ES2158959T3 - N-oxido esteres de la rapamicina impedidos y su utilizacion como medicamentos. - Google Patents
N-oxido esteres de la rapamicina impedidos y su utilizacion como medicamentos.Info
- Publication number
- ES2158959T3 ES2158959T3 ES95941467T ES95941467T ES2158959T3 ES 2158959 T3 ES2158959 T3 ES 2158959T3 ES 95941467 T ES95941467 T ES 95941467T ES 95941467 T ES95941467 T ES 95941467T ES 2158959 T3 ES2158959 T3 ES 2158959T3
- Authority
- ES
- Spain
- Prior art keywords
- sup
- oxide
- esteres
- rapamycin
- impeded
- 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
- 239000003814 drug Substances 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 title 1
- 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 1
- 229960002930 sirolimus Drugs 0.000 title 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 230000000843 anti-fungal effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 229940121375 antifungal agent Drugs 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 239000002131 composite material Substances 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 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
- 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
- A61P31/04—Antibacterial agents
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
UN COMPUESTO CON LA ESTRUCTURA (I), EN LA QUE R Y R 1 SON CADA UNO, INDEPENDIENTEMENTE, (A), (B), O HIDROGENO; R{SUP,2} Y R{SUP,3} SON CADA UNO, INDEPENDIENTEMENTE, ALQUILO, ARILALQUILO, O R{SUP,2} Y R{SUP,3} PUEDEN FORMAR CONJUNTAMENTE UN ANILLO CICLOALQUILO; R{SUP,4} ES UN RADICAL N - OXIDO HETEROCICLICO, OPCIONALMENTE SUSTITUIDO; R{SUP,5} ES ALQUILO O ARILALQUILO; R{SUP,6} Y R{SUP,7} FORMAN CONJUNTAMENTE UN N - OXIDO N - ALQUIL - HETEROCICLICO SATURADO, QUE OPCIONALMENTE PUEDE ESTAR SUSTITUIDO: K= 0-1, M= 0,1; N= 1-6; CON LA CONDICION DE QUE R Y R{SUP,1} NO SEAN AMBOS HIDROGENO, QUE ES UTIL COMO AGENTE INMUNOSUPRESOR, ANTIINFLAMATORIO, ANTIFUNGICO, ANTIPROLIFERATIVO Y ANTITUMORAL.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/345,972 US5491231A (en) | 1994-11-28 | 1994-11-28 | Hindered N-oxide esters of rapamycin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2158959T3 true ES2158959T3 (es) | 2001-09-16 |
Family
ID=23357367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES95941467T Expired - Lifetime ES2158959T3 (es) | 1994-11-28 | 1995-11-22 | N-oxido esteres de la rapamicina impedidos y su utilizacion como medicamentos. |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US5491231A (es) |
| EP (1) | EP0794955B1 (es) |
| JP (1) | JPH10509977A (es) |
| KR (1) | KR100377278B1 (es) |
| AT (1) | ATE203539T1 (es) |
| AU (1) | AU712998B2 (es) |
| BR (1) | BR9509825A (es) |
| CA (1) | CA2205577A1 (es) |
| DE (1) | DE69521907T2 (es) |
| DK (1) | DK0794955T3 (es) |
| ES (1) | ES2158959T3 (es) |
| FI (1) | FI972240A0 (es) |
| GR (1) | GR3036712T3 (es) |
| HU (1) | HUT77139A (es) |
| MX (1) | MX9703893A (es) |
| NZ (1) | NZ297661A (es) |
| PT (1) | PT794955E (es) |
| WO (1) | WO1996016967A1 (es) |
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| US5780462A (en) * | 1995-12-27 | 1998-07-14 | American Home Products Corporation | Water soluble rapamycin esters |
| US5922730A (en) * | 1996-09-09 | 1999-07-13 | American Home Products Corporation | Alkylated rapamycin derivatives |
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| US6015809A (en) * | 1998-08-17 | 2000-01-18 | American Home Products Corporation | Photocyclized rapamycin |
| US6331547B1 (en) | 1999-08-18 | 2001-12-18 | American Home Products Corporation | Water soluble SDZ RAD esters |
