UA73506C2 - Antitumour compounds activated by fibroplasts activation proteins (fap) - Google Patents

Antitumour compounds activated by fibroplasts activation proteins (fap) Download PDF

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Publication number
UA73506C2
UA73506C2 UA2001128659A UA2001128659A UA73506C2 UA 73506 C2 UA73506 C2 UA 73506C2 UA 2001128659 A UA2001128659 A UA 2001128659A UA 2001128659 A UA2001128659 A UA 2001128659A UA 73506 C2 UA73506 C2 UA 73506C2
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UA
Ukraine
Prior art keywords
compound according
compound
group
formula
formulas
Prior art date
Application number
UA2001128659A
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English (en)
Ukrainian (uk)
Original Assignee
Boehringer Ingelheim Pharma
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
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of UA73506C2 publication Critical patent/UA73506C2/uk

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/66Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
    • A61K47/67Enzyme prodrug therapy, e.g. gene directed enzyme drug therapy [GDEPT] or VDEPT
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/24Condensed ring systems having three or more rings
    • C07H15/252Naphthacene radicals, e.g. daunomycins, adriamycins
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1019Tetrapeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nanotechnology (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
UA2001128659A 1999-05-14 2000-11-05 Antitumour compounds activated by fibroplasts activation proteins (fap) UA73506C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13413699P 1999-05-14 1999-05-14
PCT/EP2000/004261 WO2000071571A2 (en) 1999-05-14 2000-05-11 Fap-activated anti-tumor compounds

Publications (1)

Publication Number Publication Date
UA73506C2 true UA73506C2 (en) 2005-08-15

Family

ID=22461925

Family Applications (1)

Application Number Title Priority Date Filing Date
UA2001128659A UA73506C2 (en) 1999-05-14 2000-11-05 Antitumour compounds activated by fibroplasts activation proteins (fap)

Country Status (28)

