investigating or analyzing materials by the use of thermal means by investigating the development of heat, i.e. calorimetry, e.g. by measuring specific heat, by measuring thermal conductivity
- G01N25/48—Investigating or analyzing materials by the use of thermal means by investigating the development of heat, i.e. calorimetry, e.g. by measuring specific heat, by measuring thermal conductivity on solution, sorption, or a chemical reaction not involving combustion or catalytic oxidation
- G01N25/4846—Investigating or analyzing materials by the use of thermal means by investigating the development of heat, i.e. calorimetry, e.g. by measuring specific heat, by measuring thermal conductivity on solution, sorption, or a chemical reaction not involving combustion or catalytic oxidation for a motionless, e.g. solid sample
- G01N25/4866—Investigating or analyzing materials by the use of thermal means by investigating the development of heat, i.e. calorimetry, e.g. by measuring specific heat, by measuring thermal conductivity on solution, sorption, or a chemical reaction not involving combustion or catalytic oxidation for a motionless, e.g. solid sample by using a differential method
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Pathology (AREA)
- Analytical Chemistry (AREA)
- Physics & Mathematics (AREA)
- Engineering & Computer Science (AREA)
- General Physics & Mathematics (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Combustion & Propulsion (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analyzing Materials Using Thermal Means (AREA)
Abstract
SE REFIERE A UN PROCEDIMIENTO DE PURIFICACION DE RAPAMICINA DE PREFERENCIA CCI-779 (TEMSIROLIMUS) CRISTALINA QUE COMPRENDE: A) CALENTAR LA RAPAMICINA SIN PURIFICAR EN ACETATO DE ETILO A 55 C APROX. Y FILTRAR; B) AGREGAR HEPTANOS EN EL CURSO DE UN PERIODO DE 60 MINUTOS APROX. A VELOCIDAD CONSTANTE; C) REDUCIR LA VELOCIDAD DE AGITACION Y ENFRIAR EL PRODUCTO HASTA APROXIMADAMENTE 7 C A 8 C A DIFERENTES VELOCIDADES HASTA LLEGAR A 9 C/HORA; D) FILTRAR EL PRODUCTO PARA OBTENER DICHA RAPAMICINA CRISTALINA. REFERIDA TAMBIEN A UN METODO PARA MEDIR LA CALIDAD DE PARTICULA DE UN COMPUESTO DE RAPAMICINA UTILIZANDO CALORIMETRIA DIFERENCIAL DE BARRIDO DONDE LA CALIDAD DE PARTICULAS ES PROPORCIONAL A LA TEMPERATURA DE FUSION DE CALOR DE DICHA MUESTRA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74800505P | 2005-12-07 | 2005-12-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20071000A1 true PE20071000A1 (es) | 2007-10-10 |
Family
ID=38117222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006001569A PE20071000A1 (es) | 2005-12-07 | 2006-12-06 | Metodos para la preparacion de rapamicina cristalina y para la medicion de la cristalinidad de los compuestos de rapamicina utilizando calorimetria diferencial de barrido |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20070128731A1 (es) |
| EP (1) | EP1957964A2 (es) |
| JP (1) | JP2009518648A (es) |
| KR (1) | KR20080077147A (es) |
| CN (1) | CN101351702A (es) |
| AR (1) | AR058283A1 (es) |
| AU (1) | AU2006322030A1 (es) |
| BR (1) | BRPI0619592A2 (es) |
| CA (1) | CA2630786A1 (es) |
| CR (1) | CR9985A (es) |
| EC (1) | ECSP088519A (es) |
| IL (1) | IL191545A0 (es) |
| NO (1) | NO20082382L (es) |
| PE (1) | PE20071000A1 (es) |
| RU (1) | RU2008120712A (es) |
| TW (1) | TW200736603A (es) |
| WO (1) | WO2007067566A2 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2749807C (en) * | 2009-01-21 | 2015-09-29 | Biocon Limited | A method for determination of sirolimus stability and process for preparing its stable form |
