DK2044080T3 - Camptothecin-derivater med antitumor-aktivitet - Google Patents

Camptothecin-derivater med antitumor-aktivitet Download PDF

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Publication number
DK2044080T3
DK2044080T3 DK07786096.3T DK07786096T DK2044080T3 DK 2044080 T3 DK2044080 T3 DK 2044080T3 DK 07786096 T DK07786096 T DK 07786096T DK 2044080 T3 DK2044080 T3 DK 2044080T3
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DK
Denmark
Prior art keywords
tumors
compound
hydrogen
mmols
aminoalkyl
Prior art date
Application number
DK07786096.3T
Other languages
English (en)
Inventor
Gabriele Fontana
Ezio Bombardelli
Carla Manzotti
Cristian Samori
Arturo Battaglia
Original Assignee
Indena Spa
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 Indena Spa filed Critical Indena Spa
Application granted granted Critical
Publication of DK2044080T3 publication Critical patent/DK2044080T3/da

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)

Claims (11)

1. Forbindelser med den almene formel (I):
(i) hvor: R er F; R1 er hydrogen, alkyl, aminoalkyl, hydroxyalkyl, nitril, alkoxyamino, aryloxy-amino, silylalkyl; R2 er hydrogen, hydroxyl, alkoxy, aminoalkyl; R3 er hydrogen, hydroxyl, alkoxy, aminoalkyl; forudsat, at når R1 er hydrogen, er R2 og R3 hydrogen; hvor alkyl-, alkoxy-, aminoalkyl- eller alkoxyminogrupperne kan indeholde 1 til 8 carbonatomer, i en lige eller forgrenet kæde, og aryloxygrupperne kan indeholde 5 til 10 carbonatomer; de farmaceutisk acceptable salte, enantiomerer, diastereomerer deraf og tilsvarende blandinger.
2. Forbindelse med formel (I) ifølge krav 1, som er: a) 5-F-camptothecin.
3. Fremgangsmåde til fremstilling af forbindelser med formel (I) ifølge krav 1, omfattende trinnene vist i det følgende skema, hvor: a) beskyttelse af prækursor-hydroxygrupperne; b) derivatisering ved 5 ved dannelse af en carbanion og reaktion med et elek-trofilt reagens; c) afbeskyttelse af hydroxygrupperne; Skema
hvor R, R1, R2 og R3 har betydningerne beskrevet ovenfor og PG er en OH-beskyttelsesgruppe.
4. Farmaceutisk sammensætning indeholdende en forbindelse med formel (I) ifølge krav 1 sammen med farmaceutisk acceptable bærere og hjælpestoffer.
5. Farmaceutisk sammensætning ifølge krav 4, som foreligger i en form, der er egnet til oral eller parenteral indgivelse.
6. Anvendelse af en forbindelse ifølge krav 1 eller 2 eller en sammensætning ifølge krav 4 eller 5 til fremstilling af et medikament til behandling af tumorer.
7. Anvendelse ifølge krav 6, hvor medikamentet anvendes til behandling af faste tumorer og leukæmier.
8. Anvendelse ifølge krav 6 eller 7, hvor medikamentet anvendes til behandling af tumorer i lungen, æggestokken, brystet, maven, leveren, prostata, sarkomer i blødt væv, øsofagus, pankreas, hoved og hals, glioblastom, kroniske og akutte myelocytiske leukæmier.
9. Forbindelse med den almene formel (I) ifølge krav 1 eller 2 til anvendelse ved behandling af tumorer.
10. Forbindelse til anvendelse ifølge krav 9, hvor tumorerne er faste tumorer eller leukæmier.
11. Forbindelse til anvendelse ifølge krav 9 eller 10, hvor tumorerne er udvalgt fra gruppen bestående af tumorer i lungen, æggestokken, brystet, maven, leveren, prostata, sarkomer i blødt væv, øsofagus, pankreas, hoved og hals, glioblastom, kroniske og akutte myelocytiske leukæmier.
DK07786096.3T 2006-07-26 2007-07-16 Camptothecin-derivater med antitumor-aktivitet DK2044080T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT001474A ITMI20061474A1 (it) 2006-07-26 2006-07-26 Derivati della camptotecina ad attivita antitumorale
PCT/EP2007/006294 WO2008012003A1 (en) 2006-07-26 2007-07-16 Camptothecin derivatives with antitumor activity

Publications (1)

Publication Number Publication Date
DK2044080T3 true DK2044080T3 (da) 2017-07-17

Family

ID=38668855

Family Applications (1)

Application Number Title Priority Date Filing Date
DK07786096.3T DK2044080T3 (da) 2006-07-26 2007-07-16 Camptothecin-derivater med antitumor-aktivitet

Country Status (20)

Country Link
US (1) US8193210B2 (da)
EP (1) EP2044080B1 (da)
JP (1) JP5313895B2 (da)
KR (1) KR101496374B1 (da)
CN (1) CN101495485B (da)
AU (1) AU2007278509B2 (da)
BR (1) BRPI0714672B8 (da)
CA (1) CA2658902C (da)
DK (1) DK2044080T3 (da)
ES (1) ES2628022T3 (da)
HK (1) HK1135692A1 (da)
IL (1) IL196652A0 (da)
IT (1) ITMI20061474A1 (da)
MX (1) MX2009000828A (da)
NO (1) NO342506B1 (da)
PL (1) PL2044080T3 (da)
PT (1) PT2044080T (da)
RU (1) RU2450007C2 (da)
SI (1) SI2044080T1 (da)
WO (1) WO2008012003A1 (da)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9379559B2 (en) 2012-02-03 2016-06-28 International Business Machines Corporation System and method of charging a vehicle using a dynamic power grid, and system and method of managing power consumption in the vehicle
PL235836B1 (pl) * 2012-10-25 2020-11-02 Inst Chemii Organicznej Polskiej Akademii Nauk Pochodne kamptotecyny, sposób ich otrzymywania i zastosowanie
CN108690036B (zh) * 2018-05-22 2021-05-25 北京海步医药科技股份有限公司 一种10-二氟甲基喜树碱类化合物及其制备方法和应用
LU102067B1 (en) 2020-09-17 2022-03-18 Narodowy Inst Lekow 7-Ethyl-10-hydroxycamptothecin derivatives for use in the treatment of cancer

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5972955A (en) * 1995-06-06 1999-10-26 Dr. Reddy's Research Foundation Water soluble C-ring analogues of 20(S)-camptothecin
IT1282673B1 (it) * 1996-02-23 1998-03-31 Ist Naz Stud Cura Dei Tumori Derivati della camptotecina e loro uso come agenti antitumorali

Also Published As

Publication number Publication date
AU2007278509A1 (en) 2008-01-31
JP2010500971A (ja) 2010-01-14
KR20090032100A (ko) 2009-03-31
CA2658902C (en) 2014-09-23
EP2044080B1 (en) 2017-05-10
RU2009102241A (ru) 2010-07-27
WO2008012003A1 (en) 2008-01-31
CA2658902A1 (en) 2008-01-31
EP2044080A1 (en) 2009-04-08
BRPI0714672B8 (pt) 2021-05-25
AU2007278509B2 (en) 2012-10-04
ES2628022T3 (es) 2017-08-01
CN101495485B (zh) 2012-04-11
US8193210B2 (en) 2012-06-05
US20100010032A1 (en) 2010-01-14
CN101495485A (zh) 2009-07-29
SI2044080T1 (sl) 2017-07-31
NO342506B1 (no) 2018-06-04
IL196652A0 (en) 2009-11-18
NO20090252L (no) 2009-01-16
RU2450007C2 (ru) 2012-05-10
BRPI0714672A2 (pt) 2013-03-26
MX2009000828A (es) 2009-02-03
PL2044080T3 (pl) 2017-10-31
PT2044080T (pt) 2017-06-15
KR101496374B1 (ko) 2015-03-04
HK1135692A1 (en) 2010-06-11
BRPI0714672B1 (pt) 2020-10-20
JP5313895B2 (ja) 2013-10-09
ITMI20061474A1 (it) 2008-01-27

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