ATE411321T1 - Wasserlösliche rapamycin-ester - Google Patents
Wasserlösliche rapamycin-esterInfo
- Publication number
- ATE411321T1 ATE411321T1 AT01970890T AT01970890T ATE411321T1 AT E411321 T1 ATE411321 T1 AT E411321T1 AT 01970890 T AT01970890 T AT 01970890T AT 01970890 T AT01970890 T AT 01970890T AT E411321 T1 ATE411321 T1 AT E411321T1
- Authority
- AT
- Austria
- Prior art keywords
- water soluble
- soluble rapamycin
- rapamycin esters
- esters
- hydroxyesters
- 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 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010017533 Fungal infection Diseases 0.000 abstract 1
- 206010062016 Immunosuppression Diseases 0.000 abstract 1
- 208000031888 Mycoses Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 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 1
- 229960002930 sirolimus Drugs 0.000 abstract 1
- 238000002054 transplantation Methods 0.000 abstract 1
- 208000019553 vascular disease Diseases 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23377600P | 2000-09-19 | 2000-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE411321T1 true ATE411321T1 (de) | 2008-10-15 |
Family
ID=22878646
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT01970890T ATE411321T1 (de) | 2000-09-19 | 2001-09-13 | Wasserlösliche rapamycin-ester |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US6432973B1 (de) |
| EP (1) | EP1319008B1 (de) |
| JP (1) | JP2004509898A (de) |
| CN (1) | CN1222529C (de) |
| AT (1) | ATE411321T1 (de) |
| AU (1) | AU2001290841A1 (de) |
| BR (1) | BR0113975A (de) |
| CA (1) | CA2421485A1 (de) |
| DE (1) | DE60136200D1 (de) |
| DK (1) | DK1319008T3 (de) |
| ES (1) | ES2313983T3 (de) |
| MX (1) | MXPA03002258A (de) |
| WO (1) | WO2002024706A2 (de) |
Families Citing this family (47)
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|---|---|---|---|---|
| EP2298299A3 (de) * | 2000-01-14 | 2012-02-29 | The Trustees Of The University Of Pennsylvania | O-methylierte Rapamycinderivate zur Linderung und Verhinderung von lymphoproliferativen Erkrankungen |
| US6670355B2 (en) * | 2000-06-16 | 2003-12-30 | Wyeth | Method of treating cardiovascular disease |
| ATE427948T1 (de) * | 2001-04-24 | 2009-04-15 | Purdue Research Foundation | Folat-mimetika und deren folatrezeptorbindende konjugate |
| JP4547911B2 (ja) | 2002-02-01 | 2010-09-22 | アリアド・ファーマシューティカルズ・インコーポレイテッド | リン含有化合物およびその用途 |
| EP1504010B1 (de) * | 2002-05-15 | 2009-03-25 | Endocyte, Inc. | Vitamin-mitomycin-konjugate |
| PT1553940E (pt) * | 2002-07-30 | 2008-05-09 | Wyeth Corp | Formulações parentéricas contendo um hidroxi-éster de rapamicina |
| US7169594B2 (en) * | 2002-08-12 | 2007-01-30 | Regents Of The University Of Michigan | Diagnosis and treatment of diseases arising from defects in the tuberous sclerosis pathway |
| EP2517730A3 (de) | 2003-01-27 | 2013-01-02 | Endocyte, Inc. | Vitaminrezeptorbindende Wirkstofffreisetzungskonjugate |
| WO2004093918A2 (en) * | 2003-04-23 | 2004-11-04 | Wyeth Holdings Corporation | Peg-wortmannin conjugates |
| AR046194A1 (es) * | 2003-11-04 | 2005-11-30 | Mayo Foundation | Metodo de tratamiento del linfoma de celulas del manto |
| EP1689436A1 (de) * | 2003-11-26 | 2006-08-16 | Entelos, Inc. | BEHANDLUNG VON RHEUMATOIDER ARTHRITIS MIT HYPOXIE-INDUZIERBAREN FAKTOR a ANTAGONISTEN |
| AR047988A1 (es) * | 2004-03-11 | 2006-03-15 | Wyeth Corp | Combinaciones antineoplásicas de cci-779 y rituximab |
| CA2562952A1 (en) | 2004-04-14 | 2005-11-10 | Wyeth | Regiospecific synthesis of rapamycin 42-ester derivatives |
| BRPI0510277A (pt) * | 2004-04-27 | 2007-10-30 | Wyeth Corp | método para marcar especificamente uma rapamicina, rapamicina especificamente marcada, composição, e, kit |
| US8288557B2 (en) * | 2004-07-23 | 2012-10-16 | Endocyte, Inc. | Bivalent linkers and conjugates thereof |
| JP2008533007A (ja) * | 2005-03-07 | 2008-08-21 | ワイス | 42−o−(2−ヒドロキシ)エチル−ラパマイシンのオキセパン異性体 |
| JP5289935B2 (ja) * | 2005-03-16 | 2013-09-11 | エンドサイト,インコーポレイテッド | プテロイン酸およびその結合体の合成と精製 |
| EP2382995A3 (de) * | 2005-08-19 | 2013-09-25 | Endocyte, Inc. | Ligandenkonjugate von Vincaalkaloiden, Analoga und Derivaten |
| US8465724B2 (en) * | 2005-08-19 | 2013-06-18 | Endocyte, Inc. | Multi-drug ligand conjugates |
| 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 |
| WO2007067565A1 (en) | 2005-12-07 | 2007-06-14 | Wyeth | Process for the preparation of purified crystalline cci-779 |
| 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 |
| 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 |
| US20080207671A1 (en) * | 2006-07-31 | 2008-08-28 | The Regents Of The University Of Michigan | Diagnosis and treatment of diseases arising from defects in the tuberous sclerosis pathway |
