UA87492C2 - Regiospecific synthesis of rapamycin 42-ester derivatives - Google Patents

Regiospecific synthesis of rapamycin 42-ester derivatives

Info

Publication number
UA87492C2
UA87492C2 UAA200610949A UAA200610949A UA87492C2 UA 87492 C2 UA87492 C2 UA 87492C2 UA A200610949 A UAA200610949 A UA A200610949A UA A200610949 A UAA200610949 A UA A200610949A UA 87492 C2 UA87492 C2 UA 87492C2
Authority
UA
Ukraine
Prior art keywords
rapamycin
ester derivatives
regiospecific synthesis
ester
regiospecific
Prior art date
Application number
UAA200610949A
Other languages
English (en)
Ukrainian (uk)
Inventor
Джианксин Гу
Пинг Каи
Марк Э. Руппен
Original Assignee
Уайет
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=UA87492(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Уайет filed Critical Уайет
Publication of UA87492C2 publication Critical patent/UA87492C2/ru

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

Описан способ региоспецифического синтеза 42-производных эстера рапамицина. Способ включает катализированное липазой ацилирование 42-гидроксирапамицина донором ацила, таким как виниловый эстер, изопропениловый эстер или ангидрид, в приемлемом органическом растворителе.
UAA200610949A 2004-04-14 2005-12-04 Regiospecific synthesis of rapamycin 42-ester derivatives UA87492C2 (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
UA87492C2 true UA87492C2 (en) 2009-07-27

Family

ID=34965235

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA200610949A UA87492C2 (en) 2004-04-14 2005-12-04 Regiospecific synthesis of rapamycin 42-ester derivatives

Country Status (23)

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

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BRPI0510277A (pt) * 2004-04-27 2007-10-30 Wyeth Corp método para marcar especificamente uma rapamicina, rapamicina especificamente marcada, composição, e, kit
EP1776370A1 (en) * 2004-08-10 2007-04-25 Wyeth a Corporation of the State of Delaware Cci-779 derivatives and methods of making same
BRPI0607932A2 (pt) * 2005-02-09 2016-11-08 Wyeth Corp polimorfo cci-779, processo para preparar polimorfo cci-779, composição farmacêutica, kit, e método para preparar uma composição farmacêutica
WO2007056175A2 (en) * 2005-11-04 2007-05-18 Wyeth 41-methoxy isotope labeled rapamycin 42-ester
KR20080077618A (ko) * 2005-12-07 2008-08-25 와이어쓰 정제된 결정체 ｃｃｉ-779 의 제조 방법
WO2007067560A2 (en) * 2005-12-07 2007-06-14 Wyeth Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate
KR20080077147A (ko) * 2005-12-07 2008-08-21 와이어쓰 결정성 라파마이신의 제조 방법 및 시차 주사 열량계를사용하는 라파마이신 화합물의 결정화도의 측정 방법
BRPI0708562A2 (pt) * 2006-03-07 2011-06-07 Wyeth Corp processos para preparar conjugados de polietileno glicor de macrolìdeos imunossupressores, um macrolìdeo imunossupressor peguilado, uma rapamicina peguilada, um everolimus peguilado, um cci-779 peguilado e um tacrolimus peguilado, e, produto
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
US8430055B2 (en) 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
US8414910B2 (en) 2006-11-20 2013-04-09 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
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US20080175887A1 (en) 2006-11-20 2008-07-24 Lixiao Wang Treatment of Asthma and Chronic Obstructive Pulmonary Disease With Anti-proliferate and Anti-inflammatory Drugs
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
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
WO2009131631A1 (en) * 2008-04-14 2009-10-29 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
CA2743491C (en) 2008-11-11 2016-10-11 Zelton Dave Sharp Inhibition of mammalian target of rapamycin
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
KR20140013000A (ko) * 2011-04-01 2014-02-04 산도즈 아게 C-42 위치에서 라파마이신의 위치선택적 아실화
AU2013270798B2 (en) * 2012-06-08 2017-09-07 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
US10751450B2 (en) 2012-06-08 2020-08-25 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
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Also Published As

Publication number Publication date
AU2005238431A1 (en) 2005-11-10
WO2005105811A1 (en) 2005-11-10
ECSP066927A (es) 2006-12-20
MXPA06011881A (es) 2006-12-14
BRPI0509852A (pt) 2007-10-23
EP1737869A1 (en) 2007-01-03
CA2562952A1 (en) 2005-11-10
PA8629901A1 (es) 2006-06-02
RU2387657C2 (ru) 2010-04-27
US20050234234A1 (en) 2005-10-20
GT200500085A (es) 2005-11-03
CR8646A (es) 2007-08-28
US7268144B2 (en) 2007-09-11
NO20065090L (no) 2006-11-13
JP4224115B2 (ja) 2009-02-12
CL2008000507A1 (es) 2008-07-04
SG152234A1 (en) 2009-05-29
IL178315A0 (en) 2007-02-11
RU2006134014A (ru) 2008-05-20
KR20070015544A (ko) 2007-02-05
CN1942476A (zh) 2007-04-04
JP2007532134A (ja) 2007-11-15
AR049019A1 (es) 2006-06-21
TW200536542A (en) 2005-11-16
PE20060253A1 (es) 2006-03-30

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