MX9306730A - Carbamatos de alcoxicarbonil y arilcarbonil de rapamicina y composicion farmaceutica que los contiene. - Google Patents
Carbamatos de alcoxicarbonil y arilcarbonil de rapamicina y composicion farmaceutica que los contiene.Info
- Publication number
- MX9306730A MX9306730A MX9306730A MX9306730A MX9306730A MX 9306730 A MX9306730 A MX 9306730A MX 9306730 A MX9306730 A MX 9306730A MX 9306730 A MX9306730 A MX 9306730A MX 9306730 A MX9306730 A MX 9306730A
- Authority
- MX
- Mexico
- Prior art keywords
- carbamates
- image
- arycarbonyl
- rapamicine
- alcoxycarbonyl
- Prior art date
Links
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
- A61P31/10—Antimycotics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
- Oncology (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención proporciona carbamatos de N-arilcarbonilo y N-alcoxicarbonilo de rapamicina de la fórmula mostrada en lo siguiente, en la que (Ver Fórmula); R1 es C-N-C-A Y R2 es H o CCH2(R4)2 o (Ver Fórmula); R1 y R2 son ambos -C-N-C-A y en donde A es alcoxi inferior o arilo o heteroarilo, R3 es H o metilo y R4 es alquilo de C1-C6, alquenilo C2-C6 o alquinilo C2-C6 que poseen actividad inmunosupresora y/o antifúngica y/o antitumoral y/o antiinflamatoria in vitro y/o inhibir la proliferación de timocito in vivo. Estos compuestos se espera que sean útiles en el tratamiento de rechazo a transplantes, enfermedades autoinmunes, infecciones por hongos, cáncer y enfermedades de inflamación.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US07/968,115 US5262423A (en) | 1992-10-29 | 1992-10-29 | Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents |
Publications (1)
Publication Number | Publication Date |
---|---|
MX9306730A true MX9306730A (es) | 1994-06-30 |
Family
ID=25513757
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX9306730A MX9306730A (es) | 1992-10-29 | 1993-10-28 | Carbamatos de alcoxicarbonil y arilcarbonil de rapamicina y composicion farmaceutica que los contiene. |
Country Status (12)
Country | Link |
---|---|
US (1) | US5262423A (es) |
EP (1) | EP0666861B1 (es) |
JP (1) | JPH08502748A (es) |
AT (1) | ATE166653T1 (es) |
AU (1) | AU5322294A (es) |
CA (1) | CA2148247A1 (es) |
DE (1) | DE69318846T2 (es) |
DK (1) | DK0666861T3 (es) |
ES (1) | ES2116471T3 (es) |
MX (1) | MX9306730A (es) |
TW (1) | TW239136B (es) |
WO (1) | WO1994010176A1 (es) |
Families Citing this family (84)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5480989A (en) * | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
US5480988A (en) * | 1992-10-13 | 1996-01-02 | American Home Products Corporation | Carbamates of rapamycin |
US5489680A (en) * | 1992-10-13 | 1996-02-06 | American Home Products Corporation | Carbamates of rapamycin |
US5434260A (en) * | 1992-10-13 | 1995-07-18 | American Home Products Corporation | Carbamates of rapamycin |
US5349060A (en) * | 1993-01-07 | 1994-09-20 | American Home Products Corporation | Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents |
US20020099067A1 (en) * | 1993-07-08 | 2002-07-25 | Ulrich Posanski | Pharmaceutical compositions for sparingly soluble therapeutic agents |
US5527907A (en) * | 1993-11-19 | 1996-06-18 | Abbott Laboratories | Macrolide immunomodulators |
WO1995014023A1 (en) * | 1993-11-19 | 1995-05-26 | Abbott Laboratories | Semisynthetic analogs of rapamycin (macrolides) being immunomodulators |
JP3745772B2 (ja) * | 1993-12-17 | 2006-02-15 | ノバルティス アクチエンゲゼルシャフト | 免疫抑制剤として有用なラパマイシン誘導体 |
US5525610A (en) * | 1994-03-31 | 1996-06-11 | American Home Products Corporation | 42-Epi-rapamycin and pharmaceutical compositions thereof |
US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
US5463048A (en) * | 1994-06-14 | 1995-10-31 | American Home Products Corporation | Rapamycin amidino carbamates |
