Show metadata Hide metadata

(19)

(11)

2 410 432

(13)

(51)

IPC

C12N15/115(2010-01-01)

C12N15/15(2006-01-01)

A61K31/712(2006-01-01)

(21) (22)

Application

2009142862/10, 2009-11-23

(24)

Start date

2009-11-23

(22)

Actual filing date

2009-11-23

(45)

Published

2011-01-27

(72)

Inventor

Spiridonova Vera AlekseevnaGolovin Andrej ViktorovichKopylov Aleksej MikhajlovichDobrovol'Skij Anatolij BorisovichMazurov Aleksej Vladimirovich

(73)

Holder

Gosudarstvennoe Uchrezhdenie Nauchno-Issledovatel'Skij Institut Fiziko-Khimicheskoj Biologii Imeni A.N. Belozerskogo Moskovskogo Gosudarstvennogo Universiteta Imeni M.V. LomonosovaFederal'Noe Gosudarstvennoe Uchrezhdenie Kardiologicheskij Nauchno-Proizvodstvennyj Kompleks Federal'Nogo Agentstva Po Vysokotekhnologichnoj Meditsinskoj Pomoshchi"

MODIFIED DNA APTAMERS INHIBITING THROMBIN ACTIVITY Russian patent published in 2011 - IPC C12N15/115 C12N15/15 A61K31/712

Abstract RU 2410432 C1

FIELD: chemistry; biochemistry.

SUBSTANCE: invention relates to biotechnology and medicine and specifically to direct thrombin inhibitors. The invention discloses a modified aptamer oligodeoxyribonucleotide of general formula d R-GTGACGTANGGTTGGTGTGGTTGGGGCGTCAC-R where d is deoxyribose (oligonucleotide contains deoxyribose in all positions), R denotes chemical substitutes. The substitute used is aminohexanol (NH₂ group), which esterifies the phosphate group on the 5' or 3' end and PEG which is bonded on the 5' and/or 3' end. At least one of the substitutes bonded on the 5' or 3' end is polyethylene glycol (PEG). The disclosed modified DNA aptamer inhibits thrombin activity in human blood plasma by prolonging thrombin clotting time, prothrombin time and activated partial thromboplastin time and inhibits thrombin-stimulated aggregation of thrombocytes. During intravenous administration to an experimental animal, the modified DNA aptamer circulates in the blood longer than the basic aptamer RE31.

EFFECT: said DNA aptamer can serve as the base for antithrombotic medicinal agents.

6 dwg, 3 ex

Similar patents RU2410432C1

Title	Year	Author	Number
APTAMER OLIGONUCLEOTIDE - DIRECT THROMBIN INHIBITOR	2008	Spiridonova Vera Alekseevna Golovin Andrej Viktorovich Kopylov Aleksej Mikhajlovich Dobrovol'Skij Anatolij Borisovich Mazurov Aleksej Vladimirovich	RU2401306C2
DNA-APTAMERS INTERACTING WITH PROTHROMBIN	2018	Spiridonova Vera Alekseevna Melnichuk Anastasiya Vladimirovna	RU2703799C1
METHOD OF INHIBITING THROMBUS FORMATION AND ACCELERATION OF FIBRINOLYSIS WITH DNA APTAMERS INHIBITING ACTIVITY OF THROMBIN IN EXPERIMENT	2014	Dobrovol'Skij Anatolij Borisovich Mazurov Aleksej Vladimirovich Spiridonova Vera Alekseevna	RU2559545C1
RNA-APTAMER WITH ABILITY TO LEARNRECOGNIZE AUTOANTIBODIES, CHARACTERISTIC FOR MULTIPLE SCLEROSIS	2017	Chaukina Valentina Viktorovna Vorobeva Mariya Aleksandrovna Nevinskij Georgij Aleksandrovich Venyaminova Aliya Gusejn Kyzy	RU2644229C1
DOSAGE FORM OF DNA-APTAMER	2019	Kopylov Aleksej Mikhajlovich Golovin Andrej Viktorovich Pavlova Galina Valerievna Zavyalova Elena Gennadievna Turashev Askar Damirovich Antipova Olga Mikhajlovna Babij Vladimir Evstakhievich	RU2730000C1
ANTICOAGULANT WITH DIRECT ACTION BASED ON MODULAR BIVALENT DNA OF APTAMER SELECTIVE TO THROMBIN	2016	Kopylov Aleksej Mikhajlovich Golovin Andrej Viktorovich Pavlova Galina Valerevna Zavyalova Elena Gennadievna Turashev Askar Damirovich Antipova Olga Mikhajlovna Babij Vladimir Evstakhievich	RU2631829C1
COMBINATORIAL METHOD FOR OBTAINING DNA-APTAMER THROMBIN INHIBITORS AND APTAMER OLIGONUCLEOTIDES (VERSIONS)	2013	Golovin Andrej Viktorovich Kopylov Aleksej Mikhajlovich Pavlova Galina Valerievna Juminova Alina Valer'Evna	RU2520094C1
THROMBIN INHIBITING DNA-APTAMERS AND METHOD OF STRUCTURE STABILISATION	2009	Golovin Andrej Viktorovich Kopylov Aleksej Mikhajlovich Reshetnikov Roman Vladimirovich Zav'Jalova Elena Gennad'Evna Pavlova Galina Valerievna Babij Vladimir Evstakhievich	RU2429293C1
DIMETHYL 7-METHYL-2-n-TOLYL-4-PHENYLPYRROLO[2,1-f] [2,1,4]TRIAZINE-5,6-DICARBOXYLATE WITH ANTICOAGULANT EFFECT	2022	Mochulskaya Nataliya Nikolaevna Kotovskaya Svetlana Konstantinovna Rusinov Vladimir Leonidovich Charushin Valerij Nikolaevich Spasov Aleksandr Alekseevich Kucheryavenko Aida Fatikhovna Gajdukova Kseniya Andreevna	RU2790375C1
INTRODUCTION OF ANTI-COAGULATING SYSTEM REG1	2007	Raskoni Kristofer P. Tonkens Ross M.	RU2568579C2

RU 2 410 432 C1

Authors

Spiridonova Vera Alekseevna

Golovin Andrej Viktorovich

Kopylov Aleksej Mikhajlovich

Dobrovol'Skij Anatolij Borisovich

Mazurov Aleksej Vladimirovich

Dates

2011-01-27—Published

2009-11-23—Filed