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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N15-113
filingDate 2013-03-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2019-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_896539bbc0e3d1e0b591010f31e32cad
publicationDate 2019-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2706198-T3
titleOfInvention Conjugates of boronic acid of oligonucleotide analogues
abstract An oligonucleotide analog comprising a backbone, a 3 'terminal and a 5' terminal, the backbone comprises a sequence of morpholino ring structures linked by inter-subunit linkages, inter-subunit bonds link a 3 'end of a morpholino ring structure to a 5 'end of an adjacent morpholino ring structure, in which each morpholino ring structure is attached to a base pairing moiety, so that the oligonucleotide analog can be linked in a sequence specific manner to a target nucleic acid , in which at least one of the inter-subunit bonds, the 3'terminal or the 5'terminal comprises a fraction of boronic ester or boronic acid covalently attached to them, in which: at least one of the ring structures Morpholino has the following structure (i): ** Formula ** in which Pi is, at each occurrence, independently a pairing fraction of bases; the intersubunitary bonds have the following structure (III): ** Formula ** in which: X is, at each occurrence, independently of structure (I), structure (II) or -NR10R11; R10 and R11 are, at each occurrence, independently hydrogen or C1-C6 alkyl; the boronic acid or boronic ester moiety has, at each occurrence, independently one of the following structures (I) or (II): ** Formula ** or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, wherein: R1 is, at each occurrence, independently H or alkyl; R2 is H or alkyl, where R2 can join with one of R3, R4, R5 or R6 to form a ring; R3, R4, R5 and R6 are, at each occurrence, independently absent, H, alkyl, aryl, hydroxy, hydroxyalkyl, aminoalkyl, alkoxy, alkoxyalkyl, aryloxy, halo, nitro, cyano, amidyl, amino, alkylamino, aminoalkyl, arylamino, aralkyl, aralkylamino, aralquiloxicarbonilaminilo, alquiloxicarbonilaminilo, ariloxicarbonilaminilo, -CO2H, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, alkyloxycarbonyl, aryloxycarbonyl, alkyloxyimino or heteroaryl, wherein one of R3, R4, R5 or R6 may join another from R3, R4, R5 or R6 to form a carbocyclic or heterocyclic ring and wherein one of R3, R4, R5 or R6 can join R2 to form a heterocyclic ring; R7, R8 and R9 are, at each occurrence, independently alkyl or alkylamino; A represents, at each occurrence, independently a 6-membered aryl or heteroaryl ring; and L1 is, at each occurrence, one of the following structures:
priorityDate 2012-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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