DK0833828T3 (da) * | 1995-06-09 | 2003-03-17 | Novartis Ag | Rapamycinderivater |
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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JP2004509898A (ja) | 2000-09-19 | 2004-04-02 | ワイス | 水溶性ラパマイシンエステル |
US6399625B1 (en) | 2000-09-27 | 2002-06-04 | Wyeth | 1-oxorapamycins |
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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DK1553940T3 (da) | 2002-07-30 | 2008-06-02 | Wyeth Corp | Patenterale formuleringer indeholdende en rapamycin-hydroxyester |
WO2004060283A2 (en) | 2002-12-16 | 2004-07-22 | Nitromed, Inc. | Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use |
US7160867B2 (en) * | 2003-05-16 | 2007-01-09 | Isotechnika, Inc. | Rapamycin carbohydrate derivatives |
US7445916B2 (en) * | 2004-04-14 | 2008-11-04 | Wyeth | Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies |
CA2562164A1 (en) * | 2004-04-27 | 2005-11-10 | Wyeth | Labeling of rapamycin using rapamycin-specific methylases |
US20110104186A1 (en) | 2004-06-24 | 2011-05-05 | Nicholas Valiante | Small molecule immunopotentiators and assays for their detection |
KR20070070184A (ko) * | 2004-10-28 | 2007-07-03 | 와이어쓰 | 자궁근종의 치료에 있어서 mTOR 억제제의 용도 |
ES2663495T3 (es) * | 2005-02-18 | 2018-04-13 | Abraxis Bioscience, Llc | Fármacos con hidrofobicidad mejorada para incorporación en dispositivos médicos |
GB0503936D0 (en) * | 2005-02-25 | 2005-04-06 | San Raffaele Centro Fond | Method |
SI1912675T1 (sl) | 2005-07-25 | 2014-07-31 | Emergent Product Development Seattle, Llc | zmanjšanje števila celic B z uporabo molekul, ki se specifično vežejo na CD37 in CD20 |
AU2006311877A1 (en) | 2005-11-04 | 2007-05-18 | Wyeth Llc | Antineoplastic combinations with mTOR inhibitor, herceptin, and/orHKI-272 |
US20080051691A1 (en) * | 2006-08-28 | 2008-02-28 | Wyeth | Implantable shunt or catheter enabling gradual delivery of therapeutic agents |
US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
US9737640B2 (en) | 2006-11-20 | 2017-08-22 | Lutonix, Inc. | Drug releasing coatings for medical devices |
US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
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 |
US8414526B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids |
US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
US8414909B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
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US20100048914A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
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PT2132228E (pt) | 2008-04-11 | 2011-10-11 | Emergent Product Dev Seattle | Imunoterapia de cd37 e sua combinação com um quimioterápico bifuncional |
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PT2365802T (pt) | 2008-11-11 | 2017-11-14 | Univ Texas | Microcápsulas de rapamicina e utilização para o tratamento de cancro |
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US9283211B1 (en) | 2009-11-11 | 2016-03-15 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
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US9896730B2 (en) | 2011-04-25 | 2018-02-20 | OSI Pharmaceuticals, LLC | Use of EMT gene signatures in cancer drug discovery, diagnostics, and treatment |
EP2532740A1 (en) | 2011-06-11 | 2012-12-12 | Michael Schmück | Antigen-specific CD4+ and CD8+ central-memory T cell preparations for adoptive T cell therapy |
US20150290176A1 (en) | 2012-10-12 | 2015-10-15 | The Board Of Regents Of The University Of Texas System | Use of mtor inhibitors to treat vascular cognitive impairment |
US20150258127A1 (en) | 2012-10-31 | 2015-09-17 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for preventing antiphospholipid syndrome (aps) |
