AR029181A1 - Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter - Google Patents
Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eterInfo
- Publication number
- AR029181A1 AR029181A1 ARP000105064A ARP000105064A AR029181A1 AR 029181 A1 AR029181 A1 AR 029181A1 AR P000105064 A ARP000105064 A AR P000105064A AR P000105064 A ARP000105064 A AR P000105064A AR 029181 A1 AR029181 A1 AR 029181A1
- Authority
- AR
- Argentina
- Prior art keywords
- rapamycin
- ether
- silil
- eter
- intermediate compound
- Prior art date
Links
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical class 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 8
- 238000000034 method Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 8
- 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 abstract 7
- 229960002930 sirolimus Drugs 0.000 abstract 7
- 239000002253 acid Substances 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 230000003301 hydrolyzing effect Effects 0.000 abstract 2
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40883099A | 1999-09-29 | 1999-09-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR029181A1 true AR029181A1 (es) | 2003-06-18 |
Family
ID=23617953
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP000105064A AR029181A1 (es) | 1999-09-29 | 2000-09-27 | Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP1216251B1 (https=) |
| JP (1) | JP4289813B2 (https=) |
| KR (1) | KR100754236B1 (https=) |
| CN (1) | CN1176925C (https=) |
| AR (1) | AR029181A1 (https=) |
| AT (1) | ATE233269T1 (https=) |
| AU (1) | AU782234B2 (https=) |
| BR (1) | BR0014433A (https=) |
| CA (1) | CA2385461C (https=) |
| CZ (1) | CZ300368B6 (https=) |
| DE (1) | DE60001510T2 (https=) |
| DK (1) | DK1216251T3 (https=) |
| EA (1) | EA004331B1 (https=) |
| ES (1) | ES2189768T3 (https=) |
| HK (1) | HK1044774B (https=) |
| HU (1) | HUP0202609A3 (https=) |
| IL (2) | IL148542A0 (https=) |
| MX (1) | MXPA02003243A (https=) |
| NO (1) | NO20021360D0 (https=) |
| NZ (1) | NZ517644A (https=) |
| PL (1) | PL200899B1 (https=) |
| TW (1) | TWI256395B (https=) |
| WO (1) | WO2001023395A2 (https=) |
| ZA (1) | ZA200201918B (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070032853A1 (en) | 2002-03-27 | 2007-02-08 | Hossainy Syed F | 40-O-(2-hydroxy)ethyl-rapamycin coated stent |
| US20050118344A1 (en) | 2003-12-01 | 2005-06-02 | Pacetti Stephen D. | Temperature controlled crimping |
| UA84881C2 (ru) * | 2003-09-03 | 2008-12-10 | Уайт | Аморфный 42-эфир рапамицина и 3-гидрокси-2-(гидроксиметил)-2-метилпропионовой кислоты и фармацевтическая композиция, содержащая его |
| AR046194A1 (es) | 2003-11-04 | 2005-11-30 | Mayo Foundation | Metodo de tratamiento del linfoma de celulas del manto |
| 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 |
| 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 |
| CA2577011A1 (en) | 2004-08-10 | 2006-04-13 | Wyeth | Cci-779 derivatives and methods of making same |
| KR101313702B1 (ko) | 2005-02-03 | 2013-10-04 | 와이어쓰 | 제피티니브 및/또는 에를로티니브 내성암 치료용 약제학적 조성물 |
| CA2595766A1 (en) | 2005-02-09 | 2006-08-17 | Wyeth | Cci-779 polymorph and use thereof |
| EP1942937A1 (en) | 2005-11-04 | 2008-07-16 | Wyeth | Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272 |
| US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| BRPI0914790A2 (pt) | 2008-06-17 | 2015-10-20 | Wyeth Llc | uso de um composto de vinorelbina e um composto de hki-272, composição farmacêutica e produto e kit para o tratamento de neoplasma |