| US6277983B1 (en) | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
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| US8236048B2 (en) | 2000-05-12 | 2012-08-07 | Cordis Corporation | Drug/drug delivery systems for the prevention and treatment of vascular disease |
| US6670355B2 (en) * | 2000-06-16 | 2003-12-30 | Wyeth | Method of treating cardiovascular disease |
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| CA2421485A1 (en) | 2000-09-19 | 2002-03-28 | Wyeth | Water soluble rapamycin esters |
| US6399625B1 (en) | 2000-09-27 | 2002-06-04 | Wyeth | 1-oxorapamycins |
| AU9486901A (en) * | 2000-09-29 | 2002-04-08 | Cordis Corp | Coated medical devices |
| US6399626B1 (en) | 2000-10-02 | 2002-06-04 | Wyeth | Hydroxyesters of 7-desmethylrapamycin |
| US6440991B1 (en) | 2000-10-02 | 2002-08-27 | Wyeth | Ethers of 7-desmethlrapamycin |
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| AU2003254168A1 (en) | 2002-07-30 | 2004-02-16 | Wyeth | Parenteral formulations containing a rapamycin hydroxyester |
| WO2004060283A2 (en) | 2002-12-16 | 2004-07-22 | Nitromed, Inc. | Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| ZA737247B (en) * | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US3993749A (en) * | 1974-04-12 | 1976-11-23 | Ayerst Mckenna And Harrison Ltd. | Rapamycin and process of preparation |
| US4885171A (en) * | 1978-11-03 | 1989-12-05 | American Home Products Corporation | Use of rapamycin in treatment of certain tumors |
| US4316885A (en) * | 1980-08-25 | 1982-02-23 | Ayerst, Mckenna And Harrison, Inc. | Acyl derivatives of rapamycin |
| US4401653A (en) * | 1981-03-09 | 1983-08-30 | Ayerst, Mckenna & Harrison Inc. | Combination of rapamycin and picibanil for the treatment of tumors |
| US4375464A (en) * | 1981-11-19 | 1983-03-01 | Ayerst, Mckenna & Harrison Inc. | Antibiotic AY24,668 and process of preparation |
| US4650803A (en) * | 1985-12-06 | 1987-03-17 | University Of Kansas | Prodrugs of rapamycin |
| US5100899A (en) * | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
| US5023264A (en) * | 1990-07-16 | 1991-06-11 | American Home Products Corporation | Rapamycin oximes |
| US5023263A (en) * | 1990-08-09 | 1991-06-11 | American Home Products Corporation | 42-oxorapamycin |
| US5023262A (en) * | 1990-08-14 | 1991-06-11 | American Home Products Corporation | Hydrogenated rapamycin derivatives |
| US5221670A (en) * | 1990-09-19 | 1993-06-22 | American Home Products Corporation | Rapamycin esters |
| US5130307A (en) * | 1990-09-28 | 1992-07-14 | American Home Products Corporation | Aminoesters of rapamycin |
| US5233036A (en) * | 1990-10-16 | 1993-08-03 | American Home Products Corporation | Rapamycin alkoxyesters |
| US5078999A (en) * | 1991-02-22 | 1992-01-07 | American Home Products Corporation | Method of treating systemic lupus erythematosus |
| US5080899A (en) * | 1991-02-22 | 1992-01-14 | American Home Products Corporation | Method of treating pulmonary inflammation |
| US5120842A (en) * | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| IL101353A0 (en) * | 1991-04-03 | 1992-11-15 | American Home Prod | Pharmaceutical compositions for treating diabetes |
| 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 |
| US5194447A (en) * | 1992-02-18 | 1993-03-16 | American Home Products Corporation | Sulfonylcarbamates of rapamycin |
| US5091389A (en) * | 1991-04-23 | 1992-02-25 | Merck & Co., Inc. | Lipophilic macrolide useful as an immunosuppressant |
| US5102876A (en) * | 1991-05-07 | 1992-04-07 | American Home Products Corporation | Reduction products of rapamycin |