WO2014160328A1 (en) | 2013-03-13 | 2014-10-02 | The Board Of Regents Of The University Of Texas System | Mtor inhibitors for prevention of intestinal polyp growth |
EP2968370A4 (en) | 2013-03-14 | 2016-09-21 | Univ Maryland | AGENT FOR ANDROGEN RECEPTOR DOWNWARD CONTROL AND USES THEREOF |
BR112016002970A2 (pt) | 2013-08-12 | 2017-09-12 | Tokai Pharmaceuticals Inc | biomarcadores para o tratamento de distúrbios neoplásicos que usa terapias direcionadas ao androgênio |
US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
EP3089737B1 (en) | 2013-12-31 | 2021-11-03 | Rapamycin Holdings, LLC | Oral rapamycin nanoparticle preparations and use |
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CA2968049A1 (en) | 2014-04-16 | 2015-10-22 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
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CN114007665A (zh) | 2019-04-11 | 2022-02-01 | 因柯利尔疗法公司 | 改善脑脊液的方法及其装置和系统 |
EP4370160A1 (en) | 2021-07-15 | 2024-05-22 | President And Fellows Of Harvard College | Compositions and methods relating to cells with adhered particles |
CN115160343B (zh) * | 2022-06-09 | 2023-11-14 | 福建省微生物研究所 | 一种雷帕霉素衍生物及其制备方法和应用 |
WO2024008799A1 (en) | 2022-07-06 | 2024-01-11 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of proliferative glomerulonephritis |
WO2024028433A1 (en) | 2022-08-04 | 2024-02-08 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of lymphoproliferative disorders |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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 |
JPH05504956A (ja) * | 1990-03-12 | 1993-07-29 | 藤沢薬品工業株式会社 | トリシクロ化合物 |
PT98990A (pt) * | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
US5080899A (en) * | 1991-02-22 | 1992-01-14 | American Home Products Corporation | Method of treating pulmonary inflammation |
US5078999A (en) * | 1991-02-22 | 1992-01-07 | American Home Products Corporation | Method of treating systemic lupus erythematosus |
US5118678A (en) * | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
US5091389A (en) * | 1991-04-23 | 1992-02-25 | Merck & Co., Inc. | Lipophilic macrolide useful as an immunosuppressant |
US5118677A (en) * | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
-
1992
- 1992-10-29 US US07/968,115 patent/US5262423A/en not_active Expired - Lifetime
-
1993
- 1993-08-21 TW TW082106771A patent/TW239136B/zh active
- 1993-10-06 AU AU53222/94A patent/AU5322294A/en not_active Abandoned
- 1993-10-06 EP EP93923284A patent/EP0666861B1/en not_active Expired - Lifetime
- 1993-10-06 AT AT93923284T patent/ATE166653T1/de not_active IP Right Cessation
- 1993-10-06 ES ES93923284T patent/ES2116471T3/es not_active Expired - Lifetime
- 1993-10-06 WO PCT/US1993/009552 patent/WO1994010176A1/en active IP Right Grant
- 1993-10-06 DK DK93923284T patent/DK0666861T3/da active
- 1993-10-06 JP JP6511079A patent/JPH08502748A/ja not_active Ceased
- 1993-10-06 CA CA002148247A patent/CA2148247A1/en not_active Abandoned
- 1993-10-06 DE DE69318846T patent/DE69318846T2/de not_active Expired - Fee Related
- 1993-10-28 MX MX9306730A patent/MX9306730A/es not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
DK0666861T3 (da) | 1998-11-09 |
DE69318846T2 (de) | 1999-01-28 |
US5262423A (en) | 1993-11-16 |
CA2148247A1 (en) | 1994-05-11 |
DE69318846D1 (en) | 1998-07-02 |
ES2116471T3 (es) | 1998-07-16 |
ATE166653T1 (de) | 1998-06-15 |
JPH08502748A (ja) | 1996-03-26 |
AU5322294A (en) | 1994-05-24 |
EP0666861A1 (en) | 1995-08-16 |
WO1994010176A1 (en) | 1994-05-11 |
TW239136B (es) | 1995-01-21 |
EP0666861B1 (en) | 1998-05-27 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant or registration | ||
HC | Change of company name or juridical status |
Owner name: PQ SILICAS UK LIMITED |
|
MM | Annulment or lapse due to non-payment of fees |