| FR2943539B1 (fr) | 2009-03-31 | 2011-07-22 | Ethypharm Sa | Composition pharmaceutique comprenant un macrolide immunosuppresseur de la famille des limus. |
| WO2013022418A1 (en) * | 2011-08-05 | 2013-02-14 | Crucible Intellectual Property Llc | Nondestructive method to determine crystallinity in amorphous alloy |
| WO2013162501A1 (en) * | 2012-04-23 | 2013-10-31 | Apple Inc. | Non-destructive determination of volumetric crystallinity of bulk amorphous alloy |
| CN108864149B (zh) | 2013-03-15 | 2022-04-05 | 生物传感器国际集团有限公司 | 雷帕霉素衍生物的纯化 |
| US9439892B2 (en) | 2013-05-16 | 2016-09-13 | Surmodics, Inc. | Macrolide particulates, methods for preparation, and medical devices associated therewith |
| EP3007679B1 (en) * | 2013-06-12 | 2020-11-11 | SurModics, Inc. | Solvent methods for preparing crystalline macrolide particulates, compositions, and articles containing particulates |
| DE102013110294B4 (de) * | 2013-09-18 | 2016-07-07 | Innora Gmbh | Limus-Depot-Formulierung auf Ballonkathetern |
| WO2015181826A1 (en) | 2014-05-27 | 2015-12-03 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Crystalline coating and release of bioactive agents |
| CN105116013A (zh) * | 2015-04-23 | 2015-12-02 | 山东农业大学 | 一种确定金属离子对蛋白酶水解大豆分离蛋白影响的方法 |
| JP6531488B2 (ja) * | 2015-05-22 | 2019-06-19 | 日産自動車株式会社 | リチウムイオン二次電池の熱履歴検知方法 |
| US10098846B2 (en) | 2016-03-31 | 2018-10-16 | Surmodics, Inc. | Drug-containing particulate composition with cationic agent, associated medical devices, and methods for treatment |
| EP3554571B1 (en) | 2016-12-16 | 2024-11-13 | Surmodics, Inc. | Hydrophobic active agent particle coatings and methods for treatment |
| US11629222B2 (en) * | 2019-07-01 | 2023-04-18 | Ethicon, Inc. | Calorimetric crystallization method for evaluation of monomer purity |
| WO2023158308A1 (en) | 2022-02-18 | 2023-08-24 | Technische Universiteit Delft | Novel method for analyzing dsc data |
| NL2031004B1 (en) * | 2022-02-18 | 2023-09-05 | Univ Delft Tech | Novel method for analyzing DSC data |
| CN116794248A (zh) * | 2023-04-20 | 2023-09-22 | 广东省药品检验所(广东省药品质量研究所、广东省口岸药品检验所) | 一种防止压片过程中堵塞机器的共处理晶体辅料评价方法 |
| CN118706889A (zh) * | 2024-05-31 | 2024-09-27 | 瀚晖制药有限公司 | 一种阿帕他胺固体制剂结晶度的检测方法 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) * | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US5358909A (en) * | 1991-02-27 | 1994-10-25 | Nippon Steel Corporation | Method of manufacturing field-emitter |
| US5358908A (en) * | 1992-02-14 | 1994-10-25 | Micron Technology, Inc. | Method of creating sharp points and other features on the surface of a semiconductor substrate |
| GB9313650D0 (en) * | 1993-07-01 | 1993-08-18 | Glaxo Group Ltd | Method and apparatus for the formation of particles |
| US5385908A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered esters of rapamycin |
| US5385909A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
| US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| EP0884585A3 (de) * | 1997-06-06 | 1999-12-29 | Netzsch Gerätebau GmbH | Vorrichtung zur Differential-Scanning-Kalorimetrie |
| GB9826882D0 (en) * | 1998-12-07 | 1999-01-27 | Novartis Ag | Organic compounds |
| US6277983B1 (en) * | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| ES2177373B1 (es) * | 1999-11-26 | 2003-11-01 | Astur Pharma Sa | Preparacion de azitromicina en su forma no cristalina |
| DK1319008T3 (da) * | 2000-09-19 | 2009-02-09 | Wyeth Corp | Vandoplöselige rapamycinestere |