Country Link
US (1) US6613879B1 (pt)
EP (1) EP1180116A2 (pt)
JP (1) JP3607201B2 (pt)
KR (1) KR20020030270A (pt)
CN (1) CN1213058C (pt)
AR (1) AR033792A1 (pt)
AU (1) AU777521B2 (pt)
BG (1) BG106096A (pt)
BR (1) BR0010564A (pt)
CA (1) CA2369933A1 (pt)
CO (1) CO5170516A1 (pt)
CZ (1) CZ20014097A3 (pt)
EA (1) EA005204B1 (pt)
EE (1) EE200100600A (pt)
HK (1) HK1048642B (pt)
HU (1) HUP0202367A3 (pt)
IL (1) IL145798A0 (pt)
MX (1) MXPA01011401A (pt)
MY (1) MY125939A (pt)
NO (1) NO20015536L (pt)
NZ (1) NZ516075A (pt)
PL (1) PL351680A1 (pt)
SK (1) SK16452001A3 (pt)
TW (1) TWI248444B (pt)
UA (1) UA73506C2 (pt)
WO (1) WO2000071571A2 (pt)
YU (1) YU80901A (pt)
ZA (1) ZA200109151B (pt)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK12872002A3 (sk) 2000-03-15 2003-05-02 Bristol-Myers Squibb Pharma Company Cielené antineoplastické lieky a ich terapeutické použitie
GB0027551D0 (en) * 2000-11-10 2000-12-27 Boehringer Ingelheim Pharma Anti-tumor compounds
GB0027552D0 (en) * 2000-11-10 2000-12-27 Boehringer Ingelheim Pharma Anti-tumor compounds
US7163923B2 (en) * 2001-05-09 2007-01-16 Celmed Oncology (Usa), Inc. Peptide deformylase activated prodrugs
US7091186B2 (en) * 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
US20030211979A1 (en) * 2002-01-30 2003-11-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg FAP-activated anti-tumor compounds
EP1333033A1 (en) * 2002-01-30 2003-08-06 Boehringer Ingelheim Pharma GmbH & Co.KG FAP-activated anti-tumor compounds
WO2003088913A2 (en) * 2002-04-18 2003-10-30 Celmed Oncology (Usa), Inc. Peptide deformylase activated prodrugs
US20040033957A1 (en) * 2002-05-10 2004-02-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg FAP-activated anti-tumor prodrugs
EP1506221A2 (en) * 2002-05-10 2005-02-16 Boehringer Ingelheim Pharma GmbH & Co.KG Fap-activated anti-tumor prodrugs
US20040001801A1 (en) * 2002-05-23 2004-01-01 Corvas International, Inc. Conjugates activated by cell surface proteases and therapeutic uses thereof
BR0315537A (pt) * 2002-11-14 2005-09-27 Celmed Oncology Usa Inc Pró-drogas ativadas por peptìdeo desformilase
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
JP2007511467A (ja) 2003-05-14 2007-05-10 タケダ サン ディエゴ インコーポレイテッド ジペプチジルペプチダーゼインヒビター
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP2008501714A (ja) 2004-06-04 2008-01-24 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006073167A1 (ja) * 2005-01-07 2006-07-13 Ono Pharmaceutical Co., Ltd. ピロリジン誘導体
AU2006246719A1 (en) 2005-05-19 2006-11-23 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
US8067248B2 (en) * 2005-12-14 2011-11-29 Luwig Institute for Cancer Research Method for diagnosing rheumatoid arthritis via assaying myofibroblast-like synoviocytes for fibroblast activation protein
WO2007087131A2 (en) * 2006-01-05 2007-08-02 The Johns Hopkins University Peptide prodrugs
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2008005479A2 (en) * 2006-07-06 2008-01-10 University Of Wyoming Charge reversible polymers
US20100184706A1 (en) * 2007-03-20 2010-07-22 Bachovchin William W Fap-activated chemotherapeutic compounds, and methods of use thereof
EP2343973B1 (en) * 2008-09-12 2016-02-17 Cadila Pharmaceuticals Ltd. Prodrugs of Sitagliptin
EP2525830B1 (en) 2010-01-22 2016-05-11 Ascendis Pharma A/S Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
EP2525829A1 (en) 2010-01-22 2012-11-28 Ascendis Pharma A/S Dipeptide-based prodrug linkers for aromatic amine-containing drugs
US20150335761A1 (en) * 2012-02-16 2015-11-26 Raymond Firestone Compositions and methods for contraception
PL2938360T3 (pl) 2012-12-28 2020-05-18 Cobiores Nv Minimalnie toksyczne proleki
EP2987794B1 (en) * 2013-04-19 2018-05-30 Jinan University Vinblastine derivatives, preparation method therefor and application thereof
EP3066091B1 (en) * 2013-11-05 2019-04-03 Astrazeneca AB Nmda antagonist prodrugs
CN113956325A (zh) * 2014-06-13 2022-01-21 塔夫茨大学信托人 Fap激活的治疗剂以及其相关用途
WO2015192124A1 (en) * 2014-06-13 2015-12-17 Trustees Of Tufts College Fap-activated therapeutic agents, and uses related thereto
CN105524141B (zh) * 2015-11-12 2019-11-26 中山大学 一种FAPa激活式肿瘤诊断多肽磁珠复合物的制备与应用
EP3222292A1 (en) 2016-03-03 2017-09-27 Heidelberg Pharma GmbH Amanitin conjugates
CN107043456B (zh) * 2017-04-19 2019-05-17 川北医学院 对氧环己酮与l-苯丙氨酸氮芥共聚物及其应用
CN110128501A (zh) * 2019-05-21 2019-08-16 北京海美源医药科技有限公司 一种靶向fap酶的喜树碱类化合物及其制备方法和应用
CN110128506B (zh) * 2019-05-22 2021-03-30 中国药科大学 一种寡肽及其应用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3915800A (en) * 1972-03-30 1975-10-28 Kelco Co Polysaccharide and bacterial fermentation process for its preparation
FR2546163B1 (fr) * 1983-05-16 1987-10-09 Centre Nat Rech Scient Nouveaux derives acyles hydrosolubles de peptides ou d'amino-acides, leur preparation et leur application
US5047401A (en) * 1985-09-09 1991-09-10 Board Of Regents, The University Of Texas System Use of dipeptide alkyl esters to treat GVHD
DE3783966T2 (de) 1986-07-29 1993-05-27 Sunstar Inc Reagens zur pruefung von periodentalen erkrankungen.
US5776892A (en) * 1990-12-21 1998-07-07 Curative Health Services, Inc. Anti-inflammatory peptides
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
US5866679A (en) 1994-06-28 1999-02-02 Merck & Co., Inc. Peptides
DE19512484A1 (de) * 1995-04-04 1996-10-17 Bayer Ag Kohlenhydratmodifizierte Cytostatika
JP2000506494A (ja) 1995-10-18 2000-05-30 メルク エンド カンパニー インコーポレーテッド 良性前立腺過形成の治療に有用な複合体
AU3224997A (en) 1996-05-29 1998-01-05 Prototek, Inc Prodrugs of thalidomide and methods for using same as modulators of t-cell function
US5952294A (en) 1996-07-31 1999-09-14 University Of Pittsburgh Of The Commonwealth System Of Higher Education Peptidyl prodrugs and methods of making and using the same
WO1998013059A1 (en) 1996-09-27 1998-04-02 Bristol-Myers Squibb Company Hydrolyzable prodrugs for delivery of anticancer drugs to metastatic cells
DE19640970A1 (de) * 1996-10-04 1998-04-16 Bayer Ag Modifizierte Cytostatika
NZ512171A (en) 1998-12-11 2004-07-30 Medarex Inc Prodrug compound comprising a therapeutic agent, an oligopeptide with a non-genetically encoded amino acid, a stabilizing group and optionally a linker group
AU772074B2 (en) 1999-04-28 2004-04-08 Vectramed, Inc. Enzymatically activated polymeric drug conjugates

