ES2189768T3 - Sintesis regioselectiva de derivados de rapamicina. - Google Patents
Sintesis regioselectiva de derivados de rapamicina.Info
- Publication number
- ES2189768T3 ES2189768T3 ES00966904T ES00966904T ES2189768T3 ES 2189768 T3 ES2189768 T3 ES 2189768T3 ES 00966904 T ES00966904 T ES 00966904T ES 00966904 T ES00966904 T ES 00966904T ES 2189768 T3 ES2189768 T3 ES 2189768T3
- Authority
- ES
- Spain
- Prior art keywords
- regional
- rapamycin
- rapamycin derivatives
- silyl ether
- elementary synthesis
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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 5
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 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 4
- 229960002930 sirolimus Drugs 0.000 abstract 4
- 239000002253 acid 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)
- Transplantation (AREA)
- Hematology (AREA)
- Oncology (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 |
|---|---|
| ES2189768T3 true ES2189768T3 (es) | 2003-07-16 |
Family
ID=23617953
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES00966904T Expired - Lifetime ES2189768T3 (es) | 1999-09-29 | 2000-09-27 | Sintesis regioselectiva de derivados de rapamicina. |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP1216251B1 (enExample) |
| JP (1) | JP4289813B2 (enExample) |
| KR (1) | KR100754236B1 (enExample) |
| CN (1) | CN1176925C (enExample) |
| AR (1) | AR029181A1 (enExample) |
| AT (1) | ATE233269T1 (enExample) |
| AU (1) | AU782234B2 (enExample) |
| BR (1) | BR0014433A (enExample) |
| CA (1) | CA2385461C (enExample) |
| CZ (1) | CZ300368B6 (enExample) |
| DE (1) | DE60001510T2 (enExample) |
| DK (1) | DK1216251T3 (enExample) |
| EA (1) | EA004331B1 (enExample) |
| ES (1) | ES2189768T3 (enExample) |
| HK (1) | HK1044774B (enExample) |
| HU (1) | HUP0202609A3 (enExample) |
| IL (2) | IL148542A0 (enExample) |
| MX (1) | MXPA02003243A (enExample) |
| NO (1) | NO20021360L (enExample) |
| NZ (1) | NZ517644A (enExample) |
| PL (1) | PL200899B1 (enExample) |
| TW (1) | TWI256395B (enExample) |
| WO (1) | WO2001023395A2 (enExample) |
| ZA (1) | ZA200201918B (enExample) |
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 |
| EP1660081A1 (en) | 2003-09-03 | 2006-05-31 | Wyeth | Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and pharmaceutical compositions containing the same |
| AR046194A1 (es) | 2003-11-04 | 2005-11-30 | Mayo Foundation | Metodo de tratamiento del linfoma de celulas del manto |
| KR20070015544A (ko) * | 2004-04-14 | 2007-02-05 | 와이어쓰 | 라파마이신 42-에스테르 유도체의 위치특이성 합성 |
| EP1751168A1 (en) | 2004-04-14 | 2007-02-14 | 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 |
| TW200616633A (en) | 2004-08-10 | 2006-06-01 | Wyeth Corp | CCI-779 derivatives and methods of making same |
| NZ556673A (en) | 2005-02-03 | 2010-03-26 | Gen Hospital Corp | Method for treating gefitinib and/or erlotinib resistant cancer with an EGFR inhibitor |
| JP2008530090A (ja) | 2005-02-09 | 2008-08-07 | ワイス | Ｃｃｉ−７７９多形及びその使用 |
| EP3488866A1 (en) | 2005-11-04 | 2019-05-29 | Wyeth LLC | 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 |
| ES2531322T3 (es) | 2008-06-17 | 2015-03-13 | Wyeth Llc | Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina |
| 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 |
| AU2011210227A1 (en) * | 2010-01-28 | 2012-08-30 | 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 |
| RU2603261C2 (ru) * | 2011-04-01 | 2016-11-27 | Сандоз Аг | Региоселективное ацилирование рапамицина в положении с-42 |
| 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 |
| JP6942141B2 (ja) * | 2016-03-14 | 2021-09-29 | ウイスコンシン アラムニ リサーチ ファンデーション | 抗がん効能を高めたオリゴ乳酸複合体及びミセル |
| 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 |
| US10980784B2 (en) | 2018-06-15 | 2021-04-20 | 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 |
| EP4069223A4 (en) | 2019-12-05 | 2023-12-20 | Janssen Pharmaceutica NV | RAPAMYCIN ANALOGS AND THEIR USES |
| 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 CA CA002385461A patent/CA2385461C/en not_active Expired - Fee Related
