SG152234A1 - Regiospecific synthesis of rapamycin 42-ester derivatives - Google Patents

Regiospecific synthesis of rapamycin 42-ester derivatives

Info

Publication number
SG152234A1
SG152234A1 SG200902515-6A SG2009025156A SG152234A1 SG 152234 A1 SG152234 A1 SG 152234A1 SG 2009025156 A SG2009025156 A SG 2009025156A SG 152234 A1 SG152234 A1 SG 152234A1
Authority
SG
Singapore
Prior art keywords
rapamycin
ester derivatives
regiospecific synthesis
ester
regiospecific
Prior art date
Application number
SG200902515-6A
Other languages
English (en)
Inventor
Gu Jianxin
Cai Ping
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=SG152234(A1) "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 SG152234A1 publication Critical patent/SG152234A1/en

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)
  • Immunology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Microbiology (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)
SG200902515-6A 2004-04-14 2005-04-12 Regiospecific synthesis of rapamycin 42-ester derivatives SG152234A1 (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
SG152234A1 true SG152234A1 (en) 2009-05-29

Family

ID=34965235

Family Applications (1)

Application Number Title Priority Date Filing Date
SG200902515-6A SG152234A1 (en) 2004-04-14 2005-04-12 Regiospecific synthesis of rapamycin 42-ester derivatives

Country Status (23)

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

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ATE385795T1 (de) 2002-07-30 2008-03-15 Wyeth Corp Parenterale formulierungen mit einem rapamycin hydroxyester
JP2007532655A (ja) * 2004-04-14 2007-11-15 ワイス ラパマイシンコンジュゲートおよび抗体のための前駆体である、ジカルボン酸とのラパマイシン４２−エステルおよびジカルボン酸とのｆｋ−５０６３２−エステルの調製プロセス
EP1740710A1 (en) * 2004-04-27 2007-01-10 Wyeth Labeling of rapamycin using rapamycin-specific methylases
AU2005292647A1 (en) * 2004-08-10 2006-04-13 Wyeth CCI-779 derivatives and methods of making same
KR20070107030A (ko) * 2005-02-09 2007-11-06 와이어쓰 Ｃｃｉ-７７９ 다형체 및 그의 용도
US7538119B2 (en) * 2005-11-04 2009-05-26 Wyeth 41-Methoxy isotope labeled rapamycin 42-ester
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
TW200732342A (en) * 2005-12-07 2007-09-01 Wyeth Corp Process for the preparation of purified crystalline CCI-779
CA2630645A1 (en) * 2005-12-07 2007-06-14 Wyeth Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate
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
US8430055B2 (en) 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
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
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US8414909B2 (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
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
US8414525B2 (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
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
US20120064143A1 (en) 2008-11-11 2012-03-15 The Board Of Regents Of The University Of Texas System 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
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
EP2694520A1 (en) * 2011-04-01 2014-02-12 Sandoz AG Regioselective acylation of rapamycin at the c-42 position
ES2574522T3 (es) * 2012-06-08 2016-06-20 Biotronik Ag Ésteres 40-O-hidrocarburo cíclico de rapamicina, composiciones y procedimientos
US10751450B2 (en) 2012-06-08 2020-08-25 Biotronik Ag Rapamycin 40-O-cyclic hydrocarbon esters, compositions and methods
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
SG11201507406YA (en) * 2013-03-15 2015-10-29 Biosensors Int Group Ltd Purification of rapamycin derivatives
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
JP7185633B2 (ja) 2017-02-17 2022-12-07 トレベナ・インコーポレイテッド ７員アザ複素環を含有するデルタ－オピオイド受容体調節化合物、その使用方法及び製造方法
ES2871499T3 (es) 2017-05-15 2021-10-29 Bard Inc C R Dispositivo médico con recubrimiento de elución de fármaco y capa intermedia
AU2018370237A1 (en) * 2017-11-20 2020-06-04 Icahn School Of Medicine At Mount Sinai Inhibiting trained immunity with a therapeutic nanobilogic composition
US11541152B2 (en) 2018-11-14 2023-01-03 Lutonix, Inc. Medical device with drug-eluting coating on modified device surface
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US20240100025A1 (en) * 2020-12-14 2024-03-28 Biotronik Ag Materials and Methods for Treating Viral and Other Medical Conditions
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ATE385795T1 (de) 2002-07-30 2008-03-15 Wyeth Corp Parenterale formulierungen mit einem rapamycin hydroxyester
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Also Published As

Publication number Publication date
CL2008000507A1 (es) 2008-07-04
UA87492C2 (en) 2009-07-27
CN1942476A (zh) 2007-04-04
RU2387657C2 (ru) 2010-04-27
CA2562952A1 (en) 2005-11-10
PA8629901A1 (es) 2006-06-02
PE20060253A1 (es) 2006-03-30
AR049019A1 (es) 2006-06-21
US7268144B2 (en) 2007-09-11
KR20070015544A (ko) 2007-02-05
BRPI0509852A (pt) 2007-10-23
GT200500085A (es) 2005-11-03
JP2007532134A (ja) 2007-11-15
WO2005105811A1 (en) 2005-11-10
EP1737869A1 (en) 2007-01-03
TW200536542A (en) 2005-11-16
JP4224115B2 (ja) 2009-02-12
AU2005238431A1 (en) 2005-11-10
ECSP066927A (es) 2006-12-20
CR8646A (es) 2007-08-28
IL178315A0 (en) 2007-02-11
NO20065090L (no) 2006-11-13
US20050234234A1 (en) 2005-10-20
RU2006134014A (ru) 2008-05-20
MXPA06011881A (es) 2006-12-14

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