CA2397354C - O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders - Google Patents

O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders Download PDF

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Publication number
CA2397354C
CA2397354C CA2397354A CA2397354A CA2397354C CA 2397354 C CA2397354 C CA 2397354C CA 2397354 A CA2397354 A CA 2397354A CA 2397354 A CA2397354 A CA 2397354A CA 2397354 C CA2397354 C CA 2397354C
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Prior art keywords
rapamycin
hydroxy
group
derivative
ethyl
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Expired - Lifetime
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CA2397354A
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English (en)
French (fr)
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CA2397354A1 (en
Inventor
Mariusz A. Wasik
Leslie M. Shaw
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University of Pennsylvania Penn
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University of Pennsylvania Penn
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Publication of CA2397354A1 publication Critical patent/CA2397354A1/en
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    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • G01N33/5047—Cells of the immune system
    • G01N33/5052—Cells of the immune system involving B-cells
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Microbiology (AREA)
  • Toxicology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CA2397354A 2000-01-14 2001-01-12 O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders Expired - Lifetime CA2397354C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17608600P 2000-01-14 2000-01-14
US60/176,086 2000-01-14
PCT/US2001/001537 WO2001051049A1 (en) 2000-01-14 2001-01-12 O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders

Publications (2)

Publication Number Publication Date
CA2397354A1 CA2397354A1 (en) 2001-07-19
CA2397354C true CA2397354C (en) 2011-07-19

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2397354A Expired - Lifetime CA2397354C (en) 2000-01-14 2001-01-12 O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders

Country Status (9)

Country Link
US (5) US7754734B2 (https=)
EP (2) EP2298299A3 (https=)
JP (3) JP2003519655A (https=)
AT (1) ATE475418T1 (https=)
AU (2) AU2001230956B2 (https=)
CA (1) CA2397354C (https=)
DE (1) DE60142677D1 (https=)
ES (1) ES2349458T3 (https=)
WO (1) WO2001051049A1 (https=)

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US6890546B2 (en) 1998-09-24 2005-05-10 Abbott Laboratories Medical devices containing rapamycin analogs
EP2298299A3 (en) * 2000-01-14 2012-02-29 The Trustees Of The University Of Pennsylvania O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders
PL409579A1 (pl) * 2001-02-19 2015-03-02 Novartis Ag Leczenie raka
AU2011226833B9 (en) * 2001-02-19 2014-07-03 Novartis Ag Cancer treatment
US7682387B2 (en) 2002-04-24 2010-03-23 Biosensors International Group, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US6939376B2 (en) * 2001-11-05 2005-09-06 Sun Biomedical, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US20040024450A1 (en) * 2002-04-24 2004-02-05 Sun Biomedical, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US7169404B2 (en) * 2003-07-30 2007-01-30 Advanced Cardiovasular Systems, Inc. Biologically absorbable coatings for implantable devices and methods for fabricating the same
US7901451B2 (en) 2004-09-24 2011-03-08 Biosensors International Group, Ltd. Drug-delivery endovascular stent and method for treating restenosis
US20080097591A1 (en) 2006-10-20 2008-04-24 Biosensors International Group Drug-delivery endovascular stent and method of use
US8067055B2 (en) * 2006-10-20 2011-11-29 Biosensors International Group, Ltd. Drug-delivery endovascular stent and method of use
US20080103584A1 (en) * 2006-10-25 2008-05-01 Biosensors International Group Temporal Intraluminal Stent, Methods of Making and Using
KR100930167B1 (ko) * 2007-09-19 2009-12-07 삼성전기주식회사 초광각 광학계
US20110098241A1 (en) * 2008-04-14 2011-04-28 Poniard Pharmaceuticals, Inc. Rapamycin analogs as anti-cancer agents
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
US9283211B1 (en) 2009-11-11 2016-03-15 Rapamycin Holdings, Llc Oral rapamycin preparation and use for stomatitis
US20170079962A1 (en) 2009-11-11 2017-03-23 Rapamycin Holdings, Llc Oral Rapamycin Preparation and Use for Stomatitus
CN102268015B (zh) * 2011-08-30 2013-08-28 成都摩尔生物医药有限公司 一种依维莫司的合成方法
US20150290176A1 (en) 2012-10-12 2015-10-15 The Board Of Regents Of The University Of Texas System Use of mtor inhibitors to treat vascular cognitive impairment
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
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
CN105254646A (zh) * 2014-05-28 2016-01-20 上海博邦医药科技有限公司 一种制备依维莫司的方法
JP6716139B2 (ja) 2015-01-19 2020-07-01 学校法人慶應義塾 内耳性難聴治療薬
JP2020507632A (ja) * 2017-02-10 2020-03-12 マウント タム セラピューティクス, インコーポレイテッドMount Tam Therapeutics, Inc. ラパマイシン類似体
EP3848065B1 (en) 2017-05-15 2023-07-26 C. R. Bard, Inc. Medical device with drug-eluting coating and intermediate layer
EP3880266B1 (en) 2018-11-14 2025-05-07 Lutonix, Inc. Medical device with drug-eluting coating on modified device surface
CN109776571B (zh) * 2019-01-31 2021-06-11 哈药慈航制药股份有限公司 一种雷帕霉素类似物及其制备方法和应用
WO2020209828A1 (en) 2019-04-08 2020-10-15 Bard Peripheral Vascular, Inc. Medical device with drug-eluting coating on modified device surface
CN110917194A (zh) * 2019-11-07 2020-03-27 福建省微生物研究所 雷帕霉素噻唑类衍生物在制备抗阿尔茨海默症药物中的应用
CN113653305B (zh) * 2021-09-07 2024-11-05 中国五冶集团有限公司 一种电动顶升操作平台
CN115323915B (zh) * 2022-10-17 2023-01-06 广州市市政工程试验检测有限公司 一种桥梁索杆检测与修复机器人

