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1. (WO2019034429) MULTIFUNCTIONAL BLOCK COPOLYMERS FOR DISSOLVING ATHEROSCLEROTIC PLAQUES
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Pub. No.: WO/2019/034429 International Application No.: PCT/EP2018/070868
Publication Date: 21.02.2019 International Filing Date: 01.08.2018
IPC:
C08G 69/40 (2006.01) ,C08G 73/02 (2006.01) ,A61K 47/34 (2017.01) ,A61P 9/00 (2006.01) ,C08G 69/10 (2006.01)
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
G
MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
69
Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
40
Polyamides containing oxygen in the form of ether groups
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
G
MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
73
Macromolecular compounds obtained by reactions forming in the main chain of the macromolecule a linkage containing nitrogen, with or without oxygen or carbon, not provided for in groups C08G12/-C08G71/238
02
Polyamines
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
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
G
MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
69
Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
02
Polyamides derived from amino carboxylic acids or from polyamines and polycarboxylic acids
08
derived from amino carboxylic acids
10
Alpha-amino-carboxylic acids
Applicants:
UNIVERSITÄT KONSTANZ [DE/DE]; Universitätsstrasse 10 78464 Konstanz, DE
Inventors:
CÖLFEN, Helmut; DE
KECKEIS, Philipp; DE
DRABINOVÁ, Eliska; CZ
Agent:
MÜLLER-BORÉ & PARTNER PATENTANWÄLTE PARTG MBB; Friedenheimer Brücke 21 80639 München, DE
Priority Data:
10 2017 007 671.514.08.2017DE
Title (EN) MULTIFUNCTIONAL BLOCK COPOLYMERS FOR DISSOLVING ATHEROSCLEROTIC PLAQUES
(FR) COPOLYMÈRES À BLOCS MULTIFONCTION POUR DISSOUDRE LES PLAQUES D'ATHÉROME
(DE) MULTIFUNKTIONELLE BLOCKCOPOLYMERE ZUR AUFLÖSUNG VON ATHEROSKLEROTISCHEN PLAQUES
Abstract:
(EN) The invention relates to a multifunctional block copolymer, which comprises a hydrophilic non-acidic polymer block (A) and also a hydrophilic acidic polymer block (B) and/or a hydrophobic polymer block (C), wherein the hydrophobic polymer block (C) is provided with a steroid or a derivative thereof and the multifunctional block copolymer has at least the structure (A)-(C), (A)-(B)-(C), (A)-(C)-(B) or a combination of the structures (A)-(B) and (A)-(C). The invention further relates to a polymeric nanoparticle that is formed by self-assembly and that is based on the multifunctional block copolymer according to the invention, to a pharmaceutical composition comprising the polymeric nanoparticle, and to the use of said composition to absorb cholesterol molecules and possibly calcium ions from atherosclerotic plaques.
(FR) La présente invention concerne un copolymère à blocs multifonction comprenant un bloc polymère (A) non-acide hydrophile et en outre un bloc polymère (B) acide hydrophile et/ou un bloc polymère (C) hydrophobe, le bloc polymère (C) hydrophobe étant pourvu d'un stéroïde ou d'un dérivé de celui-ci et le copolymère à blocs multifonction présentant au moins la structure (A)-(C), (A)-(B)-(C), (A)-(C)-(B) ou une combinaison des structures (A)-(B) et (A)-(C). La présente invention concerne en outre une nanoparticule polymère formée par auto-assemblage, sur la base du copolymère à blocs multifonction selon l'invention, une composition pharmaceutique comprenant la nanoparticule polymère ainsi que son utilisation afin d'absorber les molécules de cholestérol et, le cas échéant, les ions calcium issus des plaques d'athérome.
(DE) Die vorliegende Erfindung betrifft ein multifunktionelles Blockcopolymer, welches einen hydrophilen nicht-sauren Polymerblock (A) und weiter einen hydrophilen sauren Polymerblock (B) und/oder einen hydrophoben Polymerblock (C) umfasst, wobei der hydrophobe Polymerblock (C) mit einem Steroid oder einem Derivat hiervon versehen ist und das multifunktionelle Blockcopolymer zumindest die Struktur (A)-(C), (A)-(B)-(C), (A)-(C)-(B) oder eine Kombination aus den Strukturen (A)-(B) und (A)-(C) aufweist. Weiterhin betrifft die vorliegende Erfindung ein durch Selbstassemblierung gebildetes polymeres Nanoteilchen auf Basis des erfindungsgemäßen multifunktionellen Blockcopo!ymers, eine das polymere Nanoteilchen umfassende pharmazeutische Zusammensetzung sowie deren Verwendung zur Aufnahme von Cholesterinmolekülen und gegebenenfalls Calciumionen aus atherosklerotischen Plaques.
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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, JO, 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: German (DE)
Filing Language: German (DE)