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1. (CN101218204) Modified poly(propylene-imine) dendrimers and their use as transfection agents for anionic bioactive factors

Office : China
Application Number: 200680024847.7 Application Date: 05.07.2006
Publication Number: 101218204 Publication Date: 09.07.2008
Publication Kind : A
Prior PCT appl.: Application Number:PCTEP2006063888 ; Publication Number:2007006700 Click to see the data
IPC:
C07C 235/50
C07C 235/10
C07C 233/36
A61P 35/00
A61K 31/166
A61K 31/16
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
CPC:
C07C 233/36
C07C 235/10
C07C 235/50
C08G 83/004
Applicants: Janssen Pharmaceutica NV
詹森药业有限公司
Inventors: Tack Frederik
F·塔克
Janssen Henricus Marie
H·M·詹森
Meijer Egbert Willem
E·W·梅杰
Janicot Michel M. F.
M·M·F·贾尼科特
Brewster Marcus Eli
M·E·布鲁斯特
Agents: weixin hua duanjia rong
中国专利代理(香港)有限公司
中国专利代理(香港)有限公司
Priority Data: 05106266.9 08.07.2005 EP
Title: (EN) Modified poly(propylene-imine) dendrimers and their use as transfection agents for anionic bioactive factors
(ZH) 改性的聚(丙烯亚胺)树枝状聚合物及其作为用于阴离子生物活性因子的转染剂的用途
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.
(ZH)

本发明涉及包括阳离子内部铵基和外部非毒性端基的改性的聚(丙烯亚胺)树枝状聚合物、包括所述树枝状聚合物的药物组合物、用于制备所述树枝状聚合物的方法及其作为用于阴离子生物活性治疗因子的转染剂的用途、用于基因治疗特别是用于治疗癌症的用途。1、2、3、4或5代改性的聚(丙烯亚胺)树枝状聚合物,也包括不完全的树枝状聚合物及其混合物,包括外部端基和内部胺官能团,其特征在于:(a)基本上所有的外部端基为式(I)的基团,其中R为选自C1-10烷基、聚乙二醇基和聚乙二醇没食子基的基团;和(b)基本上所有的内部胺官能团为季铵化的阳离子铵官能团。最优选的为季铵化的化合物DAB-树枝状-(NHCOCH3)4,DAB-树枝状-(NHCOCH3)8,DAB-树枝状-(NHCOCH3)16,DAB-树枝状-(NHCOCH3)32,DAB-树枝状-(NHCOCH3)64,DAB-树枝状-(NHCOPh((EO)4OMe)3)4,DAB-树枝状-(NHCOPh((EO)4OMe)3)8,DAB-树枝状-(NHCOPh((EO)4OMe)3)16,DAB-树枝状-(NHCOPh((EO)4-OMe)3)32和DAB-树枝状-(NHCOPh((EO)4OMe)3)64


Also published as:
EP1904436JP2009501245US20100298403CA2612211EA200800279AU2006268736
WO/2007/006700