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JP3352411B2 (ja) * 1998-03-05 2002-12-03 株式会社東芝 制御システム、電力系統保護制御システムおよびプログラムを記憶した記憶媒体
JP2002544167A (ja) 1999-05-10 2002-12-24 ノバルティス アクチエンゲゼルシャフト 有機化合物
EP2298299A3 (en) * 2000-01-14 2012-02-29 The Trustees Of The University Of Pennsylvania O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders
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US6399626B1 (en) * 2000-10-02 2002-06-04 Wyeth Hydroxyesters of 7-desmethylrapamycin

Also Published As

Publication number Publication date
EP1250135B1 (en) 2010-07-28
ATE475418T1 (de) 2010-08-15
US20100305151A1 (en) 2010-12-02
US20080125457A1 (en) 2008-05-29
US7754734B2 (en) 2010-07-13
US20080182867A9 (en) 2008-07-31
US20040010002A1 (en) 2004-01-15
US20110104304A1 (en) 2011-05-05
US7781447B2 (en) 2010-08-24
JP2010090131A (ja) 2010-04-22
EP1250135A1 (en) 2002-10-23
US8759370B2 (en) 2014-06-24
WO2001051049A1 (en) 2001-07-19
AU2001230956B2 (en) 2005-08-18
EP2298299A3 (en) 2012-02-29
US8778961B2 (en) 2014-07-15
JP5180177B2 (ja) 2013-04-10
WO2001051049A9 (en) 2003-01-16
EP1250135A4 (en) 2006-06-07
HK1050145A1 (en) 2003-06-13
US8569332B2 (en) 2013-10-29
EP2298299A2 (en) 2011-03-23
ES2349458T3 (es) 2011-01-03
CA2397354A1 (en) 2001-07-19
JP5184894B2 (ja) 2013-04-17
DE60142677D1 (de) 2010-09-09
JP2008106074A (ja) 2008-05-08
AU3095601A (en) 2001-07-24
US20100290994A1 (en) 2010-11-18
JP2003519655A (ja) 2003-06-24

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