| TW200824713A (en) * | 2006-10-18 | 2008-06-16 | Wyeth Corp | Processes for the synthesis of individual isomers of mono-PEG CCI-779 |
| US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| 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 |
| 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 |
| US8414909B2 (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 |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| WO2008094181A2 (en) * | 2007-02-01 | 2008-08-07 | The Regents Of The University Of Michigan | Compositions and methods for detecting, preventing and treating seizures and seizure related disorders |
| US20100104626A1 (en) * | 2007-02-16 | 2010-04-29 | Endocyte, Inc. | Methods and compositions for treating and diagnosing kidney disease |
| CN101678124A (zh) * | 2007-03-14 | 2010-03-24 | 恩多塞特公司 | 结合配体连接的微管溶素递药缀合物 |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| CN101784565B (zh) * | 2007-06-25 | 2014-12-10 | 恩多塞特公司 | 含有亲水性间隔区接头的共轭物 |
| CA2703491C (en) | 2007-10-25 | 2017-06-13 | Endocyte, Inc. | Tubulysins and processes for preparing |
| WO2010024898A2 (en) | 2008-08-29 | 2010-03-04 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| 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 |
| WO2013126797A1 (en) | 2012-02-24 | 2013-08-29 | Purdue Research Foundation | Cholecystokinin b receptor targeting for imaging and therapy |
| US20140080175A1 (en) | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
| AU2013331440A1 (en) | 2012-10-16 | 2015-04-30 | Endocyte, Inc. | Drug delivery conjugates containing unnatural amino acids and methods for using |
| JP6770008B2 (ja) | 2016-05-10 | 2020-10-14 | 浙江海正薬業股▲ふん▼有限公司Zhejiang Hisun Pharmaceutical CO.,LTD. | 水溶性ラパマイシン誘導体 |
| WO2019184993A1 (zh) * | 2018-03-29 | 2019-10-03 | 天津键凯科技有限公司 | 聚乙二醇与雷帕霉素的结合物及其用途 |
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|---|---|---|---|---|
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| US3993749A (en) | 1974-04-12 | 1976-11-23 | Ayerst Mckenna And Harrison Ltd. | Rapamycin and process of preparation |
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| US4885171A (en) | 1978-11-03 | 1989-12-05 | American Home Products Corporation | Use of rapamycin in treatment of certain tumors |
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| US4650803A (en) | 1985-12-06 | 1987-03-17 | University Of Kansas | Prodrugs of rapamycin |
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| US5496832A (en) | 1995-03-09 | 1996-03-05 | American Home Products Corporation | Method of treating cardiac inflammatory disease |
| US5780462A (en) * | 1995-12-27 | 1998-07-14 | American Home Products Corporation | Water soluble rapamycin esters |
| US5989591A (en) | 1997-03-14 | 1999-11-23 | American Home Products Corporation | Rapamycin formulations for oral administration |
| US5985325A (en) | 1997-06-13 | 1999-11-16 | American Home Products Corporation | Rapamycin formulations for oral administration |
-
2001
- 2001-09-13 ES ES01970890T patent/ES2313983T3/es not_active Expired - Lifetime
- 2001-09-13 CA CA002421485A patent/CA2421485A1/en not_active Abandoned
- 2001-09-13 WO PCT/US2001/028575 patent/WO2002024706A2/en not_active Ceased
- 2001-09-13 DK DK01970890T patent/DK1319008T3/da active
- 2001-09-13 MX MXPA03002258A patent/MXPA03002258A/es active IP Right Grant
- 2001-09-13 AU AU2001290841A patent/AU2001290841A1/en not_active Abandoned
- 2001-09-13 AT AT01970890T patent/ATE411321T1/de not_active IP Right Cessation
- 2001-09-13 JP JP2002529116A patent/JP2004509898A/ja not_active Withdrawn
- 2001-09-13 CN CNB018159117A patent/CN1222529C/zh not_active Expired - Fee Related
- 2001-09-13 BR BR0113975-4A patent/BR0113975A/pt not_active IP Right Cessation
- 2001-09-13 DE DE60136200T patent/DE60136200D1/de not_active Expired - Fee Related
- 2001-09-13 EP EP01970890A patent/EP1319008B1/de not_active Expired - Lifetime
- 2001-09-18 US US09/954,782 patent/US6432973B1/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1319008A2 (de) | 2003-06-18 |
| WO2002024706A3 (en) | 2002-10-10 |
| US20020055518A1 (en) | 2002-05-09 |
| MXPA03002258A (es) | 2003-06-24 |
| CN1222529C (zh) | 2005-10-12 |
| US6432973B1 (en) | 2002-08-13 |
| CA2421485A1 (en) | 2002-03-28 |
| JP2004509898A (ja) | 2004-04-02 |
| WO2002024706A2 (en) | 2002-03-28 |
| DE60136200D1 (de) | 2008-11-27 |
| DK1319008T3 (da) | 2009-02-09 |
| ES2313983T3 (es) | 2009-03-16 |
| AU2001290841A1 (en) | 2002-04-02 |
| EP1319008B1 (de) | 2008-10-15 |
| CN1460108A (zh) | 2003-12-03 |
| BR0113975A (pt) | 2003-07-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |