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1. (US20100298403) MODIFIED POLY(PROPYLENE-IMINE) DENDRIMERS AND THEIR USE AS TRANSFECTION AGENTS FOR AMIONIC BIOACTIVE FACTORS ( as amended

Office : United States of America
Application Number: 11994576 Application Date: 05.07.2006
Publication Number: 20100298403 Publication Date: 25.11.2010
Publication Kind : A1
Prior PCT appl.: Application Number:EP06063888 ; Publication Number: Click to see the data
IPC:
A61K 31/7088
A61P 35/00
A61P 35/02
C08F 220/58
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7088
Compounds having three or more nucleosides or nucleotides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
02
specific for leukemia
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
F
MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
220
Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide, or nitrile thereof
02
Monocarboxylic acids having less than ten carbon atoms; Derivatives thereof
52
Amides or imides
54
Amides
58
containing oxygen in addition to the carbonamido oxygen
Applicants: JANSSEN PHARMACEUTICA N.V.
Inventors: Tack Frederik
Janssen Henricus Marie
Meijer Egbert Willem
Janicot Michel Marie Francois
Brewster Marcus Eli
Agents: PHILIP S. JOHNSON;JOHNSON &; JOHNSON
Priority Data: 05106266 08.07.2005 EP
Title: (EN) MODIFIED POLY(PROPYLENE-IMINE) DENDRIMERS AND THEIR USE AS TRANSFECTION AGENTS FOR AMIONIC BIOACTIVE FACTORS ( as amended
Abstract: front page image
(EN)

The present invention is concerned with modified poly-(propylene imine) dendrimers, comprising cationic internal ammonium groups and external non-toxic endgroups, pharmaceutical compositions comprising said dendrimers, methods for the production of said dendrimers and their use as transfections agents for anionic bioactive therapeutic factors, for use in gene therapy, in particular for the treatment of cancer. The modified poly-(propylene imine) dendrimer of generation 1, 2, 3, 4 or 5, also comprising incomplete dendrimers and mixtures thereof, comprising external end groups and internal amine functions are characterized in that:

  • (a) substantially all external endgroups are groups of formula (I)

  •  wherein R is a radical selected from the group of C1-10alkyl, polyethylene glycol radical and polyethylene glycol gallyl radical; and
  • (b) substantially all internal amine functions are quaternary cationic ammonium functions. Most preferred are the quaternized compounds DAB-dendr-(NHCOCH3)4, DAB-dendr-(NHCOCH3)8, DAB-dendr-(NHCOCH3)16, DAB-dendr-(NHCOCH3)32, DAB-dendr-(NHCOCH3)64, DAB-dendr-(NHCOPh((EO)4OMe)3)4, DAB-dendr-(NHCOPh((EO)4OMe)3)8, DAB-dendr-(NHCOPh((EO)4OMe)3)16, DAB-dendr-(NHCOPh((EO)4OMe)3)32 and DAB-dendr-(NHCOPh((EO)4OMe)3)64.


Also published as:
EP1904436JP2009501245CN101218204CA2612211EA200800279AU2006268736
WO/2007/006700