CA2067541A1 - Reduction products of rapamycin - Google Patents

Reduction products of rapamycin

Info

Publication number
CA2067541A1
CA2067541A1 CA002067541A CA2067541A CA2067541A1 CA 2067541 A1 CA2067541 A1 CA 2067541A1 CA 002067541 A CA002067541 A CA 002067541A CA 2067541 A CA2067541 A CA 2067541A CA 2067541 A1 CA2067541 A1 CA 2067541A1
Authority
CA
Canada
Prior art keywords
rapamycin
reduction products
reduction
diseases
hydroxyrapamycin
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.)
Granted
Application number
CA002067541A
Other languages
French (fr)
Other versions
CA2067541C (en
Inventor
Craig E. Caufield
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wyeth LLC
Original Assignee
Craig E. Caufield
American Home Products Corporation
Wyeth
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Craig E. Caufield, American Home Products Corporation, Wyeth filed Critical Craig E. Caufield
Publication of CA2067541A1 publication Critical patent/CA2067541A1/en
Application granted granted Critical
Publication of CA2067541C publication Critical patent/CA2067541C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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

Abstract

Reduction of rapamycin with DIBAL furnishes either the 15-hydroxyrapamycin or 15,27-bis(hydroxy)rapamycin, depending upon the reaction conditions, having the general structure (see formula I) where Y is -CO- or -CH(OH)-.

The compounds of this invention are useful in treating transplant rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, and fungal infections.
CA002067541A 1991-05-07 1992-04-29 Reduction products of rapamycin Expired - Fee Related CA2067541C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US696,692 1991-05-07
US07/696,692 US5102876A (en) 1991-05-07 1991-05-07 Reduction products of rapamycin

Publications (2)

Publication Number Publication Date
CA2067541A1 true CA2067541A1 (en) 1992-11-08
CA2067541C CA2067541C (en) 2003-06-10

Family

ID=24798163

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002067541A Expired - Fee Related CA2067541C (en) 1991-05-07 1992-04-29 Reduction products of rapamycin

Country Status (3)

Country Link
US (1) US5102876A (en)
CA (1) CA2067541C (en)
ZA (1) ZA923245B (en)