- 2000-09-27 CN CNB008163685A patent/CN1176925C/zh not_active Expired - Fee Related
- 2000-09-27 CZ CZ20021136A patent/CZ300368B6/cs not_active IP Right Cessation
- 2000-09-27 DK DK00966904T patent/DK1216251T3/da active
- 2000-09-27 WO PCT/US2000/026445 patent/WO2001023395A2/en not_active Ceased
- 2000-09-27 HK HK02106469.7A patent/HK1044774B/en not_active IP Right Cessation
- 2000-09-27 AU AU77182/00A patent/AU782234B2/en not_active Ceased
- 2000-09-27 ES ES00966904T patent/ES2189768T3/es not_active Expired - Lifetime
- 2000-09-27 HU HU0202609A patent/HUP0202609A3/hu unknown
- 2000-09-27 EP EP00966904A patent/EP1216251B1/en not_active Expired - Lifetime
- 2000-09-27 EA EA200200412A patent/EA004331B1/ru not_active IP Right Cessation
- 2000-09-27 IL IL14854200A patent/IL148542A0/xx active IP Right Grant
- 2000-09-27 NZ NZ517644A patent/NZ517644A/en unknown
- 2000-09-27 KR KR1020027004033A patent/KR100754236B1/ko not_active Expired - Fee Related
- 2000-09-27 BR BR0014433-9A patent/BR0014433A/pt not_active IP Right Cessation
- 2000-09-27 DE DE60001510T patent/DE60001510T2/de not_active Expired - Lifetime
- 2000-09-27 MX MXPA02003243A patent/MXPA02003243A/es active IP Right Grant
- 2000-09-27 AT AT00966904T patent/ATE233269T1/de not_active IP Right Cessation
- 2000-09-27 PL PL354461A patent/PL200899B1/pl not_active IP Right Cessation
- 2000-09-27 AR ARP000105064A patent/AR029181A1/es unknown
- 2000-09-27 JP JP2001526545A patent/JP4289813B2/ja 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/NO20021360L/no not_active Application Discontinuation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2124373T3 (es) | Procedimiento para la preparacion de derivados del acido n-acil-n,n',n'-etilendiamintriacetico. | |
| SV1996000026A (es) | Benzociclopentano oxazolidinonas que contienen heteroatomos | |
| BR9906287A (pt) | Bactéria pertencente ao gênero escherichia e que tem uma capacidade para produzir um l-aminoácido, e, processo para produzir um l-aminoácido | |
| BR0111206A (pt) | Derivados de arilmetilamina para uso como inibidores de triptase | |
| BRPI0010891A (pt) | geração de microespuma terapêutica. | |
| BR0011489A (pt) | Composições formadoras de pelìcula compreendendo amidos modificados e iota-carragenano e processos para a fabricação de cápsulas macias usando as mesmas | |
| IL147184A0 (en) | Substituted benzimidazole | |
| ZA89233B (en) | Topical metronidazole formulations and therapeutic uses thereof | |
| BR0015622A (pt) | Processo de limpeza que utiliza ondas ultra-sÈnicas | |
| ZA9710796B (en) | Oxyiminopregnanecarbolactones. | |
| BR0110751A (pt) | Dispositivo | |
| PT1109812E (pt) | Pirrolobenzodiazepinas | |
| AR079399A2 (es) | Procedimientos para preparar bifenazato | |
| ES2192680T3 (es) | Nuevos derivados de vitamina d con sustituyentes carbo- o heterociclicos en c-25, procedimiento para su preparacion, productos intermedios y la utilizacion para la preparacion de medicamentos. | |
| NO20032371L (no) | Makrolidsolvater | |
| MY117381A (en) | Use of 1-hydroxy-2-pyridone for the treatment of seborrheic dermatitis | |
| MXPA03001081A (es) | Medicamento anti-inflamatorio. | |
| NO20023276D0 (no) | Fremgangsmåte til å fremstille betulinsyre | |
| YU5893A (sh) | Sulfonilkarbamid i postupak za njegovo dobijanje | |
| YU13499A (sh) | Primena 1-hidroksi-2-piridona za lečenje seboroitičnog dermatitisa | |
| ES2134184T3 (es) | Empleo de etisterona para el tratamiento topico del acne o de la alopecia androgenetica. | |
| AR022017A1 (es) | Un agente para tratar el trastorno de la funcion de las celulas visuales. el metodo de tratamiento y el uso de dicho agente para la produccion de unacomposicion farmaceutica | |
| ES2166800T3 (es) | Procedimiento para la preparacion de o,s-acetales de 2,2-difluoroceteno sililo y o,s-esteres del acido alfa,alfa-difluoro-beta-sililoxi-1,3-dioxolan-4-propanoico. | |
| NZ510116A (en) | Tricyclic delta-3-piperidines as pharmaceuticals | |
| BR0013799A (pt) | Processo para a preparação de um composto, e, composto |