GT200500085A - Sintesis regioespecifica de derivados de 42-ester de rapamicina - Google Patents

Sintesis regioespecifica de derivados de 42-ester de rapamicina

Info

Publication number
GT200500085A
GT200500085A GT200500085A GT200500085A GT200500085A GT 200500085 A GT200500085 A GT 200500085A GT 200500085 A GT200500085 A GT 200500085A GT 200500085 A GT200500085 A GT 200500085A GT 200500085 A GT200500085 A GT 200500085A
Authority
GT
Guatemala
Prior art keywords
rapamycin
synthesis
regespecific
ester derivatives
derivatives
Prior art date
Application number
GT200500085A
Other languages
English (en)
Inventor
Jianxin Gu
Ping Cai
Mark E Rupen
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=GT200500085(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed filed Critical
Publication of GT200500085A publication Critical patent/GT200500085A/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)
  • 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)

Abstract

EN LA PRESENTE INVENCIÒN SE DESCRIBE UN MÈTODO PARA LA SÌNTESIS REGIOESPECÌFICA DE DERIVADOS 42ÈSTER DE RAPAMICINA. EL MÈTODO INVOLUCRA LA ACILACIÒN CATALIZADA POR LIPASA DE 42HIDROXI RAPAMICINA CON UN DONADOR DE ACILO TAL COMO UN VINILÈSTER, UN ISOPROPENILÈSTER O UN ANHÌDRIDO EN UN SOLVENTE ORGÀNICO ADECUADO.
GT200500085A 2004-04-14 2005-04-13 Sintesis regioespecifica de derivados de 42-ester de rapamicina GT200500085A (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
GT200500085A true GT200500085A (es) 2005-11-03

Family

ID=34965235

Family Applications (1)

Application Number Title Priority Date Filing Date
GT200500085A GT200500085A (es) 2004-04-14 2005-04-13 Sintesis regioespecifica de derivados de 42-ester 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)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ537829A (en) 2002-07-30 2006-09-29 Wyeth Corp Parenteral formulations containing a rapamycin hydroxyester
US7445916B2 (en) * 2004-04-14 2008-11-04 Wyeth Process for preparing rapamycin 42-esters and FK-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies
JP2007534337A (ja) * 2004-04-27 2007-11-29 ワイス ラパマイシン特異的メチラーゼを用いるラパマイシンの標識
PA8641501A1 (es) * 2004-08-10 2006-09-08 Wyeth Corp Derivados de cci-779 y metodo para su preparacion
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
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
KR20080077147A (ko) * 2005-12-07 2008-08-21 와이어쓰 결정성 라파마이신의 제조 방법 및 시차 주사 열량계를사용하는 라파마이신 화합물의 결정화도의 측정 방법
RU2008121240A (ru) * 2005-12-07 2010-01-20 Вайет (Us) Способ получения очищенного кристаллического cci-779
AU2007223963A1 (en) * 2006-03-07 2007-09-13 Wyeth Process for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
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
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
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
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
WO2010024898A2 (en) 2008-08-29 2010-03-04 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
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
PL2859001T3 (pl) * 2012-06-08 2016-08-31 Biotronik Ag 40-o-podstawiona pochodna estrowa rapamycyny i węglowodoru cyklicznego, kompozycje i metody
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
EP2972258B1 (en) * 2013-03-15 2021-08-04 Biosensors International Group, Ltd. Purification of rapamycin derivatives
CA3206208A1 (en) 2013-12-31 2015-07-09 Rapamycin Holdings, Llc Oral rapamycin nanoparticle preparations and use
US9700544B2 (en) 2013-12-31 2017-07-11 Neal K Vail Oral rapamycin nanoparticle preparations
BR112019016775A2 (pt) 2017-02-17 2020-03-31 Trevena, Inc. Compostos moduladores de receptor delta-opioide contendo aza-heterocíclico com 7 membros, métodos de uso e produção dos mesmos
EP3624863B1 (en) 2017-05-15 2021-04-14 C.R. Bard, Inc. Medical device with drug-eluting coating and intermediate layer
JP7357629B2 (ja) * 2017-11-20 2023-10-06 アイカーン スクール オブ メディスン アット マウント サイナイ 治療用ナノバイオロジー組成物での訓練された免疫の阻害
EP3880266A1 (en) 2018-11-14 2021-09-22 Lutonix, Inc. Medical device with drug-eluting coating on modified device surface
EP3952937A1 (en) 2019-04-08 2022-02-16 Bard Peripheral Vascular, Inc. Medical device with drug-eluting coating on modified device surface
EP4259100A1 (en) * 2020-12-14 2023-10-18 Biotronik Ag Materials and methods for treating viral and other medicinal conditions
AU2022239614A1 (en) 2021-03-19 2023-10-12 Icahn School Of Medicine At Mount Sinai Compounds for regulating trained immunity, and their methods of use
WO2023070605A1 (en) * 2021-10-29 2023-05-04 Trevena, Inc. Methods of preparing 6-membered aza-heterocyclic containing delta-opioid receptor modulating compounds

Family Cites Families (19)

* 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
US4316885A (en) 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
US5210030A (en) 1990-06-25 1993-05-11 Merck & Co., Inc. Process for selectively acylating immunomycin
PT98990A (pt) * 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5233036A (en) 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
US5260300A (en) 1992-11-19 1993-11-09 American Home Products Corporation Rapamycin carbonate esters as immuno-suppressant agents
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5780462A (en) 1995-12-27 1998-07-14 American Home Products Corporation Water soluble rapamycin esters
TWI256395B (en) * 1999-09-29 2006-06-11 Wyeth Corp Regioselective synthesis of rapamycin derivatives
US6277983B1 (en) 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives
CA2421485A1 (en) 2000-09-19 2002-03-28 Wyeth Water soluble rapamycin esters
NZ537829A (en) 2002-07-30 2006-09-29 Wyeth Corp Parenteral formulations containing a rapamycin hydroxyester
RU2339639C2 (ru) 2003-08-07 2008-11-27 Уайт Региоселективный синтез cci-779
EP1660081A1 (en) 2003-09-03 2006-05-31 Wyeth Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and pharmaceutical compositions containing the same
EP1701698B1 (en) 2004-01-08 2008-01-16 Wyeth a Corporation of the State of Delaware Directly compressible pharmaceutical composition for the oral admimistration of cci-779

Also Published As

Publication number Publication date
AU2005238431A1 (en) 2005-11-10
CN1942476A (zh) 2007-04-04
MXPA06011881A (es) 2006-12-14
ECSP066927A (es) 2006-12-20
JP4224115B2 (ja) 2009-02-12
UA87492C2 (en) 2009-07-27
US20050234234A1 (en) 2005-10-20
CR8646A (es) 2007-08-28
RU2006134014A (ru) 2008-05-20
KR20070015544A (ko) 2007-02-05
EP1737869A1 (en) 2007-01-03
CA2562952A1 (en) 2005-11-10
TW200536542A (en) 2005-11-16
PE20060253A1 (es) 2006-03-30
RU2387657C2 (ru) 2010-04-27
JP2007532134A (ja) 2007-11-15
SG152234A1 (en) 2009-05-29
US7268144B2 (en) 2007-09-11
PA8629901A1 (es) 2006-06-02
CL2008000507A1 (es) 2008-07-04
BRPI0509852A (pt) 2007-10-23
IL178315A0 (en) 2007-02-11
WO2005105811A1 (en) 2005-11-10
NO20065090L (no) 2006-11-13
AR049019A1 (es) 2006-06-21

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