CR8646A - Sintesis regioespecifica de derivados de ester-42 de rapamicina - Google Patents

Sintesis regioespecifica de derivados de ester-42 de rapamicina

Info

Publication number
CR8646A
CR8646A CR8646A CR8646A CR8646A CR 8646 A CR8646 A CR 8646A CR 8646 A CR8646 A CR 8646A CR 8646 A CR8646 A CR 8646A CR 8646 A CR8646 A CR 8646A
Authority
CR
Costa Rica
Prior art keywords
ester
regiospecifica
rapamicina
steresis
derivados
Prior art date
Application number
CR8646A
Other languages
English (en)
Inventor
Jianxin Gu
Ping Cai
Mark E 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=CR8646(A) "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 CR8646A publication Critical patent/CR8646A/es

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)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Hematology (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

Se describe un metodo para la sintesis regioespecifica de derivados de ester 42 de rapamicina; el metodo involucra la acilacion catalizada por lipasa de rapamicinca 42- hidroxi con un donante acilo como ester vinilico, un ester isopropenilico o un anhibrido en un solvente organico adecuado.
CR8646A 2004-04-14 2006-09-21 Sintesis regioespecifica de derivados de ester-42 de rapamicina CR8646A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US56192604P 2004-04-14 2004-04-14

Publications (1)

Publication Number Publication Date
CR8646A true CR8646A (es) 2007-08-28

Family

ID=34965235

Family Applications (1)

Application Number Title Priority Date Filing Date
CR8646A CR8646A (es) 2004-04-14 2006-09-21 Sintesis regioespecifica de derivados de ester-42 de rapamicina

Country Status (23)

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

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AR040693A1 (es) 2002-07-30 2005-04-13 Wyeth Corp Formulaciones parenterales
PL1735321T3 (pl) * 2004-04-14 2009-04-30 Wyeth Corp Proces wytwarzania 42-estrów rapamycyny i 32-estrów FK-506 z kwasem dikarboksylowym, prekursory koniugatów rapamycyny oraz przeciwciała
CN1946852A (zh) * 2004-04-27 2007-04-11 惠氏公司 利用雷帕霉素特异性甲基化酶标记雷帕霉素
CA2577011A1 (en) * 2004-08-10 2006-04-13 Wyeth Cci-779 derivatives and methods of making same
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
WO2007067566A2 (en) * 2005-12-07 2007-06-14 Wyeth Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry
CN101321770A (zh) * 2005-12-07 2008-12-10 惠氏公司 由雷帕霉素42-酯硼酸酯制备雷帕霉素42-酯的可放大方法
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.
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
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8414909B2 (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
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
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
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
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
US9737640B2 (en) 2006-11-20 2017-08-22 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
ES2645692T3 (es) 2008-11-11 2017-12-07 The Board Of Regents,The University Of Texas System Microcápsulas de rapamicina y su uso para el tratamiento del cáncer
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
WO2012131019A1 (en) * 2011-04-01 2012-10-04 Sandoz Ag Regioselective acylation of rapamycin at the c-42 position
US10751450B2 (en) 2012-06-08 2020-08-25 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
ES2574522T3 (es) * 2012-06-08 2016-06-20 Biotronik Ag Ésteres 40-O-hidrocarburo cíclico de rapamicina, composiciones y procedimientos
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
WO2014145780A1 (en) 2013-03-15 2014-09-18 Biosensors International Group, Ltd. Purification of rapamycin derivatives
EP3089737B1 (en) 2013-12-31 2021-11-03 Rapamycin Holdings, LLC Oral rapamycin nanoparticle preparations and use
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
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CN110446495B (zh) 2017-02-17 2023-09-05 特维娜有限公司 含有7元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法
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AU2018370237B2 (en) * 2017-11-20 2024-10-17 Icahn School Of Medicine At Mount Sinai Inhibiting trained immunity with a therapeutic nanobilogic composition
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Also Published As

Publication number Publication date
GT200500085A (es) 2005-11-03
WO2005105811A1 (en) 2005-11-10
ECSP066927A (es) 2006-12-20
JP2007532134A (ja) 2007-11-15
BRPI0509852A (pt) 2007-10-23
TW200536542A (en) 2005-11-16
EP1737869A1 (en) 2007-01-03
RU2006134014A (ru) 2008-05-20
RU2387657C2 (ru) 2010-04-27
PA8629901A1 (es) 2006-06-02
CN1942476A (zh) 2007-04-04
AR049019A1 (es) 2006-06-21
PE20060253A1 (es) 2006-03-30
SG152234A1 (en) 2009-05-29
CA2562952A1 (en) 2005-11-10
JP4224115B2 (ja) 2009-02-12
US20050234234A1 (en) 2005-10-20
NO20065090L (no) 2006-11-13
IL178315A0 (en) 2007-02-11
MXPA06011881A (es) 2006-12-14
UA87492C2 (en) 2009-07-27
KR20070015544A (ko) 2007-02-05
AU2005238431A1 (en) 2005-11-10
CL2008000507A1 (es) 2008-07-04
US7268144B2 (en) 2007-09-11

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