Invention Grant
- Patent Title: Helquats with heteroaromatic substituents, preparation thereof, and use thereof as G-quadruplex stabilizers
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Application No.: US15313492Application Date: 2015-05-26
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Publication No.: US09932339B2Publication Date: 2018-04-03
- Inventor: Filip Teply , Miroslav Hajek , Erika Kuzmova , Jaroslav Kozak , Veronika Komarkova , Pavla Hubalkova , Paul Eduardo Reyes-Gutierrez , Michael Jirasek , Manoj R. Sonawane , Vishwas D. Joshi , Lukas Severa , Jana Novotna
- Applicant: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE
- Applicant Address: CY Praha CZ Praha
- Assignee: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.,VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE
- Current Assignee: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.,VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE
- Current Assignee Address: CY Praha CZ Praha
- Agency: Notaro, Michalos & Zaccaria P.C.
- Priority: CZPV2014-369 20140529
- International Application: PCT/CZ2015/000052 WO 20150526
- International Announcement: WO2015/180701 WO 20151203
- Main IPC: C07D471/22
- IPC: C07D471/22 ; A61K31/475 ; A61P35/00

Abstract:
Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1′,2′, S3,4 and S3′,4′ are present, each of S1,2, S1′,2′, S3,4 and S3′,4′ independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2′, and 4′ are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5′ with C8′, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)− and (X2)− independently represent anions of pharmaceutically acceptable salts.
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