HUP0202367A2 - FAP-aktivált tumorellenes peptidek, eljárás előállításukra, azokat tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

FAP-aktivált tumorellenes peptidek, eljárás előállításukra, azokat tartalmazó gyógyszerkészítmények és alkalmazásuk

Info

Publication number
HUP0202367A2
HUP0202367A2 HU0202367A HUP0202367A HUP0202367A2 HU P0202367 A2 HUP0202367 A2 HU P0202367A2 HU 0202367 A HU0202367 A HU 0202367A HU P0202367 A HUP0202367 A HU P0202367A HU P0202367 A2 HUP0202367 A2 HU P0202367A2
Authority
HU
Hungary
Prior art keywords
group
amino
fap
pharmaceutical compositions
groups
Prior art date
Application number
HU0202367A
Other languages
English (en)
Inventor
Raymond Armand Firestone
Pilar Garin-Chesa
Dietmar Leipert
Martin Lenter
Jürgen Mack
John Edward Park
Stefan Peters
Wolfgang J. Rettig
Leila A. Telan
Original Assignee
Boehringer Ingelheim Pharma Kg
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 Kg filed Critical Boehringer Ingelheim Pharma Kg
Publication of HUP0202367A2 publication Critical patent/HUP0202367A2/hu
Publication of HUP0202367A3 publication Critical patent/HUP0202367A3/hu

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/62—Medicinal 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
    • A61K47/66—Medicinal 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
    • A61K47/67—Enzyme prodrug therapy, e.g. gene directed enzyme drug therapy [GDEPT] or VDEPT
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/62—Medicinal 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C07H15/252—Naphthacene radicals, e.g. daunomycins, adriamycins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Nanotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

kPage=A;BrkToNext=N;>(57) A találmány tárgyát az általános képletűvegyületek - ahol R1 amino-alkanoil- vagy oligopeptidoil-csoport,amelynek amino-terminális aminocsoportjához adott esetben egy blokkolócsoport kapcsolódik; Ra és Rb a kettőjük közötti N-C csoporttal együttegy adott esetben szubsztituált és adott esetben benzo- vagyciclohexanocsoporttal kondenzált heterogyűrűt képez, amelyben egy vagykét metiléncsoportot adott esetben -NH-csoport, oxigén- vagy kénatomhelyettesít; R9 hidrogénatom, alkil-, cikloalkil-, aril- vagyheteoaril-csoport; és Cyt' egy citotoxikus vagy citosztatikus vegyületmaradéka; azzal a fenntartással, hogy a háromnál több aminosavegységettartalmazó oligopeptidoilcsoportokban a Gln-csoport közvetlenül csak aSer-től eltérő csoportokhoz kapcsolódhat - és előállításuk, továbbátumorok kezelésére szolgáló gyógyszerkészítményekben prodrugként valóalkalmazásuk képezi. Ó
HU0202367A 1999-05-14 2000-05-11 Fap-activated anti-tumor peptides, process for their preparation pharmaceutical compositions comprising thereof and their use HUP0202367A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13413699P 1999-05-14 1999-05-14

Publications (2)

Publication Number Publication Date
HUP0202367A2 true HUP0202367A2 (hu) 2002-11-28
HUP0202367A3 HUP0202367A3 (en) 2003-10-28

Family

ID=22461925

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0202367A HUP0202367A3 (en) 1999-05-14 2000-05-11 Fap-activated anti-tumor peptides, process for their preparation pharmaceutical compositions comprising thereof and their use

Country Status (28)

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

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US7091186B2 (en) * 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
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US20040033957A1 (en) * 2002-05-10 2004-02-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg FAP-activated anti-tumor prodrugs
AU2003233238A1 (en) * 2002-05-10 2003-11-11 Boehringer Ingelheim Pharma Gmbh And 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
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
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WO2008116053A2 (en) * 2007-03-20 2008-09-25 Trustees Of Tufts College Fap-activated chemotherapeutic compounds, and methods of use thereof
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US9062094B2 (en) 2010-01-22 2015-06-23 Ascendis Pharma As Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
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WO2014169697A1 (zh) * 2013-04-19 2014-10-23 暨南大学 长春碱类衍生物及其制备方法和应用
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JP6744826B2 (ja) 2014-06-13 2020-08-19 バック バイオサイエンシーズ, エルエルシーBach BioSciences, LLC Ｆａｐ活性化治療剤及びそれに関連する使用
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
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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
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Also Published As

Publication number Publication date
NZ516075A (en) 2004-03-26
EP1180116A2 (en) 2002-02-20
YU80901A (sh) 2005-07-19
CO5170516A1 (es) 2002-06-27
HUP0202367A3 (en) 2003-10-28
JP2003500417A (ja) 2003-01-07
CA2369933A1 (en) 2000-11-30
NO20015536D0 (no) 2001-11-13
WO2000071571A8 (en) 2002-03-07
PL351680A1 (en) 2003-06-02
BR0010564A (pt) 2002-02-19
MY125939A (en) 2006-09-29
EE200100600A (et) 2003-02-17
AR033792A1 (es) 2004-01-07
CN1213058C (zh) 2005-08-03
NO20015536L (no) 2002-01-10
CN1374969A (zh) 2002-10-16
CZ20014097A3 (cs) 2002-02-13
WO2000071571A2 (en) 2000-11-30
TWI248444B (en) 2006-02-01
HK1048642A1 (en) 2003-04-11
MXPA01011401A (es) 2002-06-04
ZA200109151B (en) 2002-12-17
AU6559100A (en) 2000-12-12
JP3607201B2 (ja) 2005-01-05
UA73506C2 (en) 2005-08-15
SK16452001A3 (sk) 2002-03-05
AU777521B2 (en) 2004-10-21
HK1048642B (zh) 2005-10-28
EA005204B1 (ru) 2004-12-30
KR20020030270A (ko) 2002-04-24
WO2000071571A3 (en) 2001-09-07
US6613879B1 (en) 2003-09-02
EA200101155A1 (ru) 2002-10-31
IL145798A0 (en) 2002-07-25
BG106096A (bg) 2002-05-31

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