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

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

Info

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
Authority
UA
Ukraine
Prior art keywords
compound according
compound
group
formula
formulas
Prior art date
Application number
UA2001128659A
Other languages
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

Links

Classifications

    • 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)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Nanotechnology (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (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)
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 (ja)
EP (1) EP1180116A2 (ja)
JP (1) JP3607201B2 (ja)
KR (1) KR20020030270A (ja)
CN (1) CN1213058C (ja)
AR (1) AR033792A1 (ja)
AU (1) AU777521B2 (ja)
BG (1) BG106096A (ja)
BR (1) BR0010564A (ja)
CA (1) CA2369933A1 (ja)
CO (1) CO5170516A1 (ja)
CZ (1) CZ20014097A3 (ja)
EA (1) EA005204B1 (ja)
EE (1) EE200100600A (ja)
HK (1) HK1048642B (ja)
HU (1) HUP0202367A3 (ja)
IL (1) IL145798A0 (ja)
MX (1) MXPA01011401A (ja)
MY (1) MY125939A (ja)
NO (1) NO20015536L (ja)
NZ (1) NZ516075A (ja)
PL (1) PL351680A1 (ja)
SK (1) SK16452001A3 (ja)
TW (1) TWI248444B (ja)
UA (1) UA73506C2 (ja)
WO (1) WO2000071571A2 (ja)
YU (1) YU80901A (ja)
ZA (1) ZA200109151B (ja)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA02009019A (es) 2000-03-15 2003-02-12 Du Pont Pharm Co Farmacos antineoplasticos de objetivo, que se desdoblan por la peptidasa y su uso terapeutico.
GB0027552D0 (en) * 2000-11-10 2000-12-27 Boehringer Ingelheim Pharma Anti-tumor compounds
GB0027551D0 (en) * 2000-11-10 2000-12-27 Boehringer Ingelheim Pharma Anti-tumor compounds
BR0210149A (pt) * 2001-05-09 2004-06-29 Newbiotics Inc Pródrogas ativadas por deformilase de peptìdeo
US7091186B2 (en) * 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
EP1333033A1 (en) * 2002-01-30 2003-08-06 Boehringer Ingelheim Pharma GmbH & Co.KG FAP-activated anti-tumor compounds
US20030211979A1 (en) * 2002-01-30 2003-11-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg FAP-activated anti-tumor compounds
US20050096254A1 (en) * 2002-04-18 2005-05-05 Sergeeva Maria V. Peptide deformylase activated prodrugs
WO2003094972A2 (en) * 2002-05-10 2003-11-20 Boehringer Ingelheim Pharma Gmbh & Co Kg Fap-activated anti-tumor prodrugs
US20040033957A1 (en) * 2002-05-10 2004-02-19 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
AU2003290779A1 (en) * 2002-11-14 2004-06-03 Celmed Oncology (Usa), Inc. Peptide deformylase activated prodrugs
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
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
US7399869B2 (en) 2005-05-19 2008-07-15 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
EP1963537A4 (en) * 2005-12-14 2009-11-11 Ludwig Inst For Cancer Res Ltd METHOD FOR DIAGNOSING RHEUMATOID ARTHRITIS BY DETERMINING FIBROBLASTIC SYNOVIOCYTES FOR FIBROBLAST ACTIVATION PROTEIN
US20100047170A1 (en) * 2006-01-05 2010-02-25 Denmeade Samuel R 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
ES2571217T3 (es) * 2008-09-12 2016-05-24 Cadila Pharmaceuticals Ltd Profármacos de sitagliptina
WO2011089215A1 (en) 2010-01-22 2011-07-28 Ascendis Pharma As Dipeptide-based prodrug linkers for aromatic amine-containing drugs
WO2011089216A1 (en) 2010-01-22 2011-07-28 Ascendis Pharma As Dipeptide-based prodrug linkers for aliphatic 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
AU2014253584B2 (en) * 2013-04-19 2017-02-02 Jinan University Vinca Alkaloid Derivatives, Preparation Method therefor and Application thereof
PT3066091T (pt) 2013-11-05 2019-07-11 Astrazeneca Ab Pro-farmacos de antagonista de nmda
US9737556B2 (en) * 2014-06-13 2017-08-22 Trustees Of Tufts College FAP-activated therapeutic agents, and uses related thereto
EP4299134A3 (en) 2014-06-13 2024-03-27 Bach Biosciences, LLC 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
EP0255341B1 (en) 1986-07-29 1993-02-03 Sunstar Kabushiki Kaisha Reagent for testing periodontal diseases
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
EP0855910A4 (en) 1995-10-18 2000-07-05 Merck & Co Inc CONJUGATES USEFUL FOR TREATING BENIN PROSTATIC ADENOMA
CA2256669A1 (en) 1996-05-29 1997-12-04 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
DE69942128D1 (de) 1998-12-11 2010-04-22 Coulter Pharm Inc Prodrugs und verfahren zu deren herstellung
EP1176985A2 (en) 1999-04-28 2002-02-06 Vectramed, Inc. Enzymatically activated polymeric drug conjugates

Also Published As

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

Similar Documents

Publication Publication Date Title
UA73506C2 (en) Antitumour compounds activated by fibroplasts activation proteins (fap)
JP6290166B2 (ja) 注射可能な医薬調製剤の製法
AU2001266853B2 (en) Prodrug compounds with an oligopeptide having an isoleucine residue
US20030055052A1 (en) FAP-activated anti-tumor compounds
AU2001275525B2 (en) Tripeptide prodrug compounds
US20020155565A1 (en) FAP-activated anti-tumor compounds
AU2001266853A1 (en) Prodrug compounds with an oligopeptide having an isoleucine residue
EP1333033A1 (en) FAP-activated anti-tumor compounds
JP2003526683A (ja) ペプチダーゼ切断可能な標的抗新生物薬およびそれらの治療への使用
WO2002038590A1 (en) Fap-alpha-activated anti-tumor compounds
US20030232742A1 (en) FAP-activated anti-tumor compounds
EP1506221A2 (en) Fap-activated anti-tumor prodrugs
US20040033957A1 (en) FAP-activated anti-tumor prodrugs
US20030211979A1 (en) FAP-activated anti-tumor compounds
Kratzel et al. Valaminols, probably the most simplified peptide-analogs acting as pepsin inhibitors
WO2002038591A1 (en) Fap-activated anti-tumor compounds
WO2002038187A1 (en) Fap-activated anti-tumour prodrug