| US5138051A (en) * | 1991-08-07 | 1992-08-11 | American Home Products Corporation | Rapamycin analogs as immunosuppressants and antifungals |
| US5118677A (en) * | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
| US5169851A (en) * | 1991-08-07 | 1992-12-08 | American Home Products Corporation | Rapamycin analog as immunosuppressants and antifungals |
| US5151413A (en) * | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| US5177203A (en) * | 1992-03-05 | 1993-01-05 | American Home Products Corporation | Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents |
| US5302584A (en) * | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
| US5260300A (en) * | 1992-11-19 | 1993-11-09 | American Home Products Corporation | Rapamycin carbonate esters as immuno-suppressant agents |
| US5373014A (en) * | 1993-10-08 | 1994-12-13 | American Home Products Corporation | Rapamycin oximes |
| 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 |
| US5385910A (en) * | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Gem-distributed esters of rapamycin |
-
1994
- 1994-11-28 US US08/345,972 patent/US5491231A/en not_active Expired - Lifetime
-
1995
- 1995-05-24 US US08/448,843 patent/US5559122A/en not_active Expired - Lifetime
- 1995-05-24 US US08/449,168 patent/US5508285A/en not_active Expired - Lifetime
- 1995-05-24 US US08/449,167 patent/US5508290A/en not_active Expired - Lifetime
- 1995-05-24 US US08/450,769 patent/US5521194A/en not_active Expired - Lifetime
- 1995-11-22 DE DE69521907T patent/DE69521907T2/de not_active Expired - Fee Related
- 1995-11-22 MX MX9703893A patent/MX9703893A/es not_active IP Right Cessation
- 1995-11-22 AU AU42877/96A patent/AU712998B2/en not_active Ceased
- 1995-11-22 CA CA002205577A patent/CA2205577A1/en not_active Abandoned
- 1995-11-22 WO PCT/US1995/015318 patent/WO1996016967A1/en not_active Ceased
- 1995-11-22 ES ES95941467T patent/ES2158959T3/es not_active Expired - Lifetime
- 1995-11-22 JP JP8518953A patent/JPH10509977A/ja not_active Withdrawn
- 1995-11-22 DK DK95941467T patent/DK0794955T3/da active
- 1995-11-22 KR KR1019970703519A patent/KR100377278B1/ko not_active Expired - Fee Related
- 1995-11-22 EP EP95941467A patent/EP0794955B1/en not_active Expired - Lifetime
- 1995-11-22 AT AT95941467T patent/ATE203539T1/de not_active IP Right Cessation
- 1995-11-22 PT PT95941467T patent/PT794955E/pt unknown
- 1995-11-22 BR BR9509825A patent/BR9509825A/pt active Search and Examination
- 1995-11-22 NZ NZ297661A patent/NZ297661A/xx unknown
- 1995-11-22 HU HU9701851A patent/HUT77139A/hu unknown
-
1997
- 1997-05-27 FI FI972240A patent/FI972240A0/fi unknown
-
2001
- 2001-09-26 GR GR20010401569T patent/GR3036712T3/el not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| US5559122A (en) | 1996-09-24 |
| FI972240A7 (fi) | 1997-05-27 |
| GR3036712T3 (en) | 2001-12-31 |
| HK1002281A1 (en) | 1998-08-14 |
| FI972240A0 (fi) | 1997-05-27 |
| KR100377278B1 (ko) | 2003-10-04 |
| WO1996016967A1 (en) | 1996-06-06 |
| HUT77139A (hu) | 1998-03-02 |
| US5521194A (en) | 1996-05-28 |
| PT794955E (pt) | 2001-12-28 |
| ATE203539T1 (de) | 2001-08-15 |
| AU4287796A (en) | 1996-06-19 |
| DK0794955T3 (da) | 2001-09-24 |
| CA2205577A1 (en) | 1996-06-06 |
| DE69521907D1 (de) | 2001-08-30 |
| EP0794955A1 (en) | 1997-09-17 |
| US5491231A (en) | 1996-02-13 |
| DE69521907T2 (de) | 2001-11-29 |
| EP0794955B1 (en) | 2001-07-25 |
| JPH10509977A (ja) | 1998-09-29 |
| AU712998B2 (en) | 1999-11-18 |
| MX9703893A (es) | 1997-08-30 |
| US5508290A (en) | 1996-04-16 |
| BR9509825A (pt) | 1997-09-30 |
| US5508285A (en) | 1996-04-16 |
| NZ297661A (en) | 2000-01-28 |
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