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1. (WO1997018185) LIPOPOLYAMINES AS TRANSFECTION AGENTS AND PHARMACEUTICAL USES THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018185 International Application No.: PCT/FR1996/001774
Publication Date: 22.05.1997 International Filing Date: 08.11.1996
Chapter 2 Demand Filed: 16.05.1997
IPC:
A61K 38/00 (2006.01) ,A61K 47/48 (2006.01) ,C07C 237/06 (2006.01) ,C07C 237/12 (2006.01) ,C07D 495/04 (2006.01) ,C07H 15/12 (2006.01) ,C07J 41/00 (2006.01) ,C07K 5/06 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
48
the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02
having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04
the carbon skeleton being acyclic and saturated
06
having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02
having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04
the carbon skeleton being acyclic and saturated
12
having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15
Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02
Acyclic radicals, not substituted by cyclic structures
12
attached to a nitrogen atom of a saccharide radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
41
Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
Applicants:
RHONE-POULENC RORER S.A. [FR/FR]; 20, avenue Raymond-Aron F-92160 Antony, FR (AllExceptUS)
BYK, Gérardo [IL/FR]; FR (UsOnly)
SCHERMAN, Daniel [FR/FR]; FR (UsOnly)
SCHWARTZ, Bertrand [FR/FR]; FR (UsOnly)
DUBERTRET, Catherine [FR/FR]; FR (UsOnly)
Inventors:
BYK, Gérardo; FR
SCHERMAN, Daniel; FR
SCHWARTZ, Bertrand; FR
DUBERTRET, Catherine; FR
Agent:
LE COUPANEC, Pascale; Rhône-Poulenc Rorer S.A. Direction Brevets 20, avenue Raymond-Aron F-92165 Antony Cédex, FR
BECKER, Philippe; Rhône-Poulenc Rorer S.A. 20, avenue Raymond Aron F-92165 Antony Cédex, FR
Priority Data:
95/1349014.11.1995FR
Title (EN) LIPOPOLYAMINES AS TRANSFECTION AGENTS AND PHARMACEUTICAL USES THEREOF
(FR) LIPOPOLYMAMINES COMME AGENTS DE TRANSFECTION ET LEURS APPLICATIONS PHARMACEUTIQUES
Abstract:
(EN) Lipopolyamines of formula (I), wherein each of R1, R2 and R3, which are the same or different, is a hydrogen atom or a -(CH2)q-NRR' grouping, where q is independently 1, 2, 3, 4, 5 or 6 for each of the groupings R1, R2 and R3; each of m, n and p, which are the same or different, is an integer from 0 to 6; and R4 is a grouping of general formula (II), wherein each of R6 and R7, which are the same or different, is a hydrogen atom or a saturated or unsaturated C10-22 aliphatic radical, with the proviso that at least one of the two groupings is not hydrogen, u is an integer from 0 to 10, X is an oxygen or sulphur atom or an optionally monoalkylated amine grouping, Y is a carbonyl or methylene grouping, R5 is a hydrogen atom or an optionally substituted natural amino acid side chain, and r is an integer from 1 to 10, with the proviso that when r is 1, R5 is an optionally substituted natural amino acid side chain, and when r is more than 1, R5 is a hydrogen atom, are disclosed. Pharmaceutical compositions containing said lipopolyamines, and the use thereof for $i(in vitro) or $i(in vivo) nucleic acid transfection in cells, are also disclosed.
(FR) La présente invention se rapporte à des lipopolyamines de formule (I) dans laquelle R1, R2 et R3 représentent indépendamment l'un de l'autre un atome d'hydrogène ou un groupement-(CH2)q-NRR', q pouvant varier entre 1, 2, 3, 4, 5 et 6 ceci de manière indépendante entre les différens groupements R1, R2 et R3; m, n et p représentent, indépendamment l'un de l'autre, un nombre entier pouvant varier entre 0 et 6; R4 représente un groupement de formule générale (II) dans laquelle R6 et R7 représentent indépendamment l'un de l'autre un atome d'hydrogène ou un radical aliphatique, saturé ou non, en C10 à C22 avec au moins l'un des deux groupements étant différent de l'hydrogène; u est un nombre entier choisi entre 0 et 10; X représente un atome d'oxygène, de soufre ou un groupement amine monoalkylé ou non; Y représente un groupement carbonyle ou un groupement méthylène; R5 représente un atome d'hydrogène ou une chaîne latérale d'acide amine naturel, le cas échéant substituée et r représente un entier variant entre 1 et 10 avec lorsque r est égal à 1, R5 représentant une chaîne latérale d'acide aminé naturel substitué ou non et lorsque r est supérieur à 1, R5 représentant un atome d'hydrogène. Elle concerne également des compositions pharmaceutiques les contenant et leurs applications pour la transfection d'acides nucléiques, $i(in vitro) ou $i(in vivo) dans des cellules.
Designated States: AL, AU, BA, BB, BG, BR, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KP, KR, LC, LK, LR, LT, LV, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: French (FR)
Filing Language: French (FR)
Also published as:
CZPV1998-1473NO19981944SK63198MXPA/a/1998/003761IL124411ES2151185
EP0861228JP2009029790US6171612JP2000501383 CA2235721DE000069609982
PT861228KR1019990067552AU1996075768FR2741066