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1. (WO2007006700) MODIFIED POLY(PROPYLENE-IMINE) DENDRIMERS AND THEIR USE AS TRANSFECTION AGENTS FOR ANIONIC BIOACTIVE FACTORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/006700 International Application No.: PCT/EP2006/063888
Publication Date: 18.01.2007 International Filing Date: 05.07.2006
IPC:
C07C 235/50 (2006.01) ,C07C 235/10 (2006.01) ,C07C 233/36 (2006.01) ,A61P 35/00 (2006.01) ,A61K 31/166 (2006.01) ,A61K 31/16 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42
having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44
with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
50
having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02
having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
10
having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
01
having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
34
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
35
with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
36
having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
165
having aromatic rings, e.g. colchicine, atenolol, progabide
166
having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
Applicants:
JANSSEN PHARMACEUTICA N.V. [BE/BE]; Turnhoutseweg 30 B-2340 Beerse, BE (AllExceptUS)
TACK, Frederik [BE/BE]; BE (UsOnly)
JANSSEN, Henricus, Marie [NL/NL]; NL (UsOnly)
MEIJER, Egbert, Willem [NL/NL]; NL (UsOnly)
JANICOT, Michel, Marie, François [FR/BE]; BE (UsOnly)
BREWSTER, Marcus, Eli [US/BE]; BE (UsOnly)
Inventors:
TACK, Frederik; BE
JANSSEN, Henricus, Marie; NL
MEIJER, Egbert, Willem; NL
JANICOT, Michel, Marie, François; BE
BREWSTER, Marcus, Eli; BE
Common
Representative:
JANSSEN PHARMACEUTICA N.V.; Turnhoutseweg 30 B-2340 Beerse, BE
Priority Data:
05106266.908.07.2005EP
Title (EN) MODIFIED POLY(PROPYLENE-IMINE) DENDRIMERS AND THEIR USE AS TRANSFECTION AGENTS FOR ANIONIC BIOACTIVE FACTORS
(FR) DENDRIMERES DE POLY(PROPYLENE-IMINE) MODIFIES ET LEUR UTILISATION EN TANT QU'AGENTS DE TRANSFECTION DE FACTEURS BIOACTIFS ANIONIQUES
Abstract:
(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.
(FR) La présente invention concerne des dendrimères de poly(propylène imine) modifiés, comprenant des groupes ammonium internes cationiques et des groupes d'extrémité non toxiques externes, des compositions pharmaceutiques comprenant lesdits dendrimères, des méthodes de production desdits dendrimères ainsi que leur utilisation en tant qu'agents de transfection de facteurs thérapeutiques bioactifs anioniques, destinés à être utilisés en thérapie génique, en particulier pour le traitement du cancer. Les dendrimères de poly(propylène imine) modifiés de génération 1, 2, 3, 4 ou 5, comprenant également des dendrimères incomplets et des mélanges de ces derniers, comprenant des groupes d'extrémité externes et des fonctions amines internes sont caractérisés en ce que : (a) sensiblement l'ensemble des groupes d'extrémité sont des groupes représentés par la formule (I), dans laquelle R représente un radical sélectionné dans le groupe comprenant un alkyle C1-10, un radical polyéthylène glycol et un radical polyéthylène glycol gallyle ; et (b) sensiblement l'ensemble des fonctions amines internes sont des fonctions ammonium quaternaire cationiques. Les composés préférés sont les composés quaternisés 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 et DAB-dendr-(NHCOPh((EO)4OMe)3 )64.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP1904436JP2009501245US20100298403CN101218204CA2612211EA200800279
AU2006268736