| CN101676291B (zh) | 2008-09-18 | 2012-05-09 | 上海海和药物研究开发有限公司 | 一类雷帕霉素碳酸酯类似物、其药物组合物及其制备方法和用途 |
| WO2011092564A2 (en) * | 2010-01-28 | 2011-08-04 | Fresenius Kabi Oncology Ltd | Process for the preparation of temsirolimus and its intermediates |
| CN102020662B (zh) | 2011-01-07 | 2013-02-13 | 天津市炜杰科技有限公司 | 一种驮瑞塞尔制备方法 |
| WO2012131019A1 (en) * | 2011-04-01 | 2012-10-04 | Sandoz Ag | Regioselective acylation of rapamycin at the c-42 position |
| CN103421023B (zh) * | 2013-07-30 | 2015-09-23 | 福建省微生物研究所 | 一种替西罗莫司的合成工艺 |
| CN104086564B (zh) * | 2014-07-30 | 2019-02-05 | 江苏奥赛康药业股份有限公司 | 一种高纯度坦罗莫司的制备方法 |
| CN106146536B (zh) * | 2015-04-25 | 2019-07-26 | 山东新时代药业有限公司 | 一种依维莫司的制备方法 |
| WO2017158499A1 (en) * | 2016-03-14 | 2017-09-21 | Wisconsin Alumni Research Foundation | Oligolactic acid conjugates and micelles with enhanced anticancer efficacy |
| CN107561170B (zh) * | 2016-07-02 | 2021-07-30 | 山东新时代药业有限公司 | 一种坦西莫司中间体的分析检测方法 |
| CN108948045A (zh) * | 2017-05-20 | 2018-12-07 | 鲁南制药集团股份有限公司 | 一种替西罗莫司的制备方法 |
| CN108948046B (zh) * | 2017-05-20 | 2020-11-10 | 鲁南制药集团股份有限公司 | 一种替西罗莫司的中间体及其制备方法 |
| CN109206441B (zh) * | 2017-06-30 | 2022-05-20 | 正大天晴药业集团股份有限公司 | 一种依维莫司的纯化方法 |
| CN109776570A (zh) * | 2017-11-14 | 2019-05-21 | 上海医药工业研究院 | 一种依维莫司中间体、其制备方法及其应用 |
| WO2019241789A1 (en) | 2018-06-15 | 2019-12-19 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| CN109369679A (zh) * | 2018-12-24 | 2019-02-22 | 江苏卓和药业有限公司 | 一种雷帕霉素的精制方法 |
| CN109851626B (zh) * | 2019-01-08 | 2021-11-02 | 扬子江药业集团四川海蓉药业有限公司 | 一种替西罗莫司的分离纯化方法 |
| AU2020397938A1 (en) | 2019-12-05 | 2022-06-23 | Janssen Pharmaceutica Nv | Rapamycin analogs and uses thereof |
| CN113372359A (zh) * | 2020-03-10 | 2021-09-10 | 鲁南制药集团股份有限公司 | 一种坦西莫司的制备方法 |
| CN114106014B (zh) * | 2020-08-27 | 2024-03-15 | 鲁南制药集团股份有限公司 | 一种依维莫司的制备方法 |
| CN115028658A (zh) * | 2022-07-06 | 2022-09-09 | 国药集团川抗制药有限公司 | 雷帕霉素硅醇酯及其制备方法和应用 |
| GB202415232D0 (en) | 2024-10-16 | 2024-11-27 | Nacamed As | Composition |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5120842A (en) * | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5387680A (en) * | 1993-08-10 | 1995-02-07 | American Home Products Corporation | C-22 ring stabilized rapamycin derivatives |
| US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| US5563145A (en) * | 1994-12-07 | 1996-10-08 | American Home Products Corporation | Rapamycin 42-oximes and hydroxylamines |
-
2000
- 2000-09-14 TW TW089118799A patent/TWI256395B/zh active
- 2000-09-27 ES ES00966904T patent/ES2189768T3/es not_active Expired - Lifetime
- 2000-09-27 WO PCT/US2000/026445 patent/WO2001023395A2/en not_active Ceased
- 2000-09-27 JP JP2001526545A patent/JP4289813B2/ja not_active Expired - Fee Related
- 2000-09-27 AT AT00966904T patent/ATE233269T1/de not_active IP Right Cessation
- 2000-09-27 CZ CZ20021136A patent/CZ300368B6/cs not_active IP Right Cessation
- 2000-09-27 CN CNB008163685A patent/CN1176925C/zh not_active Expired - Fee Related
- 2000-09-27 PL PL354461A patent/PL200899B1/pl not_active IP Right Cessation
- 2000-09-27 BR BR0014433-9A patent/BR0014433A/pt not_active IP Right Cessation
- 2000-09-27 HU HU0202609A patent/HUP0202609A3/hu unknown
- 2000-09-27 IL IL14854200A patent/IL148542A0/xx active IP Right Grant
- 2000-09-27 AR ARP000105064A patent/AR029181A1/es unknown
- 2000-09-27 DE DE60001510T patent/DE60001510T2/de not_active Expired - Lifetime
- 2000-09-27 DK DK00966904T patent/DK1216251T3/da active
- 2000-09-27 CA CA002385461A patent/CA2385461C/en not_active Expired - Fee Related
- 2000-09-27 AU AU77182/00A patent/AU782234B2/en not_active Ceased
