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1. (WO2017157356) CYCLODEXTRI N-BASED TRANSPORTER OF NUCLEOSIDE TRIPHOSPHATE TRANSPORTER ACROSS THE CELL MEMBRANE, ITS PREPARATION AND USE
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Pub. No.: WO/2017/157356 International Application No.: PCT/CZ2017/050013
Publication Date: 21.09.2017 International Filing Date: 15.03.2017
IPC:
C08L 5/16 (2006.01) ,C08B 37/16 (2006.01) ,C07H 19/10 (2006.01) ,C07H 19/20 (2006.01)
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
L
COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
5
Compositions of polysaccharides or of their derivatives not provided for in group C08L1/ or C08L3/142
16
Cyclodextrin; Derivatives thereof
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
B
POLYSACCHARIDES; DERIVATIVES THEREOF
37
Preparation of polysaccharides not provided for in groups C08B1/-C08B35/110; Derivatives thereof
16
Cyclodextrin; Derivatives thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
06
Pyrimidine radicals
10
with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
16
Purine radicals
20
with the saccharide radical being esterified by phosphoric or polyphosphoric acids
Applicants:
USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. [CZ/CZ]; Flemingovo nam. 2 16610 Praha 6, CZ
Inventors:
KRAUS, Tomas; CZ
ZAWADA, Zbigniew; CZ
Agent:
HARTVICHOVA, Katerina; CZ
Priority Data:
PV 2016-15216.03.2016CZ
Title (EN) CYCLODEXTRI N-BASED TRANSPORTER OF NUCLEOSIDE TRIPHOSPHATE TRANSPORTER ACROSS THE CELL MEMBRANE, ITS PREPARATION AND USE
(FR) TRANSPORTEUR À BASE DE CYCLODEXTRINE OU TRANSPORTEUR DE NUCLÉOSIDE TRIPHOSPHATE À TRAVERS LA MEMBRANE CELLULAIRE, SA PRÉPARATION ET SON UTILISATION
Abstract:
(EN) Compounds of general formulae6 and 13 where X is -NH-C(NH2)=N+H2 or -N+H3, Y is a linear oligomer consisting of arginine units terminated with an aminodimethylenamide unit (-Arg)n-NH-(CH2)2-NH2, where n = 6-10, or arginine-aminocaproic units (-Arg-Aca)n- NH2, where n = 6 to 10, A- = CF3COO- or C1- and m = 1-2. Preparation and use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membranes for the purpose of incorporation of modified nucleoside triphosphates into the cellular DNA or RNA. Use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membrane for the purpose of determining the virostatic activities of modified nucleoside triphosphates. Use of compounds of general formula 6 and 13 as carriers of modified nucleoside triphosphates across the cell membrane for the purpose of determining cell proliferation and S phase of the cell cycle.
(FR) La présente invention décrit des composés de formule générale 6 et 13 où X est -NH-C(NH2)=N+H2 ou -N+H3, Y est un oligomère linéaire constitué de motifs d’arginine terminés par un motif d’aminodiméthylènamide (-Arg)n-NH-(CH2)2-NH2, où n = 6 à 10, ou de motifs d’arginine-aminocaproïque (-Arg-Aca)n- NH2, où n = 6 à 10, A- = CF3COO- ou C1- et m = 1 à 2. La présente invention décrit la préparation et l’utilisation de composés de formule générale 6 et 13 comme supports de nucléoside triphosphates à travers les membranes cellulaires en vue de l'incorporation de nucléoside triphosphates modifiés dans l’ADN ou l’ARN cellulaire. L'invention concerne également l'utilisation des composés de formule générale 6 et 13 comme supports de nucléoside triphosphates à travers la membrane cellulaire dans le but de déterminer les activités virostatiques des nucléoside triphosphates modifiés. L'invention concerne en outre l'utilisation des composés de formule générale 6 et 13 comme supports de nucléoside triphosphates modifiés à travers la membrane cellulaire dans le but de déterminer la prolifération cellulaire et la phase S du cycle cellulaire.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, 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, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)