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5378696A (en) * 1990-09-19 1995-01-03 American Home Products Corporation Rapamycin esters
US5776943A (en) * 1991-05-14 1998-07-07 American Home Products Corporation Rapamycin metabolites
US5286731A (en) * 1991-09-17 1994-02-15 American Home Products Corporation Method of treating immunoinflammatory bowel disease
GB9125660D0 (en) * 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
US5177203A (en) * 1992-03-05 1993-01-05 American Home Products Corporation Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
AU3922493A (en) * 1992-04-07 1993-11-08 Dana-Farber Cancer Institute, Inc. Inhibition of P70 S6 kinase
ZA935111B (en) * 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) * 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
MX9304868A (en) * 1992-08-13 1994-05-31 American Home Prod 27-HYDROXYRAPAMICINE, DERIVED FROM THE SAME AND PHARMACEUTICAL COMPOSITION THAT CONTAINS IT.
US5256790A (en) * 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
CA2106034A1 (en) * 1992-09-24 1994-03-25 Ralph J. Russo 21-norrapamycin
US5489680A (en) * 1992-10-13 1996-02-06 American Home Products Corporation Carbamates of rapamycin
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
US5434260A (en) * 1992-10-13 1995-07-18 American Home Products Corporation Carbamates of rapamycin
US5258389A (en) * 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5260300A (en) 1992-11-19 1993-11-09 American Home Products Corporation Rapamycin carbonate esters as immuno-suppressant agents
US5349060A (en) * 1993-01-07 1994-09-20 American Home Products Corporation Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents
AU6087894A (en) * 1993-01-14 1994-08-15 Cell Therapeutics, Inc. Acetal or ketal substituted therapeutic compounds
US5252579A (en) * 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
US5310903A (en) * 1993-03-05 1994-05-10 Merck & Co., Inc. Imidazolidyl rapamycin derivatives
US5310901A (en) * 1993-03-05 1994-05-10 Merck & Co., Inc. O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynlheteroarylrapamycin derivatives
US5504091A (en) * 1993-04-23 1996-04-02 American Home Products Corporation Biotin esters of rapamycin
EP1181938B1 (en) 1993-04-23 2007-11-14 Wyeth Rapamycin conjugates and antibodies
US7279561B1 (en) * 1993-04-23 2007-10-09 Wyeth Anti-rapamycin monoclonal antibodies
USRE37421E1 (en) 1993-07-16 2001-10-23 Smithkline Beecham Corporation Rapamycin derivatives
US5387680A (en) * 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5536729A (en) * 1993-09-30 1996-07-16 American Home Products Corporation Rapamycin formulations for oral administration
US5391730A (en) * 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5373014A (en) * 1993-10-08 1994-12-13 American Home Products Corporation Rapamycin oximes
US5378836A (en) * 1993-10-08 1995-01-03 American Home Products Corporation Rapamycin oximes and hydrazones
JP4105761B2 (en) * 1993-11-19 2008-06-25 アボット・ラボラトリーズ Semi-synthetic analog immunomodulator of rapamycin (macrolide)
US5527907A (en) * 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5385910A (en) * 1993-11-22 1995-01-31 American Home Products Corporation Gem-distributed esters of rapamycin
US5385909A (en) * 1993-11-22 1995-01-31 American Home Products Corporation Heterocyclic esters of rapamycin
US5385908A (en) * 1993-11-22 1995-01-31 American Home Products Corporation Hindered esters of rapamycin
US5389639A (en) * 1993-12-29 1995-02-14 American Home Products Company Amino alkanoic esters of rapamycin
US5362735A (en) * 1994-02-23 1994-11-08 Smithkline Beecham Corporation Rapamycin derivatives
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
US5491231A (en) * 1994-11-28 1996-02-13 American Home Products Corporation Hindered N-oxide esters of rapamycin
US5563145A (en) * 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines
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
US6015809A (en) * 1998-08-17 2000-01-18 American Home Products Corporation Photocyclized rapamycin
US6790228B2 (en) * 1999-12-23 2004-09-14 Advanced Cardiovascular Systems, Inc. Coating for implantable devices and a method of forming the same
US7807211B2 (en) 1999-09-03 2010-10-05 Advanced Cardiovascular Systems, Inc. Thermal treatment of an implantable medical device
US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
ES2313983T3 (en) 2000-09-19 2009-03-16 Wyeth RAPAMYCIN HYDROSOLUBLE ESTERS.
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
US7349971B2 (en) * 2004-02-05 2008-03-25 Scenera Technologies, Llc System for transmitting data utilizing multiple communication applications simultaneously in response to user request without specifying recipient's communication information
EP1768662A2 (en) 2004-06-24 2007-04-04 Novartis Vaccines and Diagnostics, Inc. Small molecule immunopotentiators and assays for their detection
PA8641501A1 (en) * 2004-08-10 2006-09-08 Wyeth Corp DERIVATIVES OF CCI-779 AND METHOD FOR PREPARATION
US8313763B2 (en) * 2004-10-04 2012-11-20 Tolmar Therapeutics, Inc. Sustained delivery formulations of rapamycin compounds
WO2006041942A2 (en) * 2004-10-04 2006-04-20 Qlt Usa, Inc. Ocular delivery of polymeric delivery formulations
US8414526B2 (en) * 2006-11-20 2013-04-09 Lutonix, Inc. Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
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
US8414910B2 (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
US8414525B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8430055B2 (en) * 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
JP2008305262A (en) * 2007-06-08 2008-12-18 Konica Minolta Business Technologies Inc Printer introduction method in server and thin client environment
ES2645692T3 (en) 2008-11-11 2017-12-07 The Board Of Regents,The University Of Texas System Rapamycin microcapsules and their use for cancer treatment
US20170079962A1 (en) 2009-11-11 2017-03-23 Rapamycin Holdings, Llc Oral Rapamycin Preparation and Use for Stomatitus
US10391059B2 (en) 2009-11-11 2019-08-27 Rapamycin Holdings, Inc. Oral rapamycin nanoparticle preparations and use
US9283211B1 (en) 2009-11-11 2016-03-15 Rapamycin Holdings, Llc Oral rapamycin preparation and use for stomatitis
WO2013013708A1 (en) 2011-07-26 2013-01-31 Fundació Institut D'investigació Biomèdica De Bellvitge Treatment of acute rejection in renal transplant
CN104203959B (en) 2012-06-08 2017-09-15 百多力股份公司 The O cyclic hydrocarbons ester of rapamycin 40, composition and method
US9750728B2 (en) 2012-09-29 2017-09-05 Targeted Therapeutics, Llc Method and pharmaceutical composition for inhibiting PI3K/AKT/mTOR signaling pathway
CN103705925B (en) 2012-09-29 2018-03-30 段磊 Suppress the drug regimen of PI3K/AKT/mTOR signal paths
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
US20160030401A1 (en) 2013-03-13 2016-02-04 The Board Of Regents Of The University Of Texas System Use of mtor inhibitors for prevention of intestinal polyp growth and cancer
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
EP3624863B1 (en) 2017-05-15 2021-04-14 C.R. Bard, Inc. Medical device with drug-eluting coating and intermediate layer
JP7262581B2 (en) 2018-11-14 2023-04-21 ルトニックス，インコーポレーテッド Medical device with drug eluting coating on modified device surface
JP2022528966A (en) 2019-04-08 2022-06-16 バード・ペリフェラル・バスキュラー・インコーポレーテッド Medical device with drug elution coating on modified device surface

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
ZA923245B (en) 1993-11-05
US5102876A (en) 1992-04-07
CA2067541C (en) 2003-06-10

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