Also Published As

Publication number Publication date
BG106096A (bg) 2002-05-31
TWI248444B (en) 2006-02-01
CA2369933A1 (en) 2000-11-30
AR033792A1 (es) 2004-01-07
CO5170516A1 (es) 2002-06-27
SK16452001A3 (sk) 2002-03-05
NZ516075A (en) 2004-03-26
EA200101155A1 (ru) 2002-10-31
WO2000071571A3 (en) 2001-09-07
HK1048642A1 (en) 2003-04-11
HK1048642B (zh) 2005-10-28
NO20015536L (no) 2002-01-10
AU777521B2 (en) 2004-10-21
NO20015536D0 (no) 2001-11-13
PL351680A1 (en) 2003-06-02
WO2000071571A2 (en) 2000-11-30
CZ20014097A3 (cs) 2002-02-13
EA005204B1 (ru) 2004-12-30
ZA200109151B (en) 2002-12-17
JP3607201B2 (ja) 2005-01-05
HUP0202367A2 (hu) 2002-11-28
JP2003500417A (ja) 2003-01-07
WO2000071571A8 (en) 2002-03-07
EE200100600A (et) 2003-02-17
CN1213058C (zh) 2005-08-03
BR0010564A (pt) 2002-02-19
KR20020030270A (ko) 2002-04-24
AU6559100A (en) 2000-12-12
YU80901A (sh) 2005-07-19
US6613879B1 (en) 2003-09-02
MXPA01011401A (es) 2002-06-04
IL145798A0 (en) 2002-07-25
CN1374969A (zh) 2002-10-16
HUP0202367A3 (en) 2003-10-28
EP1180116A2 (en) 2002-02-20
MY125939A (en) 2006-09-29

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