| KR20050037477A (ko) * | 2001-10-17 | 2005-04-22 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 로터-스테이터 장치와 입자 생성을 위한 방법 |
| US20060169199A1 (en) * | 2003-03-31 | 2006-08-03 | Vilmos Keri | Crystallization and purification of macrolides |
| PL1558622T3 (pl) * | 2003-07-24 | 2008-06-30 | Teva Gyogyszergyar Zartkoerueen Muekoedoe Reszvenytarsasag | Sposób oczyszczania makrolidów |
| KR20060057605A (ko) * | 2003-08-07 | 2006-05-26 | 와이어쓰 | Cci-779의 위치선택적 합성 방법 |
| AU2004270154A1 (en) * | 2003-09-03 | 2005-03-17 | Wyeth | Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and its pharmaceutical compositions containing the same |
| 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 |
| CA2562952A1 (en) * | 2004-04-14 | 2005-11-10 | Wyeth | Regiospecific synthesis of rapamycin 42-ester derivatives |
| CN1993368A (zh) * | 2004-08-10 | 2007-07-04 | 惠氏公司 | Cci-779衍生物和其制备方法 |
| AR052269A1 (es) * | 2004-12-20 | 2007-03-07 | Wyeth Corp | Analogos de rapamicina, un proceso para su elaboracion y los usos de los mismos en la preparacion de un medicamento para el tratamiento de trastornos neurologicos, proliferativos e inflamatorios. |
| RU2007119585A (ru) * | 2004-12-20 | 2009-01-27 | Вайет (Us) | Производные рапамицина и их применение при лечении неврологических заболеваний |
| RU2007129264A (ru) * | 2005-02-09 | 2009-03-20 | Вайет (Us) | Полиморф cci-779 и его применение |
| AU2006218916A1 (en) * | 2005-03-02 | 2006-09-08 | Wyeth | Recovery of CCI-779 from mother liquors |
| CN101137659A (zh) * | 2005-03-07 | 2008-03-05 | 惠氏公司 | 42-o-(2-羟基)乙基-雷帕霉素的氧杂环庚烷异构体 |
-
2006
- 2006-12-06 RU RU2008120712/28A patent/RU2008120712A/ru not_active Application Discontinuation
- 2006-12-06 CA CA002630786A patent/CA2630786A1/en not_active Abandoned
- 2006-12-06 US US11/634,694 patent/US20070128731A1/en not_active Abandoned
- 2006-12-06 EP EP06847503A patent/EP1957964A2/en not_active Withdrawn
- 2006-12-06 BR BRPI0619592A patent/BRPI0619592A2/pt not_active IP Right Cessation
- 2006-12-06 KR KR1020087013406A patent/KR20080077147A/ko not_active Withdrawn
- 2006-12-06 TW TW095145393A patent/TW200736603A/zh unknown
- 2006-12-06 AR ARP060105389A patent/AR058283A1/es unknown
- 2006-12-06 PE PE2006001569A patent/PE20071000A1/es not_active Application Discontinuation
- 2006-12-06 WO PCT/US2006/046445 patent/WO2007067566A2/en not_active Ceased
- 2006-12-06 CN CNA2006800461020A patent/CN101351702A/zh not_active Withdrawn
- 2006-12-06 AU AU2006322030A patent/AU2006322030A1/en not_active Abandoned
- 2006-12-06 JP JP2008544451A patent/JP2009518648A/ja active Pending
-
2008
- 2008-05-19 CR CR9985A patent/CR9985A/es not_active Application Discontinuation
- 2008-05-19 IL IL191545A patent/IL191545A0/en unknown
- 2008-05-26 NO NO20082382A patent/NO20082382L/no not_active Application Discontinuation
- 2008-06-09 EC EC2008008519A patent/ECSP088519A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CR9985A (es) | 2008-08-21 |
| TW200736603A (en) | 2007-10-01 |
| ECSP088519A (es) | 2008-07-30 |
| CN101351702A (zh) | 2009-01-21 |
| WO2007067566A2 (en) | 2007-06-14 |
| US20070128731A1 (en) | 2007-06-07 |
| IL191545A0 (en) | 2008-12-29 |
| CA2630786A1 (en) | 2007-06-14 |
| AR058283A1 (es) | 2008-01-30 |
| NO20082382L (no) | 2008-09-04 |
| RU2008120712A (ru) | 2010-01-20 |
| WO2007067566A3 (en) | 2008-01-24 |
| BRPI0619592A2 (pt) | 2016-09-06 |
| AU2006322030A1 (en) | 2007-06-14 |
| JP2009518648A (ja) | 2009-05-07 |
| EP1957964A2 (en) | 2008-08-20 |
| KR20080077147A (ko) | 2008-08-21 |
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