- 2000-09-27 MX MXPA02003243A patent/MXPA02003243A/es active IP Right Grant
- 2000-09-27 EA EA200200412A patent/EA004331B1/ru not_active IP Right Cessation
- 2000-09-27 NZ NZ517644A patent/NZ517644A/en unknown
- 2000-09-27 HK HK02106469.7A patent/HK1044774B/en not_active IP Right Cessation
- 2000-09-27 EP EP00966904A patent/EP1216251B1/en not_active Expired - Lifetime
- 2000-09-27 KR KR1020027004033A patent/KR100754236B1/ko not_active Expired - Fee Related
-
2002
- 2002-03-06 IL IL148542A patent/IL148542A/en not_active IP Right Cessation
- 2002-03-07 ZA ZA200201918A patent/ZA200201918B/en unknown
- 2002-03-19 NO NO20021360A patent/NO20021360D0/no not_active Application Discontinuation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR029181A1 (es) | Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter | |
| NZ523957A (en) | 6.alpha., 9.alpha.-difluoro-17.alpha.-'(2-furanylcarboxyl) oxy!-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4-diene-17-carbothioic acid S-fluoromethyl ester as an anti-inflammatory agent | |
| DE60226229D1 (de) | En derivaten | |
| ATE20894T1 (de) | Aus einheiten mit glucosamin- und uronsaeurestrukturen gebildete disaccharide, ihre herstellung und biologische anwendung. | |
| DK76889D0 (da) | Fremgangsmaade til fremstilling af organiske forbindelser | |
| DE60222273D1 (de) | Befeuchtungsmittel und dieses enthaltende kosmetika und topische präparate | |
| MX215587B (es) | Procedimiento para preparar plastificadores de ester. | |
| MY127751A (en) | Process for the preparation of dihydroxy esters and derivatives thereof | |
| FI942794A7 (fi) | Entsymaattinen hydrolyysimenetelmä C-10- ja C-13-asemaan liittyvän hydroksyyliryhmän sisältävien taksaanien valmistamiseksi, entsymaattinen ester¦intimenetelmä C-10-asemaan liittyvän asyylioksiryhmän sisältävien taksaanien valmistamiseksi ja mainittujen yhdisteiden käytt¦ | |
| ITMI941594A0 (it) | Procedimento di preparazione di acido ialuronico mediante fermentazione con streptococcus | |
| ATE204587T1 (de) | Wässrige vernetzbare beschichtungszusammensetzungen | |
| FI971912A0 (fi) | Menetelmä tärkkelysestereiden valmistamiseksi, tärkkelysesterit ja tärkkelysesterikoostumukset | |
| ES2150705T3 (es) | Derivados de ester de nitrito esteroideos utiles como farmacos antiinflamatorios. | |
| BR9915223A (pt) | Processo para a preparação contìnua de ésteres alquìlicos de ácido (met) acrìlico | |
| CO4840512A1 (es) | Derivados fluorados de la vitamina d3 posiciones farmaceuticas elaboradas a partir de estos deriva dos. | |
| NO20023276L (no) | Fremgangsmåter fremstilling av betulinsyre | |
| ES2183585T3 (es) | Procedimiento para la preparacion de derivados de (s) -3-4-dihidroxibutirico opticamente puros. | |
| DE50011097D1 (de) | PVC-haltiges Material | |
| WO1996003413B1 (en) | Regioselective sulfation | |
| DE60020130D1 (de) | Verfahren zur herstellung 3-amino-gallensaurer derivate | |
| WO1996003413A3 (en) | Regioselective sulfation | |
| FI941432A0 (fi) | Menetelmä puolisynteettisten glydosaminoglykaanien valmistamiseksi, jotka sisältävät nukleofiilisillä radikaaleilla 3-asemassa substituoitua alfa-L-galakturonihappoa | |
| ES2189169T3 (es) | Procedimiento de reduccion de alfa-amino cetonas. | |
| IT1261828B (it) | Esteri di acil l-carnitine e composizioni farmaceutiche che li contengono per il trattamento dello shock endotossico. | |
| BR9916648A (pt) | Processo para preparar ésteres glioxìlicos ou seus hidratos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |