NO20065090L - Regiospesifikk syntese av rapamycin 42-esterderivater - Google Patents

Regiospesifikk syntese av rapamycin 42-esterderivater

Info

Publication number
NO20065090L
NO20065090L NO20065090A NO20065090A NO20065090L NO 20065090 L NO20065090 L NO 20065090L NO 20065090 A NO20065090 A NO 20065090A NO 20065090 A NO20065090 A NO 20065090A NO 20065090 L NO20065090 L NO 20065090L
Authority
NO
Norway
Prior art keywords
rapamycin
region
specific synthesis
ester derivatives
ester
Prior art date
Application number
NO20065090A
Other languages
English (en)
Inventor
Ping Cai
Jianxin Gu
Markus Edward Ruppen
Original Assignee
Wyeth Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34965235&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO20065090(L) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of NO20065090L publication Critical patent/NO20065090L/no

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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • 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
    • 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
    • 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/16—Hydrolases (3) acting on ester bonds (3.1)
    • C12N9/18—Carboxylic ester hydrolases (3.1.1)
    • C12N9/20—Triglyceride splitting, e.g. by means of lipase
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
    • C12P17/188—Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Fremgangsmåte for regiospesifikk syntese av rapamycin 42-esterderivater er beskrevet. Fremgangsmåten innbefatter lipase-katalysert acylering av 42-hydroksyrapamycin med en acyldonor så som en vinylester, en isopropenylester eller et anhydrid i et egnet organisk løsningsmiddel.
NO20065090A 2004-04-14 2006-11-03 Regiospesifikk syntese av rapamycin 42-esterderivater NO20065090L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56192604P 2004-04-14 2004-04-14
PCT/US2005/012266 WO2005105811A1 (en) 2004-04-14 2005-04-12 Regiospecific synthesis of rapamycin 42-ester derivatives

Publications (1)

Publication Number Publication Date
NO20065090L true NO20065090L (no) 2006-11-13

Family

ID=34965235

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20065090A NO20065090L (no) 2004-04-14 2006-11-03 Regiospesifikk syntese av rapamycin 42-esterderivater

Country Status (23)

Country Link
US (1) US7268144B2 (no)
EP (1) EP1737869A1 (no)
JP (1) JP4224115B2 (no)
KR (1) KR20070015544A (no)
CN (1) CN1942476A (no)
AR (1) AR049019A1 (no)
AU (1) AU2005238431A1 (no)
BR (1) BRPI0509852A (no)
CA (1) CA2562952A1 (no)
CL (1) CL2008000507A1 (no)
CR (1) CR8646A (no)
EC (1) ECSP066927A (no)
GT (1) GT200500085A (no)
IL (1) IL178315A0 (no)
MX (1) MXPA06011881A (no)
NO (1) NO20065090L (no)
PA (1) PA8629901A1 (no)
PE (1) PE20060253A1 (no)
RU (1) RU2387657C2 (no)
SG (1) SG152234A1 (no)
TW (1) TW200536542A (no)
UA (1) UA87492C2 (no)
WO (1) WO2005105811A1 (no)

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NZ537829A (en) 2002-07-30 2006-09-29 Wyeth Corp Parenteral formulations containing a rapamycin hydroxyester
AU2005238432A1 (en) * 2004-04-14 2005-11-10 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
MX2007001676A (es) * 2004-08-10 2007-04-12 Wyeth Corp Derivados de 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionico y metodos para hacer los mismos.
CA2595766A1 (en) * 2005-02-09 2006-08-17 Wyeth Cci-779 polymorph and use thereof
WO2007056175A2 (en) * 2005-11-04 2007-05-18 Wyeth 41-methoxy isotope labeled rapamycin 42-ester
US7622578B2 (en) * 2005-12-07 2009-11-24 Wyeth Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate
AR058282A1 (es) * 2005-12-07 2008-01-30 Wyeth Corp Forma cristalina purificada de cci-779, un proceso para la preparacion del mismo, un metodo para monitorear la cristalizacion del cci-779, un kit y una composicion farmaceutica que lo comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer.
BRPI0619592A2 (pt) * 2005-12-07 2016-09-06 Wyeth Corp métodos para medir a qualidade da partícula de um composto de rapamicina, para determinar o tamanho de partícula médio de uma amostra e a cristalinidade de um composto de rapamicina, e para a purificação de rapamicina
MX2008011458A (es) * 2006-03-07 2008-09-24 Wyeth Corp Procedimiento para preparar conjugados de polietilenglicol solubles en agua de inmunosupresores de macrolidos.
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US8414525B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8414526B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids
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
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8414909B2 (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
US8430055B2 (en) 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
US8414910B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
TW200845960A (en) * 2007-04-05 2008-12-01 Wyeth Corp Wortmannin-rapalog conjugate and uses thereof
US20090253733A1 (en) * 2008-04-02 2009-10-08 Biointeractions, Ltd. Rapamycin carbonate esters
US20110098241A1 (en) * 2008-04-14 2011-04-28 Poniard Pharmaceuticals, Inc. Rapamycin analogs as anti-cancer agents
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
EP2365802B1 (en) 2008-11-11 2017-08-02 The Board of Regents,The University of Texas System Microcapsules of rapamycin and use for treating cancer
IT1394309B1 (it) * 2009-05-22 2012-06-06 Poli Ind Chimica Spa Nuovo approccio chimico-enzimatico alla sintesi del pimecrolimus
US9283211B1 (en) 2009-11-11 2016-03-15 Rapamycin Holdings, Llc Oral rapamycin preparation and use for stomatitis
MX2013011412A (es) * 2011-04-01 2014-04-30 Sandoz Ag Acilacion regioselectiva de rapamicina en la posicion c-42.
US10751450B2 (en) 2012-06-08 2020-08-25 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
US9408884B2 (en) * 2012-06-08 2016-08-09 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
EP2968281B1 (en) 2013-03-13 2020-08-05 The Board of Regents of The University of Texas System Mtor inhibitors for prevention of intestinal polyp growth
ES2897473T3 (es) * 2013-03-15 2022-03-01 Biosensors Int Group Ltd Purificación de derivados de la rapamicina
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
AU2014373683B2 (en) 2013-12-31 2020-05-07 Rapamycin Holdings, Llc Oral rapamycin nanoparticle preparations and use
EP4014967A1 (en) 2016-04-29 2022-06-22 Icahn School of Medicine at Mount Sinai Targeting the innate immunesystem to induce long-term tolerance and to resolve macrophage accumulation in atherosclerosis
US11225487B2 (en) 2017-02-17 2022-01-18 Trevena, Inc. 7-membered aza-heterocyclic containing δ-opioid receptor modulating compounds, methods of using and making the same
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Also Published As

Publication number Publication date
TW200536542A (en) 2005-11-16
US20050234234A1 (en) 2005-10-20
KR20070015544A (ko) 2007-02-05
RU2006134014A (ru) 2008-05-20
RU2387657C2 (ru) 2010-04-27
JP2007532134A (ja) 2007-11-15
WO2005105811A1 (en) 2005-11-10
GT200500085A (es) 2005-11-03
CL2008000507A1 (es) 2008-07-04
AU2005238431A1 (en) 2005-11-10
IL178315A0 (en) 2007-02-11
UA87492C2 (en) 2009-07-27
EP1737869A1 (en) 2007-01-03
ECSP066927A (es) 2006-12-20
AR049019A1 (es) 2006-06-21
SG152234A1 (en) 2009-05-29
CR8646A (es) 2007-08-28
CN1942476A (zh) 2007-04-04
MXPA06011881A (es) 2006-12-14
JP4224115B2 (ja) 2009-02-12
PA8629901A1 (es) 2006-06-02
US7268144B2 (en) 2007-09-11
BRPI0509852A (pt) 2007-10-23
CA2562952A1 (en) 2005-11-10
PE20060253A1 (es